| Identification | Back 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 Properties | Back 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 |
| Hazard Information | Back Directory | [Uses]
RO9021 is an orally bioavailable, novel ATP-competitive inhibitor of SYK, with an average IC50 of 5.6 nM. | [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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| Company Name: |
Musechem
|
| Tel: |
+1-800-259-7612 |
| Website: |
www.musechem.com |
| Company Name: |
Twochem Co.Ltd.
|
| Tel: |
021-58111628 15800915896 |
| Website: |
cn.twochem.com |
|