468741-42-6
Chemical Structure
BMS-554417
- CAS No.: 468741-42-6
- Formula:C28H30ClN7O2
- Molecular Weight:532.05
IUPAC Name: (S)-3-(4-(2-(4-((2-(3-chlorophenyl)-2-hydroxyethyl)amino)-2-oxo-1,2-dihydropyridin-3-yl)-7-methyl-1H-benzo[d]imidazol-5-yl)piperazin-1-yl)propanenitrile
InChIKey: VVIPLSCLYCWUQT-XMMPIXPASA-N
SMILES: N(C[C@@H](O)C1=CC(Cl)=CC=C1)C2=C(C=3NC=4C(N3)=CC(=CC4C)N5CCN(CCC#N)CC5)C(=O)NC=C2
Biological Activity: BMS-554417 is an orally active inhibitor of insulin receptor and insulin-like growth factor-I receptor (IGF-1R) kinases, with IC50 values of 50.6 nM and 67.9 nM, respectively. BMS-554417 blocks downstream signal transduction via the ERK and PI3K/Akt pathways. BMS-554417 induces G0-G1 cell cycle arrest, prevents cyclin D1 accumulation in the nucleus, triggers mitochondrial pathway-mediated apoptosis, promotes HER2 phosphorylation, and inhibits the proliferation and growth of cancer cells. BMS-554417 can be used in research related to colon cancer, ovarian cancer, and breast cancer[1][2][3].
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BMS-554417 | BMS-554417 is an orally active inhibitor of insulin receptor and insulin-like growth factor-I receptor (IGF-1R) kinases, with IC50 values of 50.6 nM and 67.9 nM, respectively. BMS-554417 blocks downstream signal transduction via the ERK and PI3K/Akt pathways. BMS-554417 induces G0-G1 cell cycle arrest, prevents cyclin D1 accumulation in the nucleus, triggers mitochondrial pathway-mediated apoptosis, promotes HER2 phosphorylation, and inhibits the proliferation and growth of cancer cells. BMS-554417 can be used in research related to colon cancer, ovarian cancer, and breast cancer. | |||||||||||||||||||||
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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 research. 2006 Jan 01;66(1):362-71.
- [2]. Ozkan EE, et al. Plasma and tissue insulin-like growth factor-I receptor (IGF-IR) as a prognostic marker for prostate cancer and anti-IGF-IR agents as novel therapeutic strategy for refractory cases: a review. Molecular and cellular endocrinology. 2011 Sep 15;344(1-2):1-24.
- [3]. Haluska P, et al. HER receptor signaling confers resistance to the insulin-like growth factor-I receptor inhibitor, BMS-536924. Molecular cancer therapeutics. 2008 Sep;7(9):2589-98.
