Description
NVP-ADW742 can inhibit the insulin-like growth factor-I receptor with IC50 of around 100 nM to 200 nM
Storage
2 years at -20 centigrade
Targets
Insulin-like growth factor-I receptor
Molecular Formula
C28H31N5O
Chemical Name
5-(3-(benzyloxy)phenyl)-7-((1r,3r)-3-(pyrrolidin-1-ylmethyl)cyclobutyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine
Solubility
DSMO 10 mg/mL Water
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.
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