1. Protein Tyrosine Kinase/RTK
  2. VEGFR
    RET
    c-Kit
  3. JNJ-38158471

JNJ-38158471 

Cat. No.: HY-18317
Handling Instructions

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.

For research use only. We do not sell to patients.

JNJ-38158471 Chemical Structure

JNJ-38158471 Chemical Structure

CAS No. : 951151-97-6

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Description

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].

IC50 & Target[1]

VEGFR-2

40 nM (IC50)

RET

180 nM (IC50)

c-Kit

500 nM (IC50)

In Vitro

JNJ-38158471 (1-500 nM; 1 hour) inhibits VEGF-stimulated VEGFR-2 autophosphorylation in HUVECs[1].
JNJ-38158471 (50-1000 nM; 12-16 hours) significantly inhibits VEGF-dependent HUVEC migration. Cellular toxicity is not observed following JNJ-38158471 treatment of HUVECs[1].

Western Blot Analysis[1]

Cell Line: Human umbilical vein endothelial cells (HUVECs)
Concentration: 1, 10, 100, 500 nM
Incubation Time: 1 hour
Result: Reduced phospoho-VEGFR2 levels at 95, 88, 77 and 73% with the concentration of 500, 100, 10 and 1 nM, respectively.
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 significant 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 efficacy 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.
Molecular Weight

364.79

Formula

C₁₅H₁₇ClN₆O₃

CAS No.

951151-97-6

SMILES

O=C(NCC)NC1=CC=C(OC2=NC=NC(N)=C2/C=N/OC)C=C1Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

JNJ-38158471JNJ38158471JNJ 38158471VEGFRRETc-KitVascular endothelial growth factor receptorSCFRCD117VEGFR-2RetKitmalignanciescancerInhibitorinhibitorinhibit

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