KTX-582

Names

[ CAS No. ]:
2573298-13-0

[ Name ]:
KTX-582

Biological Activity

[Description]:

KTX-582 is a potent IRAK4 degrader with DC50 values of 4 nM and 5 nM for IRAK4 and Ikaros, respectively. KTX-582 can induce apoptosis in MYD88MT DLBCL, and is efficient to induce in vivo tumor regressions in lymphoma model[1][2][3].

[Related Catalog]:

Signaling Pathways >> Apoptosis >> Apoptosis
Research Areas >> Cancer
Signaling Pathways >> Immunology/Inflammation >> IRAK
Signaling Pathways >> PROTAC >> PROTAC
Signaling Pathways >> Protein Tyrosine Kinase/RTK >> IRAK

[Target]

DC50: 4 nM (IRAK4), 5 nM (Ikaros)[1]


[In Vitro]

KTX-582 (compound I-41) degrades IRAK4 in whole blood monocyte and lymphocyte with IC50s of <0.05 μM[4]. KTX-582 (compound I-41) inhibits IRAK4 in human whole blood LPS TNFα with an IC50 of 0.05~1 μM[4].

[References]

[1]. Matthew Weiss. Discovery and characterization of IRAKIMiDs: degraders targeting both IRAK4 and IMiD substrates for oncology indications. Northeastern Section, ACS (NESACS).

[2]. Jennifer K. Lue, MD . Targeting MYD88-Mutant DLBCL with IRAKIMiDs: A Comparison to IRAK4 Kinase Inhibition and Evaluation of Synergy with Rational Combinations. American Society of Hematology ASH Annual Meeting

[3]. Nello Mainolfi, et al. Irak degraders and uses thereof. WO/2020/113233

Chemical & Physical Properties

[ Molecular Formula ]:
C45H51F3N8O7

[ Molecular Weight ]:
872.93

Related Compounds