2573298-13-0
Chemical Structure
KTX-582
- CAS No.: 2573298-13-0
- Formula:C45H51F3N8O7
- Molecular Weight:872.93
IUPAC Name: N-(2-((1R,4r)-4-(((3-((1r,3R)-3-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)amino)cyclobutoxy)propyl)(methyl)amino)methyl)cyclohexyl)-6-(2-hydroxypropan-2-yl)-2H-indazol-5-yl)-6-(trifluoromethyl)picolinamide
InChIKey: CKFOAVDINFHZIR-IQDGXFAKSA-N
SMILES: O=C(C1=NC(C(F)(F)F)=CC=C1)NC2=CC3=CN([C@H]4CC[C@H](CN(CCCO[C@H]5C[C@H](NC6=CC=CC(C(N7C(CC8)C(NC8=O)=O)=O)=C6C7=O)C5)C)CC4)N=C3C=C2C(C)(O)C
Biological Activity: KTX-582 is a potent IRAK4 degrader with DC50 values of 4 nM and 5 nM for IRAK4 and Ikaros, respectively. KTX-582 can induce apoptosis in MYD88MT DLBCL, and is efficient to induce in vivo tumor regressions in lymphoma model[1][2][3].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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KTX-582 | 98.65% | KTX-582 is a potent IRAK4 degrader with DC50 values of 4 nM and 5 nM for IRAK4 and Ikaros, respectively. KTX-582 can induce apoptosis in MYD88MT DLBCL, and is efficient to induce in vivo tumor regressions in lymphoma model. | ||||||||||||||||||||
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References
- [1]. Matthew Weiss. Discovery and characterization of IRAKIMiDs: degraders targeting both IRAK4 and IMiD substrates for oncology indications. Northeastern Section, ACS (NESACS).
- [2]. Jennifer K. Lue, MD . Targeting MYD88-Mutant DLBCL with IRAKIMiDs: A Comparison to IRAK4 Kinase Inhibition and Evaluation of Synergy with Rational Combinations. American Society of Hematology ASH Annual Meeting
- [3]. Vogelmann A, Robaa D, Sippl W, Jung M. Proteolysis targeting chimeras (PROTACs) for epigenetics research. Curr Opin Chem Biol. 2020 Aug;57:8-16. [Content Brief]
