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Synonyms: AU-4948 | AU4948 | CA4948 | example 1 [WO2015104688A1]
Compound class: Synthetic organic
Comment: CA-4948 is an orally available, reversible inhibitor of interleukin 1 receptor associated kinase 4 (IRAK4) . It downmodulates the IRAK4 kinase activity that is required for toll-like receptor (TLR) and interleukin-1 receptor (IL-1R) signaling in a variety of myeloid and lymphoid cell types, notably in cancer cells (e.g. diffuse large B-cell lymphoma cells) in which the MYD88 adaptor protein carries an activating mutation (MYD88L265P) . In such mutant cells NF-κB signaling is constitutively active and this is indicative of a poorer prognosis. Hence, IRAK4 inhibitors such as CA-4948 are expected to provide clinical benefit in MYD88 mutation +ve hematological cancers.
Although not formally disclosed in a peer-reviewed publication, the structure presented here is that claimed as Example 1 in Aurigene Discovery Technologies' IRAK4 inhibitor patent WO2015104688A1 . Data presented in scientific meeting abstract form indicates that CA-4948 demonstrates preclinical antitumour activity in in vitro and in vivo models .
|Compound class||Synthetic organic|
|AU-4948 | AU4948 | CA4948 | example 1 [WO2015104688A1]|
|GtoPdb PubChem SID||381118862|
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