NVP-ADW742 | HY-10252

NVP-ADW742 (ADW742) is an orally active, selective IGF-1R tyrosine kinase inhibitor with an IC50 of 0.17 μM. NVP-ADW742 inhibits insulin receptor (InsR) with an IC50 of 2.8 μM. NVP-ADW742 induces pleiotropic antiproliferative/proapoptotic biologic sequelae in tumor cells[1][2].

IC50 & Target :

IC50: 0.17 μM (IGF-1R) and 2.8 μM (InsR)[1]

In Vitro:

NVP-ADW742 (ADW742; 0.1-10 µM; 72 hours) dose-dependently inhibits serum-induced cell growth in all cell lines^[1].
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^[1].
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)^[1].

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^[1].

Molecular weight:

453.58

Formula:

C₂₈H₃₁N₅O

SMILES:

NC1=C2C(N(C=C2C3=CC=CC(OCC4=CC=CC=C4)=C3)[C@H]5C[C@@H](C5)CN6CCCC6)=NC=N1

Storage: