Cobimetinib hemifumarate

A potent, orally available MEK1 inhibitor

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库存: 现货

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数量
2mg

￥550.00

440.00

- +
5mg

￥1050.00

840.00

- +
10mg

￥1300.00

1040.00

- +
50mg

￥4262.00

3410.00

- +
100mg

￥0.00

0.00

- +
200mg

￥0.00

0.00

- +

已选 0 种 0 瓶

金额: ￥0.00

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货号: ajce55680
CAS: 1369665-02-0
别名: 考比替尼半富马酸盐; GDC-0973 hemifumarate; XL-518 hemifumarate
分子式: C25H25F3IN3O6
分子量: 647.38
纯度: >98%
溶解度: DMSO: 50 mg/mL (77.23 mM)
储存: Store at -20°C
库存: 现货

Background

Cobimetinib is a potent, orally available inhibitor of MEK1 (IC₅₀ = 4.2 nM).^1,2 It shows more than 100-fold selectivity for MEK when tested against a panel of more than 100 serine-threonine and tyrosine kinases. Cobimetinib induces differentiation and apoptosis in cancer cell lines and is more effective when combined with additional inhibitors, like PLX4032 .^2,3,4

1.Akinleye, A., Furgan, M., Mukhi, N., et al.MEK and the inhibitors: From bench to bedsideJ. Hematol. Oncol.627(2013) 2.Hoeflich, K.P., Merchang, M., Orr, C., et al.Intermittent administration of MEK inhibitor GDC-0973 plus PI3K inhibitor GDC-0941 triggers robust apoptosis and tumor growth inhibitionCancer Res.72(1)210-219(2012) 3.Medina, T.M., and Lewis, K.D.The evolution of combined molecular targeted therapies to advance the therapeutic efficacy in melanoma: A highlight of vemurafenib and cobimetinibOnco Targets Ther.93739-3752(2016) 4.Sing, A., Ruan, Y., Tippett, T., et al.Targeted inhibition of MEK1 by cobimetinib leads to differentiation and apoptosis in neuroblastoma cellsJ. Exp. Clin. Cancer Res.34(1)104(2015)