HEMTAC CDK4/6 degrader 1 是由HSP90的配体和CDK4/6连接的PROTAC，Kd值为 35.7 μM。HEMTAC CDK4/6 degrader 1 在 B16F10 黑色素瘤细胞中诱导 CDK4/6 降解。HEMTAC CDK4/6 degrader 1 将细胞周期阻滞在 G0/G1 期并诱导细胞凋亡。HEMTAC CDK4/6 degrader 1 可用于癌症研究。
| 生物活性 | HEMTAC CDK4/6 degrader 1 is aPROTACconnected by ligands forHSP90andCDK4/6with aKdvalue of 35.7 μM. HEMTAC CDK4/6 degrader 1 induces CDK4/6 degradation in B16F10 melanoma cells. HEMTAC CDK4/6 degrader 1 arrests cell cycle at G0/G1 phase and inducesapoptosis. HEMTAC CDK4/6 degrader 1 can be used in research ofcancer[1]. |
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体外研究
(In Vitro) | HEMTAC CDK4/6 degrader 1 (compound 26; 0.01-1 μM; 24 h) 在处理过的 B16F10 细胞中诱导 CDK4 和 CDK6 降解，DC50值 (产生 50% 蛋白质的药物浓度 降解) 约为 26 和 19 nM，Dmax(最大降解百分比) 分别为 88% 和 92%[1]。
HEMTAC CDK4/6 degrader 1 (0.01-100 μM; 72 h) 对多种人类癌细胞系具有抗增殖活性[1]。
HEMTAC CDK4/6 degrader 1 (250 nM; 24 or 48 h) 以剂量依赖的方式诱导 B16F10 细胞发生凋亡，并使细胞周期停滞在 G0/G1 期[1]。
Cell Viability Assay[1] | Cell Line: | B16F10, A375, HepG2, MDA-MB-231, and A549 cells | | Concentration: | 0.01-100 μM | | Incubation Time: | 72 hours | | Result: | Inhibited cell growth in a dose-dependent manner. |
Apoptosis Analysis[1] | Cell Line: | B16F10 cells | | Concentration: | 250 nM | | Incubation Time: | 48 hours | | Result: | Induced cell apoptosis in a dose-dependent manner. |
Cell Cycle Analysis[1] | Cell Line: | B16F10 cells | | Concentration: | 250 nM | | Incubation Time: | 48 hours | | Result: | Increased the amount of B16F10 cells in the G0/G1 phase. |
Western Blot Analysis[1] | Cell Line: | B16F10 cells | | Concentration: | 0.01, 0.05, 0.1, 0.5, and 1 μM | | Incubation Time: | 24 hours | | Result: | Induced CDK4/6 degradation in a dose-dependent manner. |
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体内研究
(In Vivo) | HEMTAC CDK4/6 degrader 1 (compound 26; 20 and 40 mg/kg; i.p.; 每日一次, 持续 15 天) 对携带 B16F10 黑色素瘤异种移植物的 C57BL/6J 小鼠具有抗肿瘤功效[1]。
| Animal Model: | C57BL/6J mice bearing B16F10 melanoma xenografts[1] | | Dosage: | 20 and 40 mg/kg | | Administration: | intraperitoneal injection; daily, for 15 days | | Result: | Inhibited tumor growth and resulted in fewer CDK4/6-positive cells and led to much more necrosis. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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