Ilorasertib hydrochloride

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Ilorasertib (ABT-348) hydrochloride 是一种有效的，具有口服活性和 ATP 竞争性的 aurora 抑制剂，对 aurora A, aurora B, aurora C 的 IC50 值分别为 116, 5, 1 nM。Ilorasertib hydrochloride 也是一种有效的 VEGF 和 PDGF 抑制剂。Ilorasertib hydrochloride 具有用于急性髓系白血病 (AML) 和骨髓增生异常综合征 (MDS) 的研究潜力。

Ilorasertib (ABT-348) hydrochloride is a potent, orally active and ATP-competitive aurora inhibitor with IC50s of116, 5, 1 nM for aurora A, aurora B, aurora C, respectively. Ilorasertib hydrochloride also is a potent VEGF, PDGF inhibitor. Ilorasertib hydrochloride has the potential for the research of acute myeloid leukemia (AML) and myelodysplastic syndrome (MDS).

Cell Viability Assay Cell Line:H1299, H460 cells Concentration:0, 3, 10, 30 nM Incubation Time:24 h Result:Induced a concentration-dependent increase in the extent and number of cells exhibiting polyploidy with EC50S of 5, 10 nM for H1299, H460 cells, respectively.Cell Proliferation Assay Cell Line:MV-4-11, SEM, K562, HCT-15, SW620, H1299, H460 cells Concentration:1-1000 nM Incubation Time:Result:Showed antiproliferative activity with IC50s of 0.3, 1, 103, 6, 6, 2, 2 nM for MV-4-11, SEM, K562, HCT-15, SW620, H1299, H460 cells, respectively.

Animal Model:Female SCID/beige mice Dosage:25 mg/kg Administration:Subcutaneous minipump; 24 h Result:Inhibited the histone H3 phosphorylation and the tumor drug concentration associated with 50% inhibition of histone H3 phosphorylation. Animal Model:22-26 g, female NOD/SCID mice (xenograft model of multiple myeloma (KMS11))Dosage:20 mg/kg Administration:P.o.; once weekly for 3 weeks Result:Inhibited the tumor growth in mouse.

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Cell Cycle/DNA Damage

Aurora Kinase

Aurora Kinase

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1847485-91-9

525

C25H22ClFN6O2S

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 41.67 mg/mL (79.37 mM; 超声助溶 )

Cl.Nc1ncc(-c2cnn(CCO)c2)c2scc(-c3ccc(NC(=O)Nc4cccc(F)c4)cc3)c12

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(-20℃)

With Ice Pack

≥ 2 years