| 貨號(hào) | 規(guī)格 | 價(jià)格 | 上海 | 北京 | 武漢 | 南京 | 購(gòu)買數(shù)量 |
|---|---|---|---|---|---|---|---|
S81222-1mg |
99.3% | ￥180.00 | 8 | - | - | - |
|
S81222-2mg |
99.3% | ￥290.00 | 8 | - | - | - |
|
S81222-5mg |
99.3% | ￥500.00 | 7 | - | - | - |
|
S81222-10mg |
99.3% | ￥990.00 | 6 | - | - | - |
|
S81222-25mg |
99.3% | ￥1690.00 | 5 | - | - | - |
|
S81222-50mg |
≥97% | ￥3200.00 | 貨期：2-3天 | - | - | - |
|
S81222-100mg |
≥97% | ￥4500.00 | 貨期：2-3天 | - | - | - |
|
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(chǎn)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(diǎn)： | 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(nèi)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(xiàn)： | 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： |
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| 注意： | 部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶參考交流研究之用。 |
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