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Products are for research use only. Not for human use. We do not sell to patients.

Signaling Pathway

MLN8054

HY-10180

(MLN-8054; MLN 8054)

MLN8054

MLN8054 Chemical Structure

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.

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 In-stock
100 mg $819 In-stock
200 mg Get quote
500 mg Get quote
Size Price Stock Quantity
10 mM * 1 mL in DMSO €119 In-stock
5 mg €108 In-stock
10 mg €186 In-stock
50 mg €578 In-stock
100 mg €803 In-stock
200 mg Get quote
500 mg Get quote

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Product name: MLN8054
Cat. No.: HY-10180

MLN8054 Data Sheet

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    Purity: 98.25%

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Biological Activity of MLN8054

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].

Protocol (Extracted from published papers and Only for reference)

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Chemical Information

M.Wt 476.86 Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Formula C25H15ClF2N4O2
CAS No 869363-13-3
Solvent & Solubility

DMSO ≥90mg/mL Water <1.2mg/mL Ethanol <1.2mg/mL

Preparing Stock Solutions

1 mg 5 mg 10 mg
1 mM 2.0971 mL 10.4853 mL 20.9705 mL
5 mM 0.4194 mL 2.0971 mL 4.1941 mL
10 mM 0.2097 mL 1.0485 mL 2.0971 mL

References on MLN8054

Inhibitor Kit

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