CAS NO: | 1168091-68-6 |
包装 | 价格(元) |
10 mM * 1 mL in DMSO | 电议 |
2mg | 电议 |
5mg | 电议 |
10mg | 电议 |
50mg | 电议 |
100mg | 电议 |
200mg | 电议 |
500mg | 电议 |
生物活性 | GDC-0623 (RG 7421) is a potent, ATP-uncompetitive inhibitor ofMEK1(Ki=0.13 nM, +ATP), and displays 6-fold weaker potency against HCT116 (KRAS (G13D), EC50=42 nM) versus A375 (BRAFV600E, EC50=7 nM). | ||||||||||||||||
IC50& Target[1] |
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体外研究 (In Vitro) | GDC-0623 (RG 7421) and G-573 are able to prevent MEK phosphorylation by CRAF in vitro, and able to block MEK phosphorylation by BRAF(V600E)[1]. GDC-0623 (RG 7421) is potent, ATP-uncompetitive inhibitors of MEK1 but shows distinct shifts in cellular activity compared with the other two inhibitors, only 6-fold half-maximum effective concentration (EC50) decreases[2]. | ||||||||||||||||
体内研究 (In Vivo) | GDC-0623 (RG 7421) (40 mg/kg, p.o.) shows percent tumour growth inhibition (%TGI) in MiaPaCa-2 xenograft model. GDC-0623 (RG 7421) and G-573 show superior antitumour activity compared to GDC-0623 (RG 7421) in all three KRAS models[1]. | ||||||||||||||||
Clinical Trial | |||||||||||||||||
分子量 | 456.21 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C16H14FIN4O3 | ||||||||||||||||
CAS 号 | 1168091-68-6 | ||||||||||||||||
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 : 50 mg/mL(109.60 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
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