Linsitinib

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. However, insulin receptor (InsR) signaling can compensate for IGF-1R inhibition. Linsitinib is a dual inhibitor of IGF-1R and InsR kinases (IC50s = 35 and 75 nM, respectively). It also inhibits InsR-related receptor (IC50 = 75 nM) but is without effect (IC50 > 10 µM) against a large panel of other kinases. 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. A rapid, non-invasive method to predict the pharmacodynamic response to linsitinib has been reported.Formal Name: cis-3-[8-amino-1-(2-phenyl-7-quinolinyl)imidazo[1,5-a]pyrazin-3-yl]-1-methyl-cyclobutanol. CAS Number: 867160-71-2. Synonyms: OSI-906. Molecular Formula: C26H23N5O. Formula Weight: 421.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 25 mg/ml, DMF:PBS (pH7.2) (1:30): Slightly soluble, DMSO: 20 mg/ml, Ethanol: 1 mg/ml. lambdamax: 210, 259, 352 nm. SMILES: NC1=NC=CN2C1=C(C3=CC(N=C(C4=CC=CC=C4)C=C5)=C5C=C3)N=C2[C@H]6C[C@@](C)(O)C6. InChi Code: InChI=1S/C26H23N5O/c1-26(32)14-19(15-26)25-30-22(23-24(27)28-11-12-31(23)25)18-8-7-17-9-10-20(29-21(17)13-18)16-5-3-2-4-6-16/h2-13,19,32H,14-15H2,1H3,(H2,27,28)/t19-,26+. InChi Key: PKCDDUHJAFVJJB-VLZXCDOPSA-N.