1. Cell Cycle/DNA Damage
  2. CDK
  3. CDK2 degrader 7

CDK2 degrader 7 是一种口服活性的 CDK2 降解剂,在 MKN1 细胞和 TOV21G 细胞中的 DC50 值分别为 13 nM 和 17 nM。CDK2 degrader 7 可诱导 MKN1 细胞的 G1 期阻滞。CDK2 degrader 7 在 HCC1569 (CCNE1 扩增) 异种移植模型中实现肿瘤抑制。CDK2 degrader 7 可用于 CCNE1 扩增型癌症的研究。

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CDK2 degrader 7

CDK2 degrader 7 Chemical Structure

CAS No. : 3030279-55-8

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

CDK2 degrader 7 is an orally active CDK2 degrader, with DC50 values of 13 nM (MKN1cells) and 17 nM (TOV21G cells). CDK2 degrader 7 induces G1 phase arrest in MKN1 cells. CDK2 degrader 7 achieves tumor stasis in HCC1569 (CCNE1-amplified) xenograft models. CDK2 degrader 7 can be used for the study of CCNE1-amplified cancers[1].

IC50 & Target[1]

CDK2

13 nM (DC50, MKN1cells)

CDK2

17 nM (DC50, TOV21G cells)

CDK1

2130 nM (DC50)

体外研究
(In Vitro)

CDK2 degrader 7 (Compound 37) 在 MKN1 (CCNE1 扩增) 和 TOV21G (CCNE1 非扩增) 细胞中表现出强效的 CDK2 降解活性,DC50 值分别为 13 nM 和 17 nM[1]
CDK2 degrader 7 对 MKN1 (CCNE1 扩增) 细胞表现出强效的抗增殖活性,IC50 为 9 nM,而对 TOV21G (CCNE1 非扩增) 细胞的活性较弱,IC50 为 5760 nM[1]
CDK2 degrader 7 (4.88-5000 nM, 72 h) 在 MKN1 细胞中在 78 nM 时诱导最大 G1 期阻滞 (靶向作用),在 2500 nM 时出现非靶向的 G2/M 期积累[1]

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

体内研究
(In Vivo)

CDK2 degrader 7 (Compound 37) (10-50 mg/kg, 口服, 每日一次或两次, 28 天) 在 HCC1569 (CCNE1 扩增) 异种移植模型中表现出强效的抗肿瘤活性\[1]

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

Animal Model: HCC1569 human breast carcinoma cells (6 × 106 cells + Matrigel in 0.2 mL RPMI 1640 medium) were subcutaneously implanted into the central right flank of 7-day acclimated female NOG mice[1]
Dosage: 10 mg/kg, 25 mg/kg, 50 mg/kg
Administration: p.o., once or twice daily, 28 days
Result: Achieved tumor stasis in HCC1569 (CCNE1-amplified) xenograft model.
分子量

852.89

Formula

C39H46F6N8O5S

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:
CDK2 degrader 7
目录号:
HY-175842
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