BM0003
BMS-754807
≥98% (HPLC)
别名:
(2S)-1-[4-[(5-Cyclopropyl-1H-pyrazol-3-yl)amino]pyrrolo[2,1-f][1,2,4]triazin-2-yl]-N-(6-fluoro-3-pyridinyl)-2-methyl-2-Pyrrolidinecarboxamide, BMS 754807
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关于此项目
经验公式（希尔记法）:
C23H24FN9O
化学文摘社编号:
分子量:
461.49
NACRES:
NA.77
PubChem Substance ID:
UNSPSC Code:
12352200
MDL number:
InChI key
LQVXSNNAFNGRAH-QHCPKHFHSA-N
SMILES string
C[C@@]1(C(NC2=CC=C(F)N=C2)=O)CCCN1C(N=C3NC4=NNC(C5CC5)=C4)=NN6C3=CC=C6
InChI
1S/C23H24FN9O/c1-23(21(34)26-15-7-8-18(24)25-13-15)9-3-10-32(23)22-28-20(17-4-2-11-33(17)31-22)27-19-12-16(29-30-19)14-5-6-14/h2,4,7-8,11-14H,3,5-6,9-10H2,1H3,(H,26,34)(H2,27,28,29,30,31)/t23-/m0/s1
assay
≥98% (HPLC)
form
powder
optical activity
[α]/D -86 to -96°, c = 1 in methanol
color
white to beige
solubility
DMSO: 20 mg/mL, clear
storage temp.
room temp
Gene Information
human ... IGF1R(3480), INSR(3643)
General description
BMS-754807 is a pyrrolotriazine, which is a potent dual inhibitor of insulin-like growth factor-1 receptor (IGF-1R) and insulin receptor (InsR) tyrosine kinase. It has been reported that BMS-754807 also acts as a reversible ATP-competitive antagonist of IGF-1R by restricting the catalytic domain of the IGF-1R.
Application
BMS-754807 has been used in the embryo drug treatment.
Biochem/physiol Actions
BMS-754807 is an orally available and potent dual insulin-like growth factor factor-1 receptor (IGF-1R)/ insulin receptor (InsR) tyrosine kinase inhibitor that synergistically enhances antiproliferative effects of 4-hydroxytamoxifen, letrozole, and fulvestrant in MCF-7/AC-1 cells.
BMS-754807 is an orally available and potent dual insulin-like growth factor factor-1 receptor (IGF-1R)/ insulin receptor (InsR) tyrosine kinase inhibitor.
Features and Benefits
BMS-754807 is available through a partnership with Bristol-Myers Squibb (BMS). To learn more and view other BMS compounds, visit sigma.com/BMS.
Legal Information
Sold for research purposes only under agreement from BMS.
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
法规信息
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Joan M Carboni et al.
Molecular cancer therapeutics, 8(12), 3341-3349 (2009-12-10)
BMS-754807 is a potent and reversible inhibitor of the insulin-like growth factor 1 receptor/insulin receptor family kinases (Ki, <2 nmol/L). It is currently in phase I development for the treatment of a variety of human cancers. BMS-754807 effectively inhibits the
Adele M Musicant et al.
Cell reports, 34(8), 108768-108768 (2021-02-25)
Mucoepidermoid carcinoma (MEC) is a life-threatening salivary gland cancer that is driven primarily by a transcriptional coactivator fusion composed of cyclic AMP-regulated transcriptional coactivator 1 (CRTC1) and mastermind-like 2 (MAML2). The mechanisms by which the chimeric CRTC1/MAML2 (C1/M2) oncoprotein rewires
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