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CA-4948 is a selective, potent and orally active inhibitor of interleukin-1 receptor-associated kinase 4 (IRAK4) that regulates IRAK4 function in the TLR and IL-1R signaling cascades.
In vitro, CA-4948 blocked downstream NF-κB pathway signaling, including secretion of proinflammatory cytokines, in Toll-like receptor stimulated THP1 leukemic cells.
In vivo: CA-4948 exhibits favorable DMPK properties, oral bioavailability, and is well tolerated in mice. Furthermore, IRAK4-IN-7 was previously shown to exhibit dose-dependent efficacy in ABC-DLBCL MYD88-L265P xenograft tumor models using cell lines OCI-LY3 and OCI-Ly10 and patient-derived tumors. CA-4948 led to decreased viability of MDS/AML stem cells (CD34+/CD38-/Lin-ve) in vivo studies using a THP1 leukemia xenograft model in NSG mice.
Patent. US2023210833A1 2023 Jul 06.
Patent. US2023210833A1
CA-4948 purchased from AbMole
Patent. WO2021213287A1 2021 Oct 28.
Patent. WO2021213287A1
CA-4948 purchased from AbMole
| Cell Experiment | |
|---|---|
| Cell lines | |
| Preparation method | |
| Concentrations | |
| Incubation time | |
| Animal Experiment | |
|---|---|
| Animal models | SCID Beige mice |
| Formulation | |
| Dosages | 50 mg/kg |
| Administration | p.o. |
| Molecular Weight | 417.42 |
| Formula | C21H19N7O3 |
| CAS Number | 1801343-74-7 |
| Solubility (25°C) | DMSO ≥ 10 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related IRAK Products |
|---|
| AS 2444697
AS 2444697 is a potent and selective IRAK4 inhibitor. |
| Zimlovisertib
PF06650833 (Zimlovisertib) is an inhibitor of Interleukin-1 receptor associated kinase 4 (IRAK4). |
| IRAK-1-4 Inhibitor I
IRAK-1-4 Inhibitor I is an inhibitor of interleukin-1 receptor-associated kinase 1/4 (IRAK 1/4) with IC50s of 0.3 μM and 0.2 μM, respectively. |
| Zabedosertib
Zabedosertib (BAY 1834845) is a selective, orally potent IRAK4 inhibitor with immunomodulatory and anti-inflammatory activity and an IC50 value of 3.55 nM. Zabedosertib (BAY 1834845) exhibits anti-inflammatory property against IL-β, LPS and Imiquimod induced inflammation. |
| IRAK4-IN-4
IRAK4-IN-4 is an interleukin-1 receptor-associated kinase 4 (IRAK4) inhibitor with an IC50 of 2.8 nM. |
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