2821803-61-4
2821803-61-4 structure
- Name: HEMTAC CDK4/6 degrader 1
- Chemical Name: HEMTAC CDK4/6 degrader 1
- CAS Number: 2821803-61-4
- Molecular Formula: C48H53ClN16O4
- Molecular Weight: 953.49
- Catalog: Signaling Pathways Apoptosis Apoptosis
- Create Date: 2023-04-11 11:37:18
- Modify Date: 2024-04-11 17:57:13
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HEMTAC CDK4/6 degrader 1 is a PROTAC connected by ligands for HSP90 and CDK4/6 with a Kd value 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 induces apoptosis. HEMTAC CDK4/6 degrader 1 can be used in research of cancer[1].
| Name | HEMTAC CDK4/6 degrader 1 |
|---|
| Description | HEMTAC CDK4/6 degrader 1 is a PROTAC connected by ligands for HSP90 and CDK4/6 with a Kd value 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 induces apoptosis. HEMTAC CDK4/6 degrader 1 can be used in research of cancer[1]. |
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| Related Catalog | |
| Target |
CDK4 CDK6 |
| 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. |
| 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. |
| References |
| Molecular Formula | C48H53ClN16O4 |
|---|---|
| Molecular Weight | 953.49 |