KPT-276
更新时间：2024-07-15 12:32:01
采购访问：10次
| 常用名 | (2Z)-3-[3-[3,5-双(三氟甲基)苯基]-1H-1,2,4-三唑-1-基]-1-(3,3-二氟-1-氮杂环丁基)-2-丙烯-1-酮 | CAS号 | 1421919-75-6 |
|---|---|---|---|
| 价格 | 纯度 | 98.0% | |
| 备货期 | 10天 | 库存 | 现货 |
| 产品详情（用途，包装等）
用途： KPT-276, analog of KPT-185, is an orally bioavailable selective inhibitors of nuclear export (SINE) that irreversibly bind to CRM1 and block the function of CRM1.IC50 value:Target: CRM1in vitro: A selective inhibitor of nuclear export compound KPT-276 specifically and irreversibly inhibits the nuclear export function of XPO1. The viability of 12 HMCLs treated with KTP-276 was significantly reduced. KPT-276 also actively induced apoptosis in primary MM patient samples. In gene expression analyses, two genes of probable relevance were dysregulated by KPT-276: cell division cycle 25 homolog A (CDC25A) and bromodomain-containing protein 4 (BRD4), both of which are associated with c-MYC pathway [1]. Inhibition of CRM1 by two novel selective inhibitors of nuclear export (SINE), KPT-185 and KPT-276, in MCL cells resulted in significant growth inhibition and apoptosis induction. KPT-185 also induced CRM1 accumulation in the nucleus, resulting in CRM1 degradation by the proteasome [3].in vivo: One week after leukemic cell inoculation, the mice were given KPT-276 at 150 mg/kg via oral gavage, 3 times a week, or vehicle control. KPT-276 has the identical CRM1 binding warhead and specificity as KPT-185, similar biologic activity in vitro, but superior oral bioavailability and pharmacokinetics, which allow it to be used in vivo. Mice were monitored for survival. Some mice were killed at day 21 to assess the effects of KPT-276 on leukemia burden by measuring spleen weight and white blood cell count [2]. Oral administration of KPT-276 significantly suppressed tumor growth in an MCL-bearing severe combined immunodeficient mouse model, without severe toxicity [3]. 物理化学性质： CAS号：1421919-75-6 常用中文名：(2Z)-3-[3-[3,5-双(三氟甲基)苯基]-1H-1,2,4-三唑-1-基]-1-(3,3-二氟-1-氮杂环丁基)-2-丙烯-1-酮 常用英文名：KPT-276 分子式：C16H10F8N4O 分子量：426.264 密度：1.6±0.1 g/cm3 沸点：477.2±55.0 °C at 760 mmHg 熔点：N/A 闪点：242.4±31.5 °C 储存条件：-20℃ |
上海念兴实业有限公司
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- 上海化源生化科技有限公司
- 上海市 上海市 普陀区
- 产品名：KPT-276
- 价格：
- 纯度：98.0%
- 备货期：10天
- 联系人：徐经理
- 上海源溪生物科技有限公司
- 上海市 上海市 浦东新区
- 产品名：KPT-276
- 价格： ￥需询单/1g
- 纯度：98.9%
- 备货期：1天
- 联系人：赖经理
- 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：KPT-276
- 价格： ￥340.9/5mg ￥3089.9/100mg ￥638.9/10mg ￥6952.9/250mg
- 纯度：98.0%
- 备货期：1天
- 联系人：阿拉丁
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(2Z)-3-[3-[3,5-双(三氟甲基)苯基]-1H-1,2,4-三唑-1-基]-1-(3,3-二氟-1-氮杂环丁基)-2-丙烯-1-酮生产厂家
参考价格：￥768/10 mM * 1 mL in DMSO