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OSI-027

OSI-027 structure

CAS No:
936890-98-1
Formula:
C21H22ClN6O3
Chemical Name:
OSI-027
Synonyms:
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;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;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;ASP4786;OSI-027trans-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 acidOSI-027
Categories:
Biochemical Engineering > Inhibitors

Description

OSI-027 is an ATP-competitive mTOR kinase activity inhibitor with an IC50 of 4 nM. OSI-027 targets both mTORC1 and mTORC2 with IC50s of 22 nM and 65 nM, respectively.

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.|OSI-027 has been used in trials studying the treatment of Any Solid Tumor or Lymphoma.|mTOR Kinase Inhibitor OSI-027 is an orally bioavailable mammalian target of rapamycin (mTOR) kinase inhibitor with potential antineoplastic activity. mTOR kinase inhibitor OSI-027 binds to and inhibits both the raptor-mTOR (TOR complex 1 or TORC1) and the rictor-mTOR (TOR complex 2 or TORC2) complexes of mTOR, which may result in tumor cell apoptosis and a decrease in tumor cell proliferation. mTOR is a serine/threonine kinase that is upregulated in some tumors and plays an important role downstream in the PI3K/Akt/mTOR signaling pathway.

OSI-027 Basic Attributes

Molecular Weight：

441.89078

Exact Mass：

406.175354

EC Number：

-0

UNII：

25MKH1SZ0M

NCI Thesaurus Code：

C78476

Characteristics

PSA：

131.42000

XLogP3：

3.80300

Density：

1.6±0.1 g/cm3

Flash Point：

311.5±32.9 °C

Refractive Index：

1.788

Drug Information

MeSH Entry Terms：

OSI 027

OSI-027 Use and Manufacturing

This compound is a kinase inhibitor with anti-tumor activity, used in treatment of breast cancer.

Computed Properties

Molecular Weight:406.4
XLogP3:2
Hydrogen Bond Donor Count:3
Hydrogen Bond Acceptor Count:7
Rotatable Bond Count:4
Exact Mass:406.17533859
Monoisotopic Mass:406.17533859
Topological Polar Surface Area:131
Heavy Atom Count:30
Complexity:630
Covalently-Bonded Unit Count:1
Compound Is Canonicalized:Yes

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