RO9021

SKU: orb1218802

Description

RO9021 is an orally bioavailable, novel ATP-competitive SYK inhibitor (average IC50: 5.6 nM).

Key Properties

• CAS Number: 1446790-62-0
• MW: 355.44
• Purity: >98% (HPLC)
• Formula: C₁₈H₂₅N₇O
• SMILES: Cc(cc1)c(C)nc1Nc1cc(N[C@H](CCCC2)[C@H]2N)nnc1C(N)=O
• Target: Syk
• Solubility: DMSO:3 mg/mL (8.44 mM; Need ultrasonic)

Bioactivity

• In Vitro:
  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.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

Syk