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HEMTAC CDK4/6 degrader 1
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
HEMTAC CDK4/6 degrader 1图片
CAS NO:2821803-61-4
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
HEMTAC CDK4/6 degrader 1 是由HSP90的配体和CDK4/6连接的PROTACKd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].

IC50& Target[1]

CDK4

 

CDK6

 

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.
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.
分子量

953.49

Formula

C48H53ClN16O4

CAS 号

2821803-61-4

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.