WF-47-JS03
Based on 1 Customer Validation
WF-47-JS03 is a potent, selective and brain-penetrantRET kinase inhibitor with IC50s of 1.7 nM and 5.3 nM for KIF5B-RET transfected Ba/F3 cells and CCDC6-RET transfected LC-2/ad lung cancer cells, respectively. WF-47-JS03 demonstrates >500-fold selectivity against kinase insert domain receptor (KDR).
For research use only. We do not sell to patients.
- Purity: 99.63%
- CAS No.: 2561413-77-0
- Formula: C30H38N6O2
- Molecular Weight:514.66
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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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Kinase Inhibitor Library
HY-L009
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Protein Tyrosine Kinase Compound Library
HY-L016
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Anti-Cancer Compound Library
HY-L025
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CNS-Penetrant Compound Library
HY-L028
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Anti-Lung Cancer Compound Library
HY-L075
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Anti-Liver Cancer Compound Library
HY-L101
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Membrane Protein-targeted Compound Library
HY-L149
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Membrane Receptor-targeted Compound Library
HY-L150
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Highly Selective Inhibitors Library
HY-L158
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Bioactive Compound Library Max
HY-L181
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MCE Bioactive Compound Library
HY-L001V
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Bioactive Compound Library
HY-L001
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Anti-Brain Cancer Compound Library
HY-L188
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Protein Kinase Compound Library
HY-L196
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High-Throughput Bioactive Compound Library
HY-L205
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Posttranslational Modification Library
HY-L226
Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| BaF3 | IC50 |
0.0017 μM
Compound: 1; WF-47-JS03
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Inhibition of KIF5B-RET (unknown origin) transfected in mouse Ba/F3 cells assessed as reduction in cell viability incubated for 48 hrs by brightglo-luciferase reporter gene assay
Inhibition of KIF5B-RET (unknown origin) transfected in mouse Ba/F3 cells assessed as reduction in cell viability incubated for 48 hrs by brightglo-luciferase reporter gene assay
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[PMID: 32292564] |
| BaF3 | IC50 |
0.99 μM
Compound: 1; WF-47-JS03
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Inhibition of TEL/KDR (unknown origin) transfected in mouse Ba/F3 cells assessed as reduction in cell viability incubated for 48 hrs by brightglo-luciferase reporter gene assay
Inhibition of TEL/KDR (unknown origin) transfected in mouse Ba/F3 cells assessed as reduction in cell viability incubated for 48 hrs by brightglo-luciferase reporter gene assay
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[PMID: 32292564] |
| CHO | IC50 |
1.2 μM
Compound: 1; WF-47-JS03
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Displacement of [3H]-dofetilide from human ERG expressed in CHO cells incubated for 90 mins by microbeta scintillation counting method
Displacement of [3H]-dofetilide from human ERG expressed in CHO cells incubated for 90 mins by microbeta scintillation counting method
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[PMID: 32292564] |
| LC-2-ad | IC50 |
1.5 μM
Compound: 1; WF-47-JS03
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Cytotoxicity against human LC2/ad cells assessed as reduction in cell viability incubated for 6 days by CellTiter Glo assay
Cytotoxicity against human LC2/ad cells assessed as reduction in cell viability incubated for 6 days by CellTiter Glo assay
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[PMID: 32292564] |
WF-47-JS03 inhibits Tel-KDR transfected Ba/F3 cells and Ba/F3 wild-type cell lines with IC50s of 0.99 and 1.5 μM, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female 6-8 week old Harlan Foxn1 nude mice with RIE-RET-KIF5B transgenic cell line
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Dosage:1, 3, 10 mg/kg
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Administration:Dosed orally, 1x daily for 10 days
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Result:Inhibited tumor growth in RIE KIF5B-RET xenograft mice.
Chemical Information
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CAS No. 2561413-77-0
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Appearance Solid
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Molecular Weight 514.66
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Formula C30H38N6O2
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Color White to off-white
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SMILES
NC(N1C(N=C2NC3CC(C)(C)N(C)C(C)(C)C3)=C(C4=CC(OC)=C(OC)C=C4)C=N1)=C2C5=CC=CC=C5
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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 2 years -20°C 1 year
Solvent & Solubility
DMSO : 62.5 mg/mL (121.44 mM; Need ultrasonic; 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (4.04 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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 (280 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.9430 mL | 9.7152 mL | 19.4303 mL | 48.5758 mL |
| 5 mM | 0.3886 mL | 1.9430 mL | 3.8861 mL | 9.7152 mL | |
| 10 mM | 0.1943 mL | 0.9715 mL | 1.9430 mL | 4.8576 mL | |
| 15 mM | 0.1295 mL | 0.6477 mL | 1.2954 mL | 3.2384 mL | |
| 20 mM | 0.0972 mL | 0.4858 mL | 0.9715 mL | 2.4288 mL | |
| 25 mM | 0.0777 mL | 0.3886 mL | 0.7772 mL | 1.9430 mL | |
| 30 mM | 0.0648 mL | 0.3238 mL | 0.6477 mL | 1.6192 mL | |
| 40 mM | 0.0486 mL | 0.2429 mL | 0.4858 mL | 1.2144 mL | |
| 50 mM | 0.0389 mL | 0.1943 mL | 0.3886 mL | 0.9715 mL | |
| 60 mM | 0.0324 mL | 0.1619 mL | 0.3238 mL | 0.8096 mL | |
| 80 mM | 0.0243 mL | 0.1214 mL | 0.2429 mL | 0.6072 mL | |
| 100 mM | 0.0194 mL | 0.0972 mL | 0.1943 mL | 0.4858 mL |
WF-47-JS03 Related Classifications
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