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Tyrosine Kinase/Adaptors PKA MLN8054

MLN8054

Catalog No. T6315   CAS 869363-13-3

MLN8054 is a potent and selective Aurora A kinase inhibitor with an IC50 of 4 nM.

MLN8054, CAS 869363-13-3
Pack Size Availability Price/USD Quantity
2 mg In stock 75.00
5 mg In stock 111.00
10 mg In stock 205.00
25 mg In stock 368.00
50 mg In stock 711.00
100 mg In stock 1043.00
1 mL * 10 mM (in DMSO) In stock 114.00
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Purity 98.26%
Purity 99.05%
Biological Description
Chemical Properties
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Description MLN8054 is a potent and selective Aurora A kinase inhibitor with an IC50 of 4 nM.
Targets&IC50 Aurora A : ic50 4nM ,   Aurora B : ic50 172nM ,   CK2 : ic50 20.5μM ,   Lck : ic50 3.2μM ,   PKA : ic50 19μM
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]
Kinase Assay Enzyme Assays : Recombinant murine Aurora A and Aurora B protein are expressed in Sf9 cells and purified with GST affinity chromatography. The peptide substrate for Aurora A is conjugated with biotin (Biotin-GLRRASLG). Aurora A kinase (5 nM) is assayed in 50 mM Hepes (pH 7.5)/10 mM MgCl2/5 mM DTT/0.05% Tween 20/2 μM peptide substrate/3.3 μCi/ml [γ-33P]ATP at 2 μM by using Image FlashPlates. Aurora B kinase (2 nM) is assayed with 10 μM biotinylated peptide Biotin-TKQTARKSTGGKAPR in 50 mM Tricine (pH 8.0)/2.5 mM MgCl2/5 mM DTT/10% glycerol/2% BSA/40 μCi/ml [γ-33P]ATP at 250 μM. The conditions for all other in vitro kinase assays are available upon request. MLN8054 is run in a 226 kinase screen at a 1 μM compound concentration with an ATP concentration of 10 μM for all assays.
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)
Cell lines: HCT-116, SW480, DLD-1, MCF-7, MDA-MB-231, Calu-6, H460, SKOV-3 and PC-3 cells
Animal Research
Animal Model: HCT-116 and PC-3 cells are injected s.c. into the right flank of nude mice.
Molecular Weight 476.86
Formula C25H15ClF2N4O2
CAS No. 869363-13-3

Storage

0-4℃ for short term (days to weeks), or -20℃ for long term (months).

Solubility Information

DMSO: 88 mg/mL (184.5 mM)

Ethanol: <1 mg/mL

Water: <1 mg/mL

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Solution 1

15% Captisol: 30 mg/mL

Citations

References and Literature
1. Manfredi MG, et al. Proc Natl Acad Sci U S A, 2007, 104(10), 4106-4111. 2. Moretti L, et al. Int J Radiat Oncol Biol Phys, 2011, 80(4), 1189-1197. 3. Huck JJ, et al. Mol Cancer Res, 2010, 8(3), 373-384.

Related compound libraries

This product is contained In the following compound libraries:
Bioactive Compound Library Inhibitor Library Anti-cancer Compound Library Clinical Compound Library Stem cell Differentiation Compound Library Autophagy Compound Library Epigenetics Compound Library DNA Damage & Repair Compound Library Kinase Inhibitor Library GPCR Compound Library Anti-cancer Clinical Compound Library Fluorochemical Library Anti-Metabolism Disease Compound Library Angiogenesis related Compound Library Preclinical Compound Library Cell cycle related Compound Library

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