KTX-951

• Description :

  KTX-951 is an orally active IRAK4 and IMiD (Ikaros/Aiolos) substrates PROTAC degrader (Kd = 3.5 nM) . KTX-951 has DC50s of 13 nM, 14 nM and 13 nM for IRAK4, Ikaros and Aiolos, respectively. KTX-951 has IC50 of 35 nM for OCl-Ly10 CTG. KTX-951 has antitumor activity. (Pink: IRAK4 ligand-12 (HY-48932) ; Black: Linker (HY-W382009) ; Blue: CRBN Ligand Pomalidomide (HY-10984) ) [1].

• UNSPSC :

  12352005

• Target :

  IRAK; PROTACs

• Type :

  Reference compound

• Related Pathways :

  Immunology/Inflammation; PROTAC

• Applications :

  Cancer-Kinase/protease

• Field of Research :

  Cancer

• Assay Protocol :

  https://www.medchemexpress.com/ktx-951.html

• Purity :

  98.03

• Solubility :

  DMSO : 50 mg/mL (ultrasonic)

• Smiles :

  FC(F)(C)C1=CC=CC(C(NC(C(OC)=CC2=N3)=CC2=CN3[C@H]4CC[C@@H](CC4)CN5CCC6(CC(CCNC7=C(C8=O)C(C(N8C(C(N9)=O)CCC9=O)=O)=CC=C7)C6)CC5)=O)=N1

• Molecular Formula :

  C46H52F2N8O6

• Molecular Weight :

  850.95

• References & Citations :

  [1]Walker D H, et al. Degraders targeting both IRAK4 and IMiD substrates show combinatorial effects leading to broader activity with durable and complete regressions in MYD88 mutant lymphoma xenografts in vivo. Cancer Research, 2020, 80 (16_Supplement) : 5222-5222.

• Shipping Conditions :

  Room Temperature

• Storage Conditions :

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

• Scientific Category :

  Reference compound1

• Clinical Information :

  No Development Reported

• Isoform :

  IRAK4

• CAS Number :

  [2573298-36-7]