| Identification | Back Directory | [Name]
8-[(trans-4-Aminocyclohexyl)methyl]-6-[2-chloro-4-(3-fluoro-2-pyridinyl)phenyl]-2-(methylamino)pyrido[2,3-d]pyrimidin-7(8H)-one | [CAS]
2750707-05-0 | [Synonyms]
8-[(trans-4-Aminocyclohexyl)methyl]-6-[2-chloro-4-(3-fluoro-2-pyridinyl)phenyl]-2-(methylamino)pyrido[2,3-d]pyrimidin-7(8H)-one | [Molecular Formula]
C24H22ClFN6O3 | [MOL File]
2750707-05-0.mol | [Molecular Weight]
496.92 |
| Chemical Properties | Back Directory | [Boiling point ]
676.6±65.0 °C(Predicted) | [density ]
1.421±0.06 g/cm3(Temp: 20 °C; Press: 760 Torr)(Predicted) | [form ]
Solid | [pka]
6.86±0.40(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
MRIA9 is an ATP-competitive, pan Salt-Inducible kinase (SIK) and PAK2/3 inhibitor, with IC50 values of 516 nM, 180 nM and 127 nM for SIK1, SIK2 and SIK3, respectively[1]. | [in vivo]
MRIA9 shows high oral bioavailability (F = 75-80%)[1].
| [IC 50]
SIK1; SIK2; SIK3 | [References]
[1] Roberta Tesch, et al. Structure-Based Design of Selective Salt-Inducible Kinase Inhibitors. J Med Chem. 2021 Jun 24;64(12):8142-8160. DOI:10.1021/acs.jmedchem.0c02144
[2] Monika Raab, et al. The Small-Molecule Inhibitor MRIA9 Reveals Novel Insights into the Cell Cycle Roles of SIK2 in Ovarian Cancer Cells. Cancers 2021, 13(15), 3658. |
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