CX-6258 hydrochloride hydrate

A pan-Pim kinase inhibitor

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库存: 现货

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5mg

￥1300.00

1040.00

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10mg

￥2500.00

2000.00

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50mg

￥7450.00

5960.00

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100mg

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0.00

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200mg

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货号: ajce55766
CAS: 1353858-99-7
别名: (3E)-5-氯-3-[[5-[3-[(六氢-4-甲基-1H-1,4-二氮杂卓-1-基)羰基]苯基]-2-呋喃基]亚甲基]-1,3-二氢-2H-吲哚-2-酮盐酸盐水合物
分子式: C26H27Cl2N3O4
分子量: 516.42
纯度: >98%
溶解度: DMSO: 25 mg/mL (48.41 mM)
储存: Store at -20°C
库存: 现货

Background

The family of Pim (Provirus Integration site for Moloney murine leukemia virus) proteins are serine/threonine kinases involved in cell survival and cell proliferation. CX-6258 is a potent, reversible inhibitor of Pim-1, -2, and -3 (IC₅₀s = 5, 25, and 16 nM, respectively).¹ It demonstrates excellent selectivity, inhibiting only FLT3 from a panel of 107 additional kinases. CX-6258 dose-dependently blocks the phosphorylation of the Pim targets Bad, 4E-BP1, and NKX3.1.^1,2 It acts synergistically with the chemotherapeutics doxorubicin and paclitaxel, presumably because CX-6258 impairs Pim-mediated enhanced expression of P-glycoprotein.¹ CX-6258 is orally bioavailable and inhibits the growth of MV4-11 xenografts in mice.¹

1.Haddach, M., Michaux, J., Schwaebe, M.K., et al.Discovery of CX-6258. A potent, selective, and orally efficacious pan-Pim kinases inhibitorACS Med. Chem. Lett.3(2)135-139(2011) 2.Padmanabhan, A., Gosc, E.B., and Bieberich, C.J.Stabilization of the prostate-specific tumor suppressor NKX3.1 by the oncogenic protein kinase Pim-1 in prostate cancer cellsJ. Cell. Biochem.1141050-1057(2013)