[CAS NO. 2442597-56-8] VU6015929
PRODUCTS SPECIFICATIONS [2442597-56-8]
DESCRIPTION [2442597-56-8]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 485.43 |
| Molecular Formula | C24H19F4N5O2 |
| 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 |
Summary
VU6015929 is a potent, selective and orally active dual discoidin domain receptor 1/2 (DDR1/2) inhibitor with IC 50 s of 4.67 nM and 7.39 nM, respectively. VU6015929 potently blocks collagen-induced DDR1 activation and collagen-IV production [1] .
IC50 & Target
|
DDR1 4.67 nM (IC 50 ) |
DDR2 7.39 nM (IC 50 ) |
In Vitro
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 IC 50 for VU6015929 of 0.7078 nM [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Western Blot Analysis [1]
| 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. |
In Vivo
VU6015929 (Compound 7e) is further evaluated in a rat IV (0.5 mg/kg)/PO (3 mg/kg) PK study in a 10% EtOH/40% PEG400/50% saline vehicle. VU6015929 displays a good in vitro:in vivo correlation (IVIC), with moderate in vivo clearance (CL p = 34.2 mL/min/kg), an ~3 hour half-life, moderate volume of distribution at steady state (V ss = 4.3 L/kg) and 12.5% oral bioavailability with a rapid T max (0.75 hr) [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
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
DMSO : 250 mg/mL ( 515.01 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.0600 mL | 10.3001 mL | 20.6003 mL |
| 5 mM | 0.4120 mL | 2.0600 mL | 4.1201 mL |
| 10 mM | 0.2060 mL | 1.0300 mL | 2.0600 mL |
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1.
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Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.08 mg/mL (4.28 mM); Clear solution