|1-(4-(3-氨基-1H-吲唑-4-基)苯基)-3-(2-氟-5-甲基苯基)脲|CsnPharm

CAS No.: 796967-16-3

Linifanib/利尼伐尼 Catalog No. CSN12402

Synonyms: ABT-869;AL-39324;RG-3635

Linifanib is a potent ATP-competitive VEGFR/PDGFR inhibitor for KDR, CSF-1R, Flt-1/3 and PDGFRβ with IC50 of 4 nM, 3 nM, 3 nM/4 nM and 66 nM respectively.

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 c-FMS

IC50:3nM VEGFR1

IC50:3nM VEGFR2

IC50:4nM FLT3

IC50:4nM PDGFRβ

IC50:66nM
描述Linifanib is a muti-target inhibitor with IC50 values of 3nM, 3nM, 4nM, 4nM, 14nM and 66nM for VEGFR1, CSF-1R, VEGFR2, FLT3, c-Kit and PDGFRβ(measured by kinase assays), respectively. Linifanib showed in cellular inhibition on ligand-induced phosphorylation of PDGFR-βKDR and CSF-1R with IC50 values of 2nM, 31nM and 10nM, respectively, in 3T3 transfectants, as well as VEGF-induced proliferation with IC50 value of 0.2nM for human endothelial cells^[1]. The in vivo study showed that, consistent with the inhibition of VEGFR and PDGFRβby Linifanib, oral administration of Linifanib at dose of 7.5 and 15mg/kg, BID, significantly inhibited bFGF- and VEGF-induced increases of vessel density in the cornea. Oral treatment with Linifanib at dose ranging in 1.5-12.5mg/kg, BID, could significantly reduce the tumor growth or in several orthotopic tumor models, including MDA-231 and MDA-435LM xenograft mice and rat glioma, or enhance the anti-tumor effect of paclitaxel in the models^[1].
作用机制Linifanib can bind to the ATP-binding site of CSF-1R.^[2]
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
human MOLM13 cells	-	Cytotoxicity assay	72 h	Cytotoxicity against human MOLM13 cells harboring mutant FLT3 after 72 hrs by MTS assay, GI50=0.037 μM	23618709
human MOLT4 cells	-	Proliferation assay	72 h	Antiproliferation activity against human MOLT4 after 72 hrs by MTS method, GI50=6.7 μM	21708468
human MV4-11 cells	-	Proliferation assay	72 h	Antiproliferation activity against FLT3/ITD harboring human MV4-11 cells after 72 hrs by MTS method, GI50=0.04 μM	21708468

动物研究

剂量

Mice: 25 mg/kg^[3] (p.o., BID), 1.5 mg/kg - 15 mg/kg^[1] (p.o.)

给药途径

p.o.

动物药代数据

Animal	Rats^[4]	Dogs^[4]	Monkeys^[4]
Dose	5 mg/kg (i.v./p.o.)	2.5 mg/kg (i.v./p.o.)	2.5 mg/kg (i.v./p.o.)
Administration	i.v. p.o.	i.v. p.o.	i.v. p.o.
F	27% (p.o.)	47% (p.o.)	10.6% (p.o.)
V_d	1.1 L/kg (i.v.)	1.2 L/kg (i.v.)	2.2 L/kg (i.v.)
T_1/2	3.6 h (i.v.)	2.0 h (i.v.)	3.1 h (i.v.)
AUC	6.8 µg·h/ml (p.o.)	1.5 µg·h/ml (p.o.)	0.6 µg·h/ml (p.o.)
CL	3.3 ml/min·kg (i.v.)	7.2 ml/min·kg (i.v.)	8.2 ml/min·kg (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
NCT03481842	Endometriosis ... more >> Endometriosis Ovary Endometriosis Externa Endometriosis, Rectum Collapse <<	Phase 1 Phase 2	Not yet recruiting	September 30, 2018	Switzerland ... more >> BioGene Pharmaceutical Ltd. Not yet recruiting Basel, Вâlе, Switzerland, 4057 Contact: J. Łanevska, Dr jula.edu@yahoo.com Collapse <<
NCT00707889	Advanced Colorectal Cancer ... more >> Adenocarcinoma of the Colon Adenocarcinoma of the Rectum Collapse <<	Phase 2	Completed	-	-
NCT00716534	Advanced or Metastatic Non-Sma... more >>ll Cell Lung Cancer Collapse <<	Phase 2	Completed	-	-

更多
参考文献

[1] Albert DH, Tapang P, et al. Preclinical activity of ABT-869, a multitargeted receptor tyrosine kinase inhibitor. Mol Cancer Ther. 2006;5(4):995-1006.
[2] Guo J, Marcotte PA, et al. Inhibition of phosphorylation of the colony-stimulating factor-1 receptor (c-Fms) tyrosine kinase in transfected cells by ABT-869 and other tyrosine kinase inhibitors. Mol Cancer Ther. 2006;5(4):1007-13.
[3] Jiang F, Albert DH, et al. ABT-869, a multitargeted receptor tyrosine kinase inhibitor, reduces tumor microvascularity and improves vascular wall integrity in preclinical tumor models. J Pharmacol Exp Ther. 2011 Jul;338(1):134-42.
[4] Dai Y, Hartandi K, et al. Discovery of N-(4-(3-amino-1H-indazol-4-yl)phenyl)-N'-(2-fluoro-5-methylphenyl)urea (ABT-869), a 3-aminoindazole-based orally active multitargeted receptor tyrosine kinase inhibitor. J Med Chem. 2007 Apr 5;50(7):1584-97. Epub 2007 Mar 8.

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
- 2.6638 mL
- 13.3192 mL
- 26.6383 mL
- 5 mM
- 0.5328 mL
- 2.6638 mL
- 5.3277 mL
- 10 mM
- 0.2664 mL
- 1.3319 mL
- 2.6638 mL

技术信息

CAS号

796967-16-3

储存条件

粉末: Keep in dark place,Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C21H18FN5O

运输

蓝冰

分子量

375.40

别名

ABT-869;AL-39324;RG-3635

溶解度

DMSO	135.0 mg/mL (359.6 mM)
Water	insoluble

动物实验配方

5%DMSO+40%PEG 300+5%Tween80+50%water

10 mg/mL

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NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点

NCT03481842	Endometriosis ... more >> Endometriosis Ovary Endometriosis Externa Endometriosis, Rectum Collapse <<	Phase 1 Phase 2	Not yet recruiting	September 30, 2018	Switzerland ... more >> BioGene Pharmaceutical Ltd. Not yet recruiting Basel, Вâlе, Switzerland, 4057 Contact: J. Łanevska, Dr jula.edu@yahoo.com Collapse <<
NCT00707889	Advanced Colorectal Cancer ... more >> Adenocarcinoma of the Colon Adenocarcinoma of the Rectum Collapse <<	Phase 2	Completed	-	-
NCT00716534	Advanced or Metastatic Non-Sma... more >>ll Cell Lung Cancer Collapse <<	Phase 2	Completed	-	-
NCT00718380	Solid Tumor	Phase 1	Completed	-	-
NCT00486538	Advanced Renal Cell Carcinoma	Phase 2	Completed	-	United States, California ... more >> Site Reference ID/Investigator# 7193 Sacramento, California, United States, 95817 United States, District of Columbia Site Reference ID/Investigator# 5243 Washington, District of Columbia, United States, 20010 United States, Illinois Site Reference ID/Investigator# 5384 Chicago, Illinois, United States, 60637 United States, Massachusetts Site Reference ID/Investigator# 11662 Boston, Massachusetts, United States, 02114 Site Reference ID/Investigator# 11663 Boston, Massachusetts, United States, 02114 Site Reference ID/Investigator# 5379 Boston, Massachusetts, United States, 02114 United States, New Hampshire Site Reference ID/Investigator# 5380 Lebanon, New Hampshire, United States, 03756-0001 United States, Pennsylvania Site Reference ID/Investigator# 5249 Philadelphia, Pennsylvania, United States, 19111 Site Reference ID/Investigator# 6278 Philadelphia, Pennsylvania, United States, 19111 Site Reference ID/Investigator# 6269 Pittsburgh, Pennsylvania, United States, 15232 United States, South Carolina Site Reference ID/Investigator# 7300 Charleston, South Carolina, United States, 29425 United States, Texas Site Reference ID/Investigator# 6796 Houston, Texas, United States, 77030-4009 Canada Site Reference ID/Investigator# 6566 Vancouver, Canada, V5Z 4E6 Collapse <<
NCT00733187	Advanced Solid Tumors	Phase 1	Completed	-	-
NCT00645177	Metastatic Breast Cancer	Phase 2	Completed	-	United States, California ... more >> Site Reference ID/Investigator# 8352 San Francisco, California, United States, 94115 United States, Illinois Site Reference ID/Investigator# 6920 Harvey, Illinois, United States, 60426 Mexico Site Reference ID/Investigator# 10181 Durango, DGO., Mexico, CP 34000 Collapse <<
NCT01009593	Hepatocellular Carcinoma Non-r... more >>esectable Hepatocellular Carcinoma Recurrent Carcinoma, Hepatocellular Liver Diseases Neoplasms by Histologic Type Digestive System Neoplasms Carcinoma Liver Neoplasms Neoplasms Neoplasms by Site Digestive System Diseases Adenocarcinoma Neoplasms, Glandular and Epithelial Collapse <<	Phase 3	Terminated(See termination rea... more >>son in detailed description) Collapse <<	-	-
NCT01225302	Non-Small Cell Lung Cancer	Phase 1	Completed	-	-
NCT01286974	Advanced Solid Tumors	Phase 1	Terminated(Terminated early, S... more >>ponsor Decision) Collapse <<	-	United States, Ohio ... more >> Site Reference ID/Investigator# 40942 Cleveland, Ohio, United States, 44195 Site Reference ID/Investigator# 53663 Cleveland, Ohio, United States, 44195 Collapse <<
NCT00517790	Non-Small Cell Lung Cancer (NS... more >>CLC) Collapse <<	Phase 2	Completed	-	-
NCT01365910	Recurrent Colon Cancer ... more >> Recurrent Rectal Cancer Stage IVA Colon Cancer Stage IVA Rectal Cancer Stage IVB Colon Cancer Stage IVB Rectal Cancer Collapse <<	Phase 2	Terminated(Interim analysis de... more >>termined the study did not meet criteria to proceed) Collapse <<	-	United States, Tennessee ... more >> Vanderbilt Cool Springs Franklin, Tennessee, United States, 37067 Vanderbilt-Ingram Cancer Center Nashville, Tennessee, United States, 37232-6838 Collapse <<
NCT01114191	Solid Tumors	Phase 1	Completed	-	United States, Michigan ... more >> Site Reference ID/Investigator# 35784 Detroit, Michigan, United States, 48201 United States, New Hampshire Site Reference ID/Investigator# 36527 Lebanon, New Hampshire, United States, 03756-0001 Collapse <<
NCT01413893	Advanced Solid Tumors	Phase 1	Completed	-	-
NCT01365910	-	-	Terminated(Interim analysis de... more >>termined the study did not meet criteria to proceed) Collapse <<	-	-
NCT01401933	Advanced Solid Tumors	Phase 1	Completed	-	United States, Arizona ... more >> Site Reference ID/Investigator# 49953 Tucson, Arizona, United States, 85724-5024 United States, Wisconsin Site Reference ID/Investigator# 49952 Madison, Wisconsin, United States, 53792 Collapse <<
NCT01506934	Advanced or Metastatic Solid T... more >>umors Collapse <<	Phase 1	Terminated(Sponsor decision)	-	United States, Maryland ... more >> Site Reference ID/Investigator# 51465 Baltimore, Maryland, United States, 21231 United States, Michigan Site Reference ID/Investigator# 61282 Detroit, Michigan, United States, 48201 United States, New Hampshire Site Reference ID/Investigator# 51463 Lebanon, New Hampshire, United States, 03756-0001 United States, Texas Site Reference ID/Investigator# 52122 San Antonio, Texas, United States, 78229 Collapse <<
NCT01381341	Advanced Solid Tumors	Phase 1	Completed	-	United States, Washington ... more >> Site Reference ID/Investigator# 51403 Tacoma, Washington, United States, 98405 Collapse <<
NCT00517920	Advanced Hepatocellular Carcin... more >>oma Collapse <<	Phase 2	Completed	-	United States, Pennsylvania ... more >> Site Reference ID/Investigator# 7726 Philadelphia, Pennsylvania, United States, 19107 Canada Site Reference ID/Investigator# 7169 Toronto, Canada, M5G 2M9 Site Reference ID/Investigator# 5837 Vancouver, Canada, V5Z 4E6 Singapore Site Reference ID/Investigator# 5235 Singapore, Singapore, 119228 Site Reference ID/Investigator# 5611 Singapore, Singapore, 169610 Taiwan Site Reference ID/Investigator# 6265 Taipei, Taiwan, 10002 Collapse <<
NCT00754104	Solid Tumors	Phase 1	Withdrawn	-	-

靶点	Description	IC50
c-FMS		IC50:3nM
VEGFR1		IC50:3nM
VEGFR2		IC50:4nM
FLT3		IC50:4nM
PDGFRβ		IC50:66nM

Linifanib/利尼伐尼 Catalog No. CSN12402

靶点选择性

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