2. Vitamin D Related/Nuclear Receptor Metabolic Enzyme/Protease Cell Cycle/DNA Damage
  3. Androgen Receptor HSP CDK
  4. AR/AR-V7 degrader-1

AR/AR-V7 degrader-1 是一种具有口服活性的 AR 和 AR-V7 降解剂。AR/AR-V7 degrader-1 可破坏 AR/AR‑V7 与 HSP90 之间的相互作用，使其在去势抵抗性前列腺癌细胞中发生泛素化并被降解。AR/AR-V7 degrader-1 可在前列腺癌细胞中调控细胞周期相关蛋白的表达 (下调 CDK4、CDK6、Cyclin D1、Cyclin E1；上调 P21)，诱导 G0/G1 期阻滞。AR/AR-V7 degrader-1 可抑制前列腺癌细胞的增殖和迁移。AR/AR-V7 degrader-1 抑制裸鼠去势抵抗性前列腺癌肿瘤的生长，诱导肿瘤组织中 AR 和 AR-V7 的降解。AR/AR-V7 degrader-1 可用于去势抵抗性前列腺癌的研究。

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AR/AR-V7 degrader-1

AR/AR-V7 degrader-1 Chemical Structure

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AR/AR-V7 degrader-1 相关抗体

Top Publications Citing Use of Products

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HSP40 HSP70 HSP90 HSP105 HSF1 HSP HSPA5

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CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85 CDK10 CDK15 CDK17 CDK18 CDK20 PITSLRE

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

AR/AR-V7 degrader-1 is an orally active AR and AR-V7 degrader. AR/AR-V7 degrader-1 disrupts the interaction between AR/AR-V7 and HSP90, leading to their ubiquitination and degradation in castration-resistant prostate cancer cells. AR/AR-V7 degrader-1 regulates the expression of cell cycle-related proteins in prostate cancer cells (downregulates CDK4, CDK6, Cyclin D1, Cyclin E1; upregulates P21) and induces G0/G1 phase arrest. AR/AR-V7 degrader-1 inhibits the proliferation and migration of prostate cancer cells. AR/AR-V7 degrader-1 suppresses the growth of castration-resistant prostate cancer tumors in nude mice and induces the degradation of AR and AR-V7 in tumor tissues. AR/AR-V7 degrader-1 is applicable to the research of castration-resistant prostate cancer[1].

体外研究
(In Vitro)

AR/AR-V7 degrader-1 (Compound 13) (0.25-2.5 μM) 可在 22Rv1 细胞中强效降解 AR 与 AR-V7，在 2.5 μM 浓度下实现近乎完全的降解[1]。
AR/AR-V7 degrader-1 (0.01-5 μM; 0-48 h) 可在 22Rv1 和 VCaP 细胞中通过泛素-蛋白酶体途径介导剂量和时间依赖方式的 AR 和 AR-V7 持续降解，其 DC50 值根据蛋白和细胞系的不同在 0.6617 μM 至 1.948 μM 之间[1]。
AR/AR-V7 degrader-1 可强效抑制 22Rv1 和 VCaP 细胞的增殖，其 IC50 值分别为 3.567 μM 和 3.351 μM[1]。
AR/AR-V7 degrader-1 (0-10 μM; 24 h) 可在 22Rv1 和 VCaP 细胞中调控细胞周期相关蛋白的表达 (下调 CDK4、CDK6、Cyclin D1、Cyclin E1；上调 P21)，诱导 G0/G1 期阻滞[1]。
AR/AR-V7 degrader-1 (0-2.5 μM; 0-24 h) 以剂量和时间依赖的方式下调 22Rv1 和 VCaP 细胞 中 AR/AR-V7 下游生物标志物 (PSA、TMPRSS2、FKBP51) 的表达[1]。
AR/AR-V7 degrader-1 (1-2.5 μM; 24 h post-treatment) 可呈剂量依赖性抑制 22Rv1 和 VCaP 细胞的迁移，抑制细胞恶性集落形成和侵袭[1]。
AR/AR-V7 degrader-1 (5 μM; unspecified duration, in combination with 10 μM MG132) 可促进 22Rv1 去势抵抗性前列腺癌细胞中 AR/AR-V7 与 E3 泛素连接酶 HLTF 的相互作用，并抑制 AR/AR-V7 与 HSP90 的结合[1]。

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

AR/AR-V7 degrader-1 相关抗体:

Western Blot Analysis[1]

Cell Line: 22Rv1 and VCaP CRPC cells
Concentration: 0, 0.01, 0.1, 0.5, 1, 2.5, 5 μM
Incubation Time: 0, 4, 8, 16, 24, 48 h
Result: Initiated degradation of AR and AR-V7 at approximately 0.5 μM in both cell lines.
Achieved DC50 values of 0.6617 μM for AR degradation and 0.852 μM for AR-V7 degradation in 22Rv1 cells.
Achieved DC50 values of 1.948 μM for AR degradation and 1.024 μM for AR-V7 degradation in VCaP cells.
Induced significant degradation of AR and AR-V7 within 8 h of treatment in both cell lines.

Cell Cycle Analysis[1]

Cell Line: 22Rv1 and VCaP CRPC cells
Concentration: 1-10 μM
Incubation Time: unspecified duration
Result: Markedly arrested both cell lines in the G0/G1 phase.

Western Blot Analysis[1]

Cell Line: 22Rv1 and VCaP CRPC cells
Concentration: 0, 0.5,1, 2.5μM
Incubation Time: 24 h
Result: Significantly downregulated expression of CDK4, CDK6, Cyclin D1, and Cyclin E1.
Significantly upregulated expression of P21 in both cell lines.\nDownregulated expression of PSA, TMPRSS2, and FKBP51 in both cell lines in a dose-dependent manner.
药代动力学
(Parmacokinetics)
Species Dose Route AUC0-t AUC0-∞ MRT0-t MRT0-∞ T1/2 Tmax Cmax Bioavailability
Mice[1] 30 mg/kg p.o. 13433.63 ng·h/mL 16106.59 ng·h/mL 7.88 h 12.76 h 9.23 h 1.00 h 1162.86 ng/mL 24.70 %
Mice[1] 10 mg/kg i.v. 18137.97 ng·h/mL 20709.35 ng·h/mL 6.43 h 10.18 h 8.63 h 0.083 h 5074.99 ng/mL /
体内研究
(In Vivo)

AR/AR-V7 degrader-1 (30-60 mg/kg; p.o.; daily; 14 days/single dose) 可强效抑制 Balb/c 裸鼠体内 22Rv1 去势抵抗性前列腺癌 (CRPC) 肿瘤的生长，可诱导肿瘤组织中 AR 和 AR-V7 的降解[1]。

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

Animal Model: Balb/c nude (male)[1]
Dosage: 30 mg/kg; 60 mg/kg
Administration: p.o.; daily; 14 days/single dose
Result: Significantly reduced tumor volume and tumor weight relative to vehicle control.
Produced greater tumor growth inhibition at 60 mg/kg than 30 mg/kg.
Markedly suppressed expression of AR, AR-V7, and their downstream biomarkers (PSA, FKBP51, TMPRSS2) at 60 mg/kg.
Reduced AR and Ki67 expression in tumor tissues.
Caused no significant changes in mouse body weight, indicating favorable tolerability.
Induced AR and AR-V7 degradation in tumor tissues as early as 6 hours post-administration.
Sustained suppression of both proteins through 48 hours.
Showed no significant recovery of AR/AR-V7 expression until 72 hours post-dose.
分子量

678.80

Formula

C33H33F3N6O3SSi
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

AR/AR-V7 degrader-1 相关分类

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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.

Keywords:

AR/AR-V7 degrader-1Androgen ReceptorHSPCDKHeat shock proteinsCyclin dependent kinaseAR and AR-V7 degradercastration-resistant prostate cancer22Rv1 cellsVCaP cellsBalb/c nude mice
Inhibitorinhibitorinhibit

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