WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 406251
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. )
MedKoo Cat#: 406251
Chemical Formula: C20H19ClFN5OS
Exact Mass: 431.09829
Molecular Weight: 431.91416
Elemental Analysis: C, 55.62; H, 4.43; Cl, 8.21; F, 4.40; N, 16.21; O, 3.70; S, 7.42
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
The following data is based on the product molecular weight 431.91416 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|
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.