A dual inhibitor of IGF-1R and InsR kinases (IC50s = 35 and 75 nM

Linsitinib – 10 mg

Brand:
Cayman
CAS:
867160-71-2
Storage:
-20
UN-No:
Non-Hazardous - /

The binding of insulin-like growth factor 1 (IGF-1) to the IGF-1 receptor (IGF-1R) promotes cell growth while inhibiting apoptotic pathways. Overexpression of IGF-1R is found in certain solid tumors and hematologic neoplasias.{31137,31135} However, insulin receptor (InsR) signaling can compensate for IGF-1R inhibition.{31134} Linsitinib is a dual inhibitor of IGF-1R and InsR kinases (IC50s = 35 and 75 nM, respectively).{31136} It also inhibits InsR-related receptor (IC50 = 75 nM) but is without effect (IC50 > 10 µM) against a large panel of other kinases.{31136} Linsitinib inhibits proliferation of a variety of tumor cell lines in vitro and has antitumor efficacy in an IGF-1R-driven xenograft mouse model when administered orally.{31136} A rapid, non-invasive method to predict the pharmacodynamic response to linsitinib has been reported.{31134}  

 

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Description

A dual inhibitor of IGF-1R and InsR kinases (IC50s = 35 and 75 nM, respectively); inhibits proliferation of tumor cell lines in vitro and has antitumor efficacy in an IGF-1R-driven xenograft mouse model when administered orally

Formal name: cis-3-[8-amino-1-(2-phenyl-7-quinolinyl)imidazo[1,5-a]pyrazin-3-yl]-1-methyl-cyclobutanol

Synonyms:  OSI-906

Molecular weight: 421.5

CAS: 867160-71-2

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|IGF-1R/InsR Family||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Death|Apoptosis||Research Area|Cancer|Cell Signaling|Growth Factor Receptor Signaling

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