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CX-6258,pan-Pim激酶抑制剂

CX-6258 （订货以英文为准）

编号：C126466
CAS号：1202916-90-2
分子式：C26H24N3O3CL
分子量：461.94
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C126466-5mg 阿拉丁 5mg ¥669.90
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C126466-100mg 阿拉丁 100mg ¥4899.90
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C126466-25mg 阿拉丁 25mg ¥2099.90
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产品名称 CX-6258
中文名称 CX-6258,pan-Pim激酶抑制剂
CAS号 1202916-90-2
分子式（M.F.） C26H24N3O3CL
分子量（M.W.） 461.94
储存条件 -20°C储存
溶解性25°C: DMSO
存贮条件储存温度-20°C
产品介绍CX-6258是口服活性的Pim 1，2和3激酶抑制剂，IC50为5 nM，25 nM和16 nM。
生化机理Description:IC50 Value: 5 nM (Pim 1); 25 nM (Pim 2); 16 nM (Pim 3) [1]CX-6258 is a potent, orally efficacious pan-Pim kinases Inhibitor with excellent biochemical potency and kinase selectivity.in vitro: CX-6258 inhibited Flt-3 and Pim-3 (IC50=0.134 and 0.016 uM). At 0.5 uM of CX-6258, only Pim-1, Pim-2, Pim-3, and Flt-3 of the 107 kinases tested were inhibited by more than 80%, showing excellent selectivity. CX-6258 was also shown to be a reversible inhibitor of Pim-1 (Ki=0.005 uM). CX-6258 showed robust antiproliferative potencies against all cell lines tested derived from human solid tumors and hematological malignancies. In mechanistic cellular assays with MV-4-11 human AML cells, (13) caused dose-dependent inhibition of the phosphorylation of 2 pro-survival proteins, Bad and 4E-BP1, at the Pim kinase specific sites S112 and S65 and T37/46, respectively[1]. Pim-1 inhibition using the small molecule inhibitor CX-6258 (12 mM, 3 h) diminishes endogen
别名CX6258;CX 6258;(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;CX6258;CX 6258;(3E)-5-Chloro-3-[[5-[3-[(hexahydro-4-methyl-1H-1,4-diazepin-1-yl)carbonyl]phenyl]-2-furanyl]methylene]-1,3-dihydro-2H-indol-2-one
标识符号https://www.aladdin-e.com/images/ghs/ghs07.jpg
信号词Warning
危害声明H302
个人防护设备dust mask type N95 (US), Eyeshields, Gloves
RTECSTK9187000
WGK德国3
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