MedKoo Biosciences

MK-8745
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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

MK-8745

CAS# 885325-71-3

Product data Instruction

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 Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

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:

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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.

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

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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.

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