| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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VU6015929 is a selective and orally bioavailable dual inhibitor of discoidin domain receptor 1/2 (DDR1/2) with IC50s of 4.67 nM and 7.39 nM, respectively. VU6015929 effectively inhibits the production of collagen-IV and DDR1 activation induced by collagen.
| Targets |
DDR1 (IC50 = 4.67 nM); DDR2 (IC50 = 7.39 nM)
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|---|---|
| ln Vitro |
VU6015929 (Compound 7e; 4-100 nM; 24 hours; HEK293-DDR1b cells) treatment inhibits DDR1 phosphorylation induced by collagen I in a dose-dependent manner. The IC50 for VU6015929 is 0.7078 nM, according to analysis of the phosphorylated DDR1/total DDR1 ratio[1].
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| ln Vivo |
VU6015929 (Compound 7e) is further assessed in a 10% EtOH/40% PEG400/50% saline vehicle in a rat IV (0.5 mg/kg)/PO (3 mg/kg) PK study. With a moderate in vivo clearance (CLp = 34.2 mL/min/kg), an approximately ~3-hour half-life, a moderate volume of distribution at steady state (Vss = 4.3 L/kg), and a rapid Tmax (0.75 hr)[1], VU6015929 exhibits a good in vitro:in vivo correlation (IVIC).
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| Cell Assay |
Cell Line: HEK293-DDR1b cells
Concentration: 4 nM, 20 nM, 100 nM Incubation Time: 24 hours Result: Inhibited collagen I-induced DDR1 phosphorylation in a dose dependent manner. Significantly inhibited collagen IV production. |
| References |
| Molecular Formula |
C24H19F4N5O2
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|---|---|
| Molecular Weight |
485.443
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| Exact Mass |
485.15
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| Elemental Analysis |
C, 59.38; H, 3.95; F, 15.65; N, 14.43; O, 6.59
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| Appearance |
Solid powder
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| SMILES |
CN1C=CC(=N1)C2=CN=CC(=C2)CNC3=C(C=CC(=C3)C(=O)NC4=CC(=CC=C4)OC(F)(F)F)F
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| InChi Key |
IZKVIUJIUTXIRH-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C24H19F4N5O2/c1-33-8-7-21(32-33)17-9-15(12-29-14-17)13-30-22-10-16(5-6-20(22)25)23(34)31-18-3-2-4-19(11-18)35-24(26,27)28/h2-12,14,30H,13H2,1H3,(H,31,34)
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| Chemical Name |
4-fluoro-3-[[5-(1-methylpyrazol-3-yl)pyridin-3-yl]methylamino]-N-[3-(trifluoromethoxy)phenyl]benzamide
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| Synonyms |
VU 6015929; VU6015929; VU-6015929
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: 98~250 mg/mL (201.9~515.0 mM)
Ethanol: ~12 mg/mL (~24.7 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.28 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.28 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0600 mL | 10.2999 mL | 20.5999 mL | |
| 5 mM | 0.4120 mL | 2.0600 mL | 4.1200 mL | |
| 10 mM | 0.2060 mL | 1.0300 mL | 2.0600 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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