产品
编 号：F741177
分子式：C17H20N4O2
分子量：312.37
分子式：C17H20N4O2
分子量：312.37
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
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5mg
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10mg
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25mg
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50mg
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100mg
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结构图
CAS No: 1375060-02-8
产品详情
生物活性：
SCFSkp2-IN-2 (Compound AAA-237) is a Skp2 inhibitor with a KD of 28.77 μM. AAA-237 induces apoptosis of NSCLC cells and shows antitumor activities.
体内研究：
SCFSkp2-IN-2 (Compound AAA-237) (15 or 45?mg/kg; i.p.; daily for 14 days) 在肺癌 A549 异种移植小鼠模型中显示出抗肿瘤活性。Animal Model:A549 xenograft model
Dosage:15 or 45?mg/kg
Administration:Intraperitoneal administration, daily for 14 days
Result:Significantly reduced tumor volume and weight. The tumor growth inhibition of the low dose and high dose was 55% and 64%, respectively. No obvious weight loss or abnormal behavior was observed. Reduced the expression of Ki67 in tumor tissue. Reduced the expression of Skp2 and Bcl-2 and increased the expression of p27, the cleaving of caspase 3, caspase 9, PARP and Bax.
体外研究：
SCFSkp2-IN-2 (Compound AAA-237) (0.3-3 μM; 24-72 h) 可直接与 Skp2 结合，导致 Skp2 被蛋白酶体降解。AAA-237 对 Skp2 mRNA 表达无显著影响，但对 NSCLC 细胞中 Skp2 蛋白表达有时间依赖性的抑制作用。SCFSkp2-IN-2 (0.3-3 μM; 24-72 h) 以剂量和时间依赖的方式抑制 A549 和 H1299 细胞的增殖。SCFSkp2-IN-2 (0.3-3 μM; 24-72 h) 通过调节 Skp2-Cip/Kip 和 PI3K/Akt-FOXO1 信号通路，在 G0/G1 检查点阻止细胞周期。SCFSkp2-IN-2 (0.3-3 μM; 24-72 h) 以剂量和时间依赖的方式诱导 A549 和 H1299 细胞凋亡。SCFSkp2-IN-2 (0.3 μM; 1-7 days) 诱导 NSCLC 细胞衰老。
SCFSkp2-IN-2 (Compound AAA-237) is a Skp2 inhibitor with a KD of 28.77 μM. AAA-237 induces apoptosis of NSCLC cells and shows antitumor activities.
体内研究：
SCFSkp2-IN-2 (Compound AAA-237) (15 or 45?mg/kg; i.p.; daily for 14 days) 在肺癌 A549 异种移植小鼠模型中显示出抗肿瘤活性。Animal Model:A549 xenograft model
Dosage:15 or 45?mg/kg
Administration:Intraperitoneal administration, daily for 14 days
Result:Significantly reduced tumor volume and weight. The tumor growth inhibition of the low dose and high dose was 55% and 64%, respectively. No obvious weight loss or abnormal behavior was observed. Reduced the expression of Ki67 in tumor tissue. Reduced the expression of Skp2 and Bcl-2 and increased the expression of p27, the cleaving of caspase 3, caspase 9, PARP and Bax.
体外研究：
SCFSkp2-IN-2 (Compound AAA-237) (0.3-3 μM; 24-72 h) 可直接与 Skp2 结合，导致 Skp2 被蛋白酶体降解。AAA-237 对 Skp2 mRNA 表达无显著影响，但对 NSCLC 细胞中 Skp2 蛋白表达有时间依赖性的抑制作用。SCFSkp2-IN-2 (0.3-3 μM; 24-72 h) 以剂量和时间依赖的方式抑制 A549 和 H1299 细胞的增殖。SCFSkp2-IN-2 (0.3-3 μM; 24-72 h) 通过调节 Skp2-Cip/Kip 和 PI3K/Akt-FOXO1 信号通路，在 G0/G1 检查点阻止细胞周期。SCFSkp2-IN-2 (0.3-3 μM; 24-72 h) 以剂量和时间依赖的方式诱导 A549 和 H1299 细胞凋亡。SCFSkp2-IN-2 (0.3 μM; 1-7 days) 诱导 NSCLC 细胞衰老。
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