KT-474 (SAR444656, KYM-001) | IRAK4 PROTAC

Chemical Structure : KT-474

CAS No.: 2432994-31-3

KT-474 (SAR444656, KT474, KYM-001)

Catalog No.: PC-20693Not For Human Use, Lab Use Only.

KT-474 (SAR444656, KYM-001) is a potent, selective, and orally bioavailable heterobifunctional IRAK4 PROTAC degrader with DC50 of 2 nM in OCI-Ly10 cells, IC50 of 41 nM.

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2 mg	$128	In stock
5 mg	$218	In stock
10 mg	$348	In stock
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Biological Activity

KT-474 (SAR444656, KYM-001) is a potent, selective, and orally bioavailable heterobifunctional IRAK4 PROTAC degrader with DC50 of 2 nM in OCI-Ly10 cells, IC50 of 41 nM.

KT-474 potently degrades mouse, rat, canine, cynomologous, human IRAK4 with DC50 (nM)/Dmax (%) of 4.2/89 2.1/87 9.2/72 2.9/85 1.5/100, respectively.

KT-474 potently inhibited IL-8 release, with an IC50 = 3 nM and an Imax = 91%, in vitro following stimulation of PBMCs with the TLR7/8 agonist R848.

KT-474 (30-100 mg/kg, p.o. BID) is efficacious in an imiquimod mouse model.

Physicochemical Properties

M.Wt	865.94
Formula	C44H49F2N11O6
Appearance	Solid
CAS No.
Storage	Solide Powder -20°C 12 Months; 4°C 6 Months	In Solvent -80°C 6 Months; -20°C 6 Months
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	5-((1R,4R)-2-oxa-5-azabicyclo[2.2.1]heptan-5-yl)-N-(3-(difluoromethyl)-1-((1r,4R)-4-((4-((3-(1-((S)-2,6-dioxopiperidin-3-yl)-3-methyl-2-oxo-2,3-dihydro-1H-benzo[d]imidazol-4-yl)prop-2-yn-1-yl)oxy)piperidin-1-yl)methyl)cyclohexyl)-1H-pyrazol-4-yl)pyrazolo[1,5-a]pyrimidine-3-carboxamide

References

1. Ackerman L, et al. Nat Med. 2023 Dec;29(12):3127-3136.

KT-474 (SAR444656, KT474, KYM-001)

Biological Activity

Physicochemical Properties

References

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