AS 703569

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Cenisertib (AS 703569;R763) 是一种新型强效口服 Aurora 激酶抑制剂，在体外和体内对多种肿瘤细胞均表现出显着的抗增殖活性 (A549 EC50=9 nM)。

Cenisertib (AS 703569;R763) is a novel potent, orally available inhibitor of Aurora kinases, exhibits signifficant anti-proliferative activity against a wide range of tumor cells both in vitro and in vivo (A549 EC50=9 nM); demonstrates marked inhibition of tumor growth in xenograft models of pancreatic, breast, colon, ovarian, and lung tumors and leukemia.Solid Tumors Phase 1 Discontinued.

Cenisertib (AS-703569) (1-1000 nM; for 48 hours) induces dose-dependent inhibition of proliferation in primary neoplastic mast cells (MC) .Cenisertib (5-100 nM; for 24 hours) induces a substantial G2/M cell cycle arrest at low nanomolar concentrations in all MC lines.Cenisertib (1-1000 nM; for 24 hours)induces apoptosis in HMC-1.1, HMC-1.2, C2, and NI-1 cells in a dose-dependent manner.Cenisertib (5-500 nM; for 24 hours) induces cleavage of caspase 3 in both HMC-1 sub-clones as well as in C2 and NI-1 cells. Cell Proliferation Assay Cell Line:HMC-1.1, HMC-1.2, ROSAKIT WT, ROSAKIT D816V and MCPV-1.1 mast cells Concentration:1, 5, 10, 50, 100, 500, 1000 nM Incubation Time:48 hours Result:Induced dose-dependent inhibition of proliferation in primary neoplastic MC.Cell Cycle Analysis Cell Line:HMC-1.1, HMC-1.2, C2 and NI-1 cells Concentration:5, 10, 50, 100 nM Incubation Time:24 hours Result:Induced a substantial G2/M cell cycle arrest at low nanomolar concentrations in all MC lines.Apoptosis Analysis Cell Line:HMC-1.1, HMC-1.2, C2 and NI-1 cells Concentration:1, 5, 10, 50, 100, 500, 1000 nM Incubation Time:24 hours Result:Induced apoptosis in HMC-1.1, HMC-1.2, C2, and NI-1 cells in a dose-dependent manner.Western Blot Analysis Cell Line:HMC-1.1, HMC-1.2, C2 and NI-1 cells Concentration:50, 100, 500 nM Incubation Time:24 hours Result:Induced cleavage of caspase 3 in both HMC-1 sub-clones as well as in C2 and NI-1 cells.

Cenisertib (AS-703569) (orally; 7 or 10 mg/kg/day; for 3 days followed by a 4-day rest period; for 4 weeks) significantly suppresses tumor growth. Animal Model:Female CB17 Severe Combined Immunodeficiency (SCID) mice bearing NCI-MDR tumors Dosage:7 and 10 mg/kg Administration:Orally; daily; for 3 days followed by a 4-day rest period; for 4 weeks Result:Suppressed significantly tumor growth.

R763 | Cenisertib

Cell Cycle/DNA Damage

Aurora Kinase

Aurora Kinase

Cancer

Solid Tumors

871357-89-0

451.54

C24H30FN7O

>98% (HPLC)

In Vitro:?DMSO : 250 mg/mL (553.66 mM)

O=C([C@H]1[C@](C2)([H])C=C[C@]2([H])[C@H]1NC3=NC(NC4=CC=C(N5CCN(C)CC5)C(C)=C4)=NC=C3F)N

(1S,2S,3R,4R)-3-((5-fluoro-2-((3-methyl-4-(4-methylpiperazin-1-yl)phenyl)amino)pyrimidin-4-yl)amino)bicyclo[2.2.1]hept-5-ene-2-carboxamide

(-20℃)

With Ice Pack

≥ 2 years