Tanespimycin (17-AAG)

別名:CP127374, NSC-330507, KOS 953

Tanespimycin (17-AAG, CP127374, NSC-330507, KOS 953) is a potent HSP90 inhibitor with IC50 of 5 nM in a cell-free assay, having a 100-fold higher binding affinity for HSP90 derived from tumour cells than HSP90 from normal cells. Tanespimycin (17-AAG) induces apoptosis, necrosis, autophagy and mitophagy. Phase 3.

Tanespimycin (17-AAG)化学構造

CAS No. 75747-14-7

サイズ 価格(税別) 在庫状況
10mM (1mL in DMSO) JPY 29500 国内在庫あり
JPY 22000 国内在庫あり
JPY 44500 国内在庫あり
JPY 119500 国内在庫あり
JPY 557800 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]
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文献中Selleckの製品使用例(140)

製品安全説明書

現在のバッチを見る: 純度: 99.92%
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Tanespimycin (17-AAG)関連製品

シグナル伝達経路

HSP (HSP90)阻害剤の選択性比較

Cell Data

Cell Lines Assay Type Concentration Incubation Time 活性情報 PMID
C2BBe1 Growth Inhibition Assay IC50=0.2219 μM SANGER
TE-9 Growth Inhibition Assay IC50=0.21786 μM SANGER
MFE-280 Growth Inhibition Assay IC50=0.21298 μM SANGER
769-P Growth Inhibition Assay IC50=0.2128 μM SANGER
HPAF-II Growth Inhibition Assay IC50=0.21264 μM SANGER
A172 Growth Inhibition Assay IC50=0.21022 μM SANGER
AM-38 Growth Inhibition Assay IC50=0.20848 μM SANGER
DoTc2-4510 Growth Inhibition Assay IC50=0.20769 μM SANGER
S-117 Growth Inhibition Assay IC50=0.20564 μM SANGER
U031 Growth Inhibition Assay IC50=0.20547 μM SANGER
SBC-5 Growth Inhibition Assay IC50=0.20118 μM SANGER
NCI-H1650 Growth Inhibition Assay IC50=0.20057 μM SANGER
COLO-680N Growth Inhibition Assay IC50=0.19364 μM SANGER
Capan-2 Growth Inhibition Assay IC50=0.19256 μM SANGER
RVH-421 Growth Inhibition Assay IC50=0.19116 μM SANGER
RD Growth Inhibition Assay IC50=0.19113 μM SANGER
CAL-27 Growth Inhibition Assay IC50=0.19022 μM SANGER
BCPAP Growth Inhibition Assay IC50=0.18872 μM SANGER
JEG-3 Growth Inhibition Assay IC50=0.18705 μM SANGER
NCI-H1395 Growth Inhibition Assay IC50=0.18682 μM SANGER
DEL Growth Inhibition Assay IC50=0.1845 μM SANGER
IGROV-1 Growth Inhibition Assay IC50=0.18443 μM SANGER
KNS-81-FD Growth Inhibition Assay IC50=0.18394 μM SANGER
LK-2 Growth Inhibition Assay IC50=0.18303 μM SANGER
KYSE-520 Growth Inhibition Assay IC50=0.182 μM SANGER
MDA-MB-157 Growth Inhibition Assay IC50=0.18082 μM SANGER
SCC-4 Growth Inhibition Assay IC50=0.17777 μM SANGER
KOSC-2 Growth Inhibition Assay IC50=0.17734 μM SANGER
NCI-H650 Growth Inhibition Assay IC50=0.17682 μM SANGER
MZ7-mel Growth Inhibition Assay IC50=0.17649 μM SANGER
SK-OV-3 Growth Inhibition Assay IC50=0.17571 μM SANGER
NCI-H2170 Growth Inhibition Assay IC50=0.17536 μM SANGER
NCI-H2087 Growth Inhibition Assay IC50=0.17368 μM SANGER
BB30-HNC Growth Inhibition Assay IC50=0.1733 μM SANGER
COLO-824 Growth Inhibition Assay IC50=0.17294 μM SANGER
U-2-OS Growth Inhibition Assay IC50=0.17173 μM SANGER
HT-1376 Growth Inhibition Assay IC50=0.16936 μM SANGER
SCC-9 Growth Inhibition Assay IC50=0.16716 μM SANGER
OC-314 Growth Inhibition Assay IC50=0.1669 μM SANGER
FTC-133 Growth Inhibition Assay IC50=0.1654 μM SANGER
SW1088 Growth Inhibition Assay IC50=0.16413 μM SANGER
NCI-H1299 Growth Inhibition Assay IC50=0.16285 μM SANGER
HCC1937 Growth Inhibition Assay IC50=0.16275 μM SANGER
CAL-62 Growth Inhibition Assay IC50=0.16169 μM SANGER
BxPC-3 Growth Inhibition Assay IC50=0.15966 μM SANGER
ETK-1 Growth Inhibition Assay IC50=0.159 μM SANGER
786-0 Growth Inhibition Assay IC50=0.15381 μM SANGER
NCI-H1648 Growth Inhibition Assay IC50=0.15232 μM SANGER
AsPC-1 Growth Inhibition Assay IC50=0.15225 μM SANGER
639-V Growth Inhibition Assay IC50=0.15013 μM SANGER
Mewo Growth Inhibition Assay IC50=0.14889 μM SANGER
NCI-H2347 Growth Inhibition Assay IC50=0.14839 μM SANGER
SW1573 Growth Inhibition Assay IC50=0.14758 μM SANGER
HCC1419 Growth Inhibition Assay IC50=0.14576 μM SANGER
GI-1 Growth Inhibition Assay IC50=0.14558 μM SANGER
NUGC-3 Growth Inhibition Assay IC50=0.14478 μM SANGER
MPP-89 Growth Inhibition Assay IC50=0.14125 μM SANGER
LC-2-ad Growth Inhibition Assay IC50=0.14121 μM SANGER
GP5d Growth Inhibition Assay IC50=0.14104 μM SANGER
RT-112 Growth Inhibition Assay IC50=0.14035 μM SANGER
NCI-H2452 Growth Inhibition Assay IC50=0.13956 μM SANGER
LB831-BLC Growth Inhibition Assay IC50=0.13883 μM SANGER
SK-MEL-24 Growth Inhibition Assay IC50=0.1387 μM SANGER
VMRC-RCZ Growth Inhibition Assay IC50=0.13762 μM SANGER
GAK Growth Inhibition Assay IC50=0.13567 μM SANGER
BPH-1 Growth Inhibition Assay IC50=0.1341 μM SANGER
PC-14 Growth Inhibition Assay IC50=0.13211 μM SANGER
NCI-H292 Growth Inhibition Assay IC50=0.1311 μM SANGER
HuP-T4 Growth Inhibition Assay IC50=0.12943 μM SANGER
CAMA-1 Growth Inhibition Assay IC50=0.12924 μM SANGER
A375 Growth Inhibition Assay IC50=0.12778 μM SANGER
NCI-H1666 Growth Inhibition Assay IC50=0.12774 μM SANGER
SAS Growth Inhibition Assay IC50=0.1269 μM SANGER
EW-3 Growth Inhibition Assay IC50=0.12661 μM SANGER
SNB75 Growth Inhibition Assay IC50=0.12169 μM SANGER
NCI-H1437 Growth Inhibition Assay IC50=0.12157 μM SANGER
SW1990 Growth Inhibition Assay IC50=0.12157 μM SANGER
HMV-II Growth Inhibition Assay IC50=0.1202 μM SANGER
COLO-829 Growth Inhibition Assay IC50=0.12005 μM SANGER
RXF393 Growth Inhibition Assay IC50=0.11982 μM SANGER
NCI-H28 Growth Inhibition Assay IC50=0.11817 μM SANGER
BT-549 Growth Inhibition Assay IC50=0.11799 μM SANGER
OMC-1 Growth Inhibition Assay IC50=0.11797 μM SANGER
RKO Growth Inhibition Assay IC50=0.11764 μM SANGER
KALS-1 Growth Inhibition Assay IC50=0.11393 μM SANGER
SH-4 Growth Inhibition Assay IC50=0.11356 μM SANGER
SK-MEL-28 Growth Inhibition Assay IC50=0.11321 μM SANGER
TE-8 Growth Inhibition Assay IC50=0.11264 μM SANGER
COLO-679 Growth Inhibition Assay IC50=0.11211 μM SANGER
TGBC11TKB Growth Inhibition Assay IC50=0.10903 μM SANGER
HD-MY-Z Growth Inhibition Assay IC50=0.10873 μM SANGER
NKM-1 Growth Inhibition Assay IC50=0.10666 μM SANGER
BB65-RCC Growth Inhibition Assay IC50=0.10554 μM SANGER
MMAC-SF Growth Inhibition Assay IC50=0.10531 μM SANGER
U251 Growth Inhibition Assay IC50=0.10525 μM SANGER
SiHa Growth Inhibition Assay IC50=0.10486 μM SANGER
G-401 Growth Inhibition Assay IC50=0.10353 μM SANGER
U-87-MG Growth Inhibition Assay IC50=0.10307 μM SANGER
NCI-H1581 Growth Inhibition Assay IC50=0.1029 μM SANGER
PANC-03-27 Growth Inhibition Assay IC50=0.10286 μM SANGER
A498 Growth Inhibition Assay IC50=0.1018 μM SANGER
SN12C Growth Inhibition Assay IC50=0.10107 μM SANGER
LB2241-RCC Growth Inhibition Assay IC50=0.10054 μM SANGER
EFO-27 Growth Inhibition Assay IC50=0.09997 μM SANGER
NCI-H2122 Growth Inhibition Assay IC50=0.09745 μM SANGER
MCF7 Growth Inhibition Assay IC50=0.09677 μM SANGER
NCI-H1792 Growth Inhibition Assay IC50=0.09618 μM SANGER
8-MG-BA Growth Inhibition Assay IC50=0.09472 μM SANGER
D-247MG Growth Inhibition Assay IC50=0.09455 μM SANGER
KYSE-180 Growth Inhibition Assay IC50=0.09262 μM SANGER
TE-1 Growth Inhibition Assay IC50=0.09204 μM SANGER
SK-MEL-2 Growth Inhibition Assay IC50=0.0906 μM SANGER
M059J Growth Inhibition Assay IC50=0.09027 μM SANGER
LCLC-97TM1 Growth Inhibition Assay IC50=0.08728 μM SANGER
OVCAR-8 Growth Inhibition Assay IC50=0.08622 μM SANGER
HT-1080 Growth Inhibition Assay IC50=0.08439 μM SANGER
MKN45 Growth Inhibition Assay IC50=0.08219 μM SANGER
A431 Growth Inhibition Assay IC50=0.0821 μM SANGER
L-363 Growth Inhibition Assay IC50=0.08206 μM SANGER
TGBC1TKB Growth Inhibition Assay IC50=0.08043 μM SANGER
TE-11 Growth Inhibition Assay IC50=0.07996 μM SANGER
BFTC-909 Growth Inhibition Assay IC50=0.07969 μM SANGER
M14 Growth Inhibition Assay IC50=0.07913 μM SANGER
CAL-39 Growth Inhibition Assay IC50=0.07766 μM SANGER
HuO9 Growth Inhibition Assay IC50=0.07589 μM SANGER
HCC2998 Growth Inhibition Assay IC50=0.07347 μM SANGER
MEL-HO Growth Inhibition Assay IC50=0.07255 μM SANGER
A2058 Growth Inhibition Assay IC50=0.07228 μM SANGER
Hs-578-T Growth Inhibition Assay IC50=0.07208 μM SANGER
HCC1806 Growth Inhibition Assay IC50=0.07131 μM SANGER
SW620 Growth Inhibition Assay IC50=0.07026 μM SANGER
23132-87 Growth Inhibition Assay IC50=0.0695 μM SANGER
HT-29 Growth Inhibition Assay IC50=0.06919 μM SANGER
MV-4-11 Growth Inhibition Assay IC50=0.06803 μM SANGER
GMS-10 Growth Inhibition Assay IC50=0.06699 μM SANGER
SF539 Growth Inhibition Assay IC50=0.06681 μM SANGER
SW684 Growth Inhibition Assay IC50=0.06591 μM SANGER
HEC-1 Growth Inhibition Assay IC50=0.06588 μM SANGER
MZ2-MEL Growth Inhibition Assay IC50=0.06553 μM SANGER
SF295 Growth Inhibition Assay IC50=0.06452 μM SANGER
KM12 Growth Inhibition Assay IC50=0.06348 μM SANGER
NCI-H1755 Growth Inhibition Assay IC50=0.06341 μM SANGER
LU-99A Growth Inhibition Assay IC50=0.06237 μM SANGER
EPLC-272H Growth Inhibition Assay IC50=0.06205 μM SANGER
TCCSUP Growth Inhibition Assay IC50=0.05964 μM SANGER
GT3TKB Growth Inhibition Assay IC50=0.05942 μM SANGER
LOXIMVI Growth Inhibition Assay IC50=0.05872 μM SANGER
5637 Growth Inhibition Assay IC50=0.0574 μM SANGER
YH-13 Growth Inhibition Assay IC50=0.05722 μM SANGER
NCI-H2030 Growth Inhibition Assay IC50=0.05414 μM SANGER
LB1047-RCC Growth Inhibition Assay IC50=0.05296 μM SANGER
HuO-3N1 Growth Inhibition Assay IC50=0.05237 μM SANGER
KYSE-150 Growth Inhibition Assay IC50=0.05235 μM SANGER
YKG-1 Growth Inhibition Assay IC50=0.05071 μM SANGER
SW48 Growth Inhibition Assay IC50=0.05039 μM SANGER
AN3-CA Growth Inhibition Assay IC50=0.05 μM SANGER
SKG-IIIa Growth Inhibition Assay IC50=0.04986 μM SANGER
COR-L88 Growth Inhibition Assay IC50=0.04912 μM SANGER
DOK Growth Inhibition Assay IC50=0.04902 μM SANGER
G-402 Growth Inhibition Assay IC50=0.04789 μM SANGER
KYSE-410 Growth Inhibition Assay IC50=0.04772 μM SANGER
KP-4 Growth Inhibition Assay IC50=0.04753 μM SANGER
KYSE-510 Growth Inhibition Assay IC50=0.04649 μM SANGER
PSN1 Growth Inhibition Assay IC50=0.04603 μM SANGER
CaR-1 Growth Inhibition Assay IC50=0.04549 μM SANGER
BT-474 Growth Inhibition Assay IC50=0.045 μM SANGER
MEL-JUSO Growth Inhibition Assay IC50=0.04475 μM SANGER
VA-ES-BJ Growth Inhibition Assay IC50=0.04447 μM SANGER
H9 Growth Inhibition Assay IC50=0.04371 μM SANGER
HN Growth Inhibition Assay IC50=0.04272 μM SANGER
BB49-HNC Growth Inhibition Assay IC50=0.04243 μM SANGER
Detroit562 Growth Inhibition Assay IC50=0.04239 μM SANGER
SW780 Growth Inhibition Assay IC50=0.04203 μM SANGER
ACN Growth Inhibition Assay IC50=0.04162 μM SANGER
T98G Growth Inhibition Assay IC50=0.04103 μM SANGER
HO-1-N-1 Growth Inhibition Assay IC50=0.04021 μM SANGER
TYK-nu Growth Inhibition Assay IC50=0.03985 μM SANGER
SW962 Growth Inhibition Assay IC50=0.03945 μM SANGER
Becker Growth Inhibition Assay IC50=0.03885 μM SANGER
DSH1 Growth Inhibition Assay IC50=0.03807 μM SANGER
WM-115 Growth Inhibition Assay IC50=0.03762 μM SANGER
VM-CUB-1 Growth Inhibition Assay IC50=0.03657 μM SANGER
SK-MES-1 Growth Inhibition Assay IC50=0.03606 μM SANGER
OVCAR-5 Growth Inhibition Assay IC50=0.0348 μM SANGER
CP50-MEL-B Growth Inhibition Assay IC50=0.0345 μM SANGER
GAMG Growth Inhibition Assay IC50=0.03435 μM SANGER
MDA-MB-175-VII Growth Inhibition Assay IC50=0.03354 μM SANGER
D-336MG Growth Inhibition Assay IC50=0.03309 μM SANGER
SK-UT-1 Growth Inhibition Assay IC50=0.03178 μM SANGER
HT-144 Growth Inhibition Assay IC50=0.03093 μM SANGER
H4 Growth Inhibition Assay IC50=0.0309 μM SANGER
SK-LU-1 Growth Inhibition Assay IC50=0.03082 μM SANGER
OE19 Growth Inhibition Assay IC50=0.03077 μM SANGER
SW982 Growth Inhibition Assay IC50=0.02999 μM SANGER
ME-180 Growth Inhibition Assay IC50=0.02891 μM SANGER
D-263MG Growth Inhibition Assay IC50=0.02786 μM SANGER
NCI-H23 Growth Inhibition Assay IC50=0.02665 μM SANGER
CHP-212 Growth Inhibition Assay IC50=0.02628 μM SANGER
NCI-N87 Growth Inhibition Assay IC50=0.02593 μM SANGER
NCI-H720 Growth Inhibition Assay IC50=0.02546 μM SANGER
A2780 Growth Inhibition Assay IC50=0.02531 μM SANGER
HCC2218 Growth Inhibition Assay IC50=0.02494 μM SANGER
CGTH-W-1 Growth Inhibition Assay IC50=0.02349 μM SANGER
DU-4475 Growth Inhibition Assay IC50=0.02261 μM SANGER
CHL-1 Growth Inhibition Assay IC50=0.02251 μM SANGER
A204 Growth Inhibition Assay IC50=0.02249 μM SANGER
NCI-H460 Growth Inhibition Assay IC50=0.01974 μM SANGER
AGS Growth Inhibition Assay IC50=0.01938 μM SANGER
TI-73 Growth Inhibition Assay IC50=0.01796 μM SANGER
MDA-MB-361 Growth Inhibition Assay IC50=0.01495 μM SANGER
CAL-51 Growth Inhibition Assay IC50=0.01405 μM SANGER
KS-1 Growth Inhibition Assay IC50=0.01355 μM SANGER
MIA-PaCa-2 Growth Inhibition Assay IC50=0.01009 μM SANGER
HSC-3 Growth Inhibition Assay IC50=0.00929 μM SANGER
RPMI-7951 Growth Inhibition Assay IC50=0.00717 μM SANGER
HGC-27 Growth Inhibition Assay IC50=0.0051 μM SANGER
LXF-289 Growth Inhibition Assay IC50=0.00419 μM SANGER
D-566MG Growth Inhibition Assay IC50=0.0039 μM SANGER
C32 Growth Inhibition Assay IC50=0.00304 μM SANGER
FADU Growth Inhibition Assay IC50=0.00209 μM SANGER
NCI-SNU-1 Growth Inhibition Assay IC50=0.00207 μM SANGER
IST-MEL1 Growth Inhibition Assay IC50=0.000407 μM SANGER
A549 Growth Inhibition Assay IC50=0.000303 μM SANGER
EoL-1-cell Growth Inhibition Assay IC50=0.22203 μM SANGER
G-361 Growth Inhibition Assay IC50=0.22682 μM SANGER
KYSE-270 Growth Inhibition Assay IC50=0.23084 μM SANGER
TK10 Growth Inhibition Assay IC50=0.23117 μM SANGER
ML-2 Growth Inhibition Assay IC50=0.23119 μM SANGER
MHH-ES-1 Growth Inhibition Assay IC50=0.23681 μM SANGER
BHY Growth Inhibition Assay IC50=0.23691 μM SANGER
LS-513 Growth Inhibition Assay IC50=0.23961 μM SANGER
COLO-678 Growth Inhibition Assay IC50=0.24044 μM SANGER
NCI-H747 Growth Inhibition Assay IC50=0.24169 μM SANGER
K5 Growth Inhibition Assay IC50=0.2438 μM SANGER
OS-RC-2 Growth Inhibition Assay IC50=0.24509 μM SANGER
KINGS-1 Growth Inhibition Assay IC50=0.24529 μM SANGER
SCC-25 Growth Inhibition Assay IC50=0.24563 μM SANGER
CAPAN-1 Growth Inhibition Assay IC50=0.24783 μM SANGER
ESS-1 Growth Inhibition Assay IC50=0.24805 μM SANGER
TE-6 Growth Inhibition Assay IC50=0.2575 μM SANGER
LB2518-MEL Growth Inhibition Assay IC50=0.25777 μM SANGER
COLO-800 Growth Inhibition Assay IC50=0.25812 μM SANGER
LU-134-A Growth Inhibition Assay IC50=0.26136 μM SANGER
NCI-H1155 Growth Inhibition Assay IC50=0.26162 μM SANGER
MFM-223 Growth Inhibition Assay IC50=0.26363 μM SANGER
HTC-C3 Growth Inhibition Assay IC50=0.26506 μM SANGER
HCT-116 Growth Inhibition Assay IC50=0.26599 μM SANGER
Ca-Ski Growth Inhibition Assay IC50=0.26678 μM SANGER
SBC-1 Growth Inhibition Assay IC50=0.26742 μM SANGER
NB69 Growth Inhibition Assay IC50=0.27087 μM SANGER
J82 Growth Inhibition Assay IC50=0.27265 μM SANGER
U-118-MG Growth Inhibition Assay IC50=0.27579 μM SANGER
NCI-H1355 Growth Inhibition Assay IC50=0.28074 μM SANGER
NCI-H1048 Growth Inhibition Assay IC50=0.28956 μM SANGER
SW954 Growth Inhibition Assay IC50=0.29227 μM SANGER
NMC-G1 Growth Inhibition Assay IC50=0.29277 μM SANGER
SW1710 Growth Inhibition Assay IC50=0.29494 μM SANGER
KY821 Growth Inhibition Assay IC50=0.29872 μM SANGER
HCC38 Growth Inhibition Assay IC50=0.30078 μM SANGER
NCI-SNU-5 Growth Inhibition Assay IC50=0.3054 μM SANGER
ES8 Growth Inhibition Assay IC50=0.30784 μM SANGER
COLO-792 Growth Inhibition Assay IC50=0.31251 μM SANGER
BFTC-905 Growth Inhibition Assay IC50=0.31521 μM SANGER
ChaGo-K-1 Growth Inhibition Assay IC50=0.31715 μM SANGER
Daoy Growth Inhibition Assay IC50=0.31723 μM SANGER
SJSA-1 Growth Inhibition Assay IC50=0.31847 μM SANGER
KNS-62 Growth Inhibition Assay IC50=0.32088 μM SANGER
CAKI-1 Growth Inhibition Assay IC50=0.32111 μM SANGER
UACC-62 Growth Inhibition Assay IC50=0.32227 μM SANGER
HuCCT1 Growth Inhibition Assay IC50=0.32283 μM SANGER
CTB-1 Growth Inhibition Assay IC50=0.32753 μM SANGER
NTERA-S-cl-D1 Growth Inhibition Assay IC50=0.32836 μM SANGER
T-24 Growth Inhibition Assay IC50=0.33159 μM SANGER
KYSE-70 Growth Inhibition Assay IC50=0.33283 μM SANGER
SW626 Growth Inhibition Assay IC50=0.33532 μM SANGER
LB996-RCC Growth Inhibition Assay IC50=0.33619 μM SANGER
DMS-273 Growth Inhibition Assay IC50=0.33916 μM SANGER
SW1783 Growth Inhibition Assay IC50=0.33997 μM SANGER
KU812 Growth Inhibition Assay IC50=0.34038 μM SANGER
HSC-2 Growth Inhibition Assay IC50=0.34053 μM SANGER
A3-KAW Growth Inhibition Assay IC50=0.34162 μM SANGER
COLO-684 Growth Inhibition Assay IC50=0.34501 μM SANGER
NCI-H2405 Growth Inhibition Assay IC50=0.34631 μM SANGER
NCI-H2228 Growth Inhibition Assay IC50=0.35357 μM SANGER
NB13 Growth Inhibition Assay IC50=0.36829 μM SANGER
no-11 Growth Inhibition Assay IC50=0.3695 μM SANGER
DK-MG Growth Inhibition Assay IC50=0.37188 μM SANGER
NBsusSR Growth Inhibition Assay IC50=0.37285 μM SANGER
KP-N-YS Growth Inhibition Assay IC50=0.37463 μM SANGER
CFPAC-1 Growth Inhibition Assay IC50=0.37518 μM SANGER
KARPAS-45 Growth Inhibition Assay IC50=0.37862 μM SANGER
NCI-H1793 Growth Inhibition Assay IC50=0.3851 μM SANGER
HCE-T Growth Inhibition Assay IC50=0.38603 μM SANGER
NCI-H520 Growth Inhibition Assay IC50=0.38703 μM SANGER
HCC2157 Growth Inhibition Assay IC50=0.38781 μM SANGER
EW-18 Growth Inhibition Assay IC50=0.38941 μM SANGER
RO82-W-1 Growth Inhibition Assay IC50=0.39699 μM SANGER
HuP-T3 Growth Inhibition Assay IC50=0.40143 μM SANGER
PANC-10-05 Growth Inhibition Assay IC50=0.4117 μM SANGER
NCI-H1703 Growth Inhibition Assay IC50=0.41446 μM SANGER
TE-10 Growth Inhibition Assay IC50=0.41447 μM SANGER
HOS Growth Inhibition Assay IC50=0.41682 μM SANGER
LN-405 Growth Inhibition Assay IC50=0.41687 μM SANGER
A427 Growth Inhibition Assay IC50=0.41981 μM SANGER
CAL-12T Growth Inhibition Assay IC50=0.4278 μM SANGER
SW756 Growth Inhibition Assay IC50=0.44183 μM SANGER
YAPC Growth Inhibition Assay IC50=0.4508 μM SANGER
GOTO Growth Inhibition Assay IC50=0.4516 μM SANGER
C3A Growth Inhibition Assay IC50=0.45437 μM SANGER
UM-UC-3 Growth Inhibition Assay IC50=0.4547 μM SANGER
NCI-H1573 Growth Inhibition Assay IC50=0.45569 μM SANGER
LS-411N Growth Inhibition Assay IC50=0.46527 μM SANGER
COR-L23 Growth Inhibition Assay IC50=0.46764 μM SANGER
HCE-4 Growth Inhibition Assay IC50=0.47446 μM SANGER
NCI-H2291 Growth Inhibition Assay IC50=0.47896 μM SANGER
A101D Growth Inhibition Assay IC50=0.48053 μM SANGER
HT-3 Growth Inhibition Assay IC50=0.48217 μM SANGER
HOP-62 Growth Inhibition Assay IC50=0.49865 μM SANGER
PC-3 Growth Inhibition Assay IC50=0.51507 μM SANGER
CTV-1 Growth Inhibition Assay IC50=0.52669 μM SANGER
PANC-08-13 Growth Inhibition Assay IC50=0.53177 μM SANGER
CAL-120 Growth Inhibition Assay IC50=0.53399 μM SANGER
UMC-11 Growth Inhibition Assay IC50=0.55234 μM SANGER
MSTO-211H Growth Inhibition Assay IC50=0.55762 μM SANGER
NCI-H2126 Growth Inhibition Assay IC50=0.56815 μM SANGER
SNU-C2B Growth Inhibition Assay IC50=0.57977 μM SANGER
DBTRG-05MG Growth Inhibition Assay IC50=0.58053 μM SANGER
MKN1 Growth Inhibition Assay IC50=0.58783 μM SANGER
ES3 Growth Inhibition Assay IC50=0.59124 μM SANGER
OVCAR-3 Growth Inhibition Assay IC50=0.59341 μM SANGER
ACHN Growth Inhibition Assay IC50=0.60569 μM SANGER
SW872 Growth Inhibition Assay IC50=0.60763 μM SANGER
CP66-MEL Growth Inhibition Assay IC50=0.60969 μM SANGER
NCI-H661 Growth Inhibition Assay IC50=0.61104 μM SANGER
UACC-893 Growth Inhibition Assay IC50=0.63681 μM SANGER
JVM-3 Growth Inhibition Assay IC50=0.63804 μM SANGER
SF268 Growth Inhibition Assay IC50=0.64349 μM SANGER
OCI-AML2 Growth Inhibition Assay IC50=0.65397 μM SANGER
RPMI-8226 Growth Inhibition Assay IC50=0.66323 μM SANGER
MKN28 Growth Inhibition Assay IC50=0.66624 μM SANGER
MDA-MB-453 Growth Inhibition Assay IC50=0.6718 μM SANGER
BV-173 Growth Inhibition Assay IC50=0.68679 μM SANGER
NCI-H358 Growth Inhibition Assay IC50=0.68726 μM SANGER
NCI-H1651 Growth Inhibition Assay IC50=0.7 μM SANGER
MDA-MB-415 Growth Inhibition Assay IC50=0.70829 μM SANGER
8305C Growth Inhibition Assay IC50=0.72498 μM SANGER
EFM-19 Growth Inhibition Assay IC50=0.73671 μM SANGER
RERF-LC-MS Growth Inhibition Assay IC50=0.74613 μM SANGER
A388 Growth Inhibition Assay IC50=0.76467 μM SANGER
GI-ME-N Growth Inhibition Assay IC50=0.77235 μM SANGER
IGR-1 Growth Inhibition Assay IC50=0.79043 μM SANGER
LNCaP-Clone-FGC Growth Inhibition Assay IC50=0.80004 μM SANGER
SK-MEL-3 Growth Inhibition Assay IC50=0.81508 μM SANGER
UACC-257 Growth Inhibition Assay IC50=0.82231 μM SANGER
OE33 Growth Inhibition Assay IC50=0.85101 μM SANGER
QIMR-WIL Growth Inhibition Assay IC50=0.85141 μM SANGER
NCI-H2009 Growth Inhibition Assay IC50=0.85311 μM SANGER
NCI-H522 Growth Inhibition Assay IC50=0.87783 μM SANGER
Saos-2 Growth Inhibition Assay IC50=0.87871 μM SANGER
NB17 Growth Inhibition Assay IC50=0.88025 μM SANGER
D-392MG Growth Inhibition Assay IC50=0.89356 μM SANGER
SHP-77 Growth Inhibition Assay IC50=0.90485 μM SANGER
SK-MEL-30 Growth Inhibition Assay IC50=0.91185 μM SANGER
GCIY Growth Inhibition Assay IC50=0.91843 μM SANGER
HCC70 Growth Inhibition Assay IC50=0.92059 μM SANGER
LU-65 Growth Inhibition Assay IC50=0.92591 μM SANGER
NCI-H1563 Growth Inhibition Assay IC50=0.94865 μM SANGER
KURAMOCHI Growth Inhibition Assay IC50=0.95192 μM SANGER
PA-1 Growth Inhibition Assay IC50=0.95424 μM SANGER
NOS-1 Growth Inhibition Assay IC50=0.97489 μM SANGER
NCI-H69 Growth Inhibition Assay IC50=0.97634 μM SANGER
KYSE-450 Growth Inhibition Assay IC50=0.98626 μM SANGER
8505C Growth Inhibition Assay IC50=0.99982 μM SANGER
TGBC24TKB Growth Inhibition Assay IC50=1.00084 μM SANGER
PFSK-1 Growth Inhibition Assay IC50=1.01428 μM SANGER
EKVX Growth Inhibition Assay IC50=1.03121 μM SANGER
RCM-1 Growth Inhibition Assay IC50=1.05507 μM SANGER
SW900 Growth Inhibition Assay IC50=1.0783 μM SANGER
D-542MG Growth Inhibition Assay IC50=1.07855 μM SANGER
SK-PN-DW Growth Inhibition Assay IC50=1.10056 μM SANGER
NCI-H727 Growth Inhibition Assay IC50=1.10154 μM SANGER
SW837 Growth Inhibition Assay IC50=1.10954 μM SANGER
BT-20 Growth Inhibition Assay IC50=1.11204 μM SANGER
RH-18 Growth Inhibition Assay IC50=1.13103 μM SANGER
TE-12 Growth Inhibition Assay IC50=1.13333 μM SANGER
NB10 Growth Inhibition Assay IC50=1.13344 μM SANGER
AU565 Growth Inhibition Assay IC50=1.15973 μM SANGER
OAW-42 Growth Inhibition Assay IC50=1.18306 μM SANGER
DJM-1 Growth Inhibition Assay IC50=1.19881 μM SANGER
HH Growth Inhibition Assay IC50=1.23831 μM SANGER
LAMA-84 Growth Inhibition Assay IC50=1.27394 μM SANGER
KNS-42 Growth Inhibition Assay IC50=1.30296 μM SANGER
NCI-H2052 Growth Inhibition Assay IC50=1.30507 μM SANGER
MLMA Growth Inhibition Assay IC50=1.32407 μM SANGER
NB12 Growth Inhibition Assay IC50=1.35636 μM SANGER
NCI-H1838 Growth Inhibition Assay IC50=1.36306 μM SANGER
NCI-H526 Growth Inhibition Assay IC50=1.37853 μM SANGER
LS-123 Growth Inhibition Assay IC50=1.39094 μM SANGER
HDLM-2 Growth Inhibition Assay IC50=1.39271 μM SANGER
MC-IXC Growth Inhibition Assay IC50=1.42371 μM SANGER
HCT-15 Growth Inhibition Assay IC50=1.43068 μM SANGER
NCI-H596 Growth Inhibition Assay IC50=1.45061 μM SANGER
ZR-75-30 Growth Inhibition Assay IC50=1.47082 μM SANGER
A704 Growth Inhibition Assay IC50=1.66563 μM SANGER
OVCAR-4 Growth Inhibition Assay IC50=1.69607 μM SANGER
SW1417 Growth Inhibition Assay IC50=1.72849 μM SANGER
CAS-1 Growth Inhibition Assay IC50=1.73936 μM SANGER
IST-SL1 Growth Inhibition Assay IC50=1.79759 μM SANGER
A253 Growth Inhibition Assay IC50=1.82239 μM SANGER
EW-16 Growth Inhibition Assay IC50=1.82875 μM SANGER
SK-NEP-1 Growth Inhibition Assay IC50=1.86988 μM SANGER
NCI-H226 Growth Inhibition Assay IC50=1.89359 μM SANGER
HOP-92 Growth Inhibition Assay IC50=1.96099 μM SANGER
NCI-H441 Growth Inhibition Assay IC50=2.02337 μM SANGER
LU-139 Growth Inhibition Assay IC50=2.03114 μM SANGER
SJRH30 Growth Inhibition Assay IC50=2.04253 μM SANGER
MG-63 Growth Inhibition Assay IC50=2.14111 μM SANGER
NH-12 Growth Inhibition Assay IC50=2.15006 μM SANGER
NB7 Growth Inhibition Assay IC50=2.19673 μM SANGER
LB771-HNC Growth Inhibition Assay IC50=2.20595 μM SANGER
HCC1569 Growth Inhibition Assay IC50=2.24583 μM SANGER
D-283MED Growth Inhibition Assay IC50=2.24782 μM SANGER
J-RT3-T3-5 Growth Inhibition Assay IC50=2.25351 μM SANGER
ATN-1 Growth Inhibition Assay IC50=2.33082 μM SANGER
HCC1954 Growth Inhibition Assay IC50=2.34408 μM SANGER
SCC-15 Growth Inhibition Assay IC50=2.39312 μM SANGER
COLO-668 Growth Inhibition Assay IC50=2.432 μM SANGER
LB373-MEL-D Growth Inhibition Assay IC50=2.54677 μM SANGER
no-10 Growth Inhibition Assay IC50=2.54947 μM SANGER
HT-1197 Growth Inhibition Assay IC50=2.63188 μM SANGER
DU-145 Growth Inhibition Assay IC50=2.79162 μM SANGER
SK-N-AS Growth Inhibition Assay IC50=2.84692 μM SANGER
MOLT-4 Growth Inhibition Assay IC50=2.85322 μM SANGER
EW-22 Growth Inhibition Assay IC50=2.92841 μM SANGER
DB Growth Inhibition Assay IC50=2.97759 μM SANGER
HL-60 Growth Inhibition Assay IC50=3.04376 μM SANGER
SK-N-DZ Growth Inhibition Assay IC50=3.05075 μM SANGER
NY Growth Inhibition Assay IC50=3.08542 μM SANGER
T47D Growth Inhibition Assay IC50=3.10558 μM SANGER
NCI-H2029 Growth Inhibition Assay IC50=3.22477 μM SANGER
KARPAS-299 Growth Inhibition Assay IC50=3.26027 μM SANGER
KM-H2 Growth Inhibition Assay IC50=3.3068 μM SANGER
CHP-134 Growth Inhibition Assay IC50=3.4739 μM SANGER
22RV1 Growth Inhibition Assay IC50=3.49168 μM SANGER
NB5 Growth Inhibition Assay IC50=3.50689 μM SANGER
CW-2 Growth Inhibition Assay IC50=3.55314 μM SANGER
EFO-21 Growth Inhibition Assay IC50=3.5694 μM SANGER
HuH-7 Growth Inhibition Assay IC50=3.58414 μM SANGER
ALL-PO Growth Inhibition Assay IC50=3.62335 μM SANGER
EM-2 Growth Inhibition Assay IC50=3.69011 μM SANGER
KLE Growth Inhibition Assay IC50=3.73029 μM SANGER
NEC8 Growth Inhibition Assay IC50=3.91808 μM SANGER
KP-N-YN Growth Inhibition Assay IC50=3.93476 μM SANGER
SK-MEL-1 Growth Inhibition Assay IC50=4.03518 μM SANGER
CAL-54 Growth Inhibition Assay IC50=4.0591 μM SANGER
MS-1 Growth Inhibition Assay IC50=4.16155 μM SANGER
NCI-H209 Growth Inhibition Assay IC50=4.29999 μM SANGER
NOMO-1 Growth Inhibition Assay IC50=4.32131 μM SANGER
RPMI-2650 Growth Inhibition Assay IC50=4.36327 μM SANGER
NCI-H810 Growth Inhibition Assay IC50=4.39736 μM SANGER
Ca9-22 Growth Inhibition Assay IC50=4.45691 μM SANGER
ES4 Growth Inhibition Assay IC50=4.47095 μM SANGER
ES6 Growth Inhibition Assay IC50=4.49657 μM SANGER
DMS-114 Growth Inhibition Assay IC50=4.54691 μM SANGER
ONS-76 Growth Inhibition Assay IC50=4.5795 μM SANGER
K-562 Growth Inhibition Assay IC50=4.73814 μM SANGER
MHH-NB-11 Growth Inhibition Assay IC50=4.75461 μM SANGER
Calu-3 Growth Inhibition Assay IC50=4.78548 μM SANGER
HT55 Growth Inhibition Assay IC50=4.84545 μM SANGER
SK-N-FI Growth Inhibition Assay IC50=4.85009 μM SANGER
ES1 Growth Inhibition Assay IC50=4.86057 μM SANGER
SF126 Growth Inhibition Assay IC50=4.93184 μM SANGER
ES5 Growth Inhibition Assay IC50=5.12427 μM SANGER
LoVo Growth Inhibition Assay IC50=5.15871 μM SANGER
SNU-387 Growth Inhibition Assay IC50=5.32339 μM SANGER
C8166 Growth Inhibition Assay IC50=5.36339 μM SANGER
LS-1034 Growth Inhibition Assay IC50=5.42307 μM SANGER
GR-ST Growth Inhibition Assay IC50=5.52201 μM SANGER
NCI-H1092 Growth Inhibition Assay IC50=5.72843 μM SANGER
647-V Growth Inhibition Assay IC50=5.74706 μM SANGER
EW-13 Growth Inhibition Assay IC50=5.76627 μM SANGER
KGN Growth Inhibition Assay IC50=6.09921 μM SANGER
D-423MG Growth Inhibition Assay IC50=6.40284 μM SANGER
ECC10 Growth Inhibition Assay IC50=7.10101 μM SANGER
TE-5 Growth Inhibition Assay IC50=7.41298 μM SANGER
P12-ICHIKAWA Growth Inhibition Assay IC50=7.45523 μM SANGER
NCI-H82 Growth Inhibition Assay IC50=7.45701 μM SANGER
NCI-H1993 Growth Inhibition Assay IC50=7.83063 μM SANGER
RH-1 Growth Inhibition Assay IC50=7.85244 μM SANGER
SW948 Growth Inhibition Assay IC50=7.96049 μM SANGER
CAL-33 Growth Inhibition Assay IC50=7.99938 μM SANGER
U-266 Growth Inhibition Assay IC50=8.15777 μM SANGER
CAL-72 Growth Inhibition Assay IC50=8.2032 μM SANGER
SNU-423 Growth Inhibition Assay IC50=9.36666 μM SANGER
KG-1 Growth Inhibition Assay IC50=9.58456 μM SANGER
HCC1395 Growth Inhibition Assay IC50=9.92352 μM SANGER
BE-13 Growth Inhibition Assay IC50=10.8892 μM SANGER
MKN7 Growth Inhibition Assay IC50=10.9765 μM SANGER
697 Growth Inhibition Assay IC50=11.1472 μM SANGER
LU-135 Growth Inhibition Assay IC50=11.2307 μM SANGER
ES7 Growth Inhibition Assay IC50=11.3313 μM SANGER
SK-HEP-1 Growth Inhibition Assay IC50=11.7646 μM SANGER
BEN Growth Inhibition Assay IC50=11.851 μM SANGER
NCI-H1770 Growth Inhibition Assay IC50=12.126 μM SANGER
SW13 Growth Inhibition Assay IC50=12.1541 μM SANGER
MZ1-PC Growth Inhibition Assay IC50=12.5452 μM SANGER
Mo-T Growth Inhibition Assay IC50=12.7421 μM SANGER
HLE Growth Inhibition Assay IC50=12.8215 μM SANGER
RCC10RGB Growth Inhibition Assay IC50=13.671 μM SANGER
COLO-320-HSR Growth Inhibition Assay IC50=13.7381 μM SANGER
BHT-101 Growth Inhibition Assay IC50=13.8345 μM SANGER
OCUB-M Growth Inhibition Assay IC50=14.1602 μM SANGER
MEG-01 Growth Inhibition Assay IC50=14.3708 μM SANGER
RS4-11 Growth Inhibition Assay IC50=14.742 μM SANGER
MN-60 Growth Inhibition Assay IC50=14.7894 μM SANGER
NCI-H1304 Growth Inhibition Assay IC50=15.0425 μM SANGER
Ramos-2G6-4C10 Growth Inhibition Assay IC50=15.0581 μM SANGER
NCI-H2342 Growth Inhibition Assay IC50=15.2044 μM SANGER
LAN-6 Growth Inhibition Assay IC50=15.4414 μM SANGER
JVM-2 Growth Inhibition Assay IC50=15.5748 μM SANGER
P30-OHK Growth Inhibition Assay IC50=16.0614 μM SANGER
C-33-A Growth Inhibition Assay IC50=16.6214 μM SANGER
RPMI-8866 Growth Inhibition Assay IC50=16.8496 μM SANGER
NCI-H630 Growth Inhibition Assay IC50=16.8537 μM SANGER
KYSE-140 Growth Inhibition Assay IC50=17.2028 μM SANGER
T84 Growth Inhibition Assay IC50=18.8695 μM SANGER
KU-19-19 Growth Inhibition Assay IC50=18.9608 μM SANGER
BALL-1 Growth Inhibition Assay IC50=19.3399 μM SANGER
Calu-6 Growth Inhibition Assay IC50=19.492 μM SANGER
EGI-1 Growth Inhibition Assay IC50=19.598 μM SANGER
MFH-ino Growth Inhibition Assay IC50=19.7454 μM SANGER
GB-1 Growth Inhibition Assay IC50=20.3535 μM SANGER
NCI-H1693 Growth Inhibition Assay IC50=20.6505 μM SANGER
SW1116 Growth Inhibition Assay IC50=20.9362 μM SANGER
H-EMC-SS Growth Inhibition Assay IC50=22.045 μM SANGER
D-502MG Growth Inhibition Assay IC50=22.8261 μM SANGER
IA-LM Growth Inhibition Assay IC50=23.2493 μM SANGER
SW1463 Growth Inhibition Assay IC50=23.79 μM SANGER
JAR Growth Inhibition Assay IC50=24.3293 μM SANGER
HT Growth Inhibition Assay IC50=24.4753 μM SANGER
LCLC-103H Growth Inhibition Assay IC50=24.8449 μM SANGER
SNU-449 Growth Inhibition Assay IC50=24.8741 μM SANGER
KE-37 Growth Inhibition Assay IC50=25.0928 μM SANGER
NCI-H1623 Growth Inhibition Assay IC50=27.1303 μM SANGER
MOLT-13 Growth Inhibition Assay IC50=27.3516 μM SANGER
COLO-741 Growth Inhibition Assay IC50=31.3333 μM SANGER
NB6 Growth Inhibition Assay IC50=32.2876 μM SANGER
MOLT-16 Growth Inhibition Assay IC50=33.0055 μM SANGER
IST-MES1 Growth Inhibition Assay IC50=34.0541 μM SANGER
A4-Fuk Growth Inhibition Assay IC50=35.066 μM SANGER
CAL-85-1 Growth Inhibition Assay IC50=35.2817 μM SANGER
CCRF-CEM Growth Inhibition Assay IC50=37.1536 μM SANGER
HAL-01 Growth Inhibition Assay IC50=38.4889 μM SANGER
HEL Growth Inhibition Assay IC50=43.3409 μM SANGER
EW-1 Growth Inhibition Assay IC50=43.4768 μM SANGER
MDA-MB-231 Growth Inhibition Assay IC50=45.1199 μM SANGER
ABC-1 Growth Inhibition Assay IC50=46.8538 μM SANGER
NCI-H446 Growth Inhibition Assay IC50=48.5058 μM SANGER
MHH-PREB-1 Growth Inhibition Assay IC50=49.6007 μM SANGER
DOHH-2 Growth Inhibition Assay IC50=49.6656 μM SANGER
GCT Growth Inhibition Assay IC50=49.6976 μM SANGER
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生物活性

製品説明 Tanespimycin (17-AAG, CP127374, NSC-330507, KOS 953) is a potent HSP90 inhibitor with IC50 of 5 nM in a cell-free assay, having a 100-fold higher binding affinity for HSP90 derived from tumour cells than HSP90 from normal cells. Tanespimycin (17-AAG) induces apoptosis, necrosis, autophagy and mitophagy. Phase 3.
特性 Displays very low toxicity toward normal cells.
Targets
HSP90 [1]
(Cell-free assay)
5 nM
In Vitro
In vitro

17-AAG, an analog of geldanamycin, exhibits greater than 100 times higher binding affinity for Hsp90 derived from HER-2-overexpressing cancer cells (BT474, N87, SKOV3 and SKBR3) or BT474 breast carcinoma cells with IC50 values of 5-6 nM. [1] 17-AAG causes the degradation of HER2, HER3, Akt, and both mutant and wild-type androgen receptor (AR), leading to the RB-dependent G1 growth arrest of prostate cancer cells such as LNCaP, LAPC-4, DU-145, and PC-3 with IC50 values of 25-45 nM. [2] In addition to inducing apoptosis of Ba/F3 cells transformed with wild-type BCR-ABL with an IC50 of 5.2 μM, 17-AAG has the ability to induce apoptosis of cells transformed with T315I and E255K BCR-ABL mutants with IC50 values of 2.3 μM and 1.0 μM, respectively, by inducing the degradation of both wild-type BCR-ABL protein and mutants. [3]

Kinase Assay Hsp90 binding assays
Purified native Hsp90 protein or cell lysates from HER-2-overexpressing cancer cells (BT474, N87, SKOV3 and SKBR3) or BT474 breast carcinoma cells in lysis buffer (20 mM HEPES, pH 7.3, 1 mM EDTA, 5 mM MgCl2, 100 mM KCl) are incubated with various concentrations of 17-AAG for 30 minutes at 4 °C, and then incubated with biotin-GM linked to BioMag streptavidin magnetic beads for 1 hour at 4 °C. Tubes are placed on a magnetic rack, and the unbound supernatant removed. The magnetic beads are washed three times in lysis buffer and heated for 5 minutes at 95 °C in SDS–PAGE sample buffer. Samples are analysed on SDS protein gels, and western blots done using indicated antibodies. Bands in the western blots are quantified using the Bio-rad Fluor-S MultiImager, and the percentage inhibition of binding of Hsp90 to the biotin-GM is calculated. The IC50 reported is the concentration of 17-AAG needed to cause half-maximal inhibition of binding.
細胞実験 細胞株 BT474, SKBR3, N87, SKOV3, MCF7, MDA468, Hs578T, Hs578Bst, A549, HT29, U87, SKMG3, HT1080, RPTEC, NDF, HMVEC, HMEC, HUVEC, and PBMC cells
濃度 Dissolved in DMSO, final concentrations ~10 μM
反応時間 5 days
実験の流れ

Cells are seeded in 96-well plates at 2,000 cells per well in a final culture volume of 100 μL for 24 hours before the addition of increasing concentrations of 17-AAG that is incubated for 5 days. Viable cell number is determined using the Celltiter 96 AQueous Nonradioactive Cell Proliferation Assay. The value of the background absorbance at 490 nm (A490) of wells not containing cells is subtracted. Percentage of viable cells = (A490 of 17-AAG treated sample/A490 untreated cells) × 100. The IC50 is defined as the concentration that gave rise to 50% viable cell number.

実験結果図 Methods Biomarkers 結果図 PMID
Western blot α-Synuclein / HSP90 / HSP70 / HSP32 / αB-Crystallin EGFR / PDGFR / AKT / MAPK / c-RAS pAKT / pMAPK / pRb Cleaved PARP / Survivin LATS1 / p-LATS1 / YAP / CTGF 20090920
Immunofluorescence STAT3 YAP / TAZ β-catenin / E-cadherin 27279418
Growth inhibition assay Cell viability 18682579
In Vivo
In Vivo

17-AAG displays significantly higher binding affinity for Hsp90 from 3T3-src, B16 or CT26 xenografts in nude mice with IC50 values of 8-35 nM as compared with that from the normal tissues with IC50 values of 200-600 nM. [1] Administration of 17-AAG (~50 mg/kg) causes significant decline in AR, HER2, HER3, and Akt expression in a dose-dependent manner with >50% decline at dose of 50 mg/kg, resulting in the dose-dependent inhibition of androgen-dependent (CWR22) and -independent (CWR22R and CWRSA6) prostate cancer xenografts growth by 67%, 80% and 68% at dose of 50 mg/kg, respectively. [2]

動物実験 動物モデル Male nu/nu athymic mice inoculated s.c. with androgen-dependent CWR22 xenograft, and female nu/nu athymic mice inoculated s.c. with androgen-independent xenografts CWR22R and CWRSA6
投与量 ~50 mg/kg
投与経路 Injection i.p.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00103272 Terminated
Adult Acute Basophilic Leukemia|Adult Acute Eosinophilic Leukemia|Adult Acute Megakaryoblastic Leukemia (M7)|Adult Acute Minimally Differentiated Myeloid Leukemia (M0)|Adult Acute Monoblastic Leukemia (M5a)|Adult Acute Monocytic Leukemia (M5b)|Adult Acute Myeloblastic Leukemia With Maturation (M2)|Adult Acute Myeloblastic Leukemia Without Maturation (M1)|Adult Acute Myeloid Leukemia With 11q23 (MLL) Abnormalities|Adult Acute Myeloid Leukemia With Inv(16)(p13;q22)|Adult Acute Myeloid Leukemia With t(16;16)(p13;q22)|Adult Acute Myeloid Leukemia With t(8;21)(q22;q22)|Adult Acute Myelomonocytic Leukemia (M4)|Adult Erythroleukemia (M6a)|Adult Pure Erythroid Leukemia (M6b)|Anaplastic Large Cell Lymphoma|Angioimmunoblastic T-cell Lymphoma|Extranodal Marginal Zone B-cell Lymphoma of Mucosa-associated Lymphoid Tissue|Nodal Marginal Zone B-cell Lymphoma|Recurrent Adult Acute Lymphoblastic Leukemia|Recurrent Adult Acute Myeloid Leukemia|Recurrent Adult Diffuse Large Cell Lymphoma|Recurrent Adult T-cell Leukemia/Lymphoma|Recurrent Cutaneous T-cell Non-Hodgkin Lymphoma|Recurrent Grade 1 Follicular Lymphoma|Recurrent Grade 2 Follicular Lymphoma|Recurrent Grade 3 Follicular Lymphoma|Recurrent Mantle Cell Lymphoma|Recurrent Marginal Zone Lymphoma|Recurrent Mycosis Fungoides/Sezary Syndrome|Recurrent Small Lymphocytic Lymphoma|Refractory Chronic Lymphocytic Leukemia|Small Intestine Lymphoma|Splenic Marginal Zone Lymphoma|Waldenström Macroglobulinemia
National Cancer Institute (NCI)
April 2005 Phase 1
NCT00098488 Terminated
B-cell Chronic Lymphocytic Leukemia|Prolymphocytic Leukemia|Refractory Chronic Lymphocytic Leukemia
National Cancer Institute (NCI)
April 2005 Phase 1
NCT00118248 Completed
Recurrent Thyroid Cancer|Stage IV Follicular Thyroid Cancer|Stage IV Papillary Thyroid Cancer|Thyroid Gland Medullary Carcinoma
National Cancer Institute (NCI)
December 2004 Phase 2
NCT00098423 Completed
Accelerated Phase Chronic Myelogenous Leukemia|Adult Acute Basophilic Leukemia|Adult Acute Eosinophilic Leukemia|Adult Acute Megakaryoblastic Leukemia (M7)|Adult Acute Minimally Differentiated Myeloid Leukemia (M0)|Adult Acute Monoblastic Leukemia (M5a)|Adult Acute Monocytic Leukemia (M5b)|Adult Acute Myeloblastic Leukemia With Maturation (M2)|Adult Acute Myeloblastic Leukemia Without Maturation (M1)|Adult Acute Myeloid Leukemia With 11q23 (MLL) Abnormalities|Adult Acute Myeloid Leukemia With Inv(16)(p13;q22)|Adult Acute Myeloid Leukemia With t(16;16)(p13;q22)|Adult Acute Myeloid Leukemia With t(8;21)(q22;q22)|Adult Acute Myelomonocytic Leukemia (M4)|Adult Erythroleukemia (M6a)|Adult Pure Erythroid Leukemia (M6b)|Blastic Phase Chronic Myelogenous Leukemia|Chronic Myelomonocytic Leukemia|de Novo Myelodysplastic Syndromes|Previously Treated Myelodysplastic Syndromes|Recurrent Adult Acute Lymphoblastic Leukemia|Recurrent Adult Acute Myeloid Leukemia|Refractory Anemia With Excess Blasts in Transformation|Relapsing Chronic Myelogenous Leukemia|Secondary Acute Myeloid Leukemia|Secondary Myelodysplastic Syndromes
National Cancer Institute (NCI)
November 2004 Phase 1

化学情報

分子量 585.69 化学式

C31H43N3O8

CAS No. 75747-14-7 SDF Download Tanespimycin (17-AAG) SDFをダウンロードする
Smiles CC1CC(C(C(C=C(C(C(C=CC=C(C(=O)NC2=CC(=O)C(=C(C1)C2=O)NCC=C)C)OC)OC(=O)N)C)C)O)OC
保管

In vitro
Batch:

DMSO : 100 mg/mL ( (170.73 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。)

Ethanol : 33 mg/mL

Water : 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

実験計算

モル濃度計算器

質量 濃度 体積 分子量

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)

mg/kg g μL

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

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

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よくある質問(FAQ)

質問1:
What kind of subtypes does this compound inhibit? HSP90α or HSP90β ?

回答
17-AAG can inhibit both HSP90α and HSP90β, but it is unclear how much are they affected respectively. You should note that Hsp90 derived from tumor cells has a 100-fold higher binding affinity for 17-AAG than that from normal cells according to this paper. http://www.nature.com.ezp-prod1.hul.harvard.edu/nature/journal/v425/n6956/full/nature01913.html

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