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JI-101, 血管内皮生长因子受体 2 抑制剂

    级别和纯度:
  • 10mM in DMSO
  • CAS编号: 900573-88-8
  • 分子式: C22H20BrN5O2
  • 分子量: 466.3
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库存信息

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货号 (SKU) 包装规格 是否现货 价格 数量
J655004-1ml
1ml 期货 Stock Image

基本描述

规格或纯度 10mM in DMSO
英文名称 JI-101
生化机理 JI-101 是一种口服的血管内皮生长因子受体 2(VEGFR2)、表皮生长因子受体β(PDGFRβ)和 EphB4 多激酶抑制剂,具有很强的抗癌活性。
储存温度 -80℃储存
运输条件 超低温冰袋运输
作用类型 抑制剂
作用机制 血管内皮生长因子受体 2 抑制剂
产品介绍


JI-101 is an orally available multi-kinase inhibitor of VEGFR2 , PDGFRβ and EphB4 with potent anti-cancer activity.

In Vitro

JI-101 is found to be stable in all preclinical and human liver microsomes. The % metabolized is ranged between 3.03-3.95 across the tested species liver microsomes. The % metabolized is relatively higher in mice liver microsomes followed by dog, human and rat liver microsomes. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

JI-101excreted through bile along with its mono- and di-hydroxy metabolites. Following oral administration, JI-101 is rapidly absorbed, reaching C max within 2 h. The t 1/2 of JI-101 with intravenous and oral route is found to be 1.75±0.79 and 2.66±0.13 h, respectively. The Cl and Vd by intravenous route for JI-101 are found to be 13.0±2.62 mL/min/kg and 2.11±1.42 L/kg, respectively. The tissue distribution of JI-101 is extensive with rapid and preferred uptake into lung tissue. Overall, the oral bioavailability of JI-101 is 55% and the primary route of elimination for JI-101 is feces . MCE has not independently confirmed the accuracy of these methods. They are for reference only.

IC50& Target:VEGFR2 PDGFRβ

产品属性

ALogP 3.4

名称和识别符

Isomeric SMILES COC1=C(C=C(C=C1)Br)NC(=O)NC2=C3C=CN(C3=CC=C2)CC4=CC(=NC=C4)N
关联CAS 900573-88-8
PubChem CID 11691242
MeSH Entry Terms 1-(1-(2-amino-pyridin-4-ylmethyl)-1H-indol-4-yl)-3-(5-bromo-2-methoxyphenyl)urea;JI 101;JI-101;JI101 cpd
分子量 466.3

安全和危险性(GHS)

质检证书(CoA,COO,BSE/TSE 和分析图谱)

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