885325-71-3 Usage
Uses
Used in Pharmaceutical Industry:
MK8745 is used as an anticancer agent for its ability to selectively inhibit Aurora A kinase, leading to the induction of apoptotic cell death in cancer cells. This selective targeting makes it a promising candidate for the development of cancer therapies.
Used in Cancer Research:
MK8745 is used as a research tool for studying the role of Aurora A kinase in the regulation of cell division and its potential as a therapeutic target in various types of cancer. Its ability to induce apoptotic cell death in a p53-dependent manner makes it valuable for understanding the molecular mechanisms underlying cancer progression and the development of resistance to treatment.
Used in Drug Development:
MK8745 is used as a lead compound in the development of novel drugs targeting Aurora A kinase for the treatment of cancer. Its potent and selective inhibition of the kinase makes it a valuable starting point for the design and optimization of new therapeutic agents with improved efficacy and reduced side effects.
Biological Activity
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.
Check Digit Verification of cas no
The CAS Registry Mumber 885325-71-3 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 8,8,5,3,2 and 5 respectively; the second part has 2 digits, 7 and 1 respectively.
Calculate Digit Verification of CAS Registry Number 885325-71:
(8*8)+(7*8)+(6*5)+(5*3)+(4*2)+(3*5)+(2*7)+(1*1)=203
203 % 10 = 3
So 885325-71-3 is a valid CAS Registry Number.
885325-71-3Relevant articles and documents
NOVEL AMINOPYRIDINE DERIVATIVES HAVING AURORA A SELECTIVE INHIBITORY ACTION
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Page/Page column 27, (2008/06/13)
The present invention relates to a compound represented by the general formula (I): wherein Ra and Rb are each independently hydrogen atom or lower alkyl, or alternatively Ra and Rb are combined together to form -CH2 -; Rc is halogen atom; Rd is halogen a
