CX-6258

产品详情：

更新时间： 2024-09-12 14:57:37

CAS号：1202916-90-2

常用名： (3E)-5-氯-3-[[5-[3-[(六氢-4-甲基-1H-14-二氮杂革-1-基)羰基]苯基]-2-呋喃]亚甲基]-1,3-二氢-2H-吲哚-2-酮

价格：
￥需询单/1kg ￥需询单/1g ￥需询单/1mg

纯度： 98.0%

备货期： 需询单

库存： 询单

其他详情（用途，包装）：
用途： CX-6258 is a potent, orally efficacious Pim 1/2/3 kinase(IC50=5 nM/25 nM/16 nM) inhibitor with excellent biochemical potency and kinase selectivity.IC50 Value: 5 nM/25 nM/16 nM (Pim 1/2/3) [1]Target: pan-Pimin 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 endogenous NKX3.1 steady state levels in 22RV1 and LNCaP cells. CX-6258 treatment (12 mM, 3 h) treatment diminished steady-state levels of ectopic NKX3.1 in PC3 cells. CX-6258 treatment resulted in a significant reduction in NKX3.1 half-life. While ectopically expressed NKX3.1 in control cells had a half-life of _90 min, Pim-1 inhibition reduced the half-life to _52 min [2].in vivo: CX-6258 showed dose-dependent efficacy in mice bearing MV-4-11 xenografts, with 45% and 75% TGI at 50 and 100 mg/kg/day, respectively. Treatment of mice bearing PC3 xenografts with CX-6258 p.o. 50 mg/kg was also well tolerated and produced 51% TGI. 物理化学性质： CAS号：1202916-90-2 常用中文名：(3E)-5-氯-3-[[5-[3-[(六氢-4-甲基-1H-14-二氮杂革-1-基)羰基]苯基]-2-呋喃]亚甲基]-1,3-二氢-2H-吲哚-2-酮常用英文名：CX-6258 分子式：C26H24ClN3O3 分子量：461.940 密度：1.3±0.1 g/cm3 沸点：697.8±55.0 °C at 760 mmHg 熔点：N/A 闪点：375.8±31.5 °C 储存条件：-20℃

供应商信息：

公司名：上海楼岚生物科技有限公司

认证状态： 未认证供应商

商品数： 2474件

电话： 52996696

地址： 沪南路2729弄1310号

地区： 上海市浦东新区

联系人： 孙先生

联系人电话： 021-52996696

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2024-07-15 价格：需询单 CX-6258

2022-02-19 价格：￥2099.9 CX-6258

2021-02-06 价格：￥1309.0 CX-6258

2018-02-11 价格：￥需询单 CX-6258

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(3E)-5-氯-3-[[5-[3-[(六氢-4-甲基-1H-14-二氮杂革-1-基)羰基]苯基]-2-呋喃]亚甲基]-1,3-二氢-2H-吲哚-2-酮价格

CX-6258

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