(S)-N-(4-(2-((4-morpholinophenyl)amino)pyrimidin-4-yl)phenyl)pyrrolidine-2-carboxamide
更新时间：2025-09-09 11:39:19
采购访问：49次
| 常用名 | (2S)-N-[4-[2-[[4-(4-吗啉基)苯基]氨基]-4-嘧啶基]苯基]-2-吡咯烷甲酰胺 | CAS号 | 945755-56-6 |
|---|---|---|---|
| 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： XL019 is a potent and selective JAK2 inhibitor with IC50 of 2.2 nM, 100 fold selectivity over JAK1; shows good biochemical and cellular potency against JAK2 with good selectivity against the Janus Kinase family as well as a broad kinase panel.IC50 Value: 2.2 nM (JAK2); 214.2 nM (JAK3) [1]XL019 was selected as a clinical candidate and advanced into human clinical trials where it was evaluated in patients with primary myelofibrosis, post-polycythemia vera, or post-essential thrombocythemia myelofibrosis.in vitro: Analogue XL019 was also evaluated against a selectivity panel of 118 kinases. Targets for which XL019 exhibited IC50 50-fold selectivity against all kinases tested including JAK family members JAK1 and TYK2. Further in vitro evaluation of XL019 revealed that it demonstrated a desirable CYP (1A2, 2C9, 2D6, 3A4 20 μM), hERG (16 μM), and P-glycoprotein inhibition (>20 μM) profile [1].in vivo: XL019 was administered orally to mice bearing HEL92.1.7 tumors and inhibition of STAT phosphorylation was measured after 4 h. A significant inhibition of downstream markers pSTAT1 and pSTAT3 is observed at 30, 100, and 300 mg/kg resulting in an ED50 of 42 mg/kg (pSTAT1) and 210 mg/kg (pSTAT3). XL019 had a superior pharmacodynamic profile and thus was evaluated in an efficacy experiment measuring growth inhibition of HEL.92.1.7 xenograft tumors in mice. Derivative XL019 demonstrated 60% and 70% inhibition when dosed orally at 200 mg/kg and 300 mg/kg respectively twice a day for 14 days. Harvested tumors were also subjected to immunohistochemical analysis of microvessel density (CD31), proliferation (Ki67) and apoptosis (TUNEL). Dosing at 300 mg/kg bid provided an 11.3-fold increase in apoptosis relative to vehicle control [1]. 物理化学性质： CAS号：945755-56-6 常用中文名：(2S)-N-[4-[2-[[4-(4-吗啉基)苯基]氨基]-4-嘧啶基]苯基]-2-吡咯烷甲酰胺 常用英文名：XL019 分子式：C25H28N6O2 分子量：444.529 密度：1.3±0.1 g/cm3 沸点：N/A 熔点：N/A 闪点：N/A 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：
- 上海化源生化科技有限公司
- 上海市 上海市 普陀区
- 产品名：XL019
- 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：XL019
- 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：XL019
- 价格： ￥638.9/5mg ￥5149.9/100mg ￥1029.9/10mg ￥1720.9/25mg
- 纯度：99.0%
- 备货期：1天
- 联系人：阿拉丁
查看所有供应商和价格请点击：
(2S)-N-[4-[2-[[4-(4-吗啉基)苯基]氨基]-4-嘧啶基]苯基]-2-吡咯烷甲酰胺生产厂家
参考价格：$119/10mM*1mLinDMSO