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Cat. No. Name Size Price Add Cart
KI3420BMS-554417QuoteQuote

Chemical Characteristic

Product NameBMS-554417
CAS No.468741-42-6
Molecular Weight 532
FormulaC28H30ClN7O2
Chemical Name4-[2-[4-[[(2S)-2-(3-Chlorophenyl)-2-hydroxyethyl]amino]-1,2-dihydro-2-oxo-3-pyridinyl]-7-methyl-1H-benzimidazol-5-yl]-1-piperazinepropanenitrile
SmilesC(#N)CCN1CCN(CC1)c1cc2c([nH]c(n2)c2c(=O)[nH]ccc2NC[C@@H](O)c2cc(ccc2)Cl)c(c1)C
Chemical Structure

Biological activities

BMS-554417 is a inhibitor of IGF1R/IR and inhibits focal adhesion kinase (FAK) activity.[1] The IC50s of BMS-554417 are 68, 51, and 90 nM against IGF-IR, IR, and FAK, respectively.[2] BMS-554417 has antiproliferative and proapoptotic activity in vitro and in vivo.[3] In Jurkat T-cell leukemia cells, BMS-554417 triggers apoptotic cell death via the mitochondrial pathway, and induce apoptotic cell morphologic changes at 2.5 µM.[1][3] In breast and ovarian cancer cell lines, the IC50s of BMS-554417 for proliferation ranged from 0.218 to 8.5 µM. In vitro, BMS-554417 inhibits ERK phosphorylation and causes a G0/G1 arrest and prevents nuclear accumulation of cyclin D1 in response to LR3 IGF-I. Meanwhile, BMS-554417 decreases Akt phosphorylation at Ser473 and inhibits the PI3k/Akt pathway.[3] In vivo, BMS-554417 blocks both IGF-I??ediated and insulin-mediated signaling events and reduces salivary gland tumor xenografts growth.[4] In a mouse allograft model, oral administration of BMS-554417??00 mg/kg once daily??hows significant antitumor efficacy in mice.[2]

Protocols

In vitro, BMS-554417 is dissolved in DMSO.[2]

References

[1]Haluska P, et al. In vitro and in vivo antitumor effects of the dual insulin-like growth factor-I/insulin receptor inhibitor, BMS-554417. Cancer Res. 2006, 66(1):362-371.
[2]Wang Y, et al. Inhibition of the IGF-I receptor for treatment of cancer. Kinase inhibitors and monoclonal antibodies as alternative approaches. Recent Results Cancer Res. 2007, 172:59-76.
[3]Haluska, Paul, et al. "BMS-554417, an inhibitor of the insulin-like growth factor I receptor and insulin receptor, inhibits proliferation and induces mitochondrial pathway-mediated apoptosis in cancer cell lines." Proceedings of the American Association for Cancer Research 2005.1 (2005): 1191.
[4]Zhang H, et al. Down-regulation of type I insulin-like growth factor receptor increases sensitivity of breast cancer cells to insulin. Cancer Res. 2007, 67(1):391-397.

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