Ilorasertib (ABT-348) (Synonyms: ABT-348) |
| Catalog No.GC34159 |
일로라서팁(ABT-348)(ABT-348)은 오로라 A, 오로라 B, 오로라 C에 대해 각각 IC50이 116, 5, 1nM인 강력한 경구 활성 및 ATP 경쟁 오로라 억제제입니다. Ilorasertib(ABT-348)은 또한 강력한 VEGF, PDGF 억제제입니다. 일로라서팁(ABT-348)은 급성 골수성 백혈병(AML) 및 골수이형성 증후군(MDS) 연구에 대한 잠재력이 있습니다.
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Cas No.: 1227939-82-3
Sample solution is provided at 25 µL, 10mM.
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Ilorasertib (ABT-348) is an ATP-competitive multitargeted kinase inhibitor with IC50s for inhibiting binding Aurora B (7 nM), C (1 nM), and A (120 nM), and also inhibits RET tyrosine kinase, PDGFRβ, and Flt1 with IC50s of 7 nM, 3 nM and 32 nM.
Ilorasertib is an ATP-competitive multitargeted kinase inhibitor with IC50 for inhibiting cellular autophosphorylation of Aurora B (13 nM), C (13 nM), and A (189 nM). In addition to targeting Aurora kinases, Ilorasertib is a potent inhibitor of the VEGFR and PDGFR kinase families and, to a lesser extent, the Src family of cytoplasmic tyrosine kinases. Ilorasertib induces a concentration-dependent increase in the extent and number of two NSCLC cell lines exhibiting polyploidy. The potency for inducing this response (EC50 = 5 and 10 nM). Ilorasertib shows antiproliferative activity against BCR-ABL expressing CML cells and cells expressing the gleevec-resistant BCR-ABL T315I mutation (IC50 = 47 and 260 nM)[2].
Ilorasertib (25 mg/kg, s.c.) leads to an inhibition of histone H3 phosphorylation in circulating tumor cells obtained from an engrafted leukemia model. Ilorasertib inhibits the VEGF response with a potency (ED50 = 0.2 mg/kg i.v.) in a uterine edema model. Ilorasertib (20 mg/kg, p.o.) inhibits the growth of established tumors and causes regression of advanced tumors in human xenograft models[2]. Ilorasertib demonstrates significant antitumor efficacy in both solid and hematological xenograft models after intravenous, mini-pump or parenteral once-weekly dosing[3].
[1]. Gao C, et al. Characterization of interactions and pharmacophore development for DFG-out inhibitors to RET tyrosine kinase. J Mol Model. 2015 Jul;21(7):167. [2]. Glaser KB, et al. Preclinical characterization of ABT-348, a kinase inhibitor targeting the aurora, vascular endothelial growth factor receptor/platelet-derived growth factor receptor, and Src kinase families. J Pharmacol Exp Ther. 2012 Dec;343(3):617-27. [3]. Curtin ML, et al. Thienopyridine ureas as dual inhibitors of the VEGF and Aurora kinase families. Bioorg Med Chem Lett. 2012 May 1;22(9):3208-12.
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