CS-1092
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- CAS号:
- 837364-57-5
- 英文名:
- AG-024322
- 英文别名:
- CS-1092;AG-24322;AG-024322;AG024322; AG-024322;5-[3-(5,7-difluoro-1H-benzimidazol-2-yl)-1H-indazol-5-yl]-N-ethyl-4-methyl-3-Pyridinemethanamine;3-Pyridinemethanamine, 5-[3-(5,7-difluoro-1H-benzimidazol-2-yl)-1H-indazol-5-yl]-N-ethyl-4-methyl-;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
- 中文名:
- CS-1092
- 中文别名:
- 化合物 T14136
- CBNumber:
- CB32668418
- 分子式:
- C23H20F2N6
- 分子量:
- 418.44
- MOL File:
- 837364-57-5.mol
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CS-1092化学性质
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沸点:
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668.4±65.0 °C(Predicted)
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密度:
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1.361±0.06 g/cm3(Predicted)
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储存条件:
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Store at -20°C
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酸度系数(pKa):
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7.84±0.30(Predicted)
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CS-1092性质、用途与生产工艺
AG-024322 是一种有效的 ATP 竞争性的 pan-CDK 抑制剂，抑制 CDK1， CDK2， CDK4 的 Ki 值在 1-3 nM 范围内。AG-024322 在体内表现出广谱抗肿瘤活性和清晰的靶标调控。AG-024322 诱导细胞凋亡 (apoptosis)。
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COX-1
2.3 nM (Ki)
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COX-2
3 nM (Ki)
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COX-4
2.9 nM (Ki)
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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.
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Animal Model:
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Male and female cynomolgus monkeys
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Dosage:
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2, 6, and 10 mg/kg (Toxicity analysis)
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Administration:
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Intravenous infusion; 5 days
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Result:
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Resulted in dose-dependent pancytic bone marrow hypocellularity and lymphoid depletion in lymph nodes, spleen, and/or thymus at >6 mg/kg.
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CS-1092
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2024/04/30 | HY-15491 | AG-024322 | | 1 mg | 2400元 |
| 2024/04/30 | HY-15491 | CS-1092
AG-024322 | 837364-57-5 | 5mg | 6000元 |
837364-57-5, CS-1092 相关搜索:
- C23H20F2N6
- 化合物 T14136
- 837364-57-5
- 3-Pyridinemethanamine, 5-[3-(5,7-difluoro-1H-benzimidazol-2-yl)-1H-indazol-5-yl]-N-ethyl-4-methyl-
- AG024322; AG-024322
- CS-1092
- AG-24322
- 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
- 5-[3-(5,7-difluoro-1H-benzimidazol-2-yl)-1H-indazol-5-yl]-N-ethyl-4-methyl-3-Pyridinemethanamine
- AG-024322