OSI-027
- CAS NO.:936890-98-1
- Empirical Formula: C21H22N6O3
- Molecular Weight: 406.44
- MDL number: MFCD20275101
- SAFETY DATA SHEET (SDS)
- Update Date: 2024-11-11 14:41:12
What is OSI-027?
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 ) 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). It is selective for mTOR over phosphatidylinositol 3-kinase isoforms and DNA protein kinase. OSI-027 prohibits proliferation, induces autophagy, and potentiates apoptosis in BCR-ABL transformed cells and other cancer cells at 10 μM. 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.
The Uses of OSI-027
OSI-027 is a kinase inhibitor with anti-tumor activity, used in treatment of breast cancer.
What are the applications of Application
OSI-027 is a potent mammalian target of rapamycin (mTOR) kinase inhibitor
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.
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.
Properties of OSI-027
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 |
Safety information for OSI-027
Computed Descriptors for OSI-027
New Products
(R)-3-Aminobutanenitrile Hydrochloride 4-Aminotetrahydropyran-4-carbonitrile Hydrochloride 4-AMINO-TETRAHYDRO-PYRAN-4-CARBOXYLIC ACID HCL 4-AMINO-TETRAHYDRO-PYRAN-4-CARBOXYLIC ACID 1,4-Dioxa-8-azaspiro[4.5]decane 5-Bromo-2-nitropyridine SODIUM AAS SOLUTION ZINC AAS SOLUTION BUFFER SOLUTION PH 10.0(BORATE) GOOCH CRUCIBLE SINTERED AQUANIL 5 BERYLLIUM AAS SOLUTION AMOXICILLIN (AMOXYCILLIN) TRIHYDRATE ACICLOVIR AMLODIPINE SODIUM METHYL PARABEN Methylcobalamin (vitamin B12) SODIUM VALPROATE 5-Fluoro-2-iodo-3-methylaniline Ethyl 3-(furan-2-yl)-3-hydroxypropanoate 1-Methyl-6-oxo-1,6-dihydropyridazine-3-carbonitrile 3-Bromo-2-hydroxybenzeneacetic acid 5-Iodo-3-methyl-2-nitropyridine 1-(3-Chloro-2-hydroxyphenyl)-2-propanoneRelated products of tetrahydrofuran
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