VU6015929

SKU: orb1940250

Description

VU6015929 is an inhibitor of active dual discoidin domain receptor 1/2 (DDR1/2)( IC50s of 4.67 nM and 7.39 nM, respectively).(In Vitro):VU6015929 potently blocks collagen-induced DDR1 activation and collagen-IV production, suggesting DDR1 inhibition as an exciting target for antifibrotic therapy.

Key Properties

• CAS Number: 2442597-56-8
• MW: 485.443
• Purity: >98% (HPLC)
• Formula: C₂₄H₁₉F₄N₅O₂
• SMILES: Cn1ccc(n1)-c1cncc(CNc2cc(ccc2F)C(=O)Nc2cccc(OC(F)(F)F)c2)c1
• Target: DDR
• Solubility: In Vitro: DMSO : 250 mg/mL (515.01 mM)

Bioactivity

• 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).
• 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. Western blot analysis. 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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

DDR