CAS NO: | 1637735-84-2 |
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 | FIIN-3 is an irreversible inhibitor ofFGFRwith anIC50of 13.1, 21, 31.4, and 35.3 nM forFGFR1,FGFR2,FGFR3andFGFR4, respectively. | ||||||||||||||||
IC50& Target |
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体外研究 (In Vitro) | FIIN-3 potently inhibits both WT FGFRs (EC50in the 1- to 41-nM range) and the gatekeeper mutant of FGFR2 (EC50of 64 nM). FIIN-3 also strongly inhibits EGFR, with an EC50of 43 nM. FIIN-3 shows good potency against gatekeeper mutant V564F; FIIN-3 also is potent against the gatekeeper-plus-1 mutant E565K; FIIN-3 also displays antiproliferative activity (with an EC50of 135 nM) against Ba/F3 cells transformed by the EGFR vIII fusion protein, which has a WT EGFR kinase domain. FIIN-3 shows even better activity against EGFR mutant L858R (EC50of 17 nM) and moderate activity, displaying an EC50of 231 nM, against the EGFR mutant L858R/T790M mutant. In WT FGFR2 Ba/F3 cells, FIIN-3 completely inhibits the FGFR2 autophosphorylation on Tyr656/657 at concentrations as low as 3 nM. In FGFR2 V564M Ba/F3 cells, FIIN-3 is capable of inhibiting the FGFR2 mutant V564M autophosphorylation with partial inhibition at 100 nM and complete inhibition observed at 300 nM[1]. | ||||||||||||||||
分子量 | 691.61 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C34H36Cl2N8O4 | ||||||||||||||||
CAS 号 | 1637735-84-2 | ||||||||||||||||
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 : 10 mg/mL(14.46 mM;Need ultrasonic and warming) 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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