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BM0003

Sigma-Aldrich

BMS-754807

≥98% (HPLC)

Synonym(s):

(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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About This Item

Empirical Formula (Hill Notation):
C23H24FN9O
CAS Number:
1001350-96-4
Molecular Weight:
461.49
MDL number:
MFCD18633202
UNSPSC Code:
12352200
PubChem Substance ID:
329774351
NACRES:
NA.77

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

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

InChI key

LQVXSNNAFNGRAH-QHCPKHFHSA-N

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.[1]

Application

BMS-754807 has been used in the embryo drug treatment.[2]

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.

Storage Class

11 - Combustible Solids

wgk_germany

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

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Certificates of Analysis (COA)

Lot/Batch Number
0000062405
0000062406
0000041217
0000041220
0000017029

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Distant Insulin Signaling Regulates Vertebrate Pigmentation through the Sheddase Bace2.
Zhang YM, et al.
Developmental Cell, 45(5), 580-594 (2018)
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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