VU6015929
Based on 1 publication(s) in Google Scholar
VU6015929 is a potent, selective and orally active dual discoidin domain receptor 1/2 (DDR1/2) inhibitor with IC50s of 4.67 nM and 7.39 nM, respectively. VU6015929 potently blocks collagen-induced DDR1 activation and collagen-IV production.
For research use only. We do not sell to patients.
- Purity: 99.50%
- CAS No.: 2442597-56-8
- Formula: C24H19F4N5O2
- Molecular Weight:485.43
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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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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Publications Citing Use of MedChemExpress (MCE) VU6015929
More
Biological Activity
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DDR1 4.67 nM (IC50) |
DDR2 7.39 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
0.7078 nM
Compound: 7e; VU6015929
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Inhibition of FLAG-tagged DDR1 in human HEK293 cells assessed as reduction in collagen-1-induced DDR1 phosphorylation incubated for 18 hrs by ELISA
Inhibition of FLAG-tagged DDR1 in human HEK293 cells assessed as reduction in collagen-1-induced DDR1 phosphorylation incubated for 18 hrs by ELISA
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[PMID: 31938459] |
| Sf9 | IC50 |
4.67 nM
Compound: 7e; VU6015929
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Inhibition of kinase tracer 178 binding to recombinant human His-tagged DDR1 expressed in baculovirus infected Sf9 cells incubated for 1 hr by TR-FRET based LanthaScreen Eu kinase binding assay
Inhibition of kinase tracer 178 binding to recombinant human His-tagged DDR1 expressed in baculovirus infected Sf9 cells incubated for 1 hr by TR-FRET based LanthaScreen Eu kinase binding assay
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[PMID: 31938459] |
| Sf9 | IC50 |
7.39 nM
Compound: 7e; VU6015929
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Inhibition of kinase tracer 178 binding to recombinant human His-tagged DDR2 expressed in baculovirus infected Sf9 cells incubated for 1 hr by TR-FRET based LanthaScreen Eu kinase binding assay
Inhibition of kinase tracer 178 binding to recombinant human His-tagged DDR2 expressed in baculovirus infected Sf9 cells incubated for 1 hr by TR-FRET based LanthaScreen Eu kinase binding assay
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[PMID: 31938459] |
VU6015929 (Compound 7e; 4-100 nM; 24 hours; HEK293-DDR1b cells) treatment inhibits collagen I-induced DDR1 phosphorylation in a dose dependent manner. Analysis of the phosphorylated DDR1/total DDR1 ratio reveals an IC50 for VU6015929 of 0.7078 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HEK293-DDR1b cells
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Concentration:4 nM, 20 nM, 100 nM
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Incubation Time:24 hours
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Result:Inhibited collagen I-induced DDR1 phosphorylation in a dose dependent manner. Significantly inhibited collagen IV production.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 2442597-56-8
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Appearance Solid
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Molecular Weight 485.43
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Formula C24H19F4N5O2
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Color White to yellow
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SMILES
O=C(NC1=CC=CC(OC(F)(F)F)=C1)C2=CC(NCC3=CC(C4=NN(C)C=C4)=CN=C3)=C(F)C=C2
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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
Publications (1)
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Journal Impact Factor
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Most Recent
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Mol Carcinog
DDR1/2 enhance KIT activation and imatinib resistance of primary and secondary KIT mutants in gastrointestinal stromal tumors. [Abstract]2024 Jan;63(1):75-93. PMID: 37737519
Solvent & Solubility
DMSO : 100 mg/mL (206.00 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 (4.28 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 (272 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 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 | 2.0600 mL | 10.3001 mL | 20.6003 mL | 51.5007 mL |
| 5 mM | 0.4120 mL | 2.0600 mL | 4.1201 mL | 10.3001 mL | |
| 10 mM | 0.2060 mL | 1.0300 mL | 2.0600 mL | 5.1501 mL | |
| 15 mM | 0.1373 mL | 0.6867 mL | 1.3734 mL | 3.4334 mL | |
| 20 mM | 0.1030 mL | 0.5150 mL | 1.0300 mL | 2.5750 mL | |
| 25 mM | 0.0824 mL | 0.4120 mL | 0.8240 mL | 2.0600 mL | |
| 30 mM | 0.0687 mL | 0.3433 mL | 0.6867 mL | 1.7167 mL | |
| 40 mM | 0.0515 mL | 0.2575 mL | 0.5150 mL | 1.2875 mL | |
| 50 mM | 0.0412 mL | 0.2060 mL | 0.4120 mL | 1.0300 mL | |
| 60 mM | 0.0343 mL | 0.1717 mL | 0.3433 mL | 0.8583 mL | |
| 80 mM | 0.0258 mL | 0.1288 mL | 0.2575 mL | 0.6438 mL | |
| 100 mM | 0.0206 mL | 0.1030 mL | 0.2060 mL | 0.5150 mL |
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