产品名称

英文名称：BKM120

同义词

Buparlisib、944396-07-0、NVP-BKM120、BKM120、5-(2,6-dimorpholinopyrimidin-4-yl)-4-(trifluoromethyl)pyridin-2-amine、NVP-BKM-120、BKM-120、1202777-78-3、BKM 120、Buparlisib (BKM120)、BKM120 (NVP-BKM120, Buparlisib)、NVP-BKM 120、5-(2,6-dimorpholin-4-ylpyrimidin-4-yl)-

产品性质

CAS编号：944396-07-0

分子式：C18H21F3N6O2

分子量：410.4

PubChem编号：16654980

英文别名：Buparlisib|944396-07-0|NVP-BKM120|BKM120|5-(2,6-dimorpholinopyrimidin-4-yl)-4-(trifluoromethyl)pyridin-2-amine|NVP-BKM-120|BKM-120|1202777-78-3|BKM 120|Buparlisib (BKM120)|BKM120 (NVP-BKM120, Buparlisib)|NVP-BKM 120|5-(2,6-dimorpholin-4-ylpyrimidin-4-yl)-

规格或纯度：≥99%

英文名称：BKM120

生化机理：NVP-BKM120 is a potent, selective, orally bioavailable Class I PI3 Kinase Inhibitor for treating Cancer.BKM120 is a potent and cell permeable inhibitor of the PI 3-kinase family. Specifically inhibits p110α, p110β, p110γ and p110δ with IC50 of 52 nM, 166 nM, 262 nM and 116 nM, respectively. Phosphatidylinositol 3-kinases (PI3K) belong to a family of lipid kinases that is involved in many types of cancer. NVP-BKM120 is an orally bioavailable inhibitor of class I PI3K isoforms, potently blocking, in vitro, both p110α (IC50 = 52 nM) and p110β (IC50 = 166 nM).It much less effectively inhibits the class III PI3K Vps34 and mammalian target of rapamycin and has no effect on PI4Kβ and several other kinases.2 NVP-BKM120 prevents the growth of assorted cancer cell lines when used at 5 μM and inhibits tumor growth in vivo. It can be particularly effective against certain types of cancer when combined with other modulators.Potent\xa0class I PI3K\xa0inhibitor,\xa0blocking both p110α and p110β (IC50 =\xa052 nM and 166 nM, respectively) in vitro . At 5 μM, prevents the growth of assorted cancer cell lines and inhibits tumor growth in vivo .

储存温度：-20°C储存

运输条件：超低温冰袋运输

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产品介绍：BKM120 (NVP-BKM120, Buparlisib)是一种选择性PI3K抑制，作用于p110α/β/δ/γ时，IC50分别为52 nM/166 nM/116 nM/262 nM，对VPS34， mTOR， DNAPK作用效果降低，对PI4Kβ几乎没有抑制活性。Phase 2。 A PI 3-kinase family inhibitorBKM120 is a selective PI3K inhibitor of p110α/β/δ/γ with IC50 of 52 nM/166 nM/116 nM/262 nM, respectively. Reduced potency against VPS34, mTOR, DNAPK, with little activity to PI4Kβ. Phase 2.A PI 3-kinase family inhibitor

ALogP：1.5

IUPAC Name：5-(2,6-dimorpholin-4-ylpyrimidin-4-yl)-4-(trifluoromethyl)pyridin-2-amine

INCHI：InChI=1S/C18H21F3N6O2/c19-18(20,21)13-9-15(22)23-11-12(13)14-10-16(26-1-5-28-6-2-26)25-17(24-14)27-3-7-29-8-4-27/h9-11H,1-8H2,(H2,22,23)

InChi Key：CWHUFRVAEUJCEF-UHFFFAOYSA-N

Canonical SMILES：C1COCCN1C2=NC(=NC(=C2)C3=CN=C(C=C3C(F)(F)F)N)N4CCOCC4

Isomeric SMILES：C1COCCN1C2=NC(=NC(=C2)C3=CN=C(C=C3C(F)(F)F)N)N4CCOCC4

PubChem CID：16654980

ChEMBL Ligand：CHEMBL2017974

CAS Registry No.：944396-07-0

RCSB PDB Ligand：SD5

Reactome Reaction：R-HSA-2400009

Reactome Drug：R-ALL-2399771

溶解性：DMSO 82 mg/mL Water <1 mg/mL Ethanol 2 mg/mL

象形图：

信号词：Danger

危险声明：H301 Toxic if swallowedH341 Suspected of causing genetic defectsH372 Causes damage to organs through prolonged or repeated exposure

预防措施声明：P321,P405,P501,P264,P260,P281,P270,P330,P203,P301+P316,P318,P319

产品包装