Buparlisib (BKM120)

別名：NVP-BKM120

製品コード：S2247 純度：99.93%

Buparlisib (BKM120, NVP-BKM120) is a selective PI3K inhibitor of p110α/β/δ/γ with IC50 of 52 nM/166 nM/116 nM/262 nM in cell-free assays, respectively. Reduced potency against VPS34, mTOR, DNAPK, with little activity to PI4Kβ. Buparlisib induces apoptosis. Phase 2.

CAS No. 944396-07-0

サイズ	価格(税別)	在庫状況
10mM (1mL in DMSO)	JPY 40800	国内在庫あり
5mg	JPY 25500	国内在庫あり
10mg	JPY 48000	国内在庫あり
50mg	JPY 145500	国内在庫あり
1g	JPY 595500	国内在庫あり

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（271）

製品安全説明書

現在のバッチを見る：純度： 99.93%

99.93

Buparlisib (BKM120)関連製品

関連ターゲット	p110α p110β p110δ p110γ C2β Vps34	もっと見る
関連製品	LY294002 3-MA (3-Methyladenine) Dactolisib (BEZ235) Pictilisib (GDC-0941) Wortmannin PI-103 TGX-221 ZSTK474 Omipalisib (GSK2126458) A66 PF-04691502 PIK-75 HCl IC-87114 740 Y-P (PDGFR 740Y-P) AS-605240 Taselisib (GDC 0032) SAR405 Apitolisib (GDC-0980) VPS34-IN1 PIK-90 AZD6482 Gedatolisib (PKI-587) HS-173 AS-252424 Eganelisib (IPI-549) VS-5584 (SB2343) GSK2636771 AZD8186 GSK1059615 Pilaralisib (XL147) TG100-115 CZC24832 Voxtalisib (XL765) XL147 analogue AS-604850 BGT226 (NVP-BGT226) maleate Quercetin Dihydrate VPS34 inhibitor 1 (Compound 19) Samotolisib (LY3023414) Voxtalisib (XL765) Analogue AMG319 Nemiralisib Bimiralisib (PQR309) CH5132799 PKI-402 TG100713 Paxalisib (GDC-0084) SF2523 Serabelisib (TAK-117) GDC-0326 GNE-317 Inavolisib (GDC-0077) PIK-294 PI-3065 AZD8835 Seletalisib (UCB-5857) leniolisib (CDZ 173) (E)-Akt inhibitor-IV Gallein CAY10505 Selective PI3Kδ Inhibitor 1 (compound 7n) PF-4989216 GNE-477 GNE-493	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

PI3Kシグナル伝達経路

PI3K阻害剤の選択性比較

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	活性情報	PMID
MDA-MB-361	Growth Inhibition Assay	1 μM	5 d	IC50<1 μM	24879796
ZR-75-30	Growth Inhibition Assay	1 μM	5 d	IC50<1 μM	24879796
EFM-19	Growth Inhibition Assay	1 μM	5 d	IC50<1 μM	24879796
HCC1500	Growth Inhibition Assay	1 μM	5 d	IC50<1 μM	24879796
MDA-MB-134	Growth Inhibition Assay	1 μM	5 d	IC50<1 μM	24879796
MDA-MB-175	Growth Inhibition Assay	1 μM	5 d	IC50<1 μM	24879796
LNZ308	Function Assay	5 μM	24 h	Inhibits phosphorylation of AKT	24741074
LN18	Function Assay	5 μM	24 h	Inhibits phosphorylation of AKT	24741074
U87	Growth Inhibition Assay	20 μM	72 h	IC50<5 μM	24741074
T98G	Growth Inhibition Assay	20 μM	72 h	IC50<5 μM	24741074
LNZ308	Growth Inhibition Assay	20 μM	72 h	IC50<5 μM	24741074
LN229	Growth Inhibition Assay	20 μM	72 h	IC50<5 μM	24741074
LN18	Growth Inhibition Assay	20 μM	72 h	IC50<5 μM	24741074
SJSA-1	Growth Inhibition Assay	50 μM	48 h	Inhibits cell viability	24727660
MG-63	Growth Inhibition Assay	50 μM	48 h	Inhibits cell viability	24727660
Saos-2	Growth Inhibition Assay	50 μM	48 h	Inhibits cell viability	24727660
SJSA-1	Function Assay	50 μM	48 h	Inhibits matrix metalloproteinase-2 expression	24727660
MG-63	Function Assay	50 μM	48 h	Inhibits matrix metalloproteinase-2 expression	24727660
Saos-2	Function Assay	50 μM	48 h	Inhibits matrix metalloproteinase-2 expression	24727660
SJSA-1	Function Assay	50 μM	48 h	Inhibits cell invasion	24727660
MG-63	Function Assay	50 μM	48 h	Inhibits cell invasion	24727660
Saos-2	Function Assay	50 μM	48 h	Inhibits cell invasion	24727660
U87	Function Assay	5 μM	24 h	Reduces oxygen consumption	24631147
HCT116	Function Assay	5 μM	24 h	Reduces oxygen consumption	24631147
EMT6	Function Assay	5 μM	24 h	Reduces oxygen consumption	24631147
FaDu	Function Assay	5 μM	24 h	Reduces oxygen consumption	24631147
GBM	Apoptosis Assay	2μM	48h	induced higher levels of apoptosis, and decreased cell viability	24500492
BON	Apoptosis Assay	1-5μM	24h	increases apoptosis	24443523
BON	Growth Inhibition Assay	1-5μM	72h	decreases cell proliferation	24443523
H1975	Apoptosis Assay	2μM	24h	increases apoptosis rate significantly	24337846
H1975	Growth Inhibition Assay	0.3-9.6μM	72h	IC50=1.385μM	24337846
T-ALL	Apoptosis Assay	between 1.4 and 5.3 mM at 24h and 0.9 and 5.5 mM at 48h in different cell line	24 or 48h	affects the PI3K pathway in T-ALL cell lines	24310736
BCR-ABL	Growth Inhibition Assay	0.25-10μM	4d	significantly inhibit cell proliferation	24244612
LC-1/SQSF	Function Assay	3μM	24h	decrease NRF2 protein level	23980093
Primary CLL cells	Cytotoxic Assay	2μM	24h	induces cell cytotoxicity	23850807
Primary CLL cells	Kinase Assay	2μM	30min	decreased PI3K activity	23850807
Primary CLL cells	Apoptosis Assay	1-10μM	48h	induces apoptosis in CLL cells independent of prognostic markers	23850807
human NSCLC cell lines	Apoptosis Assay	0.125-4μM	24h	IC50s ranges from 0.4-2μM	23562472
Huh7	Kinase Assay	1μM	48h	signiﬁcantly reduces phosphorylation of Akt	23489999
human HCC cell lines	Cell viability assay	0.005-1μM	48h	IC50=1μM	23489999
786-0	Growth Inhibition Assay	1-20μM	72h	IC50＜1μM	23479136
SK-HEP1	Growth Inhibition Assay	1-20μM	72h	IC50＜1μM	23479136
primary B-CLL lymphocytes	Kinase Assay	IC50 for each primary cell line	24h	inhibits p70S6K & 4E-BP1 expression	23238639
primary B-CLL lymphocytes	Apoptosis Assay	IC50 for each primary cell line	24h	IC50＜3μM for all patients	23238639
MEC2	Cytotoxicity assay	0.2-20μM	72h	IC50=0.7μM	23238639
EHEB	Cytotoxicity assay	0.2-20μM	72h	IC50=0.7μM	23238639
JVM2	Cytotoxicity assay	0.2-20μM	72h	IC50=0.9μM	23238639
human NSCLC	Kinase Assay	1μM	24h	inhibits the Akt/mTOR signaling pathway at 3h after treatment	22781393
human NSCLC	Growth Inhibition Assay	0.5-2μM	72h	IC50=1μM	22781393
Y1 cell line	Growth Inhibition Assay	0.1μM/1μM	24h	inhibits 60％ cell viability in Myc-Sctr-transfected cells	22692904
MCF7-myr-Akt	Growth Inhibition Assay	GI50=299±68nM，LD50＞10,000nM	72h	GI50=299±68nM，LD50＞10,000nM	22653967
PIK3CA-mutant MCF7	Kinase Assay	IC50=114±3nM	72h	IC50=114±3nM in reducing Akt phosphorylation levels	22653967
PIK3CA-mutant MCF7	Growth Inhibition Assay	GI50=160±91nM，LD50=980±273nM	72h	GI50=160±91nM，LD50=980±273nM	22653967
HT-29 and HCT-116	Caspase assay	5μM	24h	induces caspase activity	22543857
HCT-116/HT-29/MKN-45	Apoptosis Assay	2μM	48h	shift in G2 phase	22543857
gastric cancer cell lines	Growth Inhibition Assay	0-10μM	72h	IC50=2-5μM	22543857
colon cancer cell lines	Growth Inhibition Assay	0-10μM	72h	IC50=1μM	22543857
ARP-1	Apoptosis Assay	10μM	24h	induces MM cell apoptosis through caspase activation	22207485
MM cell lines	Growth Inhibition Assay	10μM	24h	IC50 varies among different cell lines in time and dose dependence	22207485
U87	Apoptosis Assay	2μM	72h	induces cell apoptosis and cleaved PARP and caspase-3	22065080
T-47D	Growth Inhibition Assay	1 μM	5 d	IC50<1 μM	24879796
SK-BR-3	Growth Inhibition Assay	1 μM	5 d	IC50<1 μM	24879796
UACC-732	Growth Inhibition Assay	1 μM	5 d	IC50<1 μM	24879796
BT-474	Growth Inhibition Assay	1 μM	5 d	IC50<1 μM	24879796
HCC202	Growth Inhibition Assay	1 μM	5 d	IC50<1 μM	24879796
MCF7	Growth Inhibition Assay	1 μM	5 d	IC50<1 μM	24879796
MDA-MB-415	Growth Inhibition Assay	1 μM	5 d	IC50<1 μM	24879796
MDA-MB-453	Growth Inhibition Assay	1 μM	5 d	IC50<1 μM	24879796
ZR-75-1	Growth Inhibition Assay	1 μM	5 d	IC50<1 μM	24879796
HCC38	Growth Inhibition Assay	1 μM	5 d	IC50<1 μM	24879796
HCC1419	Growth Inhibition Assay	1 μM	5 d	IC50<1 μM	24879796
UACC-812	Growth Inhibition Assay	1 μM	5 d	IC50<1 μM	24879796
HCC1187	Growth Inhibition Assay	1 μM	5 d	IC50<1 μM	24879796
KPL-1	Growth Inhibition Assay	1 μM	5 d	IC50<1 μM	24879796
SUM-225	Growth Inhibition Assay	1 μM	5 d	IC50<1 μM	24879796
EFM-192A	Growth Inhibition Assay	1 μM	5 d	IC50<1 μM	24879796
JIMT-1	Growth Inhibition Assay	1 μM	5 d	IC50<1 μM	24879796
HCC1143	Growth Inhibition Assay	1 μM	5 d	IC50<1 μM	24879796
HCC2218	Growth Inhibition Assay	1 μM	5 d	IC50<1 μM	24879796
MDA-MB-468	Growth Inhibition Assay	1 μM	5 d	IC50<1 μM	24879796
BT-20	Growth Inhibition Assay	1 μM	5 d	IC50<1 μM	24879796
MDA-MB-435	Growth Inhibition Assay	1 μM	5 d	IC50<1 μM	24879796
BT-549	Growth Inhibition Assay	1 μM	5 d	IC50<1 μM	24879796
HCC1806	Growth Inhibition Assay	1 μM	5 d	IC50<1 μM	24879796
HCC1937	Growth Inhibition Assay	1 μM	5 d	IC50<1 μM	24879796
Hs578T	Growth Inhibition Assay	1 μM	5 d	IC50<1 μM	24879796
Huh7	Function Assay	1 μM	1 h	Inhibits phosphorylation of AKT at Ser474	25004403
BNL	Function Assay	1 μM	1 h	Inhibits phosphorylation of S6	25004403
BON-1	Growth Inhibition Assay	500 nM	10 d	Inhibits cell growth	25026292
BON-1	Function Assay	500 nM	4 h	Inhibits phosphorylation of AKT at Thr308 and Ser473	25026292
QGP-1	Function Assay	500 nM	4 h	Inhibits phosphorylation of AKT at Thr308 and Ser473	25026292
HCT-15	Apotosis Assay	10 μM	48 h	Induces apoptosis in HCT-15 cells harbouring PIK3CA hotspot mutation	25152245
HCT-116	Apotosis Assay	10 μM	48 h	Induces apoptosis in HCT-116 cells harbouring PIK3CA hotspot mutation	25152245
NCI-H460	Apotosis Assay	10 μM	48 h	Induces apoptosis in NCI-H460 cells harbouring PIK3CA hotspot mutation	25152245
SKOV-3	Apotosis Assay	10 μM	48 h	Induces apoptosis in SKOV-3 cells harbouring PIK3CA hotspot mutation	25152245
BSY-1	Apotosis Assay	10 μM	48 h	Induces apoptosis in BSY-1 cells harbouring PIK3CA hotspot mutation	25152245
MKN-1	Apotosis Assay	10 μM	48 h	Induces apoptosis in MKN-1 cells harbouring PIK3CA hotspot mutation	25152245
NCI-H522	Apotosis Assay	10 μM	48 h	Induces apoptosis	25152245
OVCAR-3	Apotosis Assay	10 μM	48 h	Induces apoptosis	25152245
HBC-5	Apotosis Assay	10 μM	48 h	Induces apoptosis	25152245
RXF-631L	Apotosis Assay	10 μM	48 h	Induces apoptosis	25152245
MKN-45	Apotosis Assay	10 μM	48 h	Induces apoptosis	25152245
A549	Function Assay	500 nM	48 h	Inhibits Akt activation	25937299
A549	Growth Inhibition Assay	1 μM	72 h	Inhibits cell growth	25937299
H522	Growth Inhibition Assay	1 μM	72 h	Inhibits cell growth	25937299
SKMES-1	Cytotoxic Assay	1 μM	72 h	Induces cell death	26013318
HCT116	Function assay	10 uM	1 hr	Inhibition of PI3K/Akt in human HCT116 cells assessed as Akt phosphorylation at 10 uM after 1 hr by Western blotting analysis	25765909
A2058 melanoma	Cell cycle assay	5 uM	24 hrs	Cell cycle arrest in human A2058 melanoma cells assessed as accumulation at SubG1 phase at 5 uM after 24 hrs by propidium iodide staining based FACS analysis	28829592
A2058 melanoma	Cell cycle assay	5 uM	24 hrs	Cell cycle arrest in human A2058 melanoma cells assessed as accumulation at G2/M phase at 5 uM after 24 hrs by propidium iodide staining based FACS analysis	28829592
SKOV3	Cell cycle assay	2 uM	24 hrs	Cell cycle arrest in human SKOV3 cells assessed as accumulation at G2/M phase at 2 uM after 24 hrs by propidium iodide staining based FACS analysis	28829592
SKOV3	Cell cycle assay	2 uM	24 hrs	Cell cycle arrest in human SKOV3 cells assessed as accumulation at SubG1 phase at 2 uM after 24 hrs by propidium iodide staining based FACS analysis	28829592
HT-29	Cell cycle assay	0.111 to 3 uM	24 hrs	Cell cycle arrest in human HT-29 cells assessed as accumulation at G2/M phase at 0.111 to 3 uM after 24 hrs by propidium iodide staining based flow cytometry	30034607
LNCaP	Function Assay	1 μM		Suppresses p-AKT levels	25360799
LNCaP95	Function Assay	1 μM		Suppresses p-AKT levels	25360799
H596	Function Assay	1 μM		Impairs cell migration	26013318
HCC2450	Function Assay	1 μM		Impairs cell invasion	26013318
SNU-719	Growth Inhibition Assay		72h	IC50=3.037±0.032μM	22159814
SNU-620	Growth Inhibition Assay		72h	IC50=2.939±0.001μM	22159814
SNU-484	Growth Inhibition Assay		72h	IC50=1.728±0.045μM	22159814
SNU-16	Growth Inhibition Assay		72h	IC50=1.573±0.001μM	22159814
SNU-638	Growth Inhibition Assay		72h	IC50=2.282±0.053μM	22159814
SNU-5	Growth Inhibition Assay		72h	IC50=1.351±0.091μM	22159814
SNU-216	Growth Inhibition Assay		72h	IC50=2.692±0.082μM	22159814
AGS	Growth Inhibition Assay		72h	IC50=1.714±0.117μM	22159814
SNU-668	Growth Inhibition Assay		72h	IC50=1.579±0.074μM	22159814
SNU-1	Growth Inhibition Assay		72h	IC50=1.082±0.028μM	22159814
SNU-601	Growth Inhibition Assay		72h	IC50=0.816±0.063μM	22159814
glioma cell lines	Growth Inhibition Assay		72h	IC50=1-2μM	22065080
MCF7	Cytotoxic Assay		72 h	Cytotoxicity against human MCF7 cells expressing PI3Kalpha E545K mutant with GI50 of 0.000158 μM	24900266
DU145	Cytotoxic Assay		72 h	Cytotoxicity against human DU145 cells expressing LKB1 mutant with GI50 of 0.000435 μM	24900266
A2780	Cytotoxic Assay		72 h	Cytotoxicity against PTEN-deficient human A2780 cells with GI50 of 0.000635 μM	24900266
U87MG	Cytotoxic Assay		72 h	Cytotoxicity against PTEN-deficient human U87MG cells with GI50 of 0.000698 μM	24900266
A2780	Function Assay		1 h	Inhibition of PI3K-mediated AKT Ser473 phosphorylation with EC50 of 0.055 μM	24900266
DU145	Function Assay		1 h	Inhibition of PI3K-mediated AKT Ser473 phosphorylation in human DU145 cells harboring LKB1 mutation with EC50 of 0.073 μM	24900266
A2780	Function Assay		1 h	Inhibition of PI3K-mediated AKT Ser473 phosphorylation in PTEN-deficient human A2780 cells with EC50 of 0.074 μM	24900266
MCF7	Function Assay		1 h	Inhibition of PI3Kalpha E545K mutant-mediated AKT Ser473 phosphorylation with EC50 of 0.1 μM	24900266
U87MG	Function Assay		1 h	Inhibition of PI3K-mediated AKT Ser473 phosphorylation in PTEN-deficient human U87MG cells with EC50 of 0.13 μM	24900266
A2780	Growth Inhibition Assay		72 h	EC50=0.52 μM	24900266
HCT116	Antiproliferative assay		72 hrs	Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay, IC50 = 0.48 μM.	25765909
MCF7	Antiproliferative assay		72 hrs	Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay, IC50 = 1 μM.	25765909
U87MG	Antiproliferative assay		72 hrs	Antiproliferative activity against human U87MG cells after 72 hrs by MTT assay, IC50 = 1.64 μM.	25765909
A549	Antiproliferative assay		72 hrs	Antiproliferative activity against human A549 cells after 72 hrs by MTT assay, IC50 = 2.07 μM.	25765909
HeLa	Antiproliferative assay		72 hrs	Antiproliferative activity against human HeLa cells after 72 hrs by MTT assay, IC50 = 4.34 μM.	25765909
MDA-MB-231	Cytotoxicity assay		72 hrs	Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay, IC50 = 1.88 μM.	29107429
PC3	Cytotoxicity assay		72 hrs	Cytotoxicity against human PC3 cells after 72 hrs by MTT assay, IC50 = 5.34 μM.	29107429
T47D	Cytotoxicity assay		72 hrs	Cytotoxicity against human T47D cells after 72 hrs by MTT assay, IC50 = 6.92 μM.	29107429
MCF7	Cytotoxicity assay		72 hrs	Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay, IC50 = 11.05 μM.	29107429
Sf21	Function assay		1 hr	Inhibition of recombinant human full-length N-terminal His6-tagged p110delta/recombinant human full length p85alpha expressed in baculovirus infected Sf21 insect cells using PIP2 as substrate measured after 1 hr by Alexa633 Tracer-based fluorescence polar, IC50 = 0.125 μM.	30034607
MCF7	Antiproliferative assay		72 hrs	Antiproliferative activity against human MCF7 cells harboring PIK3CA E545K mutant after 72 hrs by MTT assay, IC50 = 0.206 μM.	30034607
Sf21	Function assay		1 hr	Inhibition of recombinant human full-length N-terminal His6-tagged p110beta/recombinant human full length p85alpha expressed in baculovirus infected Sf21 insect cells using PIP2 as substrate measured after 1 hr by Alexa633 Tracer-based fluorescence polari, IC50 = 0.234 μM.	30034607
T47D	Antiproliferative assay		72 hrs	Antiproliferative activity against human T47D cells harboring PI3KCA H1047R mutant after 72 hrs by MTT assay, IC50 = 0.286 μM.	30034607
PC3	Function assay		2 hrs	Inhibition of PI3K in human PC3 cells assessed as reduction in AKT phosphorylation at Ser473 measured after 2 hrs by fluorescence assay, IC50 = 0.365 μM.	30034607
A2058	Function assay		1 hr	Inhibition of TORC2 in human A2058 cells assessed as decrease in PKB/Akt phosphorylation at Ser473 after 1 hr by Western blot analysis, IC50 = 0.416 μM.	30359003
A2058	Function assay		1 hr	Inhibition of TORC1 in human A2058 cells assessed as decrease in S6 phosphorylation at Ser235/236 after 1 hr by Western blot analysis, IC50 = 0.553 μM.	30359003
TC32	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells	29435139
A673	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	29435139
DAOY	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells	29435139
Saos-2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells	29435139
BT-37	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells	29435139
RD	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells	29435139
SK-N-SH	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells	29435139
BT-12	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells	29435139
MG 63 (6-TG R)	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells	29435139
NB1643	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells	29435139
OHS-50	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells	29435139
SK-N-SH	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells	29435139
Rh41	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells	29435139
A673	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells)	29435139
Rh30	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells	29435139
MG 63 (6-TG R)	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells	29435139
Rh30	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells	29435139
U-2 OS	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells	29435139
Rh41	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells	29435139
RD	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for RD cells	29435139
SJ-GBM2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells	29435139
SK-N-MC	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	29435139
NB-EBc1	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells	29435139
LAN-5	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells	29435139
Rh18	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells	29435139
SK-N-MC	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells	29435139
TC32	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells	29435139
insect	Function assay			Inhibition of recombinant human His-tagged p85alpha/p110alpha E545K mutant expressed in insect cells, IC50 = 0.011 μM.	30034607
insect	Function assay			Inhibition of recombinant human His-tagged p85alpha/p110alpha E542K mutant expressed in insect cells, IC50 = 0.029 μM.	30034607
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生物活性

製品説明

Targets

p110α ^[1] (Cell-free assay)	p110δ ^[1] (Cell-free assay)	p110β ^[1] (Cell-free assay)	p110γ ^[1] (Cell-free assay)	Vps34 ^[1] (Cell-free assay)	もっとクリックする
52 nM	116 nM	166 nM	262 nM	2.4 μM	もっとクリックする

In Vitro
In vitro	BKM120 is not sensitive to Class III and Class IV PI3K's or PI4K. NVP-BKM120 shows great antiproliferation activity to PI3K deregulated cell lines including A2780, U87MG, MCF7 and DU145 with GI50 of 0.1-0.7 nM. ^[1] BKM120 induces multiple myeloma cells (ARP1, ARK, MM.1S, MM1.R and U266) apoptosis, which results in increased G1-phase cells and decreased S-phase cells. BKM120 induced CD138+ primary MM cell apoptosis and has significant lower cytotoxicity toward CD138− stromal cells. BKM120 exposure could cause upregulation of BimS and downregulation of XIAP. ^[2] BKM120 demonstrates antiproliferative activity in human gastric cancer cell lines by decreasing mTOR downstream signaling. BKM120 could increase either p-ERK or p-STAT3 in KRAS mutant gastric cancer cells. Combination with STAT3 blockade, BKM120 shows a synergism in cells harboring mutated KRAS by inducing apoptosis, but not in KRAS wild-type cells. ^[3] A recent study shows that BKM120 shows differential forms of cell death on the basis of p53 status of the cells with p53 wild-type cells undergoing apoptotic cell death and p53 mutant/deleted cells having a mitotic catastrophe cell death. BKM120 mediates mitotic catastrophe mainly through Aurora B kinase. ^[4]
Kinase Assay	PI3K biochemical assay (ATP depletion assay)
Kinase Assay	BKM120 is dissolved in DMSO and directly distributed into a black 384-well plate at 1.25 µL per well. To start the reaction, 25 µL of 10 nM PI3 kinase and 5 µg/mL 1-α-phosphatidylinositol (PI) in assay buffer (10 mM Tris pH 7.5, 5 mM MgCl₂, 20 mM NaCl, 1 mM DTT and 0.05% CHAPS) are added into each well followed by 25 µL of 2 µM ATP in assay buffer. The reaction is performed until approx 50% of the ATP is depleted and then stopped by the addition of 25 µL of KinaseGlo solution. The stopped reaction is incubated for 5 minutes and the remaining ATP is then detected via luminescence.
細胞実験	細胞株	A2780 cells.
	濃度	0-6.6 μM
	反応時間	3 days.
	実験の流れ	A2780 cells are cultured in DMEM supplemented with 10% FBS, L-glutamine, sodium pyruvate, and antibiotics. Cells are plated in the same medium at a density of 10³ cells per well, 100 μL per well into black-walled-clear-bottom plates and incubated for 3-5 hours. BKM120 supplied in DMSO (20 mM) is diluted. The diluted BKM120 solution (2 μL), is then added to cell medium (500 μL) cell medium (concentration from 0-6.6 μM). Equal volumes of this solution (100 μL) are added to the cells in 96 well plates and incubated at 37 °C for 3 days and developed using Cell Titer Glo. Inhibition of cell proliferation is determined by luminescence read using Trilux.
実験結果図	Methods	Biomarkers	結果図	PMID
	Western blot	p-MET / MET p-STAT3 / STAT3 / p-ERK / ERK / p-S6 p-ERK / ERK / LC3 Nuclear NF-κB p65 / NF-κB p65 p-FOXO3a (S253) / FOXO3a p-AKT (T308) / p-AKT (S473) / AKT		29928341
	Immunofluorescence	FOXO3a		28036259
	Growth inhibition assay	Cell viability		26673665

In Vivo
In Vivo	BKM120 completely inhibits pAktser473 in A2780 xenograft tumors at doses of 30, 60, or 100 mg/kg, respectively. BKM120 also shows antitumor activity against U87MG glioma model at doses of 30 and 60 mg/kg. ^[1] BKM120 treatment results in significantly reduced tumor volume and level of circulating human kappa chain at 5 μM/kg/day−1in ARP1 SCID mouse model, with prolonged survival. ^[2]
動物実験	動物モデル	U87MG and A2780 xenografts are established in female nu/nu mice.
	投与量	~60 mg/kg.
	投与経路	Dosed orally daily (q.d.).

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試験 (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT04338399	Active not recruiting	Head and Neck Cancer	Adlai Nortye Biopharma Co. Ltd.	December 12 2020	Phase 3
NCT02614508	Terminated	Recurrent Chronic Lymphocytic Leukemia\|Recurrent Small Lymphocytic Lymphoma\|Refractory Chronic Lymphocytic Leukemia\|Refractory Small Lymphocytic Lymphoma	Emory University\|Novartis	January 2016	Phase 1
NCT01613677	Withdrawn	Treatment for Metastatic or Locally Advanced Cervical Cancer	Novartis Pharmaceuticals\|Novartis	November 2015	Phase 2

参考
[1] Burger MT, et al. ACS Med Chem Lett, 2011, 2 (10), 774–779. [2] Zheng Y, et al. J Mol Med (Berl), 2011 Dec 30. [3] Park E, et al. Int J Oncol, 2012, 40(4), 1259-1266. [4] Koul D, et al. Clin Cancer Res, 2012, 18(1), 184-195. + 展開

参考

[4] Koul D, et al. Clin Cancer Res, 2012, 18(1), 184-195.

+ 展開

化学情報

分子量	410.39	化学式	C₁₈H₂₁F₃N₆O₂
CAS No.	944396-07-0	SDF	Download Buparlisib (BKM120) SDFをダウンロードする
Smiles	C1COCCN1C2=NC(=NC(=C2)C3=CN=C(C=C3C(F)(F)F)N)N4CCOCC4
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个月-20°Cin solvent

In vitro
Batch:

DMSO : 82 mg/mL ( (199.8 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 : 82 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
=	×	×

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。

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