WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H130269
CAS#: 2432994-31-3
Description: KT-474, also known as KT-I-417 and SAR444656, is an orally bioavailable degrader of IRAK4. KT-474 is a heterobifunctional small-molecule degrader of IRAK4 composed of ligands to the E3 ligase cereblon (CRBN) and IRAK4 joined by a chemical linker. KT-474 forms a ternary complex with CRBN and IRAK4, leading to the ubiquitination and proteasomal degradation of IRAK4. KT-474 potently degraded IRAK4 in lymphocytes and monocytes with the half-maximal degradation concentration in the 1–2 nM range and a maximum degradation of 100%. KT-474 exhibited more potent and stronger downregulation of both R848 (TLR7/8)-induced and lipopolysaccharide (LPS: TLR4)-induced IL-6 and IL-8 production by PBMCs. KT-474 also blocked TLR9-mediated NF-κB activation by CpG-B in B cells, whereas PF-06550833 had no effect
Hodoodo Cat#: H130269
Name: KT-474
CAS#: 2432994-31-3
Chemical Formula: C44H49F2N11O6
Exact Mass: 865.38
Molecular Weight: 865.940
Elemental Analysis: C, 61.03; H, 5.70; F, 4.39; N, 17.79; O, 11.09
This product is not in stock, which may be available by custom synthesis.
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Synonym: KT-I-417; KT I 417; PROTAC IRAK4 degrader-7; SAR444656; SAR-444656; SAR 444656; KT-474; KT474; KT 474; KYM-001;
IUPAC/Chemical Name: 5-((1R,4R)-2-oxa-5-azabicyclo[2.2.1]heptan-5-yl)-N-(3-(difluoromethyl)-1-(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
InChi Key: NQGKNAVUMAHSQN-PKIOHZLWSA-N
InChi Code: InChI=1S/C44H49F2N11O6/c1-52-39-27(4-2-6-34(39)57(44(52)61)35-11-12-37(58)50-43(35)60)5-3-19-62-30-13-16-53(17-14-30)22-26-7-9-28(10-8-26)56-24-33(38(51-56)40(45)46)48-42(59)32-21-47-55-18-15-36(49-41(32)55)54-23-31-20-29(54)25-63-31/h2,4,6,15,18,21,24,26,28-31,35,40H,7-14,16-17,19-20,22-23,25H2,1H3,(H,48,59)(H,50,58,60)/t26?,28?,29-,31-,35?/m1/s1
SMILES Code: O=C(C1=C2N=C(N3[C@@]4([H])CO[C@@](C4)([H])C3)C=CN2N=C1)NC5=CN(C6CCC(CN7CCC(OCC#CC8=C(C(N9C(CC%10)C(NC%10=O)=O)=CC=C8)N(C)C9=O)CC7)CC6)N=C5C(F)F
Appearance: To be determined
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: To be determined
Shelf Life: >2 years if stored properly
Drug Formulation: To be determined
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
More Info:
| Biological target: | |
| In vitro activity: | |
| In vivo activity: |
The following data is based on the product molecular weight 865.94 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
| Formulation protocol: | |
| In vitro protocol: | |
| In vivo protocol: |
1. Mullard A. Targeted protein degraders crowd into the clinic. Nat Rev Drug Discov. 2021 Apr;20(4):247-250. doi: 10.1038/d41573-021-00052-4. PMID: 33737725.
