KT474 manufacturers
- KT474
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2025-11-19
- CAS:2432994-31-3
- Min. Order: 1kg
- Purity: 98%
- Supply Ability: 1000kg
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| Product Name: | KT474 | | Synonyms: | 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;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-;JBJ-09-063 hydrochloride
KT-474;KT474 | | CAS: | 2432994-31-3 | | MF: | C44H49F2N11O6 | | MW: | 865.93 | | EINECS: | | | Product Categories: | api | | Mol File: | 2432994-31-3.mol |  |
| | KT474 Chemical Properties |
| 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 |
| | KT474 Usage And Synthesis |
| 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 |
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