Linsitinib

Linsitinib

Names
IUPAC name 3-[8-Amino-1-(2-phenyl-7-quinolyl)imidazo[1,5-a]pyrazin-3-yl]-1-methyl-cyclobutanol
Other names OSI-906
Identifiers
CAS Number	867160-71-2
ChEMBL	ChEMBL1091644
ChemSpider	21391708
Jmol interactive 3D	Image
InChI 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) Key: PKCDDUHJAFVJJB-UHFFFAOYSA-N InChI=1/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+ Key: PKCDDUHJAFVJJB-VLZXCDOPBI
SMILES C[C@]1(C[C@@H](C1)C2=NC(=C3N2C=CN=C3N)C4=CC5=C(C=CC(=N5)C6=CC=CC=C6)C=C4)O
Properties
Chemical formula	C26H23N5O
Molar mass	421.50 g·mol^−1
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa).
Infobox references

Linsitinib is an experimental drug candidate for the treatment of various types of cancer. It is an inhibitor of the insulin receptor and of the insulin-like growth factor 1 receptor (IGF-1R).^[1] This prevents tumor cell proliferation and induces tumor cell apoptosis.^[2]

Linsitinib was discovered by OSI Pharmaceuticals and is currently in Phase III clinical trials for adrenocortical carcinoma and Phase II clinical trials for lung and ovarian cancers.^[3][4]

References

1. Mulvihill, MJ; Cooke, A; Rosenfeld-Franklin, M; Buck, E; Foreman, K; Landfair, D; O'Connor, M; Pirritt, C; et al. (2009). "Discovery of OSI-906: A selective and orally efficacious dual inhibitor of the IGF-1 receptor and insulin receptor". Future medicinal chemistry 1 (6): 1153–71. doi:10.4155/fmc.09.89. PMID 21425998.
2. "Linsitinib". NCI Drug Dictionary. National Cancer Institute. Retrieved October 16, 2012.
3. "OSI Pharmaceuticals, LLC". Astellas Pharma. Retrieved October 16, 2012.
4. "Linsitinib". National Institutes of Health's clinicaltrials.gov. Retrieved October 16, 2012.