貨號	規格	價格	上海	北京	武漢	南京
S81222-1mg	99.3%	￥180.00 S81222-1mg ￥180.00 現貨	8 8	-	-	-
S81222-2mg	99.3%	￥290.00 S81222-2mg ￥290.00 現貨	8 8	-	-	-
S81222-5mg	99.3%	￥500.00 S81222-5mg ￥500.00 現貨	7 7	-	-	-
S81222-10mg	99.3%	￥990.00 S81222-10mg ￥990.00 現貨	6 6	-	-	-
S81222-25mg	99.3%	￥1690.00 S81222-25mg ￥1690.00 現貨	5 5	-	-	-
S81222-50mg	≥97%	￥3200.00 S81222-50mg ￥3200.00 2-3天	0 貨期：2-3天	-	-	-
S81222-100mg	≥97%	￥4500.00 S81222-100mg ￥4500.00 2-3天	0 貨期：2-3天	-	-	-

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產品介紹

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)

產品描述：

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)

靶點：

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

體外研究：

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

體內研究：

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

參考文獻：

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

保存條件：

-20℃

配置溶液濃度參考：

	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

注意：

部分產品我司僅能提供部分信息，我司不保證所提供信息的權威性，僅供客戶參考交流研究之用。

參考文獻

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