Home Angiogenesis Syk inhibitor RO9021 For research use only.

RO9021

RO9021 potently inhibits SYK kinase activity with an average IC50 of 5.6 nM and suppresses B-cell receptor signaling.

RO9021 Chemical Structure

RO9021 Chemical Structure

CAS: 1446790-62-0

Selleck's RO9021 has been cited by 1 publication

Purity & Quality Control

Batch: Purity: 99.43%
99.43

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Signaling Pathway

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Syk Signaling Pathway

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Biological Activity

Description RO9021 potently inhibits SYK kinase activity with an average IC50 of 5.6 nM and suppresses B-cell receptor signaling.
Targets
Syk [1]
(Cell-free assay)
5.6 nM
In vitro
In vitro 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[1].
Cell Research Cell lines Human B-cell line, Ramos
Concentrations 1 μM
Incubation Time 5 or 15 min
Method

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 Vivo
In vivo Oral administration of RO9021 inhibits arthritis progression in the mCIA model[1].
Animal Research Animal Models C57BL/6 and DBA/1J adult mice
Dosages 5 and 45 mg/kg daily
Administration oral administration

Chemical Information & Solubility

Molecular Weight 355.44 Formula

C18H25N7O
CAS No. 1446790-62-0 SDF Download RO9021 SDF
Smiles CC1=C(N=C(C=C1)NC2=CC(=NN=C2C(=O)N)NC3CCCCC3N)C
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 71 mg/mL ( (199.75 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 18 mg/mL

Water : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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