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. 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.
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- CAS No.: 2676156-05-9
- Formule: C18H14ClN3O2
- Masse moléculaire:339.78
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
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 Ki 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.
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Cell Line:Chordoma cell lines: CH22, UM-Chor1, U-CH12 and U-CH7; WS1
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Concentration:1 nM-100 μM
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Incubation Time:72 hours
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Result:Demonstrated good potential against chordoma cells, with IC50s of 1.2 μM (CH22), 3.0 μM (U-CH12), 60 μM (UM-Chor1), 74 μM (U-CH7), respectively.
Showed no toxicity towards WS1 cell (IC50 >100 μM).
Chemical Information
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CAS No. 2676156-05-9
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Masse moléculaire 339.78
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Formule C18H14ClN3O2
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SMILES
ClC(C(C#C)=C1)=CC=C1NC2=C3C(C=C(C(OC)=C3)OC)=NC=N2
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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