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DCC-2036 (Rebastinib)
| 品牌 | 厂商性质 | 产地 | 货期 |
|---|---|---|---|
| 阿拉丁 | 生产商 | 上海 | 现货 |
| 货号 | CAS号 | 操作 |
|---|---|---|
| D126373-10mg | 1020172-07-9 | 询价 |
| D126373-50mg | 1020172-07-9 | 询价 |
- 分子式 C30H28FN7O3
- 分子量553.59
属性
| 溶解性 |
|
| 存贮条件 | 储存温度-20°C |
描述
| 备注 | DCC-2036 is a conformational control Bcr-Abl inhibitor for Abl1(WT) and Abl1(T315I) with IC50 of 0.8 nM and 4 nM, also inhibits SRC, LYN, FGR, HCK, KDR, FLT3, and Tie-2, and low activity to seen towards c-Kit. Phase 1/2. |
| 生化机理 |
The lead "switch-control" inhibitor, DCC-2036, potently inhibits both unphosphorylated and phosphorylated ABL1 by inducing a type II inactive conformation, and retains efficacy against the majority of clinically relevant CML-resistance mutants, including T315I. DCC-2036 inhibits autophosphorylation of ABL and ABLT315I enzymes, and this activity was consistent with selective efficacy against Ba/F3 cells expressing BCR-ABL (IC50: 19 nmol/L), BCR-ABLT315I (IC50: 63 nmol/L), and most kinase domain mutants. These findings support continued evaluation of DCC-2036 as an important new agent for treatment-refractory CML. |
| 别名 | 1-(3-tert-butyl-1-(quinolin-6-yl)-1H-pyrazol-5-yl)-3-(2-fluoro-4-(2-(methylcarbamoyl)pyridin-4-yloxy)phenyl)urea;1-(3-tert-butyl-1-(quinolin-6-yl)-1H-pyrazol-5-yl)-3-(2-fluoro-4-(2-(methylcarbamoyl)pyridin-4-yloxy)phenyl)urea |
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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途