CX-6258 hydrochloride hydrate
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发布时间： 2024-07-15 12:31:39
CAS号：1353858-99-7
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纯度： 99.0%
备货期： 10天
库存： 现货
其他详情（用途，包装）：
用途： CX-6258 hydrochloride hydrate 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：1353858-99-7 常用中文名：CX-6258盐酸盐水合物 常用英文名：CX-6258 (hydrochloride hydrate) 分子式：C26H27Cl2N3O4 分子量：516.416 密度：N/A 沸点：N/A 熔点：N/A 闪点：N/A 储存条件：2-8℃
供应商信息：
公司名：上海念兴实业有限公司 推荐
认证状态： 已认证供应商
商品数： 403768件
电话： 18916513247
地址： 2222 Huancheng Road, Juyuan New District, Jiading District, Shanghai
地区： 上海市普陀区
联系人： 小陈
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2022-09-23 价格：￥1333.0
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CX-6258 hydrochloride hydrate价格为, 由CX-6258 hydrochloride hydrate生产厂家上海念兴实业有限公司提供，供应信息包括纯度，备货期/库存，供货能力等。>>电脑版：CX-6258 hydrochloride hydrate_价格_生产厂家【上海念兴实业有限公司】
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