MK8745
- CAS NO.:885325-71-3
- Empirical Formula: C20H19ClFN5OS
- Molecular Weight: 431.91
- MDL number: MFCD28009367
- SAFETY DATA SHEET (SDS)
- Update Date: 2024-11-01 20:20:38
What is MK8745?
The Uses of MK8745
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].
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.
Properties of MK8745
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 |
Safety information for MK8745
Signal word | Warning |
Pictogram(s) |
Exclamation Mark Irritant GHS07 |
GHS Hazard Statements |
H302:Acute toxicity,oral H315:Skin corrosion/irritation H319:Serious eye damage/eye irritation H335:Specific target organ toxicity, single exposure;Respiratory tract irritation |
Precautionary Statement Codes |
P261:Avoid breathing dust/fume/gas/mist/vapours/spray. P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing. |
Computed Descriptors for MK8745
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