Buparlisib (BKM120)

别名: NVP-BKM120 中文名称:布帕尼西

Buparlisib (BKM120, NVP-BKM120) 是一种选择性 PI3K 抑制剂,在无细胞试验中作用于p110α/β/δ/γIC50分别为 52 nM/166 nM/116 nM/262 nM。对 VPS34,mTOR,DNAPK 的作用效果下降,而对 PI4Kβ几乎没有活性。Buparlisib 可诱导凋亡。Phase 2。

Buparlisib (BKM120) Chemical Structure

Buparlisib (BKM120) Chemical Structure

CAS: 944396-07-0

规格 价格 库存 购买数量
10mM (1mL in DMSO) RMB 1138.41 现货
5mg RMB 958.23 现货
50mg RMB 4668.3 现货
1g RMB 16134.3 现货
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info@selleck.cn

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客户使用Selleck的Buparlisib (BKM120)发表文献260

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批次: 纯度: 99.93%
99.85

Buparlisib (BKM120)相关产品

相关信号通路图

PI3K抑制剂选择性比较

细胞实验数据示例

细胞系 实验类型 给药浓度 孵育时间 活性描述 文献信息
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
点击查看更多细胞系数据

生物活性

产品描述 Buparlisib (BKM120, NVP-BKM120) 是一种选择性 PI3K 抑制剂,在无细胞试验中作用于p110α/β/δ/γIC50分别为 52 nM/166 nM/116 nM/262 nM。对 VPS34,mTOR,DNAPK 的作用效果下降,而对 PI4Kβ几乎没有活性。Buparlisib 可诱导凋亡。Phase 2。
特性 BKM120是可用于口服的生物有效的PI3K抑制剂。
靶点
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)
点击更多
52 nM 116 nM 166 nM 262 nM 2.4 μM
体外研究(In Vitro)
体外研究活性 BKM120作用于解除PI3K调节的细胞系,包括A2780, U87MG, MCF7和DU145时,具有抗增殖活性,GI50为0.1-0.7 nM。[1] BKM120诱导多发性骨髓瘤细胞(ARP1, ARK, MM.1S, MM1.R和U266)凋亡,导致G1期细胞增多,S期细胞减少。BKM120诱导CD138+原代MM 细胞凋亡,且作用于CD138−基质细胞时毒性较低。BKM120可引起BimS的上调和XIAP的下调。[2]BKM120作用于人类胃癌细胞系,降低mTOR下游信号,具有抗增殖活性。BKM120作用于KRAS突变的胃癌细胞系,可以增强p-ERK或 p-STAT3。BKM120 和STAT3阻断剂联用, 作用于含突变KRAS的细胞,诱导凋亡,具有协同效应,但是作用于KRAS野生型细胞没有这种效果。[3]BKM120主要通过Aurora B激酶调节有丝分裂崩坏。[4]
激酶实验 PI3K 生化实验(ATP 消耗实验)
BKM120溶于DMSO中,按每孔1.25 µL直接加到黑色384孔板上。开始反应, 25 µL 10nM PI3K和5 µg/mL 1-α-磷酸肌醇(PI)加到实验 buffer (10 mM Tris pH 为7.5, 5 mM MgCl2, 20 mM NaCl, 1 mM DTT,及0.05% CHAPS),然后加到每孔中,随后在实验buffer中加入25 µL 2 µM ATP。反应进行直到50% ATP被消耗,然后加入25 µL KinaseGlo溶液终止反应。终止的反应温育5分钟,然后通过荧光测定残留的ATP。
细胞实验 细胞系 A2780细 胞
浓度 0-6.6 μM
孵育时间 3天
方法 A2780细胞培养在含10% FBS,L-谷氨酸,丙酮酸钠和抗生素的DMEM培养基上。细胞按每孔103个细胞的密度接种在相同培养基上,温育3到5小时。稀释溶于20 mM DMSO中的BKM120。2 µL稀释的BKM120溶液加到细胞培养基上, (浓度为0-6.6 µM)。等体积(100 µL)溶液加到96孔板中,在37oC下温育3天。使用Trilux读取荧光值而测定抑制细胞增殖的效果
实验图片 检测方法 检测指标 实验图片 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
体内研究(In Vivo)
体内研究活性 BKM120按30, 60, 或100 mg/kg剂量作用于A2780移植瘤,完全抑制pAKTser473。BKM120按 30和 60 mg/kg剂量作用于U87MG神经胶质瘤模型,显示抗癌活性。[1]BKM120每天按5μM/kg剂量处理具有持久生命力的ARP1 SCID鼠模型,导致肿瘤体积和K链水平明显降低。[2]
动物实验 Animal Models 携带U87MG 和A2780移植瘤的雌性裸鼠
Dosages ~60 mg/kg
Administration 每天口服处理
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
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

化学信息&溶解度

分子量 410.39 分子式

C18H21F3N6O2

CAS号 944396-07-0 SDF Download Buparlisib (BKM120) SDF
Smiles C1COCCN1C2=NC(=NC(=C2)C3=CN=C(C=C3C(F)(F)F)N)N4CCOCC4
储存条件(自收到货起)

体外溶解度
批次:

DMSO : 82 mg/mL ( 199.8 mM; DMSO吸湿会降低化合物溶解度,请使用新开封DMSO)

Ethanol : 82 mg/mL

Water : Insoluble

摩尔浓度计算器

体内溶解度
批次:

现配现用,请按从左到右的顺序依次添加,澄清后再加入下一溶剂

动物体内配方计算器

实验计算

摩尔浓度计算器

质量 浓度 体积 分子量

动物体内配方计算器(澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)

mg/kg g μL

第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)

% DMSO % % Tween 80 % ddH2O
%DMSO %

计算结果:

工作液浓度: mg/ml;

DMSO母液配制方法: mg 药物溶于μL DMSO溶液(母液浓度mg/mL,:如该浓度超过该批次药物DMSO溶解度,请先联系Selleck);

体内配方配制方法:μL DMSO母液,加入μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入μL ddH2O,混匀澄清。

体内配方配制方法:μL DMSO母液,加入μL Corn oil,混匀澄清。

注意:1. 首先保证母液是澄清的;
2.一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。

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