| Identification | Back Directory | [Name]
MK8745 | [CAS]
885325-71-3 | [Synonyms]
MK8745
CS-1904
MK8745 USP/EP/BP
6-[[4-(3-Chloro-2-fluorobenzoyl)piperazin-1-yl]methyl]-N-(thiazol-2-yl)pyridin-2-amine
(3-Chloro-2-fluorophenyl)(4-((6-(thiazol-2-ylamino)pyridin-2-yl)methyl)piperazin-1-yl)methanon
Methanone, (3-chloro-2-fluorophenyl)[4-[[6-(2-thiazolylamino)-2-pyridinyl]methyl]-1-piperazinyl]-
(3-chloro-2-fluorophenyl)(4-((6-(thiazol-2-ylamino)pyridin-2-yl)methyl)piperazin-1-yl)methanone. MK-8745 | [Molecular Formula]
C20 H19 Cl F N5 O S | [MDL Number]
MFCD28009367 | [MOL File]
885325-71-3.mol | [Molecular Weight]
431.91 |
| Chemical Properties | Back Directory | [Melting point ]
177-179°C | [Boiling point ]
605.5±65.0 °C(Predicted) | [density ]
1.430±0.06 g/cm3(Predicted) | [storage temp. ]
Refrigerator | [solubility ]
DMSO (Slightly), Methanol (Slightly, Heated) | [form ]
Solid | [pka]
5.20±0.10(Predicted) | [color ]
Off-White |
| Hazard Information | Back Directory | [Uses]
MK-8745 is a potent and selective Aurora A kinase inhibitor that induces apoptotic cell death in a p53-dependent manner when tested in vitro in cell lines of multiple lineages. | [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]. | [target]
Aurora A | [IC 50]
Aurora A: 0.6 nM (IC50) | [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. |
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