Anticancer agent 109 (compound 6-15) acts as an inhibitor targeting the Gas6-Axl axis, demonstrating significant anti-cancer properties. This compound suppresses the expression of Gas6, Axl, p-PI3K, and p-AKT in cancer cells, thereby inducing G1 phase arrest and promoting apoptosis of cancer cells. Additionally, Anticancer agent 109 effectively inhibits tumor growth in nude mouse tumor-bearing models [1].

抗癌剂 109 (10 μM，48 小时) 抑制 A549 细胞 Gas6 和 Axl，抑制 PANC-1 细胞 Gas6-Axl 轴相关蛋白，诱导 G1 期阻滞并促进晚期凋亡，但不改变 DNA 合成 [1]。细胞活力测定 [1] 细胞系: MCF-7; PANC-1; MDA-MB-231; HT-29; DU145; U937; A549; PANC-1 浓度: 30 μM 孵育时间: 48 小时 结果: 抑制癌细胞生长，对正常细胞的安全性提高至20倍，对癌细胞的活性比舒尼替尼高5.4倍。抑制生长的 IC 50 分别为 2.0 μM (MCF-7); 2.8 μM (MDA-MB-231); 4.6 μM (HT-29); 1.1 μM (DU145); 6.7 μM (U937); 4.2 μM (A549); 4.0 μM (PANC-1)。凋亡分析 [1] 细胞系: PANC-1 浓度: 1 μM, 5 μM, 10 μM 孵育时间: 48 小时 结果: 增加 sub-G1 分数并诱导晚期凋亡。Western Blot 分析 [1] 细胞系: A549; PANC-1 浓度: 10 μM 孵育时间: 48 小时 结果: 抑制 A549 和 PANC-1 细胞的 Gas6 和 Axl，增加 Bax/Bcl-2 表达比率，抑制 PANC-1 细胞 p-PI3K 和 p-AKT。RT-PCR [1] 细胞系: PANC-1 浓度: 3 μM, 5 μM, 10 μM 孵育时间: 48 小时 结果: 抑制 Gas6 和 Axl。

化合物 109 (3 mg/kg，腹腔注射，A549 肿瘤模型 31 天，PANC-1 肿瘤模型 85 天，每周 6 次) 在裸鼠异种移植模型中显著降低肿瘤大小和重量 [1]。Animal Model: A549 or PANC-1 xenografted in BALB/c-nu mice [1]。Dosage: 1 mg/kg; 3 mg/kg Administration: Intraperitoneal injection (i.p.) 6 times a week Result: Promoted tumor regression to around a quarter with 1 mg/kg, smaller but not eliminated with 3 mg/kg in A549 models. Promoted tumor regression to around a quarter with 3 mg/kg in PANC-1 models.