CS-2259
更新时间：2024-07-15 12:32:01
采购访问：10次
| 常用名 | CDKI-73 | CAS号 | 1421693-22-2 |
|---|---|---|---|
| 价格 | 纯度 | 99.0% | |
| 备货期 | 10天 | 库存 | 现货 |
| 产品详情（用途，包装等）
用途： CDKI-73 is a potent CDK9 inhibitor with Ki of 4 nM; shows selective toxicity to CLL cells(LD50=80 nM) versus normal B cell and normal CD34+ cell(LD50>20 uM).IC50 value: 4 nM/80 nM(Ki/LD50) [1]Target: CDK9 inhibitorin vitro: CDKI-73 was cytotoxic to all of the CLL samples tested (n = 38) with a mean LD50 value of 0.08μM ± 0.10 μM following exposure to drug for 48h. In contrast, normal B-lymphocytes (n = 10) and CD34+ normal bone marrow cells (n = 5) were significantly less susceptible to the cytotoxic effects of CDKI-73. Treatment of CLL cells with 0.1 μM CDKI-73 for 4h inhibited the phosphorylation of cdk9 and ser2 of RNA polymerase II. CDKI-73 induces a rapid loss of MCL1 protein and this is mediated by significant inhibition at the level of gene transcription. However, this inhibition is not restricted to MCL1 as similar reductions in XIAP and CCND2 were also observed following exposure to CDKI-73 for 4h [1]. CDKI-73 rapidly inhibited cellular CDK9 kinase activity and down-regulated the RNAPII phosphorylation. CDK9 shRNA was also found to down-regulate the Mnk1 expression. Both CDKI-73 and CDK9 shRNA decreased anti-apoptotic proteins Mcl-1 and Bcl-2 and induced apoptosis [2]. in vivo: CDKI-73 exhibited a favorable pharmacokinetic profile with oral bioavailability of F = 56% following a single intravenous bolus dose at 2 mg/kg and an oral dose at 10 mg/kg in mice [1]. 物理化学性质： CAS号：1421693-22-2 常用中文名：CDKI-73 常用英文名：CDKI-73 分子式：C15H15FN6O2S2 分子量：394.44700 密度：N/A 沸点：N/A 熔点：N/A 闪点：N/A 储存条件：2-8℃ |
上海念兴实业有限公司
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- 上海阿拉丁生化科技股份有限公司
- 上海市 上海市 浦东新区
- 产品名：CDKI-73
- 价格： ￥13389.9/100mg ￥3089.9/10mg ￥6385.9/25mg ￥9475.9/50mg
- 纯度：95.0%
- 备货期：1天
- 联系人：阿拉丁
- 上海化源世纪贸易有限公司
- 上海市 上海市 普陀区
- 产品名：CS-2259
- 价格：
- 纯度：99.0%
- 备货期：10天
- 联系人：徐经理
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参考价格：$462/10mM*1mLinDMSO