ChemicalBook > CAS DataBase List > JNJ-38158471
JNJ-38158471
JNJ-38158471
- CAS No.951151-97-6
- Chemical Name:JNJ-38158471
- CBNumber:CB92621141
- Molecular Formula:C15H17ClN6O3
- Formula Weight:364.79
- MOL File:951151-97-6.mol
JNJ-38158471 Property
- Density 1.42±0.1 g/cm3(Predicted)
- storage temp. Store at -20°C
- solubility DMSO: 30 mg/mL (82.24 mM);Ethanol: Insoluble
- pka 13.06±0.70(Predicted)
- form Solid
- color Gray to brown
- Water Solubility Water: Insoluble
-
Symbol(GHS)
- Signal wordWarning
- Hazard statements H315-H319-H335
- Precautionary statements P261-P264-P271-P280-P302+P352-P304+P340-P305+P351+P338-P332+P313-P337+P313-P362-P403+P233-P405-P501
JNJ-38158471 Chemical Properties,Usage,Production
- Uses JNJ-38158471 is a well tolerated, orally available, highly selective VEGFR-2 inhibitor, with an IC50 of 40 nM. JNJ-38158471 also inhibits Ret and Kit with IC50s of 180 and 500 nM, respectively[1].
-
in vivo
JNJ-38158471 (10 or 100 mg/kg; p.o.; once-daily) inhibits VEGF-induced corneal neovascularization[1].
JNJ-38158471 (10-200 mg/kg; p.o.) inhibits the growth of human tumor xenografts in a dose-dependent manner in both A431 and HCT116 models. JNJ-38158471 treatment is well tolerated, following continuous administration for 24 days, body weights were comparable with control animals[1].
JNJ-38158471 (100 mg/kg; p.o.; once-daily) treatment shows statistically signi?cant activity compare with vehicle treat animals. The body weights of both JNJ-38158471-treated and vehicle-treated groups were comparable at study end[1].Animal Model: Female C57BL/6J mice are implanted with rhVEGF165[1] Dosage: 10 or 100 mg/kg Administration: Daily oral administration for 6 days Result: Caused a marked and apparently dose-dependent inhibition of VEGF-dependent blood vessel formation (100 mg/kg, resulted in 83% inhibition; 10 mg/kg, resulted in 15% inhibition). Animal Model: Female athymic nude mice; 5-6 weeks; implanted subcutaneously human colorectal carcinoma cells (HCT116) or human epidermoid carcinoma cells (A431)[1] Dosage: 10, 50, 100, 200 mg/kg Administration: Oral administration for 35 days Result: Achieved optimum ef?cacy with the dose from 100 to 200 mg/kg daily. Animal Model: Female athymic nude mice; 5-6 weeks; implanted subcutaneously human skin melanoma cells (A375)[1] Dosage: 100 mg/kg Administration: Once-daily oral administration for 28 days Result: Inhibited 90% growth of tumor with daily doses of 100 mg/kg. Animal Model: Female C57BL/6J-Apc Min mice; 5 weeks of age[1] Dosage: 100 mg/kg Administration: Once-daily oral administration for two weeks Result: Inhibited polyp formation in the transgenic APC min-mouse model. - IC 50 VEGFR-2: 40 nM (IC50); RET: 180 nM (IC50); c-Kit: 500 nM (IC50)
- References [1] Kenneth RL, et, al. A Highly Selective, Orally Bioavailable, Vascular Endothelial Growth Factor receptor-2 Tyrosine Kinase Inhibitor Has Potent Activity in Vitro and in Vivo. Angiogenesis. 2009; 12(3): 287-96. DOI:10.1007/s10456-009-9151-7
JNJ-38158471 Preparation Products And Raw materials
Raw materials
Preparation Products
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951151-97-6, JNJ-38158471Related Search:
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- 抑制剂
- 药靶配体
- C15H17ClN6O3
- 化合物CS-2660 (JNJ-38158471),10 MM DMSO 溶液
- 1-(4-((6-氨基-5-((甲氧基亚氨基)甲基)嘧啶-4-基)氧基)-2-氯苯基)-3-乙基脲
- 化合物CS-2660 (JNJ-38158471)
- 951151-97-6
- JNJ-38158471, 10 mM in DMSO
- Urea, N-[4-[[6-amino-5-[(methoxyimino)methyl]-4-pyrimidinyl]oxy]-2-chlorophenyl]-N'-ethyl-
- VEGFR-2,JNJ 38158471,VEGFR,cancer,SCFR,malignancies,JNJ38158471,Kit,c-Kit,CD117,RET,Vascular endothelial growth factor receptor,JNJ-38158471,inhibit,Inhibitor
- CS-2660 (JNJ-38158471)
- 1-(4-((6-Amino-5-((methoxyimino)methyl)pyrimidin-4-yl)oxy)-2-chlorophenyl)-3-ethylurea
- 1-[4-[6-amino-5-[(E)-methoxyiminomethyl]pyrimidin-4-yl]oxy-2-chlorophenyl]-3-ethylurea
- CS-2660
- (E)-1-(4-((6-Amino-5-((methoxyimino)methyl)pyrimidin-4-yl)oxy)-2-chlorophenyl)-3-ethylurea
- JNJ-38158471