KT-474

• Description:

  KT-474 (KYM-001; PROTAC IRAK4 degrader-7) is an orally active PROTAC IRAK4 degrader with anti-tumor effects. KT-474 inhibits the cell cycle and induces apoptosis. KT-474 induces tumor regression in a xenograft model of MYD88-mutated ABC DLBCL. KT-474 is a click chemistry reagent, containing an alkyne group, which can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing azide groups[1][2][3].

• Product Name Alternative:

  KYM-001; PROTAC IRAK4 degrader-7

• UNSPSC:

  12352005

• Hazard Statement:

  H302, H315, H319

• Target:

  Apoptosis; IRAK; PROTACs

• Type:

  Reference compound

• Related Pathways:

  Apoptosis; Immunology/Inflammation; PROTAC

• Applications:

  Cancer-Kinase/protease

• Field of Research:

  Cancer

• Assay Protocol:

  https://www.medchemexpress.com/kt-474.html

• Purity:

  99.77

• Solubility:

  DMSO : 100 mg/mL (ultrasonic)

• Smiles:

  O=C1N(C(CCC2=O)C(N2)=O)C3=CC=CC(C#CCOC(CC4)CCN4C[C@H]5CC[C@@](N(N=C6C(F)F)C=C6NC(C7=C(N=C(N8[C@@H](CO9)C[C@@H]9C8)C=C%10)N%10N=C7)=O)([H])CC5)=C3N1C

• Molecular Formula:

  C44H49F2N11O6

• Molecular Weight:

  865.93

• Precautions:

  H302, H315, H319

• References & Citations:

  [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.|[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.

• Shipping Conditions:

  Blue Ice

• Storage Conditions:

  -20°C, 3 years (Powder)

• Scientific Category:

  Reference compound1

• Clinical Information:

  Phase 1

• Isoform:

  IRAK4

• CAS Number:

  [2432994-31-3]