| Identification | Back Directory | [Name]
2-Pyridinecarboxamide, N-[2-[trans-4-[[[3-[[trans-3-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]amino]cyclobutyl]oxy]propyl]methylamino]methyl]cyclohexyl]-6-(1-hydroxy-1-methylethyl)-2H-indazol-5-yl]-6-(trifluoromethyl)- | [CAS]
2573298-13-0 | [Synonyms]
KTX-582
2-Pyridinecarboxamide, N-[2-[trans-4-[[[3-[[trans-3-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]amino]cyclobutyl]oxy]propyl]methylamino]methyl]cyclohexyl]-6-(1-hydroxy-1-methylethyl)-2H-indazol-5-yl]-6-(trifluoromethyl)- | [Molecular Formula]
C45H51F3N8O7 | [MOL File]
2573298-13-0.mol | [Molecular Weight]
872.93 |
| Chemical Properties | Back Directory | [Boiling point ]
952.8±65.0 °C(Predicted) | [density ]
1.48±0.1 g/cm3(Predicted) | [form ]
Solid | [pka]
10.77±0.40(Predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Uses]
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]. | [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. DOI:10.1016/j.cbpa.2020.01.010
[4] Nello Mainolfi, et al. Irak degraders and uses thereof. WO/2020/113233 |
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