CAS NO: | 1397922-61-0 |
包装 | 价格(元) |
10 mM * 1 mL in DMSO | 电议 |
1mg | 电议 |
5mg | 电议 |
10mg | 电议 |
50mg | 电议 |
100mg | 电议 |
生物活性 | Pyrotinib dimaleate (SHR-1258 dimaleate) is a potent and selectiveEGFR/HER2dual inhibitor withIC50s of 13 and 38 nM, respectively[1]. | ||||||||||||||||
IC50& Target[1] |
| ||||||||||||||||
体外研究 (In Vitro) | Pyrotinib dimaleate has high potency in HER2-dependent cell lines (BT474, SK-OV-3), while showing much weaker inhibition in the HER2 negative cell line (MDA-MB-231). Pyrotinib dimaleate inhibits BT474 and SK-OV-3 cells with IC50s of 5.1 and 43 nM, respectively. Pyrotinib dimaleate displays high selectivity as HKI-272 when tested in a panel of different kinases such as KDR, c-Kit, PDGFRβ, c-Src and C-Met (c-Src with an IC50of 790 nM, and others >3000 nM)[1]. | ||||||||||||||||
体内研究 (In Vivo) | Pyrotinib dimaleate has acceptable bioavailability of 20.6%, 43.5% and 13.5% in nude mice, rats and dogs, respectively. Pyrotinib dimaleate has favorable drug-like physicochemical properties and shows relatively higher oral exposure in human subjects (oral; t1/2=15 h) with a much longer half life than that of preclinical animal species such as mouse (i.v.; t1/2=1.56 h; i.g.; t1/2=2.52 h) and rat (i.v.; t1/2=4.42 h; i.g.; t1/2=3.38 h)[1]. | ||||||||||||||||
Clinical Trial | |||||||||||||||||
分子量 | 815.22 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C40H39ClN6O11 | ||||||||||||||||
CAS 号 | 1397922-61-0 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) | ||||||||||||||||
溶解性数据 | In Vitro: H2O : ≥ 106 mg/mL(130.03 mM) DMSO : 100 mg/mL(122.67 mM;Need ultrasonic) *"≥" means soluble, but saturation unknown. 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
|