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编 号:F754547
分子式:C18H14ClN3O2
分子量:339.78
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生物活性:
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.

体外研究:
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.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.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.GAK: cyclin G associated kinase; SLK: STE20-like serine/threonine-protein kinase; STK10: serine/threonine-protein kinase 10.
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