(Z)-3-(3-(3,5-bis(trifluoromethyl)phenyl)-1H-1,2,4-triazol-1-yl)-1-(3,3-
更新时间：2022-01-29 00:23:01
采购访问：27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 | $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 |
| 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℃ |
达阳化工（杭州）有限公司
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： 浙江省 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
网址：http://www.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%
主要合作伙伴：
- 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
查看所有供应商和价格请点击：
(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