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

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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Based on 1 publication(s) in Google Scholar

JNJ-38158471 Related Antibodies

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View All VEGFR Isoform Specific Products:

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VEGFR1/Flt-1 VEGFR2/KDR/Flk-1 VEGFR3/Flt-4

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

JNJ-38158471 Related Antibodies

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Appearance

Solid

Color

Gray to brown

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
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (274.13 mM; ultrasonic and warming and heat to 80°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.7413 mL 13.7065 mL 27.4130 mL
5 mM 0.5483 mL 2.7413 mL 5.4826 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: 2.5 mg/mL (6.85 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.5 mg/mL. If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.7413 mL 13.7065 mL 27.4130 mL 68.5326 mL
5 mM 0.5483 mL 2.7413 mL 5.4826 mL 13.7065 mL
10 mM 0.2741 mL 1.3707 mL 2.7413 mL 6.8533 mL
15 mM 0.1828 mL 0.9138 mL 1.8275 mL 4.5688 mL
20 mM 0.1371 mL 0.6853 mL 1.3707 mL 3.4266 mL
25 mM 0.1097 mL 0.5483 mL 1.0965 mL 2.7413 mL
30 mM 0.0914 mL 0.4569 mL 0.9138 mL 2.2844 mL
40 mM 0.0685 mL 0.3427 mL 0.6853 mL 1.7133 mL
50 mM 0.0548 mL 0.2741 mL 0.5483 mL 1.3707 mL
60 mM 0.0457 mL 0.2284 mL 0.4569 mL 1.1422 mL
80 mM 0.0343 mL 0.1713 mL 0.3427 mL 0.8567 mL
100 mM 0.0274 mL 0.1371 mL 0.2741 mL 0.6853 mL
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JNJ-38158471 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

JNJ-38158471951151-97-6JNJ38158471JNJ 38158471VEGFRRETc-KitVascular endothelial growth factor receptorSCFRCD117VEGFR-2RetKitmalignanciescancerInhibitorinhibitorinhibit

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