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KT474

Product Name: KT474
CAS No.: 2432994-31-3
Chemical Name: KT474
Synonyms: KT474;KT-I-417;SAR-444656;KT-474 (KYM-001);PROTAC IRAK4 degrader-7;JBJ-09-063 hydrochloride KT-474;N-[3-(Difluoromethyl)-1-[trans-4-[[4-[[3-[1-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-3-methyl-2-oxo-1H-benzimidazol-4-yl]-2-propyn-1-yl]oxy]-1-piperidinyl]methyl]cyclohexyl]-1H-pyrazol-4-yl]-5-(1R,4R)-2-;N-[3-(Difluoromethyl)-1-[trans-4-[[4-[[3-[1-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-3-methyl-2-oxo-1H-benzimidazol-4-yl]-2-propyn-1-yl]oxy]-1-piperidinyl]methyl]cyclohexyl]-1H-pyrazol-4-yl]-5-(1R,4R)-2-oxa-5-azabicyclo[2.2.1]hept-5-ylpyrazolo[1,5-a]pyrimidine-3-carboxamide;Pyrazolo[1,5-a]pyrimidine-3-carboxamide, N-[3-(difluoromethyl)-1-[trans-4-[[4-[[3-[1-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-3-methyl-2-oxo-1H-benzimidazol-4-yl]-2-propyn-1-yl]oxy]-1-piperidinyl]methyl]cyclohexyl]-1H-pyrazol-4-yl]-5-(1R,4R)-2-oxa-5-azabicyclo[2.2.1]hept-5-yl-;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
CBNumber: CB98515309
Molecular Formula: C44H49F2N11O6
Formula Weight: 865.93
MOL File: 2432994-31-3.mol

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KT474 Property

Density: 1.57±0.1 g/cm3(Predicted)
solubility: Acetonitrile: Slightly soluble: 0.1-1 mg/ml
DMSO: Sparingly soluble: 1-10 mg/ml
pka: 8.20±0.46(Predicted)
form: Solid
color: White to off-white
InChIKey: NQGKNAVUMAHSQN-KDRPOVOJSA-N
SMILES: C12=C(C(NC3=CN([C@@H]4CC[C@@H](CN5CCC(OCC#CC6=C7C(=CC=C6)N(C6CCC(=O)NC6=O)C(=O)N7C)CC5)CC4)N=C3C(F)F)=O)C=NN1C=CC(N1C[C@@]3([H])C[C@]1([H])CO3)=N2

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Hazard and Precautionary Statements (GHS)

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KT474 Chemical Properties,Usage,Production

Uses

KT-474 (KYM-001) is an orally active PROTAC IRAK4 degrader with antitumor activities[1]. KT-474 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

in vivo

KT-474 (p.o.) induces tumor regression in xenograft models of MYD88-mutant ABC DLBCL^[3].

IC 50

IRAK4

References

[1] Nello Mainolfi, et al. Irak degraders and uses thereof. Patent WO2020113233A1.
[2] Ackerman L, et al. IRAK4 degrader in hidradenitis suppurativa and atopic dermatitis: a phase 1 trial. Nat Med. 2023 Dec;29(12):3127-3136. DOI:10.1038/s41591-023-02635-7
[3] Joseph F. Kelleher, et al. Abstract LB-272: KYM-001, a first-in-class oral IRAK4 protein degrader, induces tumor regression in xenograft models of MYD88-mutant ABC DLBCL alone and in combination with BTK inhibition. Cancer Res (2019) 79 (13_Supplement): LB-272.
[4] ZHENG X, JI N, CAMPBELL V, et al. Discovery of KT-474─a Potent, Selective, and Orally Bioavailable IRAK4 Degrader for the Treatment of Autoimmune Diseases[J]. Journal of Medicinal Chemistry, 2024, 81 1. DOI: 10.1021/acs.jmedchem.4c01305

KT474 Preparation Products And Raw materials

Raw materials

Preparation Products

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View Lastest Price from KT474 manufacturers

Shanghai Joiny Pharmaceutical Co.,LTD

Product: KT474 2432994-31-3
Price: US $0.00/kg
Min. Order: 1kg
Purity: 98%
Supply Ability: 1000kg
Release date: 2025-11-12

2432994-31-3, KT474Related Search:

Pyrazolo[1,5-a]pyrimidine-5-carboxamide, 2-(3-cyanophenyl)-3-(2,6-dimethyl-4-pyridinyl)-N-[(1S)-2-hydroxy-1,2-dimethylpropyl]- Pyrazolo[1,5-a]pyridine-3-carboxamide (9CI) Pyrazolo[1,5-a]pyrimidine-5-carboxamide, 2-(3-cyanophenyl)-3-(2,6-dimethyl-4-pyridinyl)-N-[(1R)-2-hydroxy-1,2-dimethylpropyl]-

Pyrazolo[1,5-a]pyrimidine-3-carboxamide, N-[3-(difluoromethyl)-1-[trans-4-[[4-[[3-[1-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-3-methyl-2-oxo-1H-benzimidazol-4-yl]-2-propyn-1-yl]oxy]-1-piperidinyl]methyl]cyclohexyl]-1H-pyrazol-4-yl]-5-(1R,4R)-2-oxa-5-azabicyclo[2.2.1]hept-5-yl-

PROTAC IRAK4 degrader-7

KT-I-417

N-[3-(Difluoromethyl)-1-[trans-4-[[4-[[3-[1-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-3-methyl-2-oxo-1H-benzimidazol-4-yl]-2-propyn-1-yl]oxy]-1-piperidinyl]methyl]cyclohexyl]-1H-pyrazol-4-yl]-5-(1R,4R)-2-oxa-5-azabicyclo[2.2.1]hept-5-ylpyrazolo[1,5-a]pyrimidine-3-carboxamide

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

JBJ-09-063 hydrochloride KT-474

KT474

KT-474 (KYM-001)

SAR-444656

2432994-31-3

C44H49F2N11O6

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