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| 品牌 | |
| 货号 | 6978 |
| 用途 | 科研医药 |
| 是否危险化学品 | |
| 包装规格 | 100g |
| 别名 | RXDX-101 |
| CAS编号 | 1108743-60-7 |
| 产地/厂商 | xxjl |
| 是否进口 |
RXDX-101
CAS 号：1108743-60-7
英文名字：Entrectinib
质量标准：>98%,TrkA/B/C，ROS1 和 ALK 抑制剂
分子式：C31H34F2N6O2
| 分子量 | 560.64 |
化学式 | C31H34F2N6O2 |
CAS号 | 1108743-60-7 |
稳定性 | 3 years -20°C powder |
2 years -80°C in solvent |
溶解性
| DMSO | 100 mg/mL (178.36 mM) |
Ethanol | 100 mg/mL (178.36 mM) 难溶或者不溶 |
Water | <1 mg/mL 难溶或者不溶 |
生物活性
| 产品描述 | Entrectinib (RXDX-101)是一种口服生物可利用的泛-TrkA/B/C，ROS1 和 ALK 抑制剂，IC50范围为 0.1~1.7 nM。Phase 2。 |
靶点 | TrkATrkBTrkCROS1ALK |
体外研究 | Entrectinib selectively blocks proliferation of ALK-dependent cell lines and potently inhibits ALK‐dependent signaling. Entrectinib also highly inhibits cell growth of the NSCLC cell line NCI‐H2228 bearing the EML4-ALK rearrangement. |
体内研究 | In mice bearing Karpas-299 and SR-786 xenografts, Entrectinib (p.o.) induces complete tumor regression. In NPM-ALK transgenic mice, Entrectinib induces complete regression of tumor masses observed in the thymus and in lymph nodes. In the NB xenograft model, Entrectinib cotreatment enhanced the efficacy of conventional chemotherapy. |
