ITK degrader 2

ITK degrader 2 (compound 30) is an orally active, PROTAC-based ITK-targeted degrader (DC50max and Tmax in mice (po; 90 mg/kg) of 0.87 μM and 2 h, respectively. At this dose, ITK degrader 2 degrades ITK by 20% (6 h) in mice[1].

Product Specifications

CAS Number

[2858738-65-3]

UNSPSC

12352005

Target

Itk; PROTACs

Type

Reference compound

Related Pathways

PROTAC; Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/itk-degrader-2.html

Solubility

10 mM in DMSO

Smiles

C[C@@]12[C@@](CC3=C(NN=C3C(NC4=C5)=CC4=CC=C5N(C)C([C@@H](N6CCN(CC6)CC7CCN(C8=CC=C(C9C(NC(CC9)=O)=O)C=N8)CC7)C)=O)C2)([H])C1(F)F

Molecular Formula

C41H49F2N9O3

Molecular Weight

753.88

References & Citations

[1]Wegrzyniak, et al. Substituted piperidinedione and dioxotetrahydropyrimidine compounds for inhibiting or degrading target proteins, compositions, comprising the same, methods of their making, and methods of their use. World Intellectual Property Organization, WO2022235698 A1 2022-11-10.