MK-2206 2HCl

製品コード：S1078 純度：99.92%

MK-2206 2HCl は高い選択性をもつ Akt1/2/3 阻害剤であり、cell-free assay における IC50 はそれぞれ 8 nM/ 12 nM/ 65 nM です。一方で、他の250種におよぶキナーゼ (kinases) に対しては活性が検出されていません。MK-2206 2HCl はがん細胞におけるオートファジー (autophagy) やアポトーシス (apoptosis) に関与します。臨床第2相試験中

CAS No. 1032350-13-2

サイズ	価格(税別)	在庫状況
10mM (1mL in DMSO)	JPY 33000	国内在庫あり
5mg	JPY 22000	国内在庫あり
25mg	JPY 59500	国内在庫あり
100mg	JPY 118500	国内在庫あり
1g	JPY 295500	国内在庫なし(納期7~10日)

代表番号: 045-509-1970\|電子メール：[email protected] よく尋ねられる質問

文献中Selleckの製品使用例（1803）

製品安全説明書

現在のバッチを見る：純度： 99.92%

99.92

MK-2206 2HCl関連製品

関連ターゲット	Akt1 Akt2 Akt3	もっと見る
関連製品	Perifosine SC79 Capivasertib (AZD5363) GSK690693 Ipatasertib (GDC-0068) Triciribine (API-2) CCT128930 Afuresertib (GSK2110183) A-674563 HCl AT7867 Oridonin Akti-1/2 PHT-427 TIC10 (ONC201) Miransertib (ARQ 092) HCl AT13148 Uprosertib (GSK2141795) Miransertib (ARQ-092) SC66 Deguelin ML-9 HCl	もっと見る
関連化合物ライブラリー	Kinase Inhibitor Library PI3K/Akt Inhibitor Library Apoptosis Compound Library Cell Cycle compound library NF-κB Signaling Compound Library	もっと見る

シグナル伝達経路

Aktシグナル伝達経路

Akt阻害剤の選択性比較

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	活性情報	PMID
Rh30	Function assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells	29435139
OHS-50	Function assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells	29435139
MG 63 (6-TG R)	Function assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells	29435139
SK-N-SH	Function assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells	29435139
BT-37	Function assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells	29435139
DAOY	Function assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells	29435139
NCI-H292	Cytotoxic Assay	3 μM	72 h	Inhibition of cell proliferation	20571069
A431	Kinase Assay	5 μM	5 h	Suppresses the signaling of Akt and Erk	20571069
HepG2	Cytotoxic Assay	10 μM	24 h	Sensitizes resistant cells to the cytotoxic effect of	21205925
Sk-Hep1	Cytotoxic Assay	10 μM	24 h	Sensitizes resistant cells to the cytotoxic effect of	21205925
OCUT1 cells harbored PIK3CA (H1047R+/+)	Growth Inhibition Assay	3 μM	5 d	IC50=0.14 μM	21289267
FTC133 cells harbored PTEN (allele deletion and R130+)	Growth Inhibition Assay	3 μM	5 d	IC50=0.18 μM	21289267
C643 cells harbored HRAS (G13R+/−)	Growth Inhibition Assay	3 μM	5 d	IC50=0.27 μM	21289267
Hth7 cells harbored NRAS (Q61R+/−)	Growth Inhibition Assay	3 μM	5 d	IC50=4.5 μM	21289267
HC11	Function Assay	10 μM	24 h	Inhibits β-casein and ADRP synthesis	22426621
CEM-S	Cytotoxic Assay	10 μM	48 h	IC50=5.1 μM	22614243
MOLT-4	Function Assay	10 μM	24 h	Blocks cells in the G0/G1 phase of the cell cycle	22614243
CEM-R	Function Assay	4 μM	4 h	Increases the amount of cleaved LC4A/B, a well-established autophagy marker	22614243
CEM-S	Function Assay	4 μM	4 h	Increases the amount of cleaved LC5A/B, a well-established autophagy marker	22614243
LoVo	Growth Inhibition Assay			IC50=1.32534 μM	SANGER
SJ-GBM2	Function assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells	29435139
C2BBe1	Growth Inhibition Assay			IC50=231.905 μM	SANGER
TGBC24TKB	Growth Inhibition Assay			IC50=36.67 μM	SANGER
Daoy	Growth Inhibition Assay			IC50=36.6538 μM	SANGER
SW48	Growth Inhibition Assay			IC50=36.2474 μM	SANGER
KURAMOCHI	Growth Inhibition Assay			IC50=36.1198 μM	SANGER
NB14	Growth Inhibition Assay			IC50=34.4684 μM	SANGER
COLO-800	Growth Inhibition Assay			IC50=34.3647 μM	SANGER
OE33	Growth Inhibition Assay			IC50=34.2855 μM	SANGER
769-P	Growth Inhibition Assay			IC50=32.3641 μM	SANGER
IST-MES1	Growth Inhibition Assay			IC50=32.2897 μM	SANGER
NCI-H2170	Growth Inhibition Assay			IC50=31.8516 μM	SANGER
OCI-AML2	Growth Inhibition Assay			IC50=31.069 μM	SANGER
HT-1197	Growth Inhibition Assay			IC50=30.0598 μM	SANGER
ES6	Growth Inhibition Assay			IC50=29.8157 μM	SANGER
PANC-03-27	Growth Inhibition Assay			IC50=29.444 μM	SANGER
ES7	Growth Inhibition Assay			IC50=29.1465 μM	SANGER
RCC10RGB	Growth Inhibition Assay			IC50=28.5417 μM	SANGER
SNU-C2B	Growth Inhibition Assay			IC50=28.2964 μM	SANGER
YAPC	Growth Inhibition Assay			IC50=28.2564 μM	SANGER
CAL-12T	Growth Inhibition Assay			IC50=28.1112 μM	SANGER
EW-13	Growth Inhibition Assay			IC50=26.0274 μM	SANGER
NCI-H1755	Growth Inhibition Assay			IC50=25.9945 μM	SANGER
BT-549	Growth Inhibition Assay			IC50=25.9011 μM	SANGER
HT-1376	Growth Inhibition Assay			IC50=25.6465 μM	SANGER
U-2-OS	Growth Inhibition Assay			IC50=25.6888 μM	SANGER
RH-18	Growth Inhibition Assay			IC50=25.5918 μM	SANGER
TE-1	Growth Inhibition Assay			IC50=25.3563 μM	SANGER
NCI-H2342	Growth Inhibition Assay			IC50=25.1953 μM	SANGER
ALL-PO	Growth Inhibition Assay			IC50=24.619 μM	SANGER
HCC2998	Growth Inhibition Assay			IC50=24.4885 μM	SANGER
SK-N-FI	Growth Inhibition Assay			IC50=24.3302 μM	SANGER
KINGS-1	Growth Inhibition Assay			IC50=24.4874 μM	SANGER
DK-MG	Growth Inhibition Assay			IC50=24.294 μM	SANGER
NMC-G1	Growth Inhibition Assay			IC50=24.2226 μM	SANGER
HCC1806	Growth Inhibition Assay			IC50=23.8709 μM	SANGER
MZ2-MEL	Growth Inhibition Assay			IC50=23.7759 μM	SANGER
S-117	Growth Inhibition Assay			IC50=23.7651 μM	SANGER
DJM-1	Growth Inhibition Assay			IC50=23.5234 μM	SANGER
M14	Growth Inhibition Assay			IC50=23.4088 μM	SANGER
NCI-H2405	Growth Inhibition Assay			IC50=23.2533 μM	SANGER
AM-38	Growth Inhibition Assay			IC50=22.8689 μM	SANGER
Rh41	Function assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells	29435139
NB1643	Function assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells	29435139
BT-12	Function assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells	29435139
RD	Function assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells	29435139
Saos-2	Function assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells	29435139
A673	Function assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	29435139
HCT116	Growth inhibition assay		72 h	IC50 = 7.5 μM	24900862
NCI-H460	Growth inhibition assay		72 h	IC50 = 5.4 μM	24900862
HeLa	Function assay		1 h	IC50 = 0.0228 μM	29100733
K1 cells harbored PIK3CA (E542K+/+)	Growth Inhibition Assay	3 μM	5 d	IC50=0.52 μM	21289267
TPC1 cells harbored RET/PTC1 rearrangement	Growth Inhibition Assay	3 μM	5 d	IC50=0.59 μM	21289267
Hth74	Growth Inhibition Assay	3 μM	5 d	IC50=2.19 μM	21289267
KAT18	Growth Inhibition Assay	3 μM	5 d	IC50=4.62 μM	21289267
SW1736	Growth Inhibition Assay	100 μM	5 d	IC50=47.56 μM	21289267
WRO	Growth Inhibition Assay	1000 μM	5 d	IC50>1000 μM	21289267
LN229	Apoptosis Assay	0.5 μM	60 h	Augments apoptogenic effects of	22057914
TAD2	Growth Inhibition Assay	1000 μM	5 d	IC50>1000 μM	21289267
T98G	Apoptosis Assay	0.5 μM	60 h	Augments apoptogenic effects of	22057914
MOLT-4	Cytotoxic Assay	10 μM	48 h	IC50=1.7 μM	22614243
CEM-R	Cytotoxic Assay	10 μM	48 h	IC50=3.3 μM	22614243
MOLT-4	Function Assay	4 μM	4 h	Increases the amount of cleaved LC3A/B, a well-established autophagy marker	22614243
HepG2 cell	Kinase Assay	20 μM	24 h	Downregulates the phosphorylation of AKT	23797319
HepG2 cell	Growth Inhibition Assay	30 μM	24 h	Inhibits cell growth	23797319
HepG2 cell	Apoptosis Assay	20 μM	24 h	Induces cell apoptosis	23797319
GEO	Growth Inhibition Assay	500 nM	72 h	Inhibits cell growth	24581231
CNE-1	Growth Inhibition Assay	10 μM	96 h	IC50=2.96 μM	25336925
CNE-2	Growth Inhibition Assay	10 μM	96 h	IC50=4.53 μM	25336925
SUNE-1	Growth Inhibition Assay	10 μM	96 h	IC50=0.52 μM	25336925
HONE-1	Growth Inhibition Assay	10 μM	96 h	IC50=3.37 μM	25336925
CNE-2	Function Assay	10 μM	48 h	Induces cell cycle arrest at G1	25336925
HONE-1	Function Assay	10 μM	48 h	Induces cell cycle arrest at G1	25336925
NEC8	Growth Inhibition Assay			IC50=0.09651 μM	SANGER
P12-ICHIKAWA	Growth Inhibition Assay			IC50=0.1162 μM	SANGER
MDA-MB-175-VII	Growth Inhibition Assay			IC50=0.13738 μM	SANGER
AsPC-1	Growth Inhibition Assay			IC50=0.22122 μM	SANGER
T47D	Growth Inhibition Assay			IC50=0.2825 μM	SANGER
HH	Growth Inhibition Assay			IC50=0.30283 μM	SANGER
MOLT-16	Growth Inhibition Assay			IC50=0.3032 μM	SANGER
ES5	Growth Inhibition Assay			IC50=0.34455 μM	SANGER
RS4-11	Growth Inhibition Assay			IC50=0.3461 μM	SANGER
KARPAS-45	Growth Inhibition Assay			IC50=0.37321 μM	SANGER
NCI-H720	Growth Inhibition Assay			IC50=0.37679 μM	SANGER
H9	Growth Inhibition Assay			IC50=0.38883 μM	SANGER
EFM-19	Growth Inhibition Assay			IC50=0.4401 μM	SANGER
SBC-1	Growth Inhibition Assay			IC50=0.44035 μM	SANGER
A4-Fuk	Growth Inhibition Assay			IC50=0.46868 μM	SANGER
NCI-H1563	Growth Inhibition Assay			IC50=0.48189 μM	SANGER
HCC1419	Growth Inhibition Assay			IC50=0.48892 μM	SANGER
H-EMC-SS	Growth Inhibition Assay			IC50=0.49939 μM	SANGER
BHT-101	Growth Inhibition Assay			IC50=0.52961 μM	SANGER
IGROV-1	Growth Inhibition Assay			IC50=0.55249 μM	SANGER
HGC-27	Growth Inhibition Assay			IC50=0.56783 μM	SANGER
MDA-MB-361	Growth Inhibition Assay			IC50=0.57761 μM	SANGER
KE-37	Growth Inhibition Assay			IC50=0.5826 μM	SANGER
HCC70	Growth Inhibition Assay			IC50=0.59827 μM	SANGER
LNCaP-Clone-FGC	Growth Inhibition Assay			IC50=0.61048 μM	SANGER
HAL-01	Growth Inhibition Assay			IC50=0.6213 μM	SANGER
HT	Growth Inhibition Assay			IC50=0.63239 μM	SANGER
MDA-MB-415	Growth Inhibition Assay			IC50=0.63626 μM	SANGER
NOS-1	Growth Inhibition Assay			IC50=0.63723 μM	SANGER
DU-145	Growth Inhibition Assay			IC50=0.64745 μM	SANGER
OCUB-M	Growth Inhibition Assay			IC50=0.70966 μM	SANGER
VA-ES-BJ	Growth Inhibition Assay			IC50=0.73025 μM	SANGER
J-RT3-T3-5	Growth Inhibition Assay			IC50=0.74403 μM	SANGER
MOLT-4	Growth Inhibition Assay			IC50=0.80582 μM	SANGER
NB7	Growth Inhibition Assay			IC50=0.82411 μM	SANGER
L-363	Growth Inhibition Assay			IC50=0.83442 μM	SANGER
NKM-1	Growth Inhibition Assay			IC50=0.86253 μM	SANGER
HOP-92	Growth Inhibition Assay			IC50=0.87223 μM	SANGER
OAW-42	Growth Inhibition Assay			IC50=0.8872 μM	SANGER
HuO9	Growth Inhibition Assay			IC50=0.92751 μM	SANGER
MFE-280	Growth Inhibition Assay			IC50=0.96465 μM	SANGER
EM-2	Growth Inhibition Assay			IC50=0.97939 μM	SANGER
NCI-H520	Growth Inhibition Assay			IC50=0.98592 μM	SANGER
LB2241-RCC	Growth Inhibition Assay			IC50=0.99734 μM	SANGER
SK-NEP-1	Growth Inhibition Assay			IC50=1.14485 μM	SANGER
LXF-289	Growth Inhibition Assay			IC50=1.17156 μM	SANGER
EPLC-272H	Growth Inhibition Assay			IC50=1.17256 μM	SANGER
COLO-684	Growth Inhibition Assay			IC50=1.23725 μM	SANGER
ES1	Growth Inhibition Assay			IC50=1.24065 μM	SANGER
DOHH-2	Growth Inhibition Assay			IC50=1.28203 μM	SANGER
CTB-1	Growth Inhibition Assay			IC50=1.2899 μM	SANGER
G-401	Growth Inhibition Assay			IC50=1.29795 μM	SANGER
Ramos-2G6-4C10	Growth Inhibition Assay			IC50=1.33701 μM	SANGER
MFM-223	Growth Inhibition Assay			IC50=1.34461 μM	SANGER
PA-1	Growth Inhibition Assay			IC50=1.35265 μM	SANGER
697	Growth Inhibition Assay			IC50=1.37616 μM	SANGER
QIMR-WIL	Growth Inhibition Assay			IC50=1.49116 μM	SANGER
HOS	Growth Inhibition Assay			IC50=1.49558 μM	SANGER
DMS-273	Growth Inhibition Assay			IC50=1.51959 μM	SANGER
ME-180	Growth Inhibition Assay			IC50=1.56891 μM	SANGER
HCC2218	Growth Inhibition Assay			IC50=1.68225 μM	SANGER
CAL-54	Growth Inhibition Assay			IC50=1.71242 μM	SANGER
OMC-1	Growth Inhibition Assay			IC50=1.74677 μM	SANGER
COR-L105	Growth Inhibition Assay			IC50=1.79737 μM	SANGER
BV-173	Growth Inhibition Assay			IC50=1.81074 μM	SANGER
RKO	Growth Inhibition Assay			IC50=1.87101 μM	SANGER
SNU-387	Growth Inhibition Assay			IC50=1.88406 μM	SANGER
SW1088	Growth Inhibition Assay			IC50=1.94606 μM	SANGER
Hs-578-T	Growth Inhibition Assay			IC50=2.11433 μM	SANGER
OC-314	Growth Inhibition Assay			IC50=2.15086 μM	SANGER
RMG-I	Growth Inhibition Assay			IC50=2.16398 μM	SANGER
NCI-H1395	Growth Inhibition Assay			IC50=2.18091 μM	SANGER
GAMG	Growth Inhibition Assay			IC50=2.23845 μM	SANGER
LB1047-RCC	Growth Inhibition Assay			IC50=2.24317 μM	SANGER
MN-60	Growth Inhibition Assay			IC50=2.29923 μM	SANGER
OAW-28	Growth Inhibition Assay			IC50=2.29951 μM	SANGER
NCI-H2228	Growth Inhibition Assay			IC50=2.31552 μM	SANGER
ABC-1	Growth Inhibition Assay			IC50=2.33253 μM	SANGER
LS-513	Growth Inhibition Assay			IC50=2.33484 μM	SANGER
KS-1	Growth Inhibition Assay			IC50=2.38191 μM	SANGER
NB69	Growth Inhibition Assay			IC50=2.38983 μM	SANGER
VM-CUB-1	Growth Inhibition Assay			IC50=2.39083 μM	SANGER
D-423MG	Growth Inhibition Assay			IC50=2.41044 μM	SANGER
EW-18	Growth Inhibition Assay			IC50=2.41939 μM	SANGER
YH-13	Growth Inhibition Assay			IC50=2.46153 μM	SANGER
T-24	Growth Inhibition Assay			IC50=2.47881 μM	SANGER
ES8	Growth Inhibition Assay			IC50=2.49287 μM	SANGER
ES3	Growth Inhibition Assay			IC50=2.49759 μM	SANGER
RXF393	Growth Inhibition Assay			IC50=2.60487 μM	SANGER
RPMI-8226	Growth Inhibition Assay			IC50=2.62953 μM	SANGER
AGS	Growth Inhibition Assay			IC50=2.72137 μM	SANGER
HCC1395	Growth Inhibition Assay			IC50=2.75187 μM	SANGER
MV-4-11	Growth Inhibition Assay			IC50=2.75266 μM	SANGER
A204	Growth Inhibition Assay			IC50=2.83872 μM	SANGER
MCF7	Growth Inhibition Assay			IC50=2.86117 μM	SANGER
SNU-423	Growth Inhibition Assay			IC50=2.89242 μM	SANGER
NCI-H1048	Growth Inhibition Assay			IC50=2.96865 μM	SANGER
GR-ST	Growth Inhibition Assay			IC50=3.04611 μM	SANGER
EoL-1-	Growth Inhibition Assay			IC50=3.07058 μM	SANGER
HuH-7	Growth Inhibition Assay			IC50=3.09464 μM	SANGER
OS-RC-2	Growth Inhibition Assay			IC50=3.1119 μM	SANGER
EW-3	Growth Inhibition Assay			IC50=3.19529 μM	SANGER
NCI-H747	Growth Inhibition Assay			IC50=3.20694 μM	SANGER
EW-16	Growth Inhibition Assay			IC50=3.21879 μM	SANGER
DOK	Growth Inhibition Assay			IC50=3.22859 μM	SANGER
HCC2157	Growth Inhibition Assay			IC50=3.38179 μM	SANGER
OVCAR-3	Growth Inhibition Assay			IC50=3.40786 μM	SANGER
NCI-H1623	Growth Inhibition Assay			IC50=3.41224 μM	SANGER
H4	Growth Inhibition Assay			IC50=3.45626 μM	SANGER
SW1710	Growth Inhibition Assay			IC50=3.46678 μM	SANGER
RT-112	Growth Inhibition Assay			IC50=3.52388 μM	SANGER
DMS-114	Growth Inhibition Assay			IC50=3.62278 μM	SANGER
AN3-CA	Growth Inhibition Assay			IC50=3.62456 μM	SANGER
KNS-62	Growth Inhibition Assay			IC50=3.63338 μM	SANGER
SJRH30	Growth Inhibition Assay			IC50=3.69122 μM	SANGER
G-402	Growth Inhibition Assay			IC50=3.70711 μM	SANGER
MHH-PREB-1	Growth Inhibition Assay			IC50=3.72038 μM	SANGER
P30-OHK	Growth Inhibition Assay			IC50=3.80976 μM	SANGER
RVH-421	Growth Inhibition Assay			IC50=3.81788 μM	SANGER
LU-134-A	Growth Inhibition Assay			IC50=3.88428 μM	SANGER
ECC10	Growth Inhibition Assay			IC50=3.93622 μM	SANGER
TGW	Growth Inhibition Assay			IC50=4.02305 μM	SANGER
MLMA	Growth Inhibition Assay			IC50=4.02966 μM	SANGER
SCC-25	Growth Inhibition Assay			IC50=4.06566 μM	SANGER
TYK-nu	Growth Inhibition Assay			IC50=4.09534 μM	SANGER
LAMA-84	Growth Inhibition Assay			IC50=4.14191 μM	SANGER
Calu-3	Growth Inhibition Assay			IC50=4.24416 μM	SANGER
NCI-H460	Growth Inhibition Assay			IC50=4.26443 μM	SANGER
EGI-1	Growth Inhibition Assay			IC50=4.37778 μM	SANGER
NCI-H292	Growth Inhibition Assay			IC50=4.38146 μM	SANGER
HCE-T	Growth Inhibition Assay			IC50=4.41579 μM	SANGER
EW-11	Growth Inhibition Assay			IC50=4.41838 μM	SANGER
ATN-1	Growth Inhibition Assay			IC50=4.44304 μM	SANGER
NB5	Growth Inhibition Assay			IC50=4.53697 μM	SANGER
KLE	Growth Inhibition Assay			IC50=4.70198 μM	SANGER
CAL-39	Growth Inhibition Assay			IC50=4.72146 μM	SANGER
TI-73	Growth Inhibition Assay			IC50=4.80609 μM	SANGER
HO-1-N-1	Growth Inhibition Assay			IC50=4.942 μM	SANGER
786-0	Growth Inhibition Assay			IC50=4.94673 μM	SANGER
SK-N-DZ	Growth Inhibition Assay			IC50=4.96142 μM	SANGER
NCI-H446	Growth Inhibition Assay			IC50=5.20009 μM	SANGER
ETK-1	Growth Inhibition Assay			IC50=5.21165 μM	SANGER
BT-20	Growth Inhibition Assay			IC50=5.21353 μM	SANGER
MEL-HO	Growth Inhibition Assay			IC50=5.37336 μM	SANGER
CAL-27	Growth Inhibition Assay			IC50=5.46339 μM	SANGER
SW872	Growth Inhibition Assay			IC50=5.59428 μM	SANGER
RPMI-2650	Growth Inhibition Assay			IC50=5.66199 μM	SANGER
PFSK-1	Growth Inhibition Assay			IC50=5.72732 μM	SANGER
SF295	Growth Inhibition Assay			IC50=5.80633 μM	SANGER
Becker	Growth Inhibition Assay			IC50=5.86472 μM	SANGER
Saos-2	Growth Inhibition Assay			IC50=5.8653 μM	SANGER
SK-OV-3	Growth Inhibition Assay			IC50=5.99816 μM	SANGER
VMRC-RCZ	Growth Inhibition Assay			IC50=6.08773 μM	SANGER
EW-22	Growth Inhibition Assay			IC50=6.19649 μM	SANGER
BT-474	Growth Inhibition Assay			IC50=6.233 μM	SANGER
BFTC-909	Growth Inhibition Assay			IC50=6.30345 μM	SANGER
NB12	Growth Inhibition Assay			IC50=6.39071 μM	SANGER
D-263MG	Growth Inhibition Assay			IC50=6.45169 μM	SANGER
SNB75	Growth Inhibition Assay			IC50=6.60143 μM	SANGER
A704	Growth Inhibition Assay			IC50=6.6306 μM	SANGER
NCI-H1693	Growth Inhibition Assay			IC50=6.63604 μM	SANGER
LN-405	Growth Inhibition Assay			IC50=6.79672 μM	SANGER
CHL-1	Growth Inhibition Assay			IC50=6.80079 μM	SANGER
A498	Growth Inhibition Assay			IC50=6.81961 μM	SANGER
TE-12	Growth Inhibition Assay			IC50=6.83817 μM	SANGER
TE-6	Growth Inhibition Assay			IC50=6.93038 μM	SANGER
AU565	Growth Inhibition Assay			IC50=6.96957 μM	SANGER
RD	Growth Inhibition Assay			IC50=6.98284 μM	SANGER
SW1463	Growth Inhibition Assay			IC50=7.11168 μM	SANGER
LU-99A	Growth Inhibition Assay			IC50=7.14322 μM	SANGER
NCI-H28	Growth Inhibition Assay			IC50=7.2924 μM	SANGER
MC-IXC	Growth Inhibition Assay			IC50=7.48576 μM	SANGER
GP5d	Growth Inhibition Assay			IC50=7.48764 μM	SANGER
GB-1	Growth Inhibition Assay			IC50=7.54804 μM	SANGER
CAL-33	Growth Inhibition Assay			IC50=7.66233 μM	SANGER
MSTO-211H	Growth Inhibition Assay			IC50=7.67336 μM	SANGER
TE-5	Growth Inhibition Assay			IC50=7.79334 μM	SANGER
D-566MG	Growth Inhibition Assay			IC50=8.04429 μM	SANGER
JVM-3	Growth Inhibition Assay			IC50=8.15268 μM	SANGER
T98G	Growth Inhibition Assay			IC50=8.18067 μM	SANGER
HCC1954	Growth Inhibition Assay			IC50=8.45104 μM	SANGER
SF126	Growth Inhibition Assay			IC50=8.45936 μM	SANGER
LB996-RCC	Growth Inhibition Assay			IC50=8.53257 μM	SANGER
SKG-IIIa	Growth Inhibition Assay			IC50=8.63069 μM	SANGER
NCI-SNU-1	Growth Inhibition Assay			IC50=8.64643 μM	SANGER
LB771-HNC	Growth Inhibition Assay			IC50=8.64696 μM	SANGER
SCC-4	Growth Inhibition Assay			IC50=8.68219 μM	SANGER
CAMA-1	Growth Inhibition Assay			IC50=8.77146 μM	SANGER
D-502MG	Growth Inhibition Assay			IC50=8.78629 μM	SANGER
ESS-1	Growth Inhibition Assay			IC50=8.88704 μM	SANGER
HEC-1	Growth Inhibition Assay			IC50=8.89866 μM	SANGER
NB10	Growth Inhibition Assay			IC50=9.02224 μM	SANGER
8505C	Growth Inhibition Assay			IC50=9.04232 μM	SANGER
EFO-27	Growth Inhibition Assay			IC50=9.16412 μM	SANGER
HN	Growth Inhibition Assay			IC50=9.16628 μM	SANGER
DSH1	Growth Inhibition Assay			IC50=9.2087 μM	SANGER
NBsusSR	Growth Inhibition Assay			IC50=9.27402 μM	SANGER
LS-123	Growth Inhibition Assay			IC50=9.31761 μM	SANGER
SHP-77	Growth Inhibition Assay			IC50=9.39935 μM	SANGER
ACN	Growth Inhibition Assay			IC50=9.53277 μM	SANGER
U251	Growth Inhibition Assay			IC50=9.65544 μM	SANGER
A431	Growth Inhibition Assay			IC50=9.80238 μM	SANGER
5637	Growth Inhibition Assay			IC50=9.84984 μM	SANGER
MDA-MB-157	Growth Inhibition Assay			IC50=9.92878 μM	SANGER
A101D	Growth Inhibition Assay			IC50=9.99974 μM	SANGER
YKG-1	Growth Inhibition Assay			IC50=10.2006 μM	SANGER
LAN-6	Growth Inhibition Assay			IC50=10.2164 μM	SANGER
OVCAR-5	Growth Inhibition Assay			IC50=10.2433 μM	SANGER
A549	Growth Inhibition Assay			IC50=10.3973 μM	SANGER
no-11	Growth Inhibition Assay			IC50=10.4353 μM	SANGER
SF539	Growth Inhibition Assay			IC50=10.9041 μM	SANGER
A388	Growth Inhibition Assay			IC50=11.3897 μM	SANGER
DEL	Growth Inhibition Assay			IC50=11.424 μM	SANGER
SW954	Growth Inhibition Assay			IC50=11.4668 μM	SANGER
TK10	Growth Inhibition Assay			IC50=11.5271 μM	SANGER
SW756	Growth Inhibition Assay			IC50=11.5294 μM	SANGER
PC-3	Growth Inhibition Assay			IC50=11.5764 μM	SANGER
ONS-76	Growth Inhibition Assay			IC50=11.636 μM	SANGER
A427	Growth Inhibition Assay			IC50=11.7093 μM	SANGER
MEG-01	Growth Inhibition Assay			IC50=11.7509 μM	SANGER
BB30-HNC	Growth Inhibition Assay			IC50=11.7982 μM	SANGER
NCI-H1299	Growth Inhibition Assay			IC50=11.8093 μM	SANGER
GCT	Growth Inhibition Assay			IC50=11.8228 μM	SANGER
D-247MG	Growth Inhibition Assay			IC50=11.9663 μM	SANGER
CFPAC-1	Growth Inhibition Assay			IC50=11.9782 μM	SANGER
EKVX	Growth Inhibition Assay			IC50=12.0313 μM	SANGER
CAL-51	Growth Inhibition Assay			IC50=12.0716 μM	SANGER
BB49-HNC	Growth Inhibition Assay			IC50=12.1177 μM	SANGER
RPMI-7951	Growth Inhibition Assay			IC50=12.1854 μM	SANGER
RH-1	Growth Inhibition Assay			IC50=12.2184 μM	SANGER
BCPAP	Growth Inhibition Assay			IC50=12.4749 μM	SANGER
GCIY	Growth Inhibition Assay			IC50=12.5209 μM	SANGER
KNS-81-FD	Growth Inhibition Assay			IC50=12.5869 μM	SANGER
KYSE-140	Growth Inhibition Assay			IC50=12.8595 μM	SANGER
Ca-Ski	Growth Inhibition Assay			IC50=12.9041 μM	SANGER
TGBC1TKB	Growth Inhibition Assay			IC50=12.9115 μM	SANGER
HCC1187	Growth Inhibition Assay			IC50=13.1912 μM	SANGER
SJSA-1	Growth Inhibition Assay			IC50=13.2327 μM	SANGER
CTV-1	Growth Inhibition Assay			IC50=13.345 μM	SANGER
WM-115	Growth Inhibition Assay			IC50=13.6483 μM	SANGER
CHP-212	Growth Inhibition Assay			IC50=13.9739 μM	SANGER
SCC-15	Growth Inhibition Assay			IC50=13.9775 μM	SANGER
BPH-1	Growth Inhibition Assay			IC50=14.1664 μM	SANGER
SW780	Growth Inhibition Assay			IC50=14.5025 μM	SANGER
NCI-H2291	Growth Inhibition Assay			IC50=14.5878 μM	SANGER
JEG-3	Growth Inhibition Assay			IC50=14.6326 μM	SANGER
CAL-120	Growth Inhibition Assay			IC50=14.7027 μM	SANGER
NCI-H23	Growth Inhibition Assay			IC50=14.7997 μM	SANGER
MS-1	Growth Inhibition Assay			IC50=14.9611 μM	SANGER
PC-14	Growth Inhibition Assay			IC50=14.9654 μM	SANGER
D-283MED	Growth Inhibition Assay			IC50=15.0111 μM	SANGER
OE19	Growth Inhibition Assay			IC50=15.1541 μM	SANGER
CAS-1	Growth Inhibition Assay			IC50=15.4184 μM	SANGER
NCI-H727	Growth Inhibition Assay			IC50=15.4221 μM	SANGER
SiHa	Growth Inhibition Assay			IC50=15.7594 μM	SANGER
BFTC-905	Growth Inhibition Assay			IC50=15.7694 μM	SANGER
MDA-MB-453	Growth Inhibition Assay			IC50=16.1642 μM	SANGER
HuP-T3	Growth Inhibition Assay			IC50=16.6373 μM	SANGER
SK-LU-1	Growth Inhibition Assay			IC50=16.6956 μM	SANGER
Detroit562	Growth Inhibition Assay			IC50=16.7318 μM	SANGER
HCC1569	Growth Inhibition Assay			IC50=16.8337 μM	SANGER
SK-MES-1	Growth Inhibition Assay			IC50=16.8419 μM	SANGER
BB65-RCC	Growth Inhibition Assay			IC50=17.0479 μM	SANGER
LOXIMVI	Growth Inhibition Assay			IC50=17.0707 μM	SANGER
SW1783	Growth Inhibition Assay			IC50=17.128 μM	SANGER
NH-12	Growth Inhibition Assay			IC50=17.3303 μM	SANGER
UACC-257	Growth Inhibition Assay			IC50=17.5512 μM	SANGER
KOSC-2	Growth Inhibition Assay			IC50=17.6757 μM	SANGER
KG-1	Growth Inhibition Assay			IC50=17.6937 μM	SANGER
M059J	Growth Inhibition Assay			IC50=17.703 μM	SANGER
MHH-NB-11	Growth Inhibition Assay			IC50=17.9673 μM	SANGER
EW-1	Growth Inhibition Assay			IC50=18.1382 μM	SANGER
CAL-85-1	Growth Inhibition Assay			IC50=18.2357 μM	SANGER
639-V	Growth Inhibition Assay			IC50=18.3354 μM	SANGER
C32	Growth Inhibition Assay			IC50=18.4727 μM	SANGER
KM-H2	Growth Inhibition Assay			IC50=18.5232 μM	SANGER
A253	Growth Inhibition Assay			IC50=18.7286 μM	SANGER
NCI-N87	Growth Inhibition Assay			IC50=18.9008 μM	SANGER
8-MG-BA	Growth Inhibition Assay			IC50=19.0646 μM	SANGER
GI-ME-N	Growth Inhibition Assay			IC50=19.1546 μM	SANGER
8305C	Growth Inhibition Assay			IC50=19.2286 μM	SANGER
TE-8	Growth Inhibition Assay			IC50=19.3024 μM	SANGER
KYSE-270	Growth Inhibition Assay			IC50=20.0217 μM	SANGER
HL-60	Growth Inhibition Assay			IC50=20.0941 μM	SANGER
Mo-T	Growth Inhibition Assay			IC50=20.1665 μM	SANGER
NCI-H1355	Growth Inhibition Assay			IC50=20.3374 μM	SANGER
HT-1080	Growth Inhibition Assay			IC50=20.5497 μM	SANGER
MIA-PaCa-2	Growth Inhibition Assay			IC50=20.6883 μM	SANGER
NCI-H441	Growth Inhibition Assay			IC50=20.7379 μM	SANGER
LCLC-97TM1	Growth Inhibition Assay			IC50=20.8134 μM	SANGER
HT-3	Growth Inhibition Assay			IC50=21.5631 μM	SANGER
22RV1	Growth Inhibition Assay			IC50=21.5685 μM	SANGER
LK-2	Growth Inhibition Assay			IC50=21.5953 μM	SANGER
CW-2	Growth Inhibition Assay			IC50=21.6069 μM	SANGER
KYSE-510	Growth Inhibition Assay			IC50=21.6095 μM	SANGER
CGTH-W-1	Growth Inhibition Assay			IC50=21.7166 μM	SANGER
NCI-H661	Growth Inhibition Assay			IC50=22.034 μM	SANGER
KU-19-19	Growth Inhibition Assay			IC50=22.1697 μM	SANGER
NCI-H2122	Growth Inhibition Assay			IC50=22.2432 μM	SANGER
NCI-H526	Growth Inhibition Assay			IC50=22.3895 μM	SANGER
NCI-H69	Growth Inhibition Assay			IC50=441.083 μM	SANGER
HCC38	Growth Inhibition Assay			IC50=401.593 μM	SANGER
NCI-H2052	Growth Inhibition Assay			IC50=398.472 μM	SANGER
NB17	Growth Inhibition Assay			IC50=392.596 μM	SANGER
SBC-5	Growth Inhibition Assay			IC50=386.985 μM	SANGER
K-562	Growth Inhibition Assay			IC50=383.36 μM	SANGER
T84	Growth Inhibition Assay			IC50=374.712 μM	SANGER
LU-135	Growth Inhibition Assay			IC50=367.035 μM	SANGER
TE-9	Growth Inhibition Assay			IC50=363.589 μM	SANGER
IST-SL1	Growth Inhibition Assay			IC50=347.401 μM	SANGER
BE-13	Growth Inhibition Assay			IC50=344.167 μM	SANGER
NCI-H1993	Growth Inhibition Assay			IC50=342.365 μM	SANGER
MOLT-13	Growth Inhibition Assay			IC50=342.326 μM	SANGER
NCI-H630	Growth Inhibition Assay			IC50=332.294 μM	SANGER
KP-N-YN	Growth Inhibition Assay			IC50=341.123 μM	SANGER
C3A	Growth Inhibition Assay			IC50=311.802 μM	SANGER
HEL	Growth Inhibition Assay			IC50=309.983 μM	SANGER
NCI-H810	Growth Inhibition Assay			IC50=310.57 μM	SANGER
LU-65	Growth Inhibition Assay			IC50=304.32 μM	SANGER
L-428	Growth Inhibition Assay			IC50=297.616 μM	SANGER
FADU	Growth Inhibition Assay			IC50=297.51 μM	SANGER
IGR-1	Growth Inhibition Assay			IC50=295.659 μM	SANGER
HDLM-2	Growth Inhibition Assay			IC50=294.409 μM	SANGER
C8166	Growth Inhibition Assay			IC50=278.506 μM	SANGER
TGBC11TKB	Growth Inhibition Assay			IC50=278.178 μM	SANGER
RERF-LC-MS	Growth Inhibition Assay			IC50=276.007 μM	SANGER
COLO-680N	Growth Inhibition Assay			IC50=272.527 μM	SANGER
NB6	Growth Inhibition Assay			IC50=270.1 μM	SANGER
GAK	Growth Inhibition Assay			IC50=253.002 μM	SANGER
RPMI-8866	Growth Inhibition Assay			IC50=249.27 μM	SANGER
NCI-H2347	Growth Inhibition Assay			IC50=247.713 μM	SANGER
LS-1034	Growth Inhibition Assay			IC50=246.266 μM	SANGER
SH-4	Growth Inhibition Assay			IC50=246.09 μM	SANGER
CCRF-CEM	Growth Inhibition Assay			IC50=243.795 μM	SANGER
COLO-320-HSR	Growth Inhibition Assay			IC50=216.125 μM	SANGER
KNS-42	Growth Inhibition Assay			IC50=216.574 μM	SANGER
RCM-1	Growth Inhibition Assay			IC50=214.762 μM	SANGER
DBTRG-05MG	Growth Inhibition Assay			IC50=207.909 μM	SANGER
SW982	Growth Inhibition Assay			IC50=207.948 μM	SANGER
SW1116	Growth Inhibition Assay			IC50=207.077 μM	SANGER
HuCCT1	Growth Inhibition Assay			IC50=204.208 μM	SANGER
NCI-H650	Growth Inhibition Assay			IC50=202.103 μM	SANGER
COLO-678	Growth Inhibition Assay			IC50=201.45 μM	SANGER
HT-29	Growth Inhibition Assay			IC50=201.212 μM	SANGER
SCC-9	Growth Inhibition Assay			IC50=191 μM	SANGER
KYSE-150	Growth Inhibition Assay			IC50=191.888 μM	SANGER
OVCAR-4	Growth Inhibition Assay			IC50=188.333 μM	SANGER
NCI-SNU-5	Growth Inhibition Assay			IC50=186.84 μM	SANGER
CAL-72	Growth Inhibition Assay			IC50=185.054 μM	SANGER
NCI-H82	Growth Inhibition Assay			IC50=180.165 μM	SANGER
MZ7-mel	Growth Inhibition Assay			IC50=178.467 μM	SANGER
no-10	Growth Inhibition Assay			IC50=178.134 μM	SANGER
MDA-MB-231	Growth Inhibition Assay			IC50=177.503 μM	SANGER
HCE-4	Growth Inhibition Assay			IC50=166.845 μM	SANGER
NY	Growth Inhibition Assay			IC50=165.314 μM	SANGER
A673	Growth Inhibition Assay			IC50=161.705 μM	SANGER
SAS	Growth Inhibition Assay			IC50=162.678 μM	SANGER
Capan-2	Growth Inhibition Assay			IC50=160.553 μM	SANGER
KU812	Growth Inhibition Assay			IC50=158.674 μM	SANGER
NCI-H1304	Growth Inhibition Assay			IC50=154.694 μM	SANGER
CAPAN-1	Growth Inhibition Assay			IC50=153.064 μM	SANGER
BEN	Growth Inhibition Assay			IC50=153.928 μM	SANGER
KYSE-450	Growth Inhibition Assay			IC50=151.539 μM	SANGER
GT3TKB	Growth Inhibition Assay			IC50=149.928 μM	SANGER
SK-MEL-3	Growth Inhibition Assay			IC50=147.878 μM	SANGER
OVCAR-8	Growth Inhibition Assay			IC50=145.636 μM	SANGER
CP50-MEL-B	Growth Inhibition Assay			IC50=144.501 μM	SANGER
COR-L88	Growth Inhibition Assay			IC50=142.14 μM	SANGER
Ca9-22	Growth Inhibition Assay			IC50=139.833 μM	SANGER
HCT-116	Growth Inhibition Assay			IC50=137.217 μM	SANGER
LB2518-MEL	Growth Inhibition Assay			IC50=135.993 μM	SANGER
U-87-MG	Growth Inhibition Assay			IC50=133.604 μM	SANGER
NCI-H2087	Growth Inhibition Assay			IC50=131.483 μM	SANGER
NCI-H1651	Growth Inhibition Assay			IC50=131.243 μM	SANGER
A2780	Growth Inhibition Assay			IC50=128.988 μM	SANGER
BALL-1	Growth Inhibition Assay			IC50=126.23 μM	SANGER
COLO-679	Growth Inhibition Assay			IC50=126.753 μM	SANGER
SF268	Growth Inhibition Assay			IC50=126.158 μM	SANGER
SN12C	Growth Inhibition Assay			IC50=124.176 μM	SANGER
NCI-H1770	Growth Inhibition Assay			IC50=125.514 μM	SANGER
NCI-H2452	Growth Inhibition Assay			IC50=122.21 μM	SANGER
SK-MEL-30	Growth Inhibition Assay			IC50=123.244 μM	SANGER
ML-2	Growth Inhibition Assay			IC50=121.676 μM	SANGER
SW1990	Growth Inhibition Assay			IC50=120.951 μM	SANGER
D-392MG	Growth Inhibition Assay			IC50=117.398 μM	SANGER
NCI-H1793	Growth Inhibition Assay			IC50=109.28 μM	SANGER
GOTO	Growth Inhibition Assay			IC50=107.777 μM	SANGER
HLE	Growth Inhibition Assay			IC50=105.282 μM	SANGER
NCI-H209	Growth Inhibition Assay			IC50=100.121 μM	SANGER
SW684	Growth Inhibition Assay			IC50=98.6654 μM	SANGER
NCI-H2029	Growth Inhibition Assay			IC50=96.9566 μM	SANGER
NCI-H1792	Growth Inhibition Assay			IC50=96.8992 μM	SANGER
SCH	Growth Inhibition Assay			IC50=96.3877 μM	SANGER
COLO-792	Growth Inhibition Assay			IC50=95.2564 μM	SANGER
SK-MEL-1	Growth Inhibition Assay			IC50=92.9106 μM	SANGER
TE-10	Growth Inhibition Assay			IC50=91.5611 μM	SANGER
KYSE-410	Growth Inhibition Assay			IC50=91.4042 μM	SANGER
KP-N-YS	Growth Inhibition Assay			IC50=89.9028 μM	SANGER
IST-MEL1	Growth Inhibition Assay			IC50=86.8872 μM	SANGER
KARPAS-299	Growth Inhibition Assay			IC50=86.1977 μM	SANGER
NCI-H1581	Growth Inhibition Assay			IC50=85.4641 μM	SANGER
DoTc2-4510	Growth Inhibition Assay			IC50=84.2185 μM	SANGER
KY821	Growth Inhibition Assay			IC50=84.0892 μM	SANGER
HTC-C3	Growth Inhibition Assay			IC50=83.4702 μM	SANGER
HSC-3	Growth Inhibition Assay			IC50=83.3071 μM	SANGER
PANC-08-13	Growth Inhibition Assay			IC50=81.1768 μM	SANGER
A3-KAW	Growth Inhibition Assay			IC50=80.2154 μM	SANGER
CAL-62	Growth Inhibition Assay			IC50=80.095 μM	SANGER
JAR	Growth Inhibition Assay			IC50=79.0546 μM	SANGER
KYSE-180	Growth Inhibition Assay			IC50=77.5454 μM	SANGER
PANC-10-05	Growth Inhibition Assay			IC50=77.4243 μM	SANGER
MC116	Growth Inhibition Assay			IC50=75.5708 μM	SANGER
U-266	Growth Inhibition Assay			IC50=75.4516 μM	SANGER
NCI-H1437	Growth Inhibition Assay			IC50=74.4048 μM	SANGER
NCI-H522	Growth Inhibition Assay			IC50=72.3413 μM	SANGER
COLO-668	Growth Inhibition Assay			IC50=71.8451 μM	SANGER
Mewo	Growth Inhibition Assay			IC50=71.505 μM	SANGER
KYSE-70	Growth Inhibition Assay			IC50=70.7835 μM	SANGER
LCLC-103H	Growth Inhibition Assay			IC50=70.6705 μM	SANGER
SK-HEP-1	Growth Inhibition Assay			IC50=69.9486 μM	SANGER
HuO-3N1	Growth Inhibition Assay			IC50=68.3238 μM	SANGER
SW620	Growth Inhibition Assay			IC50=66.2039 μM	SANGER
LB831-BLC	Growth Inhibition Assay			IC50=65.8481 μM	SANGER
MZ1-PC	Growth Inhibition Assay			IC50=65.5649 μM	SANGER
NCI-H1092	Growth Inhibition Assay			IC50=65.0095 μM	SANGER
KGN	Growth Inhibition Assay			IC50=64.5514 μM	SANGER
BHY	Growth Inhibition Assay			IC50=64.1245 μM	SANGER
C-33-A	Growth Inhibition Assay			IC50=64.0957 μM	SANGER
NCI-H596	Growth Inhibition Assay			IC50=62.7496 μM	SANGER
LS-411N	Growth Inhibition Assay			IC50=61.3903 μM	SANGER
HD-MY-Z	Growth Inhibition Assay			IC50=60.5294 μM	SANGER
647-V	Growth Inhibition Assay			IC50=60.1347 μM	SANGER
COLO-824	Growth Inhibition Assay			IC50=60.0719 μM	SANGER
TCCSUP	Growth Inhibition Assay			IC50=59.5279 μM	SANGER
JVM-2	Growth Inhibition Assay			IC50=58.9506 μM	SANGER
MHH-ES-1	Growth Inhibition Assay			IC50=58.4814 μM	SANGER
FTC-133	Growth Inhibition Assay			IC50=58.0969 μM	SANGER
NTERA-S-cl-D1	Growth Inhibition Assay			IC50=57.778 μM	SANGER
HPAF-II	Growth Inhibition Assay			IC50=56.4073 μM	SANGER
MKN7	Growth Inhibition Assay			IC50=56.0285 μM	SANGER
UACC-62	Growth Inhibition Assay			IC50=55.1046 μM	SANGER
IA-LM	Growth Inhibition Assay			IC50=54.6322 μM	SANGER
ChaGo-K-1	Growth Inhibition Assay			IC50=49.4793 μM	SANGER
HT55	Growth Inhibition Assay			IC50=49.1474 μM	SANGER
KYSE-520	Growth Inhibition Assay			IC50=48.4016 μM	SANGER
U-118-MG	Growth Inhibition Assay			IC50=48.3702 μM	SANGER
CAKI-1	Growth Inhibition Assay			IC50=48.2845 μM	SANGER
SW1573	Growth Inhibition Assay			IC50=47.3736 μM	SANGER
RO82-W-1	Growth Inhibition Assay			IC50=46.9822 μM	SANGER
KM12	Growth Inhibition Assay			IC50=45.9076 μM	SANGER
NCI-H1155	Growth Inhibition Assay			IC50=45.8967 μM	SANGER
TE-11	Growth Inhibition Assay			IC50=45.4842 μM	SANGER
PSN1	Growth Inhibition Assay			IC50=45.2548 μM	SANGER
SK-N-AS	Growth Inhibition Assay			IC50=43.6019 μM	SANGER
NCI-H1573	Growth Inhibition Assay			IC50=43.3477 μM	SANGER
Calu-6	Growth Inhibition Assay			IC50=43.2382 μM	SANGER
HCC1937	Growth Inhibition Assay			IC50=42.7843 μM	SANGER
UMC-11	Growth Inhibition Assay			IC50=41.263 μM	SANGER
HSC-2	Growth Inhibition Assay			IC50=40.9113 μM	SANGER
BxPC-3	Growth Inhibition Assay			IC50=40.5686 μM	SANGER
COLO-741	Growth Inhibition Assay			IC50=40.1304 μM	SANGER
NOMO-1	Growth Inhibition Assay			IC50=39.8274 μM	SANGER
LC-2-ad	Growth Inhibition Assay			IC50=39.5512 μM	SANGER
MG-63	Growth Inhibition Assay			IC50=39.3424 μM	SANGER
EFO-21	Growth Inhibition Assay			IC50=38.9349 μM	SANGER
SW1417	Growth Inhibition Assay			IC50=38.0552 μM	SANGER
DU-4475	Growth Inhibition Assay			IC50=36.9033 μM	SANGER
CaR-1	Growth Inhibition Assay			IC50=33.9822 μM	SANGER
HT-144	Growth Inhibition Assay			IC50=33.863 μM	SANGER
LU-139	Growth Inhibition Assay			IC50=33.6605 μM	SANGER
SW626	Growth Inhibition Assay			IC50=33.1776 μM	SANGER
COR-L23	Growth Inhibition Assay			IC50=32.9073 μM	SANGER
DB	Growth Inhibition Assay			IC50=30.4942 μM	SANGER
ZR-75-30	Growth Inhibition Assay			IC50=30.2383 μM	SANGER
GI-1	Growth Inhibition Assay			IC50=27.721 μM	SANGER
SK-PN-DW	Growth Inhibition Assay			IC50=27.6012 μM	SANGER
NCI-H226	Growth Inhibition Assay			IC50=27.4578 μM	SANGER
SW948	Growth Inhibition Assay			IC50=27.1344 μM	SANGER
HuP-T4	Growth Inhibition Assay			IC50=27.0879 μM	SANGER
SNU-449	Growth Inhibition Assay			IC50=27.0803 μM	SANGER
SW962	Growth Inhibition Assay			IC50=26.5021 μM	SANGER
CHP-134	Growth Inhibition Assay			IC50=26.3867 μM	SANGER
GMS-10	Growth Inhibition Assay			IC50=26.2353 μM	SANGER
NUGC-3	Growth Inhibition Assay			IC50=26.2103 μM	SANGER
NB13	Growth Inhibition Assay			IC50=26.0949 μM	SANGER
MPP-89	Growth Inhibition Assay			IC50=25.0458 μM	SANGER
SK-MEL-2	Growth Inhibition Assay			IC50=23.8133 μM	SANGER
ES4	Growth Inhibition Assay			IC50=23.4232 μM	SANGER
NCI-H1650	Growth Inhibition Assay			IC50=22.764 μM	SANGER
SK-N-MC	Function assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	29435139
NB-EBc1	Function assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells	29435139
LAN-5	Function assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells	29435139
Rh18	Function assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells	29435139
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生物活性

製品説明

特性

The first allosteric small molecule inhibitor of Akt to enter clinical development.

Targets

Akt1 ^[1] (Cell-free assay)	Akt2 ^[1] (Cell-free assay)	Akt3 ^[1] (Cell-free assay)
8 nM	12 nM	65 nM

In Vitro
In vitro	MK-2206 is an allosteric inhibitor and is activated by the pleckstrin homology domain. MK-2206 inhibits auto-phosphorylation of both Akt T308 and S473. MK-2206 also prevents Akt-mediated phosphorylation of downstream signaling molecules, including TSC2, PRAS40 and ribosomal S6 proteins. ^[1] MK-2206 inhibits Ras wild-type (WT) cell lines (A431, HCC827, and NCI-H292) more potently when compared to Ras-mutant cell lines (NCI-H358, NCI-H23, NCI-H1299, and Calu-6). MK-2206 also shows synergistic responses in combination with cytotoxic agents in lung NCI-H460 or ovarian A2780 tumor cells. ^[2] MK-2206 or siRNA-mediated Akt inhibition strongly activates autophagy in human glioma cells. However, eukaryotic elongation factor-2 (eEF-2) silencing suppresses MK-2206-induced-autophagy, with a promotion of apoptotic cell death. ^[3]
Kinase Assay	Akt kinases assay
Kinase Assay	Akt kinases are assayed by a GSK-derived biotinylated peptide substrate. The extent of peptide phosphorylation is determined by Homogeneous Time Resolved Fluorescence (HTRF) using a lanthanide chelate (Lance)-coupled monoclonal antibody specific for the phosphopeptide in combination with a streptavidin-linked allophycocyanin (SA-APC) fluorophore which will bind to the biotin moiety on the peptide. When the Lance and APC are in proximity, a non-radiative energy transfer takes place from the Lance to the APC, followed by emission of light from APC at 655 nm. 10X assay buffer: 500 mM HEPES, pH7.5, 1% PEG, 16.6 mM EDTA, 1 mM EGTA, 1% BSA, 20 mM 9-glycerol phosphate; Quench buffer 50 mM HEPES pH 7.3, 16.6 mM EDTA, 0.1% BSA, 0.1% Triton X-100, 0.17 nM labeled monoclonal antibody, 0.0067 mg/mL SA-APC; ATP/MgCl₂ working solution: 1X Assay buffer, 1 mM DTT, 1X PIC, 5% glycerol, active Akt; Peptide working solution: 1X Assay buffer, 1 mM DTT, 1X PIC, 5% glycerol, 2 TM GSK biotinylated peptide. The reaction is assembled by adding 16 µL of ATP/MgCl₂ working solution to the appropriate wells. MK-2206 or vehicle (1.0 µL) is added followed by 10 µL of peptide working solution. The reaction is started by adding 13 μL of the enzyme working solution and mixing. The reaction is allowed to proceed for 50 min and then stopped by the addition of 60 µL HTRF quench buffer. The stopped reactions are incubated at room temperature for at least 30 min and then read in the instrument.
細胞実験	細胞株	A431, HCC827, NCI-H292, NCI-H358, NCI-H23, NCI-H1299, Calu-6 and NCI-H460 cells
	濃度	0, 0.3, 1 and 3 μM
	反応時間	72 or 96 hours
	実験の流れ	MK-2206 is dissolved in DMSO as a stock solution and diluted by culture media before use. Cells are seeded at a density of 2-3 × 10³ in 96-well plates and incubated for 24 hours. Then MK-2206 (0, 0.3, 1 and 3 μM) is added to the cells. Cell proliferation is determined after 72 or 96 hours.
実験結果図	Methods	Biomarkers	結果図	PMID
	Western blot	p-AKT(T308) / p-AKT(S473) / pGSK3β(S9) / pFOXO1 / pPRAS(T246) / pBAD / pS6K(T389) / p4E-BP1		22932669
	Growth inhibition assay	Cell viability		24665203
	Immunofluorescence	LC3 CFTR/LC3 HMGA2		24490764
	ELISA	VEGFA		29449553

In Vivo
In Vivo	MK-2206 shows 60% TGI and inhibits more than 70 % of phospho-Akt1/2 (T308 and S473) in A2780 ovarian cancer xenografts at a dose of 240 mg/kg. ^[1] MK-2206 exhibits significant antitumor activity in NCI-H292 xenograft in combination. ^[2]
動物実験	動物モデル	SK-OV-3, NCI-H292, HCC70, PC-3, and NCI-H460 models in male CD1-nude mice
	投与量	120 mg/kg
	投与経路	Orally administered

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試験 (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT01480154	Active not recruiting	Advanced Malignant Solid Neoplasm\|Stage III Cutaneous Melanoma AJCC v7\|Stage III Prostate Cancer AJCC v7\|Stage III Renal Cell Cancer AJCC v7\|Stage IIIA Cutaneous Melanoma AJCC v7\|Stage IIIB Cutaneous Melanoma AJCC v7\|Stage IIIC Cutaneous Melanoma AJCC v7\|Stage IV Cutaneous Melanoma AJCC v6 and v7\|Stage IV Prostate Cancer AJCC v7\|Stage IV Renal Cell Cancer AJCC v7	National Cancer Institute (NCI)	November 23 2011	Phase 1
NCT01466868	Terminated	Diffuse Large B Cell Lymphoma	Centre Leon Berard\|National Cancer Institute France	November 2011	Phase 2

参考
[1] Yan L, AACR Annual Meeting 2009: Abstract Number: DDT01-1. [2] Hirai H, et al. Mol Cancer Therapy, 2010, 9(7), 1956-1967. [3] Cheng Y, et al, Cancer Res, 2011, 71(7), 2654-2663. [4] WO2008070016 (A2) + 展開

参考

[4] WO2008070016 (A2)

+ 展開

化学情報

分子量	480.39	化学式	C₂₅H₂₁N₅O.2HCl
CAS No.	1032350-13-2	SDF	Download MK-2206 2HCl SDFをダウンロードする
Smiles	C1CC(C1)(C2=CC=C(C=C2)C3=C(C=C4C(=N3)C=CN5C4=NNC5=O)C6=CC=CC=C6)N.Cl.Cl
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1年-80°Cin solvent
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	１ケ月-20°Cin solvent

In vitro
Batch:

DMSO : 25 mg/mL ( (52.04 mM)；吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Water : 2 mg/mL

Ethanol : Insoluble

モル濃度計算器

in vivo Batch: Add solvents to the product individually and in order.					投与溶液組成計算機
	Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	0.63mg/ml (1.31mM)	Taking the 1 mL working solution as an example, add 50 μL of 12.5 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to make it clear. Volume up to 1 mL. The mixed solution should be used immediately for optimal results.	投与溶液組成計算機
Clear solution	5% DMSO 1 95% corn oil	0.4mg/ml (0.83mM)	Taking the 1 mL working solution as an example, add 50 μL of 8 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	4.8mg/ml (9.99mM)	Taking the 1 mL working solution as an example, add 50 μL of 96 mg/ml clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

実験計算

モル濃度計算器

質量	濃度	体積	分子量
=	×	×

希釈計算器分子量計算器

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

投与量 mg/kg 動物平均体重 g 投与体積（動物毎）μL 動物数匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH₂O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

技術サポート

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よくある質問（FAQ）

質問1:
What is your recommendation for preparing the solution and how would you deliver it to the mice (i.p. or gavage)?

回答
You can resuspend MK-2206 in 15% Captisol at up to 17mg/ml. It's a suspension and is for oral gavage use only.

質問2:
I would want to know if MK-2206 could cross the blood brain barrier?

回答
MK-2206 can cross BBB based on the following reference: https://clinicaltrials.gov/ct2/show/NCT01249105.

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