JNJ-38158471
Based on 1 Customer Validation
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.
- Purity: 97.02%
- CAS No.: 951151-97-6
- Formula: C15H17ClN6O3
- Molecular Weight:364.79
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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All VEGFR Isoforms
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Biological Activity
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VEGFR-2 40 nM (IC50) |
RET 180 nM (IC50) |
c-Kit 500 nM (IC50) |
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.
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Cell Line:Human umbilical vein endothelial cells (HUVECs)
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Concentration:1, 10, 100, 500 nM
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Incubation Time:1 hour
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Result:Reduced phospoho-VEGFR2 levels at 95, 88, 77 and 73% with the concentration of 500, 100, 10 and 1 nM, respectively.
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.
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Animal Model:Female C57BL/6J mice are implanted with rhVEGF165[1]
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Dosage:10 or 100 mg/kg
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Administration:Daily oral administration for 6 days
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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).
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Animal Model:Female athymic nude mice; 5-6 weeks; implanted subcutaneously human colorectal carcinoma cells (HCT116) or human epidermoid carcinoma cells (A431)[1]
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Dosage:10, 50, 100, 200 mg/kg
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Administration:Oral administration for 35 days
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Result:Achieved optimum efficacy with the dose from 100 to 200 mg/kg daily.
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Animal Model:Female athymic nude mice; 5-6 weeks; implanted subcutaneously human skin melanoma cells (A375)[1]
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Dosage:100 mg/kg
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Administration:Once-daily oral administration for 28 days
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Result:Inhibited 90% growth of tumor with daily doses of 100 mg/kg.
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Animal Model:Female C57BL/6J-Apc Min mice; 5 weeks of age[1]
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Dosage:100 mg/kg
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Administration:Once-daily oral administration for two weeks
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Result:Inhibited polyp formation in the transgenic APC min-mouse model.
Chemical Information
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CAS No. 951151-97-6
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Appearance Solid
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Molecular Weight 364.79
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Formula C15H17ClN6O3
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Color Gray to brown
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SMILES
O=C(NCC)NC1=CC=C(OC2=NC=NC(N)=C2/C=N/OC)C=C1Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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
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Data Sheet (278 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
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 |
JNJ-38158471 Related Classifications
HY-18317 Related Classifications
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