2573298-13-0

2573298-13-0 structure

Name: KTX-582
Chemical Name: KTX-582
CAS Number: 2573298-13-0
Molecular Formula: C₄₅H₅₁F₃N₈O₇
Molecular Weight: 872.93
Catalog: Signaling Pathways Apoptosis Apoptosis
Create Date: 2022-11-21 18:35:02
Modify Date: 2024-04-09 11:46:55
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].

Name	KTX-582

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

Molecular Formula	C₄₅H₅₁F₃N₈O₇
Molecular Weight	872.93