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KTX-951

CAT: 0804-HY-148290-01Size: 1 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-148290-01Size:1 mg
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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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 ; Black: Linker (HY-W382009) ; Blue: CRBN Ligand Pomalidomide (HY-10984) ).
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.
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

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