KTX-951

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].

Product Specifications

CAS Number

[2573298-36-7]

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.