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CAS No.: 900573-88-8

JI-101 Catalog No. CSN18549

Synonyms: CGI1842

JI-101 is an oral multi-kinase inhibitor that targets vascular endothelial growth factor receptor type 2 (VEGFR-2), platelet derived growth factor receptor β (PDGFR-β), and ephrin type-B receptor 4 (EphB4).

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生物活性

实验方案

技术信息

生物活性

描述JI-101 is an oral multi-kinase inhibitor that targets three receptor tyrosine kinases (RTKs) involved in multiple stages of tumor angiogenesis: vascular endothelial growth factor receptor 2 (VEGFR‐2), platelet‐derived growth factor receptor β (PDGFR‐β), and ephrin type‐B receptor 4 (EphB4). The transport rate of JI-101 in Caco-2 human intestinal epithelial cells from AàB and BàA was 22.9 and 7.36*10^-6cm/sec, respectively. The efflux ratio was found to be 0.32. In human plasma, the average matrix factor values of JI-101 were shown as +1.86 (CV 6.03%), +2.26 (CV 4.36%) and +0.92 (CV: 2.86%) at low quality control (27.1 ng/mL), medium quality control (751 ng/mL) and high quality control (1051 ng/mL) concentrations, respectively. In Sprague Dawley rats following intravenous (i.v.) administration of JI-101, the plasma concentrations of JI-101 decreased with a terminal half-life of 2.66 ± 0.13h. The clearance and volume of distribution after i.v. administration was 13.0 ± 2.62 ml/min/kg and 2.11 ± 1.42 l/kg, respectively. Two hours after the oral administration of JI-101 at 30 mg/kg, the maximum concentration of JI-101 was found in small intestine followed by lungs, liver, and kidney in rats. At 5h time point, the tissue to plasma ratio was 51.99, 17.36, 12.27, and 8.92 in lung, liver, small intestine, and kidney, respectively.
作用机制JI-101 inhibits VEGFR‐2, PDGFR‐β, and EphB4 by directly binding to their sites, thereby mediating antiangiogenic and antineoplastic activities mediated by these kinases.

动物研究

剂量

Rat: 1 mg/kg - 10 mg/kg^[2] (i.v.); 3 mg/kg - 30 mg/kg^[2] (p.o.)

给药途径

i.v., p.o.

动物药代数据

Animal	Rats^[2]
Dose	30 mg/kg (p.o.) 3 mg/kg (i.v.)
Administration	p.o. i.v.
F	54.7% (p.o.)
V_d	2.11 ± 1.42 L/kg (i.v.)
T_1/2	2.66 ± 0.13 h (p.o.) 1.75 ± 0.79 h (i.v.)
T_max	2.00 ± 1.41 ng/ml (p.o.)
CL	13.0 ± 2.62 ml/min/kg (i.v.)
AUC_0→∞	21516 ± 3796 ng·h/ml (p.o.) 3927 ± 724 ng·h/ml (i.v.)
C_max/C₀	2644 ± 753 ng/ml (p.o.) 5093 ± 677 ng/ml (i.v.)

临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT01149434	Cancer Neuroe... more >>ndocrine Ovarian Cancer Colon Cancer Collapse <<	Phase 1 Phase 2	Terminated(Lack of drug effica... more >>cy) Collapse <<	-	United States, Utah ... more >> Huntsman Cancer Institute Salt Lake City, Utah, United States, 84112 Collapse <<
NCT01149434	-	-	Terminated(Lack of drug effica... more >>cy) Collapse <<	-	-
NCT00842335	Advanced Solid Tumors	Phase 1 Phase 2	Completed	-	United States, Arizona ... more >> Premiere Oncology of Arizona Scottsdale, Arizona, United States, 85258 Collapse <<

更多
参考文献

[1] Werner TL, Wade ML, et al. A pilot study of JI-101, an inhibitor of VEGFR-2, PDGFR-β, and EphB4 receptors, in combination with everolimus and as a single agent in an ovarian cancer expansion cohort. Invest New Drugs. 2015 Dec;33(6):1217-24.
[2] Gurav SD, Gilibili RR, 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.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.1444 mL
- 10.7220 mL
- 21.4440 mL
- 5 mM
- 0.4289 mL
- 2.1444 mL
- 4.2888 mL
- 10 mM
- 0.2144 mL
- 1.0722 mL
- 2.1444 mL

技术信息

CAS号

900573-88-8

储存条件

粉末: Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C22H20BrN5O2

运输

蓝冰

分子量

466.33

别名

CGI1842

溶解度

DMSO	50.0 mg/mL (107.2 mM)

动物实验配方

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