KT-474 hydrochloride | IRAK4 PROTAC | Probechem Biochemicals

Chemical Structure : KT-474 hydrochloride

CAS No.: 2751703-31-6

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KT-474 hydrochloride (Tipasertideg, SAR444656, KYM-001)

货号: PC-28663Not For Human Use, Lab Use Only.

KT-474 hydrochloride (Tipasertideg, 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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10 mg	￥2480	In stock
25 mg	￥4280	In stock
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100 mg		Get quote

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生物&药学活性

KT-474 hydrochloride (Tipasertideg, 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.

物理化学性质&存储条件

分子量	902.40
分子式	C44H50ClF2N11O6
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
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-(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 hydrochloride

参考文献

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

KT-474 hydrochloride (Tipasertideg, SAR444656, KYM-001)

生物&药学活性

物理化学性质&存储条件

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KT-474 hydrochloride (Tipasertideg, SAR444656, KYM-001)

生物&药学活性

物理化学性质&存储条件

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