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KI3430NVP-ADW7424 mg$320

Chemical Characteristic

Product NameNVP-ADW742
CAS No.475488-23-4
Molecular Weight 453.58
FormulaC28H31N5O
Chemical Name5-(3-phenylmethoxyphenyl)-7-[3-(pyrrolidin-1-ylmethyl)cyclobutyl]pyrrolo[2,3-d]pyrimidin-4-amine
Smilesc1nc2c(c(n1)N)c(cn2C1C[C@@H](C1)CN1CCCC1)c1cc(ccc1)OCc1ccccc1
Chemical Structure

Biological activities

NVP-ADW742 is a small molecule ATP-competitive inhibitor of the IGF-I receptor (IGF-IR) with an IC50 of 0.17 µM.[1] NVP-ADW742 inhibits the growth of cells that are highly dependent on IGF-I signaling. NVP-ADW742 inhibits IGF-I signaling with an IC50 of 0.1??.2 µM, which correlated well with an IC50 for IGF-1-mediated growth of 0.2 ??.4 µM.[2] In vitro, NVP-ADW742 inhibits the growth of and induces apoptosis in multiple SCLC cell lines. In SCLC cell lines, NVP-ADW742 also blocks IGF-I-mediated VEGF expression. In the WBA cell line, NVP-ADW742 only partially inhibits Akt activity and enhances cytotoxicity.[1] In the H209 cell lines. NVP-ADW742 enhances both the growth suppressive effects and cytotoxicity of etoposide in a dose-dependent fashion.[2] In vivo, in a mouse model of diffuse multiple myeloma (MM), administration of NVP-ADW742??0 mg/kg twice daily??hows inhibiting tumor growth, prolonging survival and enhancing the antitumor effect of cytotoxic chemotherapy.[3]

Protocols

In vitro, NVP-ADW742 is dissolved in DMSO.[2]

References

[1] Warshamana-Greene GS, et al. The insulin-like growth factor-I receptor kinase inhibitor, NVP-ADW742, sensitizes small cell lung cancer cell lines to the effects of chemotherapy. Clin Cancer Res. 2005, 11(4):1563-1571.
[2] Mitsiades CS, et al. Inhibition of the insulin-like growth factor receptor-1 tyrosine kinase activity as a therapeutic strategy for multiple myeloma, other hematologic malignancies, and solid tumors. Cancer Cell. 2004, 5(3):221-230.
[3] Warshamana-Greene GS, et al. The insulin-like growth factor-I (IGF-I) receptor kinase inhibitor NVP-ADW742, in combination with STI571, delineates a spectrum of dependence of small cell lung cancer on IGF-I and stem cell factor signaling. Mol Cancer Ther. 2004, 3(5):527-535.

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