品牌	货号	产品规格	价格(RMB)	库存（上海）	北京	武汉	南京
源叶(MedMol)	S81222-1mg	97%	￥180.00元	8	-	-	-
源叶(MedMol)	S81222-2mg	97%	￥290.00元	8	-	-	-
源叶(MedMol)	S81222-5mg	97%	￥500.00元	7	-	-	-
源叶(MedMol)	S81222-10mg	97%	￥990.00元	6	-	-	-
源叶(MedMol)	S81222-25mg	97%	￥1690.00元	5	-	-	-
源叶(MedMol)	S81222-50mg	97%	￥3200.00元	预计交期：2-3天	-	-	-
源叶(MedMol)	S81222-100mg	97%	￥4500.00元	预计交期：2-3天	-	-	-

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产品介绍

GDC-0623 (RG 7421) is a potent, ATP-uncompetitive inhibitor of MEK1 (Ki=0.13 nM, +ATP), and displays 6-fold weaker potency against HCT116 (KRAS (G13D), EC50=42 nM) versus A375 (BRAFV600E, EC50=7 nM)

产品描述： GDC-0623 (RG 7421) is a potent, ATP-uncompetitive inhibitor of MEK1 (Ki=0.13 nM, +ATP), and displays 6-fold weaker potency against HCT116 (KRAS (G13D), EC50=42 nM) versus A375 (BRAFV600E, EC50=7 nM)

靶点： MEK1:0.13 nM (Ki, +ATP);Apoptosis; MEK

体外研究：
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). 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

体内研究：
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

参考文献：
1. Hatzivassiliou G, et al. Mechanism of MEK inhibition determines efficacy in mutant KRAS- versus BRAF-driven cancers. Nature. 2013 Sep 12;501(7466):232-6. 2. Takahashi RH, et al. Elucidating the Mechanisms of Formation for Two Unusual Cytochrome P450-Mediated Fused Ring Metabolites of GDC-0623, a MAPK/ERK Kinase Inhibitor. Drug Metab Dispos. 2015 Dec;43(12):1929-1933.

溶解性： soluble in DMSO

保存条件： -20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.192 ml	10.96 ml	21.92 ml
5 mM	0.438 ml	2.192 ml	4.384 ml
10 mM	0.219 ml	1.096 ml	2.192 ml
50 mM	0.044 ml	0.219 ml	0.438 ml

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部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

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GDC-0623 97%

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