Alisertib

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

一种有效且高度选择性的 Aurora A 抑制剂，IC50 为 1.2 nM；对 Aurora B (IC50=396.5 nM) 和 205 激酶组的活性较低。

A potent and highly selective inhibitor of Aurora A with IC50 of 1.2 nM; has less activity against Aurora B (IC50=396.5 nM) and a 205-kinase panel; inhibits proliferation of human tumor cell lines in vitro and produces tumor growth inhibition in solid tumor xenograft models.(In Vitro):Levetiracetam increases the transcription of HDACs and recruits corepressor complex on O6-Methylguanine-DNA-methyltransferase (MGMT) promoter, thus silencing its activity.Levetiracetam sensitizes (40 μg/mL) glioblastoma multiforme stem-like cells (GSCs) to Temozolomide (250 μM) treatment.MGMT expression is downregulated in GCSCs treated with Levetiracetam?(40 μg/mL).(In Vivo):Levetiracetam (10, 25, or 50?mg/kg) suppresses behavioral and electrographic seizure activity during neonatal hypoxia.

Alisertib (MLN 8237) 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. The decreased activity of Alisertib (MLN 8237) for the T217D/W277E Aurora A/TPX2 complex may reflect the increased affinity for ATP induced by cofactor binding to Aurora A.Alisertib (MLN 8237) inhibits cell proliferation with IC50s ranging from 15 to 469 nM in different tumer cell lines.

Alisertib (MLN 8237) (30 mg/kg, p.o.) significantly reduces tumor burden and increases overall survival in xenograft-murine model of human-MM.Alisertib (3-30 mg/kg; p.o.; once daily for 3 weeks) causes tumor growth inhibition in solid tumor xenograft models. Animal Model:Nude mice bearing HCT-116 colon tumor xenograft Dosage:3, 10, or 30 mg/kg Administration:P.o.; once daily for 3 weeks Result:Resulted in a dose-dependent TGI (tumor growth inhibition) of 43.3%, 84.2%, and 94.7% for the 3, 10, and 30 mg/kg groups,respectively.

MLN 8237 | MLN8237 | MLN-8237

Cell Cycle/DNA Damage

Aurora Kinase

AuroraA|AuroraB

Cancer

——

1028486-01-2

518.9235

C27H20ClFN4O4

>98% (HPLC)

DMSO: 9.33 mg/mL

O=C(O)C1=CC=C(NC2=NC=C3C(C4=CC=C(Cl)C=C4C(C5=C(OC)C=CC=C5F)=NC3)=N2)C=C1OC

Benzoic acid, 4-[[9-chloro-7-(2-fluoro-6-methoxyphenyl)-5H-pyrimido[5,4-d][2]benzazepin-2-yl]amino]-2-methoxy-

(-20℃)

With Ice Pack

≥ 2 years