MK-8745
featured

    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 406251

CAS#: 885325-71-3

Description: MK-8745 is a novel Aurora-A specific inhibitor. MK8745 induced apoptotic cell death in a p53-dependent manner when tested in vitro in cell lines of multiple lineages. Exposure of p53 wild-type cells to MK8745 resulted in the induction of p53 phosphorylation (ser15) and an increase in p53 protein expression. p53-dependent apoptosis by MK8745 was further confirmed in HCT 116 p53(-/-) cells transfected with wild-type p53. (source: Cell Cycle. 2012 Feb 15;11(4):807-17. )


Chemical Structure

img
MK-8745
CAS# 885325-71-3

Theoretical Analysis

MedKoo Cat#: 406251
Name: MK-8745
CAS#: 885325-71-3
Chemical Formula: C20H19ClFN5OS
Exact Mass: 431.10
Molecular Weight: 431.914
Elemental Analysis: C, 55.62; H, 4.43; Cl, 8.21; F, 4.40; N, 16.21; O, 3.70; S, 7.42

Price and Availability

Size Price Availability Quantity
100mg USD 550
200mg USD 950
500mg USD 1850
1g USD 2950
2g USD 5250
Bulk inquiry

Synonym: MK-8745; MK 8745; MK8745.

IUPAC/Chemical Name: (3-chloro-2-fluorophenyl)(4-((6-(thiazol-2-ylamino)pyridin-2-yl)methyl)piperazin-1-yl)methanone.

InChi Key: YCRFPWKUUNKNDN-UHFFFAOYSA-N

InChi Code: InChI=1S/C20H19ClFN5OS/c21-16-5-2-4-15(18(16)22)19(28)27-10-8-26(9-11-27)13-14-3-1-6-17(24-14)25-20-23-7-12-29-20/h1-7,12H,8-11,13H2,(H,23,24,25)

SMILES Code: O=C(C1=CC=CC(Cl)=C1F)N2CCN(CC3=NC(NC4=NC=CS4)=CC=C3)CC2

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:         

Product Data:
Biological target: MK-8745 is an aurora A kinase inhibitor with an IC50 of 0.6 nM.
In vitro activity: This study demonstrates that treatment with MK-8745, a novel Aurora-A specific inhibitor, leads to cell cycle arrest at the G2/M phase with accumulation of tetraploid nuclei followed by cell death in non-Hodgkin lymphoma (NHL) cell lines. The sensitivity of the cell lines to MK-8745 is correlated with the expression level of Aurora-A activator. The siRNA knockdown of Aurora-A activator TPX2 (targeting protein for Xenopus kinase-like protein 2) increased MK-8745 sensitivity in less-MK-8745-sensitive NHL cell lines, whereas overexpression of TPX2 in high-MK-8745-sensitive NHL cell lines increased drug resistance. Reference: Leuk Lymphoma. 2012 Mar;53(3):462-71. https://pubmed.ncbi.nlm.nih.gov/21879811/
In vivo activity: TBD

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 68.7 158.98
Ethanol 1.0 2.32

Preparing Stock Solutions

The following data is based on the product molecular weight 431.91 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol: 1. Chowdhury A, Chowdhury S, Tsai MY. A novel Aurora kinase A inhibitor MK-8745 predicts TPX2 as a therapeutic biomarker in non-Hodgkin lymphoma cell lines. Leuk Lymphoma. 2012 Mar;53(3):462-71. doi: 10.3109/10428194.2011.619018. Epub 2011 Oct 24. PMID: 21879811. 2. Nair JS, Ho AL, Schwartz GK. The induction of polyploidy or apoptosis by the Aurora A kinase inhibitor MK8745 is p53-dependent. Cell Cycle. 2012 Feb 15;11(4):807-17. doi: 10.4161/cc.11.4.19323. Epub 2012 Feb 15. PMID: 22293494; PMCID: PMC3318110.
In vitro protocol: 1. Chowdhury A, Chowdhury S, Tsai MY. A novel Aurora kinase A inhibitor MK-8745 predicts TPX2 as a therapeutic biomarker in non-Hodgkin lymphoma cell lines. Leuk Lymphoma. 2012 Mar;53(3):462-71. doi: 10.3109/10428194.2011.619018. Epub 2011 Oct 24. PMID: 21879811. 2. Nair JS, Ho AL, Schwartz GK. The induction of polyploidy or apoptosis by the Aurora A kinase inhibitor MK8745 is p53-dependent. Cell Cycle. 2012 Feb 15;11(4):807-17. doi: 10.4161/cc.11.4.19323. Epub 2012 Feb 15. PMID: 22293494; PMCID: PMC3318110.
In vivo protocol: TBD

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.
=
x
x
g/mol

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / CoA (available online).

Reconstitution Calculator

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

=
÷

Dilution Calculator

Calculate the dilution required to prepare a stock solution.
x
=
x

1: Shionome Y, Yan L, Liu S, Saeki T, Ouchi T. Integrity of p53 associated pathways determines induction of apoptosis of tumor cells resistant to Aurora-A kinase inhibitors. PLoS One. 2013;8(1):e55457. doi: 10.1371/journal.pone.0055457. Epub 2013 Jan 31. PubMed PMID: 23383195; PubMed Central PMCID: PMC3561291.

2: Nair JS, Ho AL, Schwartz GK. The induction of polyploidy or apoptosis by the Aurora A kinase inhibitor MK8745 is p53-dependent. Cell Cycle. 2012 Feb 15;11(4):807-17. doi: 10.4161/cc.11.4.19323. Epub 2012 Feb 15. PubMed PMID: 22293494; PubMed Central PMCID: PMC3318110.

3: Chowdhury A, Chowdhury S, Tsai MY. A novel Aurora kinase A inhibitor MK-8745 predicts TPX2 as a therapeutic biomarker in non-Hodgkin lymphoma cell lines. Leuk Lymphoma. 2012 Mar;53(3):462-71. doi: 10.3109/10428194.2011.619018. Epub 2011 Oct 24. PubMed PMID: 21879811.