For research use only. Not for therapeutic Use.
RO9021 is an orally bioavailable, novel ATP-competitive inhibitor of SYK, with an average IC50 of 5.6 nM.
RO9021 is a highly selective SYK inhibitor with low S-scores of 0.003 for S(99) and 0.015 for S(90), indicating that SYK is the only kinase with 99% competition with RO9021 in a total of 392 tested kinases. RO9021 inhibits anti-IgM induced phosphorylation of BTK, PLCγ2, AKT and ERK, indicating that blockade of SYK kinase activity by RO9021 results in attenuation of BCR downstream signaling cascade. RO9021 selectively suppresses B-cell receptor signaling. RO9021 also displays a similar inhibitory potency (IC50=22.8±1.7 nM) in a FcεR-mediated mast cell activation and degranulation assay[1].
| Catalog Number | I001722 |
| CAS Number | 1446790-62-0 |
| Synonyms | 6-[[(1R,2S)-2-aminocyclohexyl]amino]-4-[(5,6-dimethylpyridin-2-yl)amino]pyridazine-3-carboxamide |
| Molecular Formula | C18H25N7O |
| Purity | ≥95% |
| InChI | InChI=1S/C18H25N7O/c1-10-7-8-15(21-11(10)2)23-14-9-16(24-25-17(14)18(20)26)22-13-6-4-3-5-12(13)19/h7-9,12-13H,3-6,19H2,1-2H3,(H2,20,26)(H2,21,22,23,24)/t12-,13+/m0/s1 |
| InChIKey | XJZVCDVZCRLIKN-QWHCGFSZSA-N |
| SMILES | CC1=C(N=C(C=C1)NC2=CC(=NN=C2C(=O)N)NC3CCCCC3N)C |
| Reference | [1]. Cheng Liao, 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. [2]. 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. |
