CS-1092
中文名称 | CS-1092 |
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中文同义词 | 化合物 T14136 |
英文名称 | AG-024322 |
英文同义词 | AG-024322;5-[3-(5,7-difluoro-1H-benzimidazol-2-yl)-1H-indazol-5-yl]-N-ethyl-4-methyl-3-Pyridinemethanamine;N-((5-((19E)-3-(4,6-DIFLUORO-2H-BENZO[D]IMIDAZOL-2-YLIDENE)-2,3-DIHYDRO-1H-INDAZOL-5-YL)-4-METHYLPYRIDIN-3-YL)METHYL)ETHANAMINE;AG-24322;CS-1092;AG024322; AG-024322;3-Pyridinemethanamine, 5-[3-(5,7-difluoro-1H-benzimidazol-2-yl)-1H-indazol-5-yl]-N-ethyl-4-methyl- |
CAS号 | 837364-57-5 |
分子式 | C23H20F2N6 |
分子量 | 418.44 |
EINECS号 | |
相关类别 | |
Mol文件 | 837364-57-5.mol |
结构式 | ![]() |
CS-1092 性质
沸点 | 668.4±65.0 °C(Predicted) |
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密度 | 1.361±0.06 g/cm3(Predicted) |
储存条件 | Store at -20°C |
酸度系数(pKa) | 7.84±0.30(Predicted) |
形态 | 固体 |
颜色 | 白色至米白色 |
COX-1 2.3 nM (Ki) |
COX-2 3 nM (Ki) |
COX-4 2.9 nM (Ki) |
AG-024322 (0.1-30 μM; 24 hours) is less toxic at concentrations below 3 µM, the viability of human PBMCs as measured by ATP content with a TC 50 value of 1.4 µM for human PBMCs.AG-024322 (0-120 nM) exhibits growth inhibition effects on HCT-116 cells. It is slightly less potent in the functional cellular assay with an IC 50 of 120 nM.
AG-024322 (intravenous infusion; 2, 6, and 10 mg/kg; 5 days) exhibits no-adverse-effect at 2 mg/kg with mean plasma AUC (0-24.5) of 2.11 g.h/mL. At 6 mg/kg produces pancytic bone marrow hypocellularity, lymphoid depletion. And vascular injury at the injection site renal tubular degeneration occurs at 10 mg/kg.AG-024322 (20 mg/kg) inhibits the growth of established human tumor xenografts of different origins with tumor growth inhibition (TGI) ranging from 32% to 86.4%.It also exhibits anti-tumor effects as a dose-pdependent manner.AG-024322 (20 mg/kg) causes a 65% TGI in the MV522 tumor model. It results a 52% TGI at 1/2 of the maximum tolerated dose (MTD) and only slight anti-tumor activity at 1/4 of the MTD.
Animal Model: | Male and female cynomolgus monkeys |
Dosage: | 2, 6, and 10 mg/kg (Toxicity analysis) |
Administration: | Intravenous infusion; 5 days |
Result: | Resulted in dose-dependent pancytic bone marrow hypocellularity and lymphoid depletion in lymph nodes, spleen, and/or thymus at >6 mg/kg. |
安全信息
更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
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2024/08/19 | HY-15491 | AG-024322 | 1 mg | 2400元 | |
2024/08/19 | HY-15491 | CS-1092 AG-024322 | 837364-57-5 | 5mg | 6000元 |