1. Protein Tyrosine Kinase/RTK
  2. Discoidin Domain Receptor
  3. VU6015929

VU6015929 

Cat. No.: HY-135401 Purity: 98.10%
Handling Instructions

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.

VU6015929 Chemical Structure

VU6015929 Chemical Structure

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 374 In-stock
Estimated Time of Arrival: December 31
5 mg USD 350 In-stock
Estimated Time of Arrival: December 31
10 mg USD 550 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1650 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2250 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products
  • Biological Activity

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Description

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[1].

IC50 & Target[1]

DDR1

4.67 nM (IC50)

DDR2

7.39 nM (IC50)

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 IC50 for VU6015929 of 0.7078 nM[1].

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 (CLp = 34.2 mL/min/kg), an ~3 hour half-life, moderate volume of distribution at steady state (Vss = 4.3 L/kg) and 12.5% oral bioavailability with a rapid Tmax (0.75 hr)[1].

Molecular Weight

485.43

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

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
In Vitro: 

DMSO : 250 mg/mL (515.01 mM; Need ultrasonic)

Preparing
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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    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

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (4.28 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

VU6015929VU 6015929VU-6015929Discoidin Domain ReceptorDDR1DDR2phosphorylatedoralbioavailabilitycollagen-IVantifibroticInhibitorinhibitorinhibit

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Product name:
VU6015929
Cat. No.:
HY-135401
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