2. PROTAC Vitamin D Related/Nuclear Receptor Apoptosis
  3. PROTACs Estrogen Receptor/ERR Apoptosis
  4. PROTAC ERα Degrader-4

PROTAC ERα Degrader-4 是一种高效和高选择性的雌激素受体 (Estrogen Receptor/ERR) ERα 亚型 PROTACs，含有 OBHSAs、linker 和 E3 连接酶配体。PROTAC ERα Degrader-4 对 Tamoxifen (HY-13757A) 敏感和耐药的 ER+BC 细胞和 ERα 突变的 BC 细胞具有良好的细胞抑制和 ERα 降解活性。PROTAC ERα Degrader-4 能够诱导自噬 (Apoptosis)，可用于癌症研究。

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PROTAC ERα Degrader-4 Chemical Structure

PROTAC ERα Degrader-4 Chemical Structure

CAS No. : 2521299-80-7

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Customer Review

PROTAC ERα Degrader-4 相关抗体

Top Publications Citing Use of Products

查看 PROTACs 亚型特异性产品:

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

查看 Estrogen Receptor/ERR 亚型特异性产品:

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Estrogen receptor ERα ERβ ERRα ERRβ ERRγ

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PROTAC ERα Degrader-4 is a highly potent and selectivePROTAC ERα degrader (Ki: 5.08 μM). PROTAC ERα Degrader-4 contains OBHSAs, linker and E3 ligase ligands. PROTAC ERα Degrader-4 shows excellent cell inhibitory and ERα degradation activity against Tamoxifen-sensitive and -resistant ER+ breast cancer (BC) cells and ERα-mutated BC cells. PROTAC ERα Degrader-4 can induce apoptosis and can be used for cancer research.

IC50 & Target[1]

ERα

5.08 μM (Ki)

ERβ

26.20 μM (Ki)

体外研究
(In Vitro)

PROTAC ERα Degrader-4 (Compound ZD12) (1 μM, 12 小时) 显著降解 Tamoxifen 敏感的 MCF-7 细胞中的 ERα[1]。
PROTAC ERα Degrader-4 (2 μM, 12 小时) 可以降解 T47D 细胞中的野生型 ERα 和T47DD538G 和 T47DY537S 细胞中的突变型 ERα[1]。
PROTAC ERα Degrader-4 (1-10 μM, 72 小时) 抑制 Tamoxifen (HY-13757A) 敏感的 MCF-7 细胞生长， IC50 值为0.05 μM[1]。
PROTAC ERα Degrader-4 (1-10 μM, 72 小时) 诱导 MCF-7 细胞的凋亡和细胞周期阻滞[1]。
PROTAC ERα Degrader-4 (0.01-10 μM, 12 小时) 有效降解 MCF-7 细胞中的 ERα 蛋白[1]。

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

PROTAC ERα Degrader-4 相关抗体:

Cell Viability Assay[1]

Cell Line: MCF-7 cells
Concentration: 0.01-10 μM
Incubation Time: 72 hours
Result: Had inhibitory activity in Tamoxifen-sensitive MCF-7 cells, with the IC50 value of 0.05 μM.

Apoptosis Analysis[1]

Cell Line: MCF-7 cells
Concentration: 1.0 μM, 5 μM, 5.0 μM
Incubation Time: 72 hours
Result: Induced apoptosis.

Cell Cycle Analysis[1]

Cell Line: MCF-7 cells
Concentration: 0.01-10 μM
Incubation Time: 72 hours
Result: Induced cell cycle arrest.

Western Blot Analysis[1]

Cell Line: MCF-7 cells
Concentration: 0.01-10 μM
Incubation Time: 12 hours
Result: Efficiently degraded ERα protein in the range of 0.01 to10 μM, whereas ERα protein levels recovered slightly at a high concentration of 10 μM
体内研究
(In Vivo)

PROTAC ERα Degrader-4 (Compound ZD12) (5 μM/kg，腹腔注射；两天 1 次) 在 LCC2 异种移植肿瘤模型中表现出强大的抗肿瘤活性和 ERα 降解活性[1]。
PROTAC ERα Degrader-4 (静脉注射 5 mg/kg) 显示 T1/2 为 4.61 小时，清除率为 64.4 mL/min/kg[1]。

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

Animal Model: LCC2 orthotopic xenograft tumor models[1]
Dosage: 5 μM/kg
Administration: Intravenous injection (i.p.)
Result: Exhibited potent antitumor activity and ERα degradation effect in tumor tissues.
Animal Model: BALB/C female mice (Pharmacokinetic assay)[1]
Dosage: 5 mg/kg; 20 mg/kg
Administration: Intravenous injection (i.v.); Oral gavage (p.o.)
Result: Pharmacokinetic parameters for PROTAC ERα Degrader-4 (Compound ZD12) in BALB/C female mice [1]
ND: not detected.
Route Dose (mg/kg) CL (mL/min/kg) Tmax (h) T1/2 (h) Cmax (ng/mL) AUC (h•ng/mL)
i.v. 5 64.4 0.08 4.61 3635.73 1342
p.o. 20 ND ND ND ND ND
分子量

1074.23

Formula

C55H62F3N5O10S2
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

PROTAC ERα Degrader-4 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
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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.

Keywords:

PROTAC ERα Degrader-42521299-80-7PROTAC ERα Degrader4PROTAC ERα Degrader 4PROTACsEstrogen Receptor/ERRApoptosisPROTAC ERα DegraderMCF-7primary astrocytesER-positive breast cancerxenograft tumor modelsInhibitorinhibitorinhibit

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