NVP-ADW742 b

SKU: orb1221539

Description

NVP-ADW742 is an IGF-1R inhibitor with IC50 of 0.17 μM >16-fold more potent against IGF-1R than InsR; little activity to HER2 PDGFR VEGFR-2 Bcr-Abl and c-Kit.

Key Properties

• CAS Number: 475488-23-4
• MW: 453.58
• Purity: >98% (HPLC)
• Formula: C₂₈H₃₁N₅O
• SMILES: C1CCN(C1)CC2CC(C2)N3C=C(C4=C3N=CN=C4N)C5=CC(=CC=C5)OCC6=CC=CC=C6
• Target: IGF-1R
• Solubility: DMSO:10 mg/mL (22.04 mM) warmed;Ethanol:3 mg/mL (6.61 mM);Water:<1 mg/mL

Bioactivity

• In Vivo:
  NVP-ADW742 (ADW742; 10 mg/kg for IP or 50 mg/kg for orally; twice daily for 19 days) significantly suppresses tumor growth and prolongs the survival of mice. Animal model: 6-to 8-week-old male SCID/NOD mice with diffuse skeletal lesions of luciferase-expressing MM cells. Dosage: 10 mg/kg (IP) or 50 mg/kg (orally). Administration: IP or orally; twice daily for 19 days. Result: Significantly suppressed tumor growth and prolonged the survival of mice.
• In Vitro:
  NVP-ADW742 (ADW742; 0.1-10 μM; 72 hours) dose-dependently inhibits serum-induced cell growth in all cell lines. NVP-ADW742 (0.1-9 μM; 20 min) blocks IGF-1-induced phosphorylation of IGF-1R and its known downstream target Akt at submicromolar concentrations. NVP-ADW742 has much higher IC50 values for other kinases (IC50>10 μM for HER2, PDGFR, VEGFR-2, or Bcr-Abl p210; and IC50>5 μM for c-Kit). Cell Viability Assay Cell line: A panel of cell lines from multiple myeloma (MM), other hematologic malignancies and solid tumors. Concentration: 0.1, 0.5, 1, 2, 5, 10 μM Incubation time: 72 hours. Result: Dose-dependently inhibited serum-induced cell growth in all cell lines. Western blot analysis. Cell line: NWT-21 cells. Concentration: 0.1, 0.3, 1, 3, 9 μM Incubation time: 20 min. Result: Blocked IGF-1-induced phosphorylation of IGF-1R and its known downstream target Akt at submicromolar concentrations.

Storage & Handling

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

Alternative Names

ADW | GSK 552602A | ADW742

Quick Database Links

Gene Symbol

IGF-1R