CX 6258 hydrochloride hydrate
产品详情：
更新时间： 2023-09-30 18:56:13
CAS号：1353858-99-7
常用名：
价格：
$需询单/100g
$需询单/1kg
$需询单/100kg
$需询单/1000kg
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 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：达阳化工（杭州）有限公司 推荐
认证状态： 已认证供应商
商品数： 50181件
电话： +86571-88938639
地址： 浙江省杭州市西湖区文三路259号2栋9楼
地区： 杭州市西湖区
联系人： 王小姐
联系人电话： +86-571-8893-8639
邮件：enquiry@dycnchem.com
主要市场：Mainly in Southeast Asia and European and American markets
年贸易额：10 to 20 million USD
外贸占销售比例：90%
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其他供应商价格：
2022-09-23 价格：￥1333.0
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CX 6258 hydrochloride hydrate价格为$需询单/100g, 由CX 6258 hydrochloride hydrate生产厂家达阳化工（杭州）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【达阳化工（杭州）有限公司】
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