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].

Product Specifications

CAS Number

[2573298-13-0]

UNSPSC

12352005

Target

Apoptosis; IRAK; PROTACs

Type

Reference compound

Related Pathways

Apoptosis; Immunology/Inflammation; PROTAC

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/ktx-582.html

Purity

98.77

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

O=C(C1=NC(C(F)(F)F)=CC=C1)NC2=CC3=CN([C@H]4CC[C@H](CN(CCCO[C@H]5C[C@H](NC6=CC=CC(C(N7C(CC8)C(NC8=O)=O)=O)=C6C7=O)C5)C)CC4)N=C3C=C2C(C)(O)C

Molecular Formula

C45H51F3N8O7

Molecular Weight

872.93

References & Citations

[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|[4]Vogelmann A, Robaa D, Sippl W, Jung M. Proteolysis targeting chimeras (PROTACs) for epigenetics research. Curr Opin Chem Biol. 2020 Aug;57:8-16.