KTX-582

Modify Date: 2024-04-09 11:46:55

KTX-582 structure	Common Name	KTX-582
	CAS Number	2573298-13-0	Molecular Weight	872.93
	Density	N/A	Boiling Point	N/A
	Molecular Formula	C₄₅H₅₁F₃N₈O₇	Melting Point	N/A
	MSDS	N/A	Flash Point	N/A

Use of KTX-582

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

KTX-582

Use of KTX-582

Names

KTX-582 Biological Activity

Chemical & Physical Properties