CAS NO: | 927880-90-8 |
包装 | 价格(元) |
10 mM * 1 mL in DMSO | 电议 |
5mg | 电议 |
10mg | 电议 |
25mg | 电议 |
50mg | 电议 |
100mg | 电议 |
200mg | 电议 |
生物活性 | RAF265 is a potent and orally activeRAF/VEGFR2inhibitor. | ||||||||||||||||
IC50& Target[1] |
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体外研究 (In Vitro) | The MTT assay reveals that in HT29 and MDAMB231 cells, RAF265 alone shows significant activity with IC20values of 1 to 3 μM and IC50values of 5 to 10 μM. In A549 and HCT116 cells, IC20values are 1 μM for both, but RAF265 concentrations up to 10 μM do not reach IC50values. However, in the presence of 1 nM RAD001, the IC50for RAF265 is 5 μM in A549 cells and 10 μM in HCT116 cells[1]. | ||||||||||||||||
体内研究 (In Vivo) | In single-compound efficacy studies, optimal dosing of RAD001 and RAF265 is 5 to 12 mg/kg daily and 30 mg/kg every two days, respectively. However, combination tolerability studies in nontumor-bearing mice defin dose-limiting toxicity as a 10% weight loss with the combination of RAD001 at a dose of 12 mg/kg daily and RAF265 at a dose of 20 mg/kg every two days. Therefore, the combination of RAF265 at a dose of 12 mg/kg qd and RAD001 at a dose of 12 mg/kg qd seems to be the maximal tolerated dose. RAD001 and RAF265 are both given at a dose of 12 mg/kg qd, alone or concurrently, over 6 days. After a 2-day stop, the compounds are given for another 6 days, and the treatment is then stopped. To confirm the potential of the combination of RAF265 and RAD001, the antitumor effect of the combination is tested in HCT116 xenografts (KRASmut,PIK3CAmut). In HCT116 xenografts, RAD001 or RAF265 given alone shows 60% to 65% and 71% to 72% TVI%, respectively[1]. | ||||||||||||||||
Clinical Trial | |||||||||||||||||
分子量 | 518.41 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C24H16F6N6O | ||||||||||||||||
CAS 号 | 927880-90-8 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 |
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溶解性数据 | In Vitro: DMSO : ≥ 26 mg/mL(50.15 mM) Ethanol : 10 mg/mL(19.29 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
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