8-[(trans-4-Aminocyclohexyl)methyl]-6-[2-chloro-4-(3-fluoro-2-pyridinyl)phenyl]-2-(methylamino)pyrido[2,3-d]pyrimidin-7(8H)-one

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8-[(trans-4-Aminocyclohexyl)methyl]-6-[2-chloro-4-(3-fluoro-2-pyridinyl)phenyl]-2-(methylamino)pyrido[2,3-d]pyrimidin-7(8H)-one Basic information
Product 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
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;Pyrido[2,3-d]pyrimidin-7(8H)-one, 8-[(trans-4-aminocyclohexyl)methyl]-6-[2-chloro-4-(3-fluoro-2-pyridinyl)phenyl]-2-(methylamino)-
CAS:2750707-05-0
MF:C24H22ClFN6O3
MW:496.92
EINECS:
Product Categories:
Mol File:2750707-05-0.mol
8-[(trans-4-Aminocyclohexyl)methyl]-6-[2-chloro-4-(3-fluoro-2-pyridinyl)phenyl]-2-(methylamino)pyrido[2,3-d]pyrimidin-7(8H)-one Structure
8-[(trans-4-Aminocyclohexyl)methyl]-6-[2-chloro-4-(3-fluoro-2-pyridinyl)phenyl]-2-(methylamino)pyrido[2,3-d]pyrimidin-7(8H)-one Chemical Properties
Boiling point 676.6±65.0 °C(Predicted)
density 1.421±0.06 g/cm3(Temp: 20 °C; Press: 760 Torr)(Predicted)
pka6.86±0.40(Predicted)
form Solid
color White to off-white
Safety Information
MSDS Information
8-[(trans-4-Aminocyclohexyl)methyl]-6-[2-chloro-4-(3-fluoro-2-pyridinyl)phenyl]-2-(methylamino)pyrido[2,3-d]pyrimidin-7(8H)-one Usage And Synthesis
UsesMRIA9 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 50SIK1; 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.
8-[(trans-4-Aminocyclohexyl)methyl]-6-[2-chloro-4-(3-fluoro-2-pyridinyl)phenyl]-2-(methylamino)pyrido[2,3-d]pyrimidin-7(8H)-one Preparation Products And Raw materials
Tag:8-[(trans-4-Aminocyclohexyl)methyl]-6-[2-chloro-4-(3-fluoro-2-pyridinyl)phenyl]-2-(methylamino)pyrido[2,3-d]pyrimidin-7(8H)-one(2750707-05-0) Related Product Information
G-5555 8-[(trans-4-Aminocyclohexyl)methyl]-6-[2-chloro-4-(3-fluoro-2-pyridinyl)phenyl]-2-(methylamino)pyrido[2,3-d]pyrimidin-7(8H)-one Pyrido[2,3-d]pyrimidin-7(8H)-one, 8-[(trans-5-amino-1,3-dioxan-2-yl)methyl]-6-[2-chloro-4-(6-methyl-2-pyridinyl)phenyl]-2-(methylamino)-, hydrochloride (1:1) Doxorubicin hydrochloride Ruxolitinib 2-Deoxy-D-glucose