Zimlovisertib

SKU: orb1296160

Description

Zimlovisertib (PF-06650833) is a potent, selective, and orally bioavailable IRAK4 inhibitor, demonstrating low nanomolar IC50 values in cellular assays. It is a valuable research tool for investigating IRAK4's role in oncology, autoimmune, and inflammatory diseases, with utility in both in vitro and in vivo experimental models.

Research Area

Immunology & Inflammation, Signal Transduction

Key Properties

• CAS Number: 1817626-54-2
• MW: 361.37
• Purity: 98.21% (May vary between batches)
• Formula: C₁₈H₂₀FN₃O₄
• SMILES: O(C[C@@H]1[C@H](CC)[C@H](F)C(=O)N1)C=2C3=C(C=C(C(N)=O)C(OC)=C3)C=CN2
• Target: IRAK
• Solubility: DMSO:150 mg/mL (415.09 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (11.07 mM)

Bioactivity

• Target IC50:
  IRAK4:0.2 nM
• In Vivo:
  PF06650833 (0.3-30 mg/kg; p.o; for 2.5 hours; male SD rats) treatment significantly inhibits LPS-induced TNF-α in a dose dependent manner. Mean exposures of PF06650833 in plasma are 2.1 nM, 7.7 nM, 19 nM and 150 nM free, respectively, at 2.5 hours after oral administration of PF06650833 at 0.3, 1, 3, and 30 mg/kg. The fraction unbound in rat plasma of PF06650833 is 0.3.
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• In Vitro:
  The kinome selectivity profile of PF06650833 (Compound 40) is assessed in a panel of 278 kinases at 200 nM inhibitor concentration using the ATP Km for each kinase. Approximately 100% inhibition is observed for IRAK4. Lactam PF06650833 is assessed in a whole-cell functional VEGF2R assay (PAE-KDR cell line). No activity is observed at concentrations up to and including 30 μM. In a voltage clamp assay, PF06650833 inhibits hERG current by 25% at 100 μM.
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• Animal Research:
  Animal Model: Male Sprague-Dawley rats. Dosage: 0.1 mg/kg, 1 mg/kg, 3 mg/kg, 30 mg/kg. Administration: Oral administration; for 2.5 hours

Storage & Handling

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

Alternative Names

Inhibitor, IRAK4, IRAK-4, IRAK, IL-1R associated kinase, Interleukin-1 receptor associated kinase, inhibit, Zimlovisertib, PF06650833, PF-06650833, PF 06650833

Compound Identifiers

PubChem CID

118414016