| Identification | Back Directory | [Name]
OSI-027 | [CAS]
936890-98-1 | [Synonyms]
CS-436
CPD2801
OSI-027
ASP4786
OSI-027, >=98%
OSI027;OSI 027
OSI-027 USP/EP/BP
OSI-027;OSI 027;ASP4786
trans-4-[4-Amino-5-(7-methoxy-1H-i
(1r,4r)-4-(4-Amino-5-(7-methoxy-1H-indol-2-yl)imidazo-[5,1-f][1,2,4]triazin-7-yl)cyclohexaneca
4-(4-Amino-5-(7-methoxy-1H-indol-2-yl)imidazo[5,1-f] [1,2,4]Triazin-7-yl)cyclohexanecarboxylic Acid
trans-4-[4-Amino-5-(7-methoxy-1H-indol-2-yl)imidazo[5,1-f][1,2,4]triazin-7-yl]cyclohexanecarboxylic acid
(1r,4r)-4-(4-amino-5-(7-methoxy-1H-indol-2-yl)imidazo[1,5-f][1,2,4]triazin-7-yl)cyclohexanecarboxylic acid
CYCLOHEXANECARBOXYLIC ACID, 4-[4-AMINO-5-(7-METHOXY-1H-INDOL-2-YL)IMIDAZO[5,1-F][1,2,4]TRIAZIN-7-YL]-, TRANS-
4-(4-aMino-5-(7-Methoxy-1H-indol-2-yl)-1,2-dihydroiMidazo[5,1-f][1,2,4]triazin-7-yl)cyclohexanecarboxylic acid hydrochloride
trans-4-[4-Amino-5-(7-methoxy-1H-indol-2-yl)imidazo[5,1-f][1,2,4]triazin-7-yl]cyclohexanecarboxylic acid OSI-027
OSI-027 trans-4-[4-Amino-5-(7-methoxy-1H-indol-2-yl)imidazo[5,1-f][1,2,4]triazin-7-yl]cyclohexanecarboxylic acid | [Molecular Formula]
C21H22N6O3 | [MDL Number]
MFCD20275101 | [MOL File]
936890-98-1.mol | [Molecular Weight]
406.44 |
| Chemical Properties | Back Directory | [Melting point ]
>149°C (subl.) | [density ]
1.59 | [storage temp. ]
Hygroscopic, -20°C Freezer, Under inert atmosphere | [solubility ]
DMSO (Slightly) | [form ]
Solid | [pka]
4.44±0.10(Predicted) | [color ]
Pale Beige to Light Beige |
| Hazard Information | Back Directory | [Description]
The mammalian target of rapamycin (mTOR) is a serine-threonine kinase that is central to two protein complexes, mTORC1 and mTORC2. These complexes are differentially regulated (e.g., only mTORC1 is sensitive to rapamycin (Item No. 13346)) and regulate different pathways. OSI-027 is an inhibitor of the catalytic site of mTOR and, as a result, inhibits both mTORC1 and mTORC2 (IC50s = 22 and 65 nM, respectively).1,2 It is selective for mTOR over phosphatidylinositol 3-kinase isoforms and DNA protein kinase.2 OSI-027 prohibits proliferation, induces autophagy, and potentiates apoptosis in BCR-ABL transformed cells and other cancer cells at 10 μM.1,3,4 OSI-027 is effective in vivo, blocking the phosphorylation of targets of mTORC1 and mTORC2 and suppressing tumor growth in several different human xenograft models.2,5 | [Uses]
OSI-027 is a kinase inhibitor with anti-tumor activity, used in treatment of breast cancer.
| [Definition]
ChEBI: 4-[4-amino-5-(7-methoxy-2-indolylidene)-1H-imidazo[5,1-f][1,2,4]triazin-7-yl]-1-cyclohexanecarboxylic acid is a member of indoles. | [target]
mTORC | [References]
[1] bhagwat s v, gokhale p c, crew a p, et al. preclinical characterization of osi-027, a potent and selective inhibitor of mtorc1 and mtorc2: distinct from rapamycin. molecular cancer therapeutics, 2011, 10(8): 1394-1406. |
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