MK-8745 | CAS#885325-71-3 | Aurora A inhibitor

MedKoo Cat#: 406251 | Name: MK-8745

Description:

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

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

MK-8745

CAS#885325-71-3

Theoretical Analysis

MedKoo Cat#: 406251

Name: MK-8745

CAS#: 885325-71-3

Chemical Formula: C20H19ClFN5OS

Exact Mass: 431.0983

Molecular Weight: 431.91

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
100mg	USD 550.00	2 Weeks
200mg	USD 950.00	2 Weeks
500mg	USD 1,850.00	2 Weeks
1g	USD 2,950.00	2 Weeks
2g	USD 5,250.00	2 Weeks

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Related CAS #

No Data

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

Product Data

Instruction

View handling instruction

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

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

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

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.

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:

In vivo protocol:

TBD

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.