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JI-101

目录号: PL09005 纯度: ≥99%

JI-101是有口服活性的有抗癌活性的多靶点激酶抑制剂，可抑制 VEGFR2，PDGFRβ 和 EphB4。

CAS No. :900573-88-8

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中文名称	JI-101
中文别名	1-[1-[(2-氨基吡啶-4-基)甲基]-1H-吲哚-4-基]-3-(5-溴-2-甲氧基苯基)脲
英文名称	JI-101
英文别名	JI-101;1-[1-[(2-aminopyridin-4-yl)methyl]indol-4-yl]-3-(5-bromo-2-methoxyphenyl)urea;JI 101;980M4N37DH;1-(1-((2-aminopyridin-4-yl)methyl)-1H-indol-4-yl)-3-(5-bromo-2-methoxyphenyl)urea.;1-(1-((2-AMINOPYRIDIN-4-YL)METHYL)-1H-INDOL-4-YL)-3-(5-BROMO-2-METHOXYPHENYL)UREA;BCP16892;NSC762381;NSC801003;DB12744;SB16904;Urea, N-(1-((2-amino-4-pyridinyl)methyl)-1;Urea, N-(1-((2-amino-4-pyridinyl)methyl)-1H-indol-4-yl)-N'-(5-bromo-2-methoxyphenyl)-;N-[1-[(2-Amino-4-pyridinyl)methyl]-1H-indol-4-yl]-N′-(5-bromo-2-methoxyphenyl)urea (ACI);1-[1-[(2-Aminopyridin-4-yl)methyl]-1H-indol-4-yl]-3-(5-bromo-2-methoxyphenyl)urea;1-[1-[(2-Aminopyridin-4-yl)methyl]indol-4-yl]-3-(5-bromo-2-methoxyphenyl)urea;CGI 1842
Cas No.	900573-88-8
分子式	C₂₂H₂₀BrN₅O₂
分子量	466.33
包装储存	Powder -20°C 3 years；4°C 2 years
详情描述	JI-101是有口服活性的有抗癌活性的多靶点激酶抑制剂，可抑制 VEGFR2，PDGFRβ 和 EphB4。

产品详情

JI-101是有口服活性的有抗癌活性的多靶点激酶抑制剂，可抑制 VEGFR2，PDGFRβ 和 EphB4。

生物活性

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

性状

Solid

IC50 & Target[1][2]

VEGFR2 PDGFRβ

体外研究(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. has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(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. has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder -20°C 3 years；4°C 2 years

ClinicalTrial

参考文献

[1]. Gurav SD, et al. Pharmacokinetics, tissue distribution and identification of putative metabolites of JI-101 - a novel triple kinase inhibitor in rats. Arzneimittelforschung. 2012 Jan;62(1):27-34.

溶解度数据	In Vitro: DMSO : ≥ 100 mg/mL (214.44 mM)配制储备液

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

JI-101

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