MLN8054

SKU: orb1300877

Description

MLN8054 is a highly selective small molecule inhibitor of Aurora A kinase, exhibiting potent activity with an IC50 of 4 nM. It is a valuable research tool for studying mitotic progression and has been utilized in both in vitro cellular assays and in vivo xenograft models to investigate oncology and cell cycle biology.

Research Area

Cardiovascular Research, Cell Biology, Epigenetics & Chromatin, Metabolism Research, Signal Transduction, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 869363-13-3
• MW: 476.86
• Purity: 99.05% (May vary between batches)
• Formula: C₂₅H₁₅ClF₂N₄O₂
• SMILES: OC(=O)c1ccc(Nc2ncc3CN=C(c4cc(Cl)ccc4-c3n2)c2c(F)cccc2F)cc1
• Target: Aurora Kinase,Src,PKA,Casein Kinase
• Solubility: Ethanol:< 1 mg/mL (insoluble or slightly soluble);H2O:< 1 mg/mL (insoluble or slightly soluble);DMSO:88 mg/mL (184.54 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (6.92 mM)

Bioactivity

• Target IC50:
  Aurora A:4 nM
• In Vivo:
  In HCT-116 tumor-bearing mice, oral administration of MLN8054 at 3 mg/kg, 10 mg/kg, and 30 mg/kg once daily results in dose-dependent tumor growth inhibition (TGI: 76% and 84% for 10 mg/kg and 30 mg/kg, respectively). MLN8054 demonstrates similar antitumor activity in PC-3 tumor xenografts in nude mice. In HCT-116 xenograft-bearing animals, MLN8054 induces DNA and tubulin staining of tumor tissue in nuclear and cell body areas, consistent with a senescent phenotype, by increasing senescence-associated beta-galactosidase activity.
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• In Vitro:
  MLN8054 is an ATP-competitive, reversible inhibitor of recombinant Aurora A kinase with an IC50 of 4 nM, demonstrating over 40-fold selectivity for Aurora A compared to Aurora B. In vitro, MLN8054 inhibits growth across various cell lines from diverse tissues with IC50 values ranging from 0.11 μM to 1.43 μM. It selectively inhibits Aurora A over Aurora B in cultured cells, and impedes cell proliferation by inducing G2/M accumulation and spindle defects in multiple human tumor cell lines. A recent study indicates that MLN8054 sensitizes androgen-resistant prostate cancer to radiation by inhibiting Aurora A kinase, leading to sustained DNA double-strand breaks.
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• Cell Research:
  Human tumor cell lines are grown in 96-well cell culture dishes according to the distributor's recommendations. MLN8054, diluted in DMSO, is added to the cells in 2-fold serial dilutions to achieve final concentrations ranging from 10 mM to 0.04 mM. MLN8054 at each dilution is added in triplicate with each replicate on a separate plate. Cells treated with DMSO (n = 6 wells per plate; 0.2% final concentration) serves as the untreated control. The cells are treated with MLN8054 for 96 hours at 37 °C in a humidified cell culture chamber. Cell viability in each cell line is measured by using the Cell Proliferation ELISA, BrdU colorimetric kit according to the manufacturer's recommendation(Only for Reference)
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Storage & Handling

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

Alternative Names

PKA, Inhibitor, Lck, inhibit, MLN 8054, MLN8054, MLN-8054, CaseinKinase, Casein Kinase, CK2, Aurora A, Aurora B, Aurora Kinase, AuroraKinase

Compound Identifiers

PubChem CID

11712649