BMS-554417 - CAS 468741-42-6
Catalog number: 468741-42-6
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C28H30ClN7O2
Molecular Weight:
532.04
COA:
Inquire
Targets:
Others
Description:
BMS-554417 is a novel inhibitor of IGF-IR, which inhibits IGF-IR and insulin receptor kinase activity and proliferation in vitro, with the IC50 for proliferation ranged from 120 nmol/L (Colo205) to >8.5 micromol/L (OV202).
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Purity:
≥98%
Appearance:
Solid powder
Synonyms:
3-[4-[(2Z)-2-[4-[[(2S)-2-(3-chlorophenyl)-2-hydroxyethyl]amino]-2-oxopyridin-3-ylidene]-7-methyl-1,3-dihydrobenzimidazol-5-yl]piperazin-1-yl]propanenitrile;
Solubility:
Soluble in DMSO
Storage:
Store at -20 °C
MSDS:
Inquire
Application:
A novel inhibitor of IGF-IR
Quality Standard:
Enterprise standard
Shelf Life:
As supplied, 2 years from the QC date provided on the Certificate of Analysis, when stored properly.
Quantity:
Milligrams-Grams
InChIKey:
ATYVNAJZCAQFEZ-GJSRYIRCSA-N
InChI:
1S/C28H30ClN7O2/c1-18-14-21(36-12-10-35(11-13-36)9-3-7-30)16-23-26(18)34-27(33-23)25-22(6-8-31-28(25)38)32-17-24(37)19-4-2-5-20(29)15-19/h2,4-6,8,14-16,24,32-34,37H,3,9-13,17H2,1H3/b27-25-/t24-/m1/s1
Canonical SMILES:
CC1=CC(=CC2=C1NC(=C3C(=CC=NC3=O)NCC(C4=CC(=CC=C4)Cl)O)N2)N5CCN(CC5)CCC#N
Current Developer:
Bristol-Myers Squibb
1.In vitro and in vivo antitumor effects of the dual insulin-like growth factor-I/insulin receptor inhibitor, BMS-554417.
Haluska P1, Carboni JM, Loegering DA, Lee FY, Wittman M, Saulnier MG, Frennesson DB, Kalli KR, Conover CA, Attar RM, Kaufmann SH, Gottardis M, Erlichman C. Cancer Res. 2006 Jan 1;66(1):362-71.
The insulin-like growth factor receptor (IGF-IR) and insulin receptor are either overactivated and/or overexpressed in a wide range of tumor types and contribute to tumorigenicity, proliferation, metastasis, and drug resistance. Here, we show that BMS-554417, a novel small molecule developed as an inhibitor of IGF-IR, inhibits IGF-IR and insulin receptor kinase activity and proliferation in vitro, and reduces tumor xenograft size in vivo. In a series of carcinoma cell lines, the IC50 for proliferation ranged from 120 nmol/L (Colo205) to >8.5 micromol/L (OV202). The addition of stimulatory ligands was unnecessary for the antiproliferative effect in MCF-7 and OV202 cells. BMS-554417 treatment inhibited IGF-IR and insulin receptor signaling through extracellular signal-related kinase as well as the phosphoinositide 3-kinase/Akt pathway, as evidenced by decreased Akt phosphorylation at Ser473. At doses that inhibited proliferation, the compound also caused a G0-G1 arrest and prevented nuclear accumulation of cyclin D1 in response to LR3 IGF-I.
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CAS 468741-42-6 BMS-554417

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