1. Vitamin D Related/Nuclear Receptor
  2. Estrogen Receptor/ERR
  3. ZN-c5

ZN-c5 是一种选择性且口服有效的雌激素受体 (estrogen receptor) 降解剂。ZN-c5 在细胞实验中显示出更强的活性 (MCF-7, IC50 = 0.3 nM),并与 ERαERβ 具有高亲和力结合 (IC50 分别为 0.4 nM 和 0.8 nM)。ZN-c5 在 MCF-7 小鼠异种移植模型和 WHIM20 异种移植模型中抑制肿瘤生长。ZN-c5 可用于乳腺癌的研究。

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ZN-c5

ZN-c5 Chemical Structure

CAS No. : 2136606-87-4

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查看 Estrogen Receptor/ERR 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

ZN-c5 is a selective and orally active estrogen receptor degrader. ZN-c5 exhibits high potency in the cellular assay (MCF-7, IC50 = 0.3 nM) and binds with high affinity to ERα and ERβ (IC50 = 0.4 nM and 0.8 nM, respectively). ZN-c5 inhibits tumor growth in MCF-7 mouse xenograft model and WHIM20 xenograft model. ZN-c5 can be used for the study of breast cancer[1].

体外研究
(In Vitro)

ZN-c5 (100 nM, 24 h) 在乳腺癌细胞系 (MCF-7、ZR-75-1、CAMA-1、HCC1500 和 HCC1428 细胞) 中诱导 ERα 降解[1]

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

Western Blot Analysis[1]

Cell Line: MCF-7, ZR-75-1, CAMA-1, HCC1500 and HCC1428 cells
Concentration: 100 nM
Incubation Time: 24 h
Result: Induced ERα degradation in breast cancer cell lines.
体内研究
(In Vivo)

ZN-c5 (1-40 mg/kg,口服,每日一次,持续 28 天) 在 MCF-7 小鼠异种移植模型中显示出显著的肿瘤生长抑制作用[1]
ZN-c5 (40 mg/kg,口服,每日一次,持续 90 天) 在 WHIM20 异种移植模型 (ESR1 突变模型 (Y537S)) 中诱导肿瘤生长抑制[1]

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

Animal Model: BALB/c nude mice were inoculated subcutaneously on the second right mammary fat pad with the single cell suspension of 95% viable tumor cells (1.5 × 107) in 200 μL medium Matrigel mixture (1:1 ratio) without serum[1]
Dosage: 1, 5, 40 mg/kg
Administration: p.o. once daily for 28 days
Result: Resulted in complete tumor growth inhibition at 5 mg/kg.
Animal Model: Female athymic BALB/c nude mice were implanted with a single cell suspension of 1.5 × 106 WHIM20 cells[1]
Dosage: 40 mg/kg
Administration: p.o. once daily for 90 days
Result: Induced tumor growth inhibition and showed no loss in body weight.
分子量

434.48

Formula

C26H24F2N2O2

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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  • 稀释计算器

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Help & FAQs
  • 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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ZN-c5
目录号:
HY-175260
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