ca-4948-analog

Description: IRAK4-IN-7 (CA-4948 analog; AU-4948) is a novel, potent, selective, and orally active small molecule inhibitor of IRAK4 (interleukin-1 receptor-associated kinase 4) which has the potential to be used as a therapeutic agent for hematological cancers with dysregulated TLR/MYD88/IRAK4 signaling. CA-4948 has high in vivo activity in a TLR4-induced cytokine release model. 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. IRAK4 kinase activity is required for toll-like receptor (TLR) and interleukin-1 receptor (IL-1R) signaling in a variety of myeloid and lymphoid cell types. Recruitment of IRAK4 to these receptors and its subsequent activation is facilitated by the MYD88 adaptor protein, which is mutated in ca.22% of DLBCL cases.

References: AACR Annual Meeting 2017; April 1-5, 2017;

Related CAS #: 1801344-14-8 (CA-4948); 1801343-74-7 (CA-4948 analog)