CAS NO: | 2216753-97-6 |
包装 | 价格(元) |
5mg | 电议 |
10mg | 电议 |
50mg | 电议 |
100mg | 电议 |
生物活性 | Zeteletinib (BOS-172738; DS-5010) is an orally active, selectiveRETkinaseinhibitor with nanomolar potency againstRETand >300-fold selectivity against VEGFR2. Zeteletinib shows exquisite potency for the wild typeRET,RETV804M/Lgatekeeper mutants, and the most common oncogenicRETmutationM918T. Zeteletinib has potent antitumor activity[1][2][3]. | ||||||||||||||||
IC50& Target[1] |
| ||||||||||||||||
体外研究 (In Vitro) | In biochemical assays of 106 kinases, RET and platelet-derived growth factor receptor (PDGFR) alpha/beta were inhibited more than 80% by 193 nM Zeteletinib (BOS-172738; DS-5010). The IC50values of Zeteletinib against RET, RET-GKm (V804L) were single digit nano-molar even under a condition of high concentration of ATP; besides it against KDR was more than 1000 nM[1]. | ||||||||||||||||
体内研究 (In Vivo) | In a Ba/F3-RET subcutaneous tumor model, Zeteletinib (BOS-172738; DS-5010) dosing at 10 mg/kg twice daily (bid) induces tumor regression[1]. | ||||||||||||||||
Clinical Trial | |||||||||||||||||
分子量 | 500.47 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C25H23F3N4O4 | ||||||||||||||||
CAS 号 | 2216753-97-6 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 |
| ||||||||||||||||
溶解性数据 | In Vitro: DMSO : 100 mg/mL(199.81 mM;Need ultrasonic) 配制储备液
* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百
|