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Chemical Structure| 2432994-31-3 Chemical Structure| 2432994-31-3

Structure of KT-474
CAS No.: 2432994-31-3

Chemical Structure| 2432994-31-3

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KT-474 is a PROTAC IRAK4 degrader that demonstrates significant antitumor effects by mediating anticancer signals through IRAK4 targeted degradation.

Synonyms: PROTAC IRAK4 degrader-7; KYM-001; SAR444656

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Product Details of KT-474

CAS No. :2432994-31-3
Formula : C44H49F2N11O6
M.W : 865.93
SMILES Code : O=C1N(C=2C(=C(C#CCOC3CCN(C[C@H]4CC[C@@H](CC4)N5C=C(NC(=O)C6=C7N(N=C6)C=CC(=N7)N8[C@@]9(C[C@](C8)(OC9)[H])[H])C(C(F)F)=N5)CC3)C=CC2)N1C)C%10C(=O)NC(=O)CC%10
Synonyms :
PROTAC IRAK4 degrader-7; KYM-001; SAR444656
MDL No. :N/A

Safety of KT-474

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319
Precautionary Statements:P501-P270-P264-P280-P302+P352-P337+P313-P305+P351+P338-P362+P364-P332+P313-P301+P312+P330

Related Pathways of KT-474

TLR

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
PBMCs 200 nM 16-24 hours To assess the degradation of IRAK4 in PBMCs. Results showed that KT-474 robustly decreased IRAK4 levels in all immune cell types. PMID: 39084489
Monocytes 500 nM 20 hours To assess the effect of KT-474 on IRAK4 degradation and cytokine production in monocytes. Results showed that KT-474 decreased IRAK4 protein levels and inhibited inflammatory cytokine production. PMID: 39084489
PBMCs 300 nM 24 hours To evaluate the degradation selectivity of KT-474 across the proteome. Results showed that IRAK4 was the only protein significantly downregulated. PMID: 39151120
PBMCs 300 nM 24 hours To assess the selectivity of KT-474 in human PBMCs. Results showed that KT-474 is selective for IRAK4. PMID: 37957373
PBMCs 1 nM (DC50), 30 nM (DC90) 24, 48, 72, 96 hours To assess IRAK4 degradation in PBMCs. Results showed maximal degradation of IRAK4 in PBMCs is achieved by 24 hours, with sustained degradation over 96 hours (Max. degradation ~90% compared to DMSO control). Emily Lurier etal.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice Imiquimod induced mouse model of psoriasis Oral 30 mg/kg and 100 mg/kg Twice a day for 3 days To assess the anti-inflammatory efficacy of 17 in an imiquimod-induced mouse model of psoriasis. Results showed potent anti-inflammatory efficacy, comparable to topical steroid administration. PMID: 39151120

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.15mL

0.23mL

0.12mL

5.77mL

1.15mL

0.58mL

11.55mL

2.31mL

1.15mL

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