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RO9021
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
RO9021图片
CAS NO:1446790-62-0
规格:≥98%
包装与价格:
包装价格(元)
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)355.44
FormulaC18H25N7O
CAS No.1446790-62-0
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 71 mg/mL (199.8 mM)
Water: <1 mg/mL
Ethanol: 10 mg/mL (28.1 mM)
Solubility (In vivo) O=C(C1=NN=C(N[C@H]2[C@@H](N)CCCC2)C=C1NC3=NC(C)=C(C)C=C3)N
Synonyms RO9021; RO 9021; RO-9021
实验参考方法
In Vitro

In vitro activity: RO9021 suppresses BCR signaling in human peripheral blood mononuclear cells (PBMC) and whole blood, FcγR signaling in human monocytes, and FcεR signaling in human mast cells and blocks osteoclastogenesis from mouse bone marrow macrophages in vitro. Toll-like Receptor(TLR) 9 signaling in human Bcells was inhibited by RO9021, resulting in decreased levels of plasmablasts, immunoglobulin (Ig)M and IgG upon B-cell differentiation. RO9021 also potently inhibited type I interferon production by human plasmacytoid dendritic cells (pDC) upon TLR9 activation. This effect is specific to TLR9 as RO9021 did not inhibit TLR4- or JAK-STAT-mediated signaling. RO9021 does not appreciably inhibit the JAK-STAT pathway.


Kinase Assay: 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.


Cell Assay: The human B-cell line, Ramos, was pretreated with 1 μM RO9021 prior to anti-IgM antibody-induced cross-linking of the BCR. The activation of various BCR signaling components was assessed by western blot using phosphospecific antibodies.

In VivoAnimal study showed that the oral administration of RO9021could significanly inhibit the arthritis progression in the mCIA model, with well observed pharmacokinetics-pharmacodynamic correlation.
Animal modelC57BL/6 and DBA/1J mice
Formulation & Dosage 5, 45 mg/kg daily; Oral gavage
References

Arthritis Res Ther. 2013 Oct 4;15(5):R146.