XL019

产品详情：

发布时间： 2024-07-15 12:37:53

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：

纯度： 98.0%

备货期： 10天

库存： 现货

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：上海念兴实业有限公司推荐

认证状态： 已认证供应商

商品数： 403768件

电话： 18916513247

地址： 2222 Huancheng Road, Juyuan New District, Jiading District, Shanghai

地区： 上海市普陀区

联系人： 小陈

联系人电话： 0086-021-52280163

邮件：sales@echemcloud.com

网址：http://www.echemcloud.com

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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

XL019

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