JNJ-38158471

Product NameJNJ-38158471
CAS951151-97-6
MFC15H17ClN6O3
MW364.79
EINECS
MOL File951151-97-6.mol

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

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 signicant 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 efcacy 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

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