MLN8054 NEW
| Price | $48 | $65 | $81 |
| Package | 1mg | 2mg | 5mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-19 |
Product Details
| Product Name: MLN8054 | CAS No.: 869363-13-3 |
| Purity: 98.26% | Supply Ability: 10g |
| Release date: 2024/11/19 |
Product Introduction
Bioactivity
| Name | MLN8054 |
| Description | MLN8054 is a potent and selective Aurora A kinase inhibitor with an IC50 of 4 nM. |
| 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) |
| 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. |
| 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. [1] 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. [1] 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. [2] |
| 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. [1] 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. [3] |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | Ethanol : < 1 mg/mL (insoluble or slightly soluble) DMSO : 88 mg/mL (184.5 mM) H2O : < 1 mg/mL (insoluble or slightly soluble) |
| Keywords | inhibit | MLN-8054 | MLN8054 | Aurora Kinase | MLN 8054 | Inhibitor |
| Inhibitors Related | Nintedanib | Capivasertib | Vemurafenib | Acefylline | Staurosporine | 8-Bromo-cAMP sodium salt | Emodin | Ibrutinib | Dasatinib | Ponatinib | Palmatine | JAK1/2/3 Inhibitor 1 |
| Related Compound Libraries | Highly Selective Inhibitor Library | Bioactive Compound Library | Tyrosine Kinase Inhibitor Library | Kinase Inhibitor Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Bioactive Compounds Library Max | Anti-Cancer Drug Library | Anti-Cancer Active Compound Library |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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| Product name | Price | Suppliers | Update time | |
|---|---|---|---|---|
| $1980.00/50mg |
VIP1Y
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TargetMol Chemicals Inc.
|
2024-10-23 |
United States- Since: 2011-01-07
- Address: 36?Washington?Street, Wellesley?Hills
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