RO9021

SKU: orb1307784

Description

RO9021 is a potent and orally bioavailable small molecule inhibitor targeting spleen tyrosine kinase (SYK) with an average IC50 of 5.6 nM. It serves as a valuable research tool for investigating SYK-dependent signaling pathways in both cellular assays and in vivo models of immunology and oncology.

Research Area

Cardiovascular Research, Signal Transduction

Key Properties

• CAS Number: 1446790-62-0
• MW: 355.44
• Purity: 97.19% (May vary between batches)
• Formula: C₁₈H₂₅N₇O
• SMILES: Cc1ccc(Nc2cc(N[C@@H]3CCCC[C@@H]3N)nnc2C(N)=O)nc1C
• Target: Syk
• Solubility: DMSO:3 mg/mL (8.44 mM)

Bioactivity

• Target IC50:
  Syk:5.6 nM
• In Vitro:
  RO9021 effectively inhibits the anti-IgM induced phosphorylation of key signaling proteins including BTK, PLCγ2, AKT, and ERK, thereby demonstrating its capacity to block SYK kinase activity and consequently attenuate the B-cell receptor (BCR) downstream signaling cascade. This compound selectively targets B-cell receptor signaling, underscored by its role as a highly selective inhibitor of SYK. Its selectivity is evidenced by low S-scores of 0.003 for S(99) and 0.015 for S(90), indicating that among 392 kinases tested, SYK is the sole kinase significantly competed by RO9021 with 99% effectiveness. Moreover, RO9021 exhibits comparable inhibitory potency (IC50=22.8±1.7 nM) in assays measuring FcεR-mediated mast cell activation and degranulation, highlighting its broad potential in modulating immune responses .
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

inhibit, Inhibitor, RO9021, RO-9021, RO 9021, SYK, Syk, Spleen tyrosine kinase

Compound Identifiers

PubChem CID

71626896