Potent and selective dual inhibitor of the IGF-1 receptor and insulin receptor
Linsitinib is a potent and selective dual inhibitor of the IGF-1 receptor (IC50 = 35 nM) and insulin receptor (IC50 = 75 nM); it inhibits ligand-dependent auto-phosphorylation of both receptor tyrosine kinases and prevents ligand-induced activation of downstream pathways including pAKT, pERK1/2 and p-p70S6K. The compound is selective for IGF-1R, IR and IRR in a panel of 88 kinases. Lisintinib inhibits proliferation in a variety of tumor cell lines and shows robust
in vivo
antitumor efficacy in an IGF-1R-driven LSN xenograft model. Orally bioavailable.
| Marque | Tocris Bioscience |
|---|---|
| Réf. B-LABO | BL-RE-158076 |
| Réf. fabricant | 18748776 |
| Nom chimique ou matériau | cis-3-[8-Amino-1-(2-phenyl-7-quinolinyl)imidazo[1,5-a]pyrazin-3-yl]-1-methylcyclobutanol |
| CAS | 867160-71-2 |
| Quantité | 10 mg |
| Cible | IGF-I R/IGF1R |
| Formule moléculaire | C<sub>26</sub>H<sub>23</sub>N<sub>5</sub>O |
| Pureté | 0.98 |
