| Identification | Back Directory | [Name]
2-Pyridinecarboxamide, 6-(1,1-difluoroethyl)-N-[2-[trans-4-[[2-[2-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]amino]ethyl]-7-azaspiro[3.5]non-7-yl]methyl]cyclohexyl]-6-methoxy-2H-indazol-5-yl]- | [CAS]
2573298-36-7 | [Synonyms]
KTX-951
2-Pyridinecarboxamide, 6-(1,1-difluoroethyl)-N-[2-[trans-4-[[2-[2-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]amino]ethyl]-7-azaspiro[3.5]non-7-yl]methyl]cyclohexyl]-6-methoxy-2H-indazol-5-yl]- | [Molecular Formula]
C46H52F2N8O6 | [MOL File]
2573298-36-7.mol | [Molecular Weight]
850.95 |
| Hazard Information | Back Directory | [Uses]
KTX-951 is an orally active IRAK4 and IMiD (Ikaros/Aiolos) substrates PROTAC degrader. KTX-951 has DC50 of 13 nM, 14 nM and 13 nM for IRAK4, Ikaros and Aiolos, respectively. TX-951 has antitumor activity.(Pink: IRAK4 ligand-12 (HY-48932); Black: Linker (HY-W382009); Blue: CRBN Ligand Pomalidomide (HY-10984))[1] | [in vivo]
KTX-951 (10 mg/kg；Oral administration) has an oral bioavailability (F%) of 22% and an AUC of 2.6 μM hr in rats[1].
KTX-951 (10 mg/kg；Oral administration) has an oral bioavailability (F%) of 57% in dogs[1]. | [IC 50]
IRAK4: 3.5 nM (Kd); IRAK4: 18 nM (DC50) | [References]
[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. |
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