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]-

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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]- Suppliers list
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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]- Basic information
Product 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]-
Synonyms: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]-;KTX-951;6-(1,1-difluoroethyl)-N-{6-methoxy-2-[(1r,4r)-4-{[2-(2-{[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxo-2,3-dihydro-1H-isoindol-4-yl]amino}ethyl)-7-azaspiro[3.5]nonan-7-yl]methyl}cyclohexyl]-2H-indazol-5-yl}pyridine-2-carboxamide;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]-2-pyridinecarboxamide
CAS:2573298-36-7
MF:C46H52F2N8O6
MW:850.95
EINECS:
Product Categories:
Mol File:2573298-36-7.mol
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]- Structure
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]- Chemical Properties
density 1.47±0.1 g/cm3(Predicted)
pka10.75±0.40(Predicted)
form Solid
color Light yellow to yellow
Safety Information
MSDS Information
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]- Usage And Synthesis
UsesKTX-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 50IRAK4: 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.
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]- Preparation Products And Raw materials
Tag: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]-(2573298-36-7) Related Product Information
INDEX NAME NOT YET ASSIGNED 2-Pyridinecarboxamide, N-[2-[trans-4-[[2-[[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]amino]methyl]-7-azaspiro[3.5]non-7-yl]methyl]cyclohexyl]-6-(1-hydroxy-1-methylethyl)-2H-indazol-5-yl]-6-(trifluoromethyl)- 2-Pyridinecarboxamide, N-[2-[trans-4-[[2-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]amino]-7-azaspiro[3.5]non-7-yl]methyl]cyclohexyl]-6-(1-hydroxy-1-methylethyl)-2H-indazol-5-yl]-6-(trifluoromethyl)- INDEX NAME NOT YET ASSIGNED 2-Pyridinecarboxamide, N-[2-[trans-4-[[[3-[[trans-3-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]amino]cyclobutyl]oxy]propyl]methylamino]methyl]cyclohexyl]-6-(1-hydroxy-1-methylethyl)-2H-indazol-5-yl]-6-(trifluoromethyl)- 2-Pyridinecarboxamide, N-[2-[trans-4-[[4-[[trans-3-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]amino]cyclobutyl]oxy]-1-piperidinyl]methyl]cyclohexyl]-6-(1-hydroxy-1-methylethyl)-2H-indazol-5-yl]-6-(trifluoromethyl)-