化合物 UNC-CA359 T61077

Product Introduction
Bioactivity


英文名: UNC-CA359

描述: UNC-CA359 is a highly potent inhibitor of the epidermal growth factor receptor (EGFR), demonstrating an IC50 value of 18 nM. With strong anti-tumor activity, UNC-CA359 holds significant potential for chordoma research [1].

体外活性: UNC-CA359 (compound 45) loses activity on U-CH1, leaves some activity on U-CH2, and maintains inhibition on EGFR, with IC 50 s of >100 μM, 35 μM, and 18 nM, respectively [1]. UNC-CA359 (1 nM-0.1 mM; 72 h) has activity against chordoma with IC 50 s 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. Cell Cytotoxicity Assay [1] Cell Line: Chordoma cell lines: CH22, UM-Chor1, U-CH12 and U-CH7; WS1 Concentration: 1 nM-100 μM Incubation Time: 72 hours Result: Demonstrated good potential against chordoma cells, with IC 50 s 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 (IC 50 >100 μM).

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途