Alisertib | CAS:1028486-01-2

Chemscene社は、高品質な低分子化合物を提供しているメーカーです。
Chemscene社のAlisertib(CAS:1028486-01-2)をご紹介します。

※本製品は研究用です。研究用以外には使用できません。

Name:Alisertib; MLN 8237
Cat. No. :CS-0106
CAS No. :1028486-01-2
Formula:C27H20ClFN4O4
M. Wt. : 518.92
Solubility:DMSO: 9.33 mg/mL

Alisertib (MLN 8237) is a selective Aurora A inhibitor with IC50 of 1.2 nM, and is more selective for Aurora A than Aurora B.IC50 & Target: IC50: 1.2 nM (Aurora A)[3]In Vitro: Alisertib leads the MM cells to mitotic spindle abnormalities, mitotic accumulation, as well as inhibition of cell proliferation through apoptosis and senescence. Alisertib up-regulates p53 and tumor suppressor genes p21 and p27[1]. The decreased activity of MLN8054/Alisertib for the T217D/W277E Aurora A/TPX2 complex may reflect the increased affinity for ATP induced by cofactor binding to Aurora A[2]. Alisertib inhibits cell proliferation with IC50 values ranging from 15 to 469 nM in different tumer cell lines[3].In Vivo: Alisertib (Alisertib, 30 mg/kg, p.o.) significantly reduces tumor burden and increases overall survival in xenograft-murine model of human-MM[1]. Alisertib (20, 30 mg/kg, p.o.) causes tumor growth inhibition in solid tumor xenograft models and regressions in in vivo models of lymphoma, and reduces FLT uptake in HCT-116 xenograft tumors[3].

Manfredi MG, et al. Characterization of Alisertib (MLN8237), an investigational small-molecule inhibitor of aurora A kinase using novel in vivo pharmacodynamic assays.Clin Cancer Res. 2011 Dec 15;17(24):7614-7624. Sloane DA, et al. Drug-Resistant Aurora A Mutants for Cellular Target Validation of the Small Molecule Kinase Inhibitors MLN8054 and MLN8237 ACS Chem. Biol., 2010, 5 (6), pp 563-576 Güllü G, et al. A novel Aurora-A kinase inhibitor MLN8237 induces cytotoxicity and cell-cycle arrest in multiple myeloma Blood June 24, 2010 vol. 115 no. 25 5202-5213