GLPBio

MK-8745

Catalog No.: GC10442Purity:>99.00%
COASDSData Sheet
Aurora A inhibitor,potent and selective

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

MK-8745
Cas No.: 885325-71-3
10mM (in 1mL DMSO)In Stock
$31.00
1
5mgIn Stock
$28.00
1
10mgIn Stock
$45.00
1
50mgIn Stock
$135.00
1
Tel: (909) 407-4943 / (909) 689-7124Email: sales@glpbio.com

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    610, 366–372 (2022)
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    Cell
    187(9):2288-2304 (2024)
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    183(7):1867-1883 (2020)
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Description

MK-8745 is a novel and selective inhibitor of Aurora A with IC50 value of 0.6 nM [1].

Aurora A kinase is a member of mitotic serine/threonine kinases and plays an important role in cellular division by controlling chromatid segregation. It has been reported that abnormal expression of Aurora A is correlated with the high occurrence of cancer and its expression determines cell sensitivity to MK-8745 treatment [1].

MK-8745 is a potent Aurora A inhibitor. When tested with p53-/+ cell lines, MK-8745 treatment induced apoptotic cell death in a p53-dependent manner through inhibiting Aurora A activity [1]. In non-Hodgkin lymphoma (NHL) cell lines, MK-8745 treatment arrested cell cycle in G2/M phase and induced cell death via inhibiting Aurora A kinase [2]. In HCT 116 Puma (-), HCT116 p21 (-), HCT116 Bax(-) and HCT116 Chk2(-) cell lines, MK-8745 treatment induced cell apoptosis with the percent of 25%, 22%, 25%, and 22%, respectively [3].

In female athymic nude mice model subcutaneous xenografted with HCT116 Puma (-), HCT116 p21 (-), HCT116 Bax(-) and HCT116 Chk2(-) cells, administration of MK-8745 significantly inhibited tumor growth [3].

References:
[1].  Nair, J.S., A.L. Ho, and G.K. Schwartz, The induction of polyploidy or apoptosis by the Aurora A kinase inhibitor MK8745 is p53-dependent. Cell Cycle, 2012. 11(4): p. 807-17.
[2].  Chowdhury, A., S. Chowdhury, and M.Y. Tsai, A novel Aurora kinase A inhibitor MK-8745 predicts TPX2 as a therapeutic biomarker in non-Hodgkin lymphoma cell lines. Leuk Lymphoma, 2012. 53(3): p. 462-71.
[3].   Shionome, Y., et al., Integrity of p53 associated pathways determines induction of apoptosis of tumor cells resistant to Aurora-A kinase inhibitors. PLoS One, 2013. 8(1): p. e55457.

Protocol

Cell experiment [1]:

Cell lines

Human non-Hodgkin lymphoma cell lines(NHL cell lines)

Preparation method

The solubility of this compound in DMSO is >21.6mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

1μM for 24 h and 48 h

Applications

In NHL cell lines, MK-8745 treatment for 48 h significantly decreased the cell number in TPX2 (targeting protein for Xenopus kinaselike protein 2) knockdown in cells in comparison to control cells. MK-8745 treatment induced an approximately 160-fold increase in cell death by 96 h and led to cell cycle arrest at the G2/M phase with accumulation of tetraploid nuclei followed by cell death in NHL cell lines.
Animal experiment [2]:

Animal models

Female athymic mice at the age of 4 to 5 weeks (HCT116 isogenic cells were transplanted into both flanks of mice)

Dosage form

s.c, 800 nM for 7 to 12 days.

Application

Xenograft experiments indicated that MK-8745 showed anti-tumor activity, however, it did not regress tumors completely, and drug-resistant tumors still remained in mice. Tumor growth of HCT116 Puma(-), HCT116 p21(-), HCT116 Bax(-) and HCT116 Chk2(-) cells was significantly inhibited with MK-8745 in female athymic mice.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Chowdhury, A., S. Chowdhury, M.Y., et al. Tsai, A novel Aurora kinase A inhibitor MK-8745 predicts TPX2 as a therapeutic biomarker in non-Hodgkin lymphoma cell lines. Leuk Lymphoma, 2012. 53(3): p. 462-71

[2]. Shionome, Y., et al. Integrity of p53 associated pathways determines induction of apoptosis of tumor cells resistant to Aurora-A kinase inhibitors. PLoS One, 2013. 8(1): p. e55457.

Product Documents

Purity:>99.00%Appearance:A solid
COASDSData Sheet

Chemical Properties

CAS No.
885325-71-3
Chemical Name
(3-chloro-2-fluorophenyl)(4-((6-(thiazol-2-ylamino)pyridin-2-yl)methyl)piperazin-1-yl)methanone
SMILES
ClC1=C(F)C(C(N2CCN(CC3=NC(NC4=NC=CS4)=CC=C3)CC2)=O)=CC=C1
Molecular Formula
C20H19ClFN5OS
Molecular Weight
431.91
Solubility
≥ 21.6mg/mL in DMSO
Storage
Store at -20° C
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.

CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility

g/mol

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