CA-4948
Catalog No.S8562
Molecular Weight(MW): 417.42
CA-4948 is a reversible kinase inhibitor that modulates IRAK4 function in both the toll-like receptor (TLR) and interleukin 1 receptor (IL-1R) signaling cascades, and demonstrates pharmacodynamic and antitumor activity in in vitro and in vivo nonclinical models.
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Biological Activity
| Description | CA-4948 is a reversible kinase inhibitor that modulates IRAK4 function in both the toll-like receptor (TLR) and interleukin 1 receptor (IL-1R) signaling cascades, and demonstrates pharmacodynamic and antitumor activity in in vitro and in vivo nonclinical models. | |
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| In vitro |
In vitro, CA-4948 blocked downstream NF-κB pathway signaling, including secretion of proinflammatory cytokines, in Toll-like receptor stimulated THP1 leukemic cells[2]. |
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| In vivo | CA-4948 exhibits favorable DMPK properties, oral bioavailability, and is well tolerated in mice. Furthermore, CA-4948 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[1]. drug treatment 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[2]. |
Protocol
| Animal Research: |
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Solubility (25°C)
| In vitro | DMSO | 30 mg/mL (71.87 mM) |
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| Water | Insoluble | |
| Ethanol | Insoluble |
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Information
| Molecular Weight | 417.42 |
|---|---|
| Formula | C21H19N7O3 |
| CAS No. | 1801343-74-7 |
| Storage | powder |
| in solvent | |
| Synonyms | N/A |
Bio Calculators
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