RO9021

Catalog No.S7286 Batch:S728602

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Technical Data

Formula

C18H25N7O
Molecular Weight 355.44 CAS No. 1446790-62-0
Solubility (25°C)* In vitro DMSO 71 mg/mL (199.75 mM)
Ethanol 18 mg/mL (50.64 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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 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].
In vivo Oral administration of RO9021 inhibits arthritis progression in the mCIA model[1].

Protocol (from reference)

Cell Assay:

[1]
  • 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.
Animal Study:

[1]
  • Animal Models

    C57BL/6 and DBA/1J adult mice

  • Dosages

    5 and 45 mg/kg daily

  • Administration

    oral administration

Selleck's RO9021 has been cited by 1 publication

Heterogeneity of Patient-Derived Acute Myeloid Leukemia Cells Subjected to SYK In Vitro Inhibition [ Int J Mol Sci, 2022, 23(23)14706] PubMed: 36499034

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.