1. Cell Cycle/DNA Damage PROTAC
  2. CDK PROTACs
  3. PROTAC CDK2/4/6 Degrader-1

PROTAC CDK2/4/6 Degrader-1 是一种口服活性 CDK2/CDK4/CDK6 PROTAC 降解剂。PROTAC CDK2/4/6 Degrader-1 是一种前药,由 PROTAC CDK2/4/6 Degrader-2 (HY-185121) 通过与氯甲基新戊酸酯的一步反应转化而来。PROTAC CDK2/4/6 Degrader-1 可用于恶性黑色素瘤的相关研究。
(粉色: Aurora A 配体 (HY-168440);蓝色: Cereblon 配体 (HY-10984);黑色: 连接子)。

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PROTAC CDK2/4/6 Degrader-1

PROTAC CDK2/4/6 Degrader-1 Chemical Structure

CAS No. : 2541626-55-3

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PROTAC CDK2/4/6 Degrader-1 is an orally active CDK2/CDK4/CDK6 PROTAC degrader. PROTAC CDK2/4/6 Degrader-1 is a prodrug derived from PROTAC CDK2/4/6 Degrader-2 via one-step reaction with chloromethyl pivalate. PROTAC CDK2/4/6 Degrader-1 can be used for malignant melanoma research[1]. (Pink: Aurora A ligand (HY-168440); Blue: Cereblon ligand (HY-10984); Black: linker).

IC50 & Target[1]

CDK2/cyclinE

 

CDK6

 

CDK4

 

体外研究
(In Vitro)

PROTAC CDK2/4/6 Degrader-1 (compound 11) 是PROTAC CDK2/4/6 Degrader-2 (HY-185121) (compound 3) 经过氯甲基新戊酸酯的一步反应转化而成的前药。PROTAC CDK2/4/6 Degrader-2 是PROTAC CDK2/4/6 降解剂,降解 CDK 2/4/6 蛋白及复合物诱导黑色素瘤细胞的细胞周期和细胞凋亡[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

PROTAC CDK2/4/6 Degrader (compound 11) (200 mg/kg,口服,每日一次,持续 15 天) 在 B16F10 移植瘤小鼠模型中能显著抑制肿瘤生长并介导 CDK2/4/6 的降解[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: B16F10 cells induced- C57BL/6J mice[1]
Dosage: 200 mg/kg
Administration: o.p., 15 days
Result: Significantly suppressed tumor sizes.
No Noticeable difference in body weight.
分子量

861.98

Formula

C46H55N9O8

CAS 号
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.

纯度 & 产品资料
参考文献
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
PROTAC CDK2/4/6 Degrader-1
目录号:
HY-171826
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