(S)-N-(4-(2-((4-morpholinophenyl)amino)pyrimidin-4-yl)phenyl)pyrrolidine-2-carboxamide

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更新时间： 2025-09-09 11:39:19

CAS号：945755-56-6

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

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： 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℃

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

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%

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其他供应商价格：

2024-07-15 价格：需询单 XL019

2022-11-29 价格：￥需询单 XL019

2020-12-08 价格：￥需询单 XL019

2022-03-04 价格：￥638.9 XL019

2023-09-11 价格：￥需询单 XL019

2018-02-27 价格：￥需询单 XL019

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(2S)-N-[4-[2-[[4-(4-吗啉基)苯基]氨基]-4-嘧啶基]苯基]-2-吡咯烷甲酰胺价格

(S)-N-(4-(2-((4-morpholinophenyl)amino)pyrimidin-4-yl)phenyl)pyrrolidine-2-carboxamide

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