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HomeProduct name listOSI-027

OSI-027

OSI-027 Structural

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

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