
GDC-0623
CAS No. 1168091-68-6
GDC-0623 ( GDC0623 | GDC-0632 | GDC 0632 | G868 | G 868 | G-868 )
产品货号. M17163 CAS No. 1168091-68-6
GDC-0623 是一种有效的 ATP 非竞争性 MEK1 抑制剂,Ki 为 0.13 nM。
纯度: >98% (HPLC)






规格 | 价格/人民币 | 库存 | 数量 |
2MG | ¥543 | 有现货 |
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5MG | ¥988 | 有现货 |
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10MG | ¥1596 | 有现货 |
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25MG | ¥2730 | 有现货 |
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50MG | ¥3823 | 有现货 |
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100MG | ¥5484 | 有现货 |
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200MG | 获取报价 | 有现货 |
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500MG | 获取报价 | 有现货 |
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1G | 获取报价 | 有现货 |
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生物学信息
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产品名称GDC-0623
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注意事项本公司产品仅用于科研实验,不得用于人体或动物的临床与诊断
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产品简述GDC-0623 是一种有效的 ATP 非竞争性 MEK1 抑制剂,Ki 为 0.13 nM。
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产品描述GDC-0623, also known as G-868, is an orally active, selective MEK inhibitor with potential antineoplastic activity. MEK inhibitor GDC-0623 specifically inhibits mitogen-activated protein kinase kinase (MEK or MAP/ERK kinase), resulting in inhibition of growth factor-mediated cell signaling and tumor cell proliferation. MEK is a key component of the RAS/RAF/MEK/ERK signaling pathway that regulates cell growth; constitutive activation of this pathway has been implicated in many cancers. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).(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). 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.(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.
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体外实验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.
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体内实验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.
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同义词GDC0623 | GDC-0632 | GDC 0632 | G868 | G 868 | G-868
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通路Others
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靶点Other Targets
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受体MEK1
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研究领域Cancer
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适应症——
化学信息
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CAS Number1168091-68-6
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分子量456.21
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分子式C16H14FIN4O3
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纯度>98% (HPLC)
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溶解度DMSO : ≥ 30 mg/mL. 65.76 mM
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SMILESOCCONC(=O)C1=C(NC2=C(F)C=C(I)C=C2)N2C=NC=C2C=C1
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化学全称5-((2-fluoro-4-iodophenyl)amino)-N-(2-hydroxyethoxy)imidazo[1,5-a]pyridine-6-carboxamide
运输与储存
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储存条件(-20℃)
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运输条件With Ice Pack
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稳定性≥ 2 years
参考文献




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