Alisertib

SKU: orb1227119

Description

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.

Key Properties

• CAS Number: 1028486-01-2
• MW: 518.9235
• Purity: >98% (HPLC)
• Formula: C₂₇H₂₀ClFN₄O₄
• SMILES: 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
• Target: Aurora Kinase
• Solubility: DMSO: 9.33 mg/mL

Bioactivity

• In Vivo:
  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.
• In Vitro:
  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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

MLN 8237 | MLN8237 | MLN-8237

Quick Database Links

Gene Symbol

Aurora Kinase