产品名称

英文名称：GSK2126458 (GSK458)

同义词

Omipalisib、1086062-66-9、GSK2126458、GSK-2126458、2,4-difluoro-N-(2-methoxy-5-(4-(pyridazin-4-yl)quinolin-6-yl)pyridin-3-yl)benzenesulfonamide、GSK 2126458、2,4-difluoro-N-[2-methoxy-5-(4-pyridazin-4-ylquinolin-6-yl)pyridin-3-yl]benzenesulfonamide、GSK-212、2,4-

产品性质

CAS编号：1086062-66-9

分子式：C25H17F2N5O3S

分子量：505.5

EC号：629-873-1

PubChem编号：25167777

英文别名：Omipalisib|1086062-66-9|GSK2126458|GSK-2126458|2,4-difluoro-N-(2-methoxy-5-(4-(pyridazin-4-yl)quinolin-6-yl)pyridin-3-yl)benzenesulfonamide|GSK 2126458|2,4-difluoro-N-[2-methoxy-5-(4-pyridazin-4-ylquinolin-6-yl)pyridin-3-yl]benzenesulfonamide|GSK-212|2,4-

规格或纯度：≥98%

英文名称：GSK2126458 (GSK458)

生化机理：GSK2126458 (GSK458) is an orally active, highly potent and selective ATP site inhibitor against phosphoinositide 3-kinase (PI3K p110α CI50 = 40 pM; p100 α/δ/γ/β Ki = 19/24/60/130 pM; p110α E542K/E545K/H1047R Ki = 8/8/9 pM), mTOR (mTORC1/C2 Ki = 180/300 pM) and DNA-PK (IC50 = 280 pM) with >10,000-fold selectivity over more than 240 other kinases evaluated. GSK458 inhibits cellular AKT pS473 and growth of breast cancer cells in cultures (pAKT/growth IC50 = 0.41/3 nM/T-47D and 0.18/2.4/BT-474) and in vivo (0.3-3 mg/kg, 5x per wk for 3 wks p.o. in mice).

储存温度：-20°C储存

运输条件：超低温冰袋运输

备注：2mg卖完停产，不再备货

产品介绍：Omipalisib (GSK2126458, GSK458)是一种高选择性的，有效的p110α/β/γ/δ和 mTORC1/2抑制剂，无细胞试验中Ki分别为0.019 nM/0.13 nM/0.024 nM/0.06 nM和0.18 nM/0.3 nM。Omipalisib 可诱导自噬。GSK2126458 is a highly selective and potent inhibitor of PI3K with Ki of 0.019 nM/0.13 nM/0.024 nM/0.06 nM and 0.18 nM/0.3 nM for p110α/β/δ/γ, mTORC1/2 , respectively.

ALogP：3.3

IUPAC Name：2,4-difluoro-N-[2-methoxy-5-(4-pyridazin-4-ylquinolin-6-yl)pyridin-3-yl]benzenesulfonamide

INCHI：InChI=1S/C25H17F2N5O3S/c1-35-25-23(32-36(33,34)24-5-3-18(26)12-21(24)27)11-17(13-29-25)15-2-4-22-20(10-15)19(7-8-28-22)16-6-9-30-31-14-16/h2-14,32H,1H3

InChi Key：CGBJSGAELGCMKE-UHFFFAOYSA-N

Canonical SMILES：COC1=C(C=C(C=N1)C2=CC3=C(C=CN=C3C=C2)C4=CN=NC=C4)NS(=O)(=O)C5=C(C=C(C=C5)F)F

Isomeric SMILES：COC1=C(C=C(C=N1)C2=CC3=C(C=CN=C3C=C2)C4=CN=NC=C4)NS(=O)(=O)C5=C(C=C(C=C5)F)F

关联CAS：1086062-66-9

PubChem CID：25167777

MeSH Entry Terms：2,4-difluoro-N-(2-(methyloxy)-5-(4-(4-pyridazinyl)-6-quinolinyl)-3-pyridinyl)benzenesulfonamide;GSK 212;GSK 2126458;GSK-212;GSK-2126458;GSK212;GSK2126458;omipalisib

溶解性：溶于DMSO, 最高浓度 (mg/mL) 10.11, 最高浓度(mM) 20

熔点：184-186°C

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 exposureH361 Suspected of damaging fertility or the unborn child

预防措施声明：P280,P321,P405,P501,P264,P260,P281,P270,P330,P203,P301+P316,P318,P319

产品包装