PKM2-IN-6 (compound 7d) is a potent PKM2 inhibitor that can be administered orally and demonstrates an IC 50 value of 23 nM. It triggers apoptosis and causes cell cycle arrest in the G2 phase, while also reducing the mRNA levels of both PKM1 and PKM2. Additionally, PKM2-IN-6 exhibits anticancer properties and shows promise for research in triple-negative breast cancer [1].

PKM2-IN-6 (compound 7d)（0, 20, 40, 60, 80, 100 μM; 48 h）对COLO-205、A-549、MCF-7细胞显示细胞毒性，IC 50 值分别为18.33、47.00、19.80 μM [1]。PKM2-IN-6（14.38 μM; 48 h）诱导细胞凋亡和细胞周期停滞于G2期 [1]。PKM2-IN-6（14.38 μM; 24 h）在mRNA水平上显著降低PKM1和PKM2的表达 [1]。细胞毒性测定[1]：细胞系COLO-205、A-549、MCF-7；浓度0, 20, 40, 60, 80, 100 μM；孵育时间48 h；结果：显示对COLO-205、A-549、MCF-7细胞的IC 50 分别为18.33、47.00、19.80 μM。RT-PCR[1]：细胞系4T1细胞；浓度14.38 μM；孵育时间24 h；结果：显著降低PKM1和PKM2的mRNA表达。凋亡分析[1]：细胞系4T1细胞；浓度14.38 μM；孵育时间48 h；结果：2D培养中，存活细胞从对照组的82.64%降至5.44%，晚期凋亡细胞为50.32%，坏死细胞为44.08%；3D培养中，存活细胞从对照组的89.05%降至52.45%，晚期凋亡细胞为9.84%，坏死细胞为36.62%。

PKM2-IN-6, administered at doses of 25 and 50 mg/kg orally each day for three weeks, can reduce tumor volume and weight in female CD-1 nude mice (6-8 weeks) injected with 4T1-Red-FLuc cells [1].