Cat No.
CEI-0008
Description
NVP-ADW742 can inhibit the insulin-like growth factor-I receptor with IC50 of around 100 nM to 200 nM
Alias
ADW742
Synonyms
ADW742
CAS No.
475488-23-4
Targets
Insulin-like growth factor-I receptor
Chemical Name
5-(3-(benzyloxy)phenyl)-7-((1r,3r)-3-(pyrrolidin-1-ylmethyl)cyclobutyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine
M.Wt
453.58
Purity
>99%
Solubility
DSMO 10 mg/mL Water
Storage
2 years at -20 centigrade
In vitro
NVP-ADW742 can inhibit the insulin-like growth factor-I receptor with IC50 of around 100 nM to 200 nM. NVP-ADW742 is a potent and selective IGF-IR kinase inhibitor that can efficiently inhibit the growth of cells that are highly dependent on IGF-I signaling. By inhibiting IGF-IR signaling, NVP-ADW742 can inhibit the growth of H526 cell line with IC50 of 0.4 mM. SCF-mediated Kit phosphorylation and Akt activation were inhibited with IC(50) values in the 1-5 mM.
In vivo
NVP-ADW742 monotherapy or its combination with cytotoxic chemotherapy had significant antitumor activity in an orthotopic xenograft MM model, providing in vivo proof of principle for therapeutic use of selective IGF-1R inhibitors in cancer.
