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ChemicalBook--->CAS DataBase List--->1446790-62-0

1446790-62-0

1446790-62-0 Structure

1446790-62-0 Structure
IdentificationBack Directory
[Name]

RO9021
[CAS]

1446790-62-0
[Synonyms]

RO9021
CS-2533
RO-0921;RO 0921
3-Pyridazinecarboxamide, 6-[[(1R,2S)-2-aminocyclohexyl]amino]-4-[(5,6-dimethyl-2-pyridinyl)amino]-
6-((1R,2S)-2-amino-cyclohexylamino)-4-(5,6-dimethyl-pyridin-2-ylamino)-pyridazine-3-carboxylic acid amide
[Molecular Formula]

C18H25N7O
[MDL Number]

MFCD28502091
[MOL File]

1446790-62-0.mol
[Molecular Weight]

355.44
Chemical PropertiesBack Directory
[Boiling point ]

618.5±55.0 °C(Predicted)
[density ]

1.288±0.06 g/cm3(Predicted)
[storage temp. ]

Store at -20°C
[solubility ]

Soluble in DMSO
[form ]

A solid
[pka]

14.25±0.50(Predicted)
[color ]

White to off-white
Spectrum DetailBack Directory
[Spectrum Detail]

RO9021(1446790-62-0)1HNMR
Hazard InformationBack Directory
[Biological Activity]

ro9021 is a syk inhibitor.spleen tyrosine kinase (syk) is identified as a critical integrator of intracellular signals regulated by activated immunoreceptors, such as fc receptors and bcell receptors (bcr), which are of great importantance for the function and development of lymphoid cells.
[in vitro]

previous study found that in addition to the suppression of bcell receptor signaling in human peripheral blood mononuclear cells and whole blood, fcγr signaling in human monocytes, and fc r signaling in human mast cells, ro9021 could also block the in vitro osteoclastogenesis from mouse bone marrow macrophages. moreover, the toll-like receptor 9 signaling in human bcells could be blocked by ro9021, leading to the decreased levels of plasmablasts, immunoglobulin (ig) g and igm upon b-cell differentiation. in addition, ro9021 could also potently inhibit type i interferon production by human plasmacytoid dendritic cells (pdc) via tlr9 activation, and such effect was found to be specific to tlr9 since ro9021 did not show inhibitary effect on tlr4- or jak-stat-mediated signaling [1].
[in vivo]

animal study showed that the oral administration of ro9021could significanly inhibit the arthritis progression in the mcia model, with well observed pharmacokinetics-pharmacodynamic correlation [1].
[IC 50]

5.6 nm
[References]

[1] liao c, et al. selective inhibition of spleen tyrosine kinase (syk) with a novel orally bioavailable small molecule inhibitor, ro9021, impinges on various innate and adaptive immune responses: implications for syk inhibitors in autoimmune disease therapy. arthritis res ther. 2013 oct 4;15(5):r146.
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