UNC-CA359 

UNC-CA359 is a potent epidermal growth factor receptor (EGFR) inhibitor, with an IC₅₀ value of 18 nM. UNC-CA359 exhibits strong anti-tumor activity, can be used to Chordoma research^[1]. UNC-CA359 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

IC50: 18 nM (EGFR)^[1]

UNC-CA359 (compound 45) loses activity on U-CH1, leaves some activity on U-CH2, and maintains inhibition on EGFR, with IC₅₀s of >100 μM, 35 μM, and 18 nM, respectively^[1].
UNC-CA359 (1 nM-0.1 mM; 72 h) has activity against chordoma with IC₅₀s of 1.2 μM (CH22), and 3.0 μM (U-CH12), respectively^[1].
UNC-CA359 shows UNC-CA359 (compound 102) has three main collateral kinase targets, and shows high potency towards SLK/STK10 with a promising selectivity ratio (NAK over SLK/STK10) of 22, while the binding constant K_i values are 3.4 nM (GAK), 0.33 μM (SLK), 0.075 μM (STK10), respectively^[2].
GAK: cyclin G associated kinase; SLK: STE20-like serine/threonine-protein kinase; STK10: serine/threonine-protein kinase 10.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

339.78

C₁₈H₁₄ClN₃O₂

2676156-05-9

ClC(C(C#C)=C1)=CC=C1NC2=C3C(C=C(C(OC)=C3)OC)=NC=N2

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Bieberich AA, et al. Optimization of the 4-anilinoquin(az)oline scaffold as epidermal growth factor receptor (EGFR) inhibitors for chordoma utilizing a toxicology profiling assay platform. Sci Rep. 2022 Jul 27. 12(1):12820.  [Content Brief]

  [2]. Asquith CRM, et al. Design and Analysis of the 4-Anilinoquin(az)oline Kinase Inhibition Profiles of GAK/SLK/STK10 Using Quantitative Structure-Activity Relationships. ChemMedChem. 2020 Jan 7. 15(1):26-49.  [Content Brief]