1. Cell Cycle/DNA Damage
    Epigenetics
  2. Aurora Kinase

MLN8054 (Synonyms: MLN-8054; MLN 8054)

Cat. No.: HY-10180 Purity: 98.25%
Data Sheet SDS Handling Instructions

MLN8054 is a potent and selective inhibitor of Aurora A with IC50 of 4 nM; exhibits more than 40-fold selective for Aurora A than Aurora B.

For research use only. We do not sell to patients.
MLN8054 Chemical Structure

MLN8054 Chemical Structure

CAS No. : 869363-13-3

Size Price Stock Quantity
10 mM * 1 mL in DMSO $121 In-stock
5 mg $110 In-stock
10 mg $190 In-stock
50 mg $590 Backordered
100 mg $819 Backordered
200 mg   Get quote  
500 mg   Get quote  

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Description

MLN8054 is a potent and selective inhibitor of Aurora A with IC50 of 4 nM; exhibits more than 40-fold selective for Aurora A than Aurora B. IC50 Value: 4 nM [1] Target: Aurora A in vitro: MLN8054 is an ATP-competitive, reversible inhibitor of recombinant Aurora A kinase with an IC50 of 4 nM, which shows >40-fold more selective inhibitory activity for Aurora A compared with Aurora B. In vitro, MLN8054 exhibits the activity of growth inhibition across various cell lines from diverse tissue origins with IC50 values ranging from 0.11 μM to 1.43 μM. In addition, MLN8054 selectively inhibits Aurora A over Aurora B in cultured cells, and inhibits cell proliferation by promoting G2/M accumulation and spindle defects in multiple cultured human tumor cells lines [1]. A recent study shows that MLN8054 sensitizes androgen-resistant prostate cancer to radiation by inhibiting Aurora A kinase, which is associated with sustained DNA double-strand breaks[2]. in vivo: In the HCT-116 tumor-bearing mice, MLN8054, administered orally at 3 mg/kg, 10 mg/kg, and 30 mg/kg once a day, leads to dose-dependent tumor growth inhibition (TGI: 76% and 84% for 10 mg/kg and 30 mg/kg). MLN8054 also shows similar antitumor activity in the PC-3 tumor xenograft in nude mice [1]. In the HCT-116 xenograft-bearing animals, MLN8054 induces DNA and tubulin staining of tumor tissue in nuclear and cell body area, consistent with a senescent phenotype by increasing senescence-associated beta-galactosidase activity [3].

Clinical Trial
NCT Number Sponsor Condition Start Date Phase
NCT00249301 Millennium Pharmaceuticals, Inc. Breast Neoplasm|Colon Neoplasm|Pancreatic Neoplasm|Bladder Neoplasm October 2005 Phase 1
NCT00652158 Millennium Pharmaceuticals, Inc. Advanced Malignancies April 2006 Phase 1
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References
M.Wt

476.86

Formula

C₂₅H₁₅ClF₂N₄O₂

CAS No.

869363-13-3

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

10 mM in DMSO

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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MLN8054
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HY-10180
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