Basic information Safety Supplier Related

JNJ-38158471

Basic information Safety Supplier Related

JNJ-38158471 Basic information

Product Name:
JNJ-38158471
Synonyms:
  • JNJ-38158471
  • (E)-1-(4-((6-Amino-5-((methoxyimino)methyl)pyrimidin-4-yl)oxy)-2-chlorophenyl)-3-ethylurea
  • CS-2660
  • 1-[4-[6-amino-5-[(E)-methoxyiminomethyl]pyrimidin-4-yl]oxy-2-chlorophenyl]-3-ethylurea
  • 1-(4-((6-Amino-5-((methoxyimino)methyl)pyrimidin-4-yl)oxy)-2-chlorophenyl)-3-ethylurea
  • CS-2660 (JNJ-38158471)
  • VEGFR-2,JNJ 38158471,VEGFR,cancer,SCFR,malignancies,JNJ38158471,Kit,c-Kit,CD117,RET,Vascular endothelial growth factor receptor,JNJ-38158471,inhibit,Inhibitor
  • Urea, N-[4-[[6-amino-5-[(methoxyimino)methyl]-4-pyrimidinyl]oxy]-2-chlorophenyl]-N'-ethyl-
CAS:
951151-97-6
MF:
C15H17ClN6O3
MW:
364.79
Mol File:
951151-97-6.mol
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JNJ-38158471 Chemical Properties

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
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JNJ-38158471 Usage And Synthesis

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-38158471Supplier

SYN|thesis med chem P/L
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Shanghai Lollane Biological Technology Co.,Ltd.
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021-52996696，15000506266 15000506266
Pharmacodia (Beijing) Co.,Ltd
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+86-400-851-9921
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Shanghai EFE Biological Technology Co., Ltd.
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021-65675885 18964387627
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Shanghai YuanYe Biotechnology Co., Ltd.
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021-61312847; 18021002903
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3008007409@qq.com
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