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Linsitinib

Linsitinib structure

CAS No:
867160-71-2
Formula:
C26H23N5O
Chemical Name:
Linsitinib
Synonyms:
Cyclobutanol,3-[8-amino-1-(2-phenyl-7-quinolinyl)imidazo[1,5-a]pyrazin-3-yl]-1-methyl-,cis-;cis-3-[8-Amino-1-(2-phenyl-7-quinolinyl)imidazo[1,5-a]pyrazin-3-yl]-1-methylcyclobutanol;OSI 906;Linsitinib;OSI 906AA
Categories:
Biochemical Engineering > Inhibitors

Description

Losmapimod is a dual inhibitor of the IGF-1 receptor and insulin receptor with IC50s of 35 and 75 nM, respectively.

3-[8-amino-1-(2-phenyl-7-quinolinyl)-3-imidazo[1,5-a]pyrazinyl]-1-methyl-1-cyclobutanol is a member of quinolines and a member of cyclobutanes.|An orally bioavailable small molecule inhibitor of the insulin-like growth factor 1 receptor (IGF-1R) with potential antineoplastic activity. IGF-1R inhibitor OSI-906 selectively inhibits IGF-1R, which may result in the inhibition of tumor cell proliferation and the induction of tumor cell apoptosis.|Linsitinib is an orally bioavailable small molecule inhibitor of the insulin-like growth factor 1 receptor (IGF-1R) with potential antineoplastic activity. Linsitinib selectively inhibits IGF-1R, which may result in the inhibition of tumor cell proliferation and the induction of tumor cell apoptosis. Overexpressed in a variety of human cancers, IGF-1R stimulates cell proliferation, enables oncogenic transformation, and suppresses apoptosis.

Linsitinib Basic Attributes

Molecular Weight：

421.51

Exact Mass：

421.49

EC Number：

1533716-785-6

UNII：

15A52GPT8T

NCI Thesaurus Code：

C70982

Characteristics

PSA：

89.3

XLogP3：

4.2

Density：

1.4±0.1 g/cm3

Refractive Index：

1.748

Drug Information

Drug Indication：

Investigated for use/treatment in cancer/tumors (unspecified) and solid tumors.

Pharmacology：

In laboratory studies of 28 human tumor cell lines, OSI-906 reduced growth of 15 cell lines representative of colorectal, lung, breast, pancreatic, and pediatric tumors and in mouse models. OSI-906 was particularly effective against tumors that are highly IGF-dependent such as colorectal cancers. According to the researchers, OSI-906 not only slowed tumor growth in mice, but decreased the size of some pre-existing tumors.

Mechanism of Action：

IGF-1R stimulates proliferation, enables onogenic transformation, and suppresses apoptosis. Inhibitors of IGF-1R are expected to have broad utility in oncology since the over-expression of IGF-1R and/or its ligands or the down-regulation of ligand binding proteins occurs in numerous human malignancies including lung, colon, breast, prostate, brain and skin cancers. In addition, signaling through the IGF system has been implicated in protecting tumor cells from apoptosis induced by anti-cancer treatments such as cytotoxic agents and EGFR inhibitors.

MeSH Entry Terms：

3-(8-amino-1-(2-phenylquinolin-7-yl)imidazo(1,5-a)pyrazin-3-yl)-1-methylcyclobutanol

Linsitinib Use and Manufacturing

Uses

Linsitinib is a small-molecule dual insulin-like growth factor-1 receptor (IGF-IR) and insulin receptor (IR) kinase inhibitor. IGF-I receptor (IGF-IR) has been implicated in the promotion of tumorigenesis, metastasis and resistance to cancer therapies and thus Linsitinib may be a useful anticancer agent.

Use Classification：

Human drugs -> Rare disease (orphan)

Computed Properties

Molecular Weight:421.5
XLogP3:4.2
Hydrogen Bond Donor Count:2
Hydrogen Bond Acceptor Count:5
Rotatable Bond Count:3
Exact Mass:421.19026037
Monoisotopic Mass:421.19026037
Topological Polar Surface Area:89.3
Heavy Atom Count:32
Complexity:663
Covalently-Bonded Unit Count:1
Compound Is Canonicalized:Yes

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Linsitinib(OSI-906)

CAS No.: 867160-71-2

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