CA-4948

SKU: orb1298434

Description

CA-4948 (Emavusertib) is a small molecule inhibitor targeting IRAK4 and FLT3 kinases. It has demonstrated anti-tumor activity in preclinical research, showing efficacy in both in vitro cellular assays and in vivo models of hematological malignancies.

Research Area

Cardiovascular Research, Cell Biology, Immunology & Inflammation, Signal Transduction

Key Properties

• CAS Number: 1801344-14-8
• MW: 491.5
• Purity: 99.88% (May vary between batches)
• Formula: C₂₄H₂₅N₇O₅
• SMILES: Cc1cc(ccn1)-c1nc(co1)C(=O)Nc1cc2oc(nc2nc1N1CC[C@@H](O)C1)N1CCOCC1
• Target: IRAK,FLT,MyD88,Apoptosis,NF-κB
• Solubility: 10% DMSO+40% PEG300+5% Tween-80+45% Saline:2 mg/mL (4.07 mM);H2O:< 0.1 mg/mL (insoluble);DMSO:27.78 mg/mL (56.52 mM)

Bioactivity

• In Vitro:
  CA-4948, demonstrated good cellular activity in ABC DLBCL and AML cell lines. Inhibition of TLR signaling leading to decreased IL-6 levels was also observed in whole blood assays. CA-4948 demonstrated moderate to high selectivity in a panel of 329 kinases as well as exhibited desirable ADME and PK profiles including good oral bioavailability in mice, rat, and dog and showed >90% tumor growth inhibition in relevant tumor models with excellent correlation with in vivo PD modulation. CA-4948 was well tolerated in toxicity studies in both mouse and dog at efficacious exposure. The overall profile of CA-4948 prompted us to select it as a clinical candidate for evaluation in patients with relapsed or refractory hematologic malignancies including non-Hodgkin lymphoma and acute myeloid leukemia.
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Storage & Handling

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

Alternative Names

Cluster of differentiation antigen 135, CD135, CA 4948, CA-4948, CA4948, arthritis, Inhibitor, FLT3, Fms like tyrosine kinase 3, Emavusertib, Myd88, inhibit, IL-1R, IL-1R associated kinase, Interleukin-1 receptor associated kinase, IRAK, IRAK4, inflammation, lymphoma, rheumatoid, Toll

Compound Identifiers

PubChem CID

118224491