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].

• 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.

• Shipping Conditions :

  Room Temperature

• Storage Conditions :

  -20°C, 3 years; 4°C, 2 years (Powder)

• Scientific Category :

  Reference compound1

• Clinical Information :

  No Development Reported