| Identification | Back Directory | [Name]
MELK-8a | [CAS]
1922153-17-0 | [Synonyms]
MELK-8a
Piperazine, 1-methyl-4-[4-[4-[3-(4-piperidinylmethoxy)-4-pyridinyl]-1H-pyrazol-1-yl]phenyl]- | [Molecular Formula]
C25H32N6O | [MOL File]
1922153-17-0.mol | [Molecular Weight]
432.56 |
| Chemical Properties | Back Directory | [Boiling point ]
596.4±50.0 °C(Predicted) | [density ]
1.25±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO: 3 mg/mL (5.93 mM);Water: 22 mg/mL (43.52 mM);Ethanol: Insoluble | [form ]
Solid | [pka]
10.28±0.10(Predicted) | [color ]
Off-white to light yellow |
| Hazard Information | Back Directory | [Uses]
MELK-8a (NVS-MELK8a) is a highly potent and selective maternal embryonic leucine zipper kinase (MELK) inhibitor with IC50 of 2 nM. MELK-8a also inhibits Flt3 (ITD), Haspin, PDGFRα with IC50s of 0.18, 0.19, and 0.42 μM, respectively. MELK plays an essential role in regulating cell mitosis in a subset of cancer cells[1]. | [References]
[1] B Barry Touré, et al. Toward the Validation of Maternal Embryonic Leucine Zipper Kinase: Discovery, Optimization of Highly Potent and Selective Inhibitors, and Preliminary Biology Insight. J Med Chem. 2016 May 26;59(10):4711-23. DOI:10.1021/acs.jmedchem.6b00052 |
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