475488-23-4

Basic information

• Product Name: 5-(3-Benzyloxyphenyl)-7-[trans-3-[(pyrrolidin-1-yl)methyl]cyclobutyl]-7H-pyrrolo[2,3-d]pyrimidin-4-amine
• Synonyms: 5-(3-Benzyloxyphenyl)-7-[trans-3-[(pyrrolidin-1-yl)methyl]cyclobutyl]-7H-pyrrolo[2,3-d]pyrimidin-4-amine;ADW 742;GSK 552602A;NVP-ADW742(ADW742);ADW;NVP-ADW7;5-(3-Benzyloxyphenyl)-7-[trans-3-[(pyrrolidin-1-yl)methyl]cyclobutyl]-7H-pyrrolo[2,3-d]pyrimidin-4-amine NVP-ADW742 GSK 552602A;ADW 742 GSK 552602A
• CAS NO: 475488-23-4
• Molecular Formula: C28H31N5O
• Molecular Weight: 453.59
• Product Categories: Inhibitors
• Mol File: 475488-23-4.mol
• Article Data: 1

Chemical Properties

• Boiling Point: 677.5±55.0 °C(Predicted)
• Appearance: /
• Density: 1.31
• Solubility: Soluble in DMSO
• PKA: 10.00±0.20(Predicted)
• CAS DataBase Reference: 5-(3-Benzyloxyphenyl)-7-[trans-3-[(pyrrolidin-1-yl)methyl]cyclobutyl]-7H-pyrrolo[2,3-d]pyrimidin-4-amine(CAS DataBase Reference)
• NIST Chemistry Reference: 5-(3-Benzyloxyphenyl)-7-[trans-3-[(pyrrolidin-1-yl)methyl]cyclobutyl]-7H-pyrrolo[2,3-d]pyrimidin-4-amine(475488-23-4)
• EPA Substance Registry System: 5-(3-Benzyloxyphenyl)-7-[trans-3-[(pyrrolidin-1-yl)methyl]cyclobutyl]-7H-pyrrolo[2,3-d]pyrimidin-4-amine(475488-23-4)

Safety Data

• Hazardous Substances Data: 475488-23-4(Hazardous Substances Data)

Usage

Uses

NVP-ADW742 is an IGF-1R inhibitor with IC50?of 0.17 μM.

Biological Activity

nvp-adw742 is a novel inhibitor of ifg-1receptor (igf-1r) kinase with the ic50 value of 0.17μm [1].nvp-adw742 has shown above 16-fold effective function against igf-1r than insulin receptor (insr). furthermore, nvp-adw742 has also been reported to inhibit other kinases , with the ic50 values of ＞10μm for her2, pdgfr, vegfr-2, or bcr-abl p210, and the ic50 values ＞5μm for c-kit [1]. besides, nvp-adw742 combined with etoposide and carboplatin has been reported to inhibit cell growth and induce cytotoxicity by mtt assay using the small cell lung cancer (sclc), including h526, h146, wba and h209 cell lines. in addition, nvp-adw742 has been revealed to completely inhibit the expression of vegf mrna which induced by igf-i in h526 cells [2].

references

[1] mitsiades cs1, mitsiades ns, mcmullan cj, poulaki v, shringarpure r, akiyama m, hideshima t, chauhan d, joseph m, libermann ta, garcía-echeverría c, pearson ma, hofmann f, anderson kc, kung 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 mar; 5(3):221-30.[2]warshamana-greene gs1, litz j, buchdunger e, garcía-echeverría c, hofmann f, krystal gw. 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 feb 15;11(4):1563-71.

Relevant articles and documents

CANCER TREATMENT METHOD

The present invention relates to a method of treating cancer in a mammal and to pharmaceutical combinations useful in such treatment. In particular, the method relates to a cancer treatment method that includes administering an erb family inhibitor and an IGF-1R inhibitor to a mammal suffering from a cancer.