2. Vitamin D Related/Nuclear Receptor Apoptosis
  3. Androgen Receptor Apoptosis
  4. SC912

:SC912 是一种AR-V7(IC50 = 0.36 μM) 抑制剂，拥有安全性，高效性和选择性，直接和 AR-FL 和 AR-V7 蛋白结合，抑制了核定位和染色质结合能力。通过抑制增殖，诱导细胞周期停止和凋亡来发挥抗癌活性。

MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

SC912 Chemical Structure

SC912 Chemical Structure

1.  客户无需承担相应的运输费用。

2.  同一机构（单位）同一产品试用装仅限申领一次，同一机构（单位）一年内

     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户。

规格 是否有货
50 mg   询价  
100 mg   询价  
250 mg   询价  

* Please select Quantity before adding items.

Customer Review

SC912 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

SC912 is an AR-V7 inhibitor (IC50 = 0.36 μM). SC912 possesses safety, potency and selectivity. SC912 binds directly to AR-FL and AR-V7 proteins, inhibites nuclear localization and chromatin binding capabilities. SC912 exerts anticancer activity through inhibition of proliferation, induction of cell cycle arrest and apoptosis[1].

体外研究
(In Vitro)

SC912 (0.1-10 μM; 24h) 在 PC3 细胞中有效抑制了 AR 激活，对 GR 和 PR 没有抑制作用 (AR IC50 = 0.57 μM)[1]。
SC912 (0.03-100 μM; 1h) 对删除 AR-NTD (氨基酸 507-531) 的 293 T 细胞，与 AR-FL 和 AR-V7 的结合减弱。氨基酸 507-53 1对于对其对抗性活动至关重要[1]。
SC912 (2 μM; 24 h） 在 LNCaP95 细胞模型中，强烈抑制了由 AR-V7 唯一调控的 AR 调控基因 (PSA, FKBP5, TMPRSS2) 的转录，表明有效抑制了 AR-V 7介导的转录活性[1]。
SC912 (1 μM; 0-24 h）在 LNCaP, VCaP 和 22Rv1 细胞中，引起 G1 期阻滞，引起细胞凋亡[1]。
SC912 (3 μM; 5 h） 处理后在 LNCaP 和 LNCaP-AR-V7 细胞中显著减少了 AR-FL 和 AR-V7 的核内积聚，这表明能够有效阻断 AR-V7 的核定位。显著降低了 AR 蛋白与染色质的结合[1]。

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

SC912 相关抗体:

Apoptosis Analysis[1]

Cell Line: LNCaP, VCaP, 22Rv1cell, PC3
Concentration: 1 μM
Incubation Time: 24 h
Result: SC912 led to significant PARP cleavage in LNCaP, VCaP, and 22Rv1 cells, indicating effective induction of apoptosis. Flow cytometry analysis showed an increase in the percentage of apoptotic cells in LNCaP, VCaP, and 22Rv1 cell lines with SC912. This further supported the finding that SC912 induces apoptosis effectively in AR-positive cells.

Real Time qPCR[1]

Cell Line: LNCaP, VCaP, 22Rv1
Concentration: 0, 0.1, 0.3, 1, 3 μM
Incubation Time: 24 h
Result: SC912-dependent dose (0.33 μM) impaired the transcription of AR-regulated genes (PSA, FKBP5 and TMPRSS2) in these prostate cancer cell lines.This indicates effective inhibition of AR signaling by SC912. The inhibition of gene expression was dose-dependent.

Cell Cycle Analysis[1]

Cell Line: LNCaP, VCaP, 22Rv1cell, PC3
Concentration: 3 μM
Incubation Time: 48 h
Result: Induced a significant G1/S phase arrest in the treated cells. This effect was dose-dependent, with higher concentrations of SC912 leading to a more pronounced accumulation of cells in the G1 phase, suggesting a blockade in the transition from G1 to S phase.
体内研究
(In Vivo)

SC912 (60 mg/kg; i.p.; 一周五次持续三周) 能有效抑制 VCaP 肿瘤的生长。小鼠的体重没有明显减轻，表明给药剂量具有良好的耐受性[1]。
SC912 (90 mg/kg; i.p.; 一周五次持续三周) 即使高度去势抵抗的 22Rv1 模型中，也能减轻肿瘤生长[1]。

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

Animal Model: NOD-SCID mice implanted with VCaP cells [1]
Dosage: 60 mg/kg, five times a week for 3 weeks
Administration: i.p.
Result: SC912 was found to effectively repress tumor growth in the xenograft models. This was evidenced by a marked reduction in tumor size in mice treated with SC912 compared to those treated with vehicle controls. The serum levels of human PSA, a marker of AR activity, were considerably lower , indicating effective inhibition of AR signaling.
Animal Model: mice implanted with 22Rv1 cells [1]
Dosage: 90 mg/kg, five times a week for 3 weeks
Administration: i.p.
Result: SC912 markedly mitigated tumor progression in this highly castration-resistant 22Rv1 model. The growth rate of tumors was significantly reduced in the SC912-treated group compared to the vehicle-treated controls. Reduction in tumor size was associated with a significant decrease in AR-driven gene expression within the tumors, highlighting SC912’s capability to interrupt AR-V7-mediated signaling pathways even under high AR-V7 expressing conditions.
分子量

493.27

Formula

C22H13Cl2F3N4O2
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

SC912 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)
× = ×
C1   V1   C2   V2
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:

SC912SC 912SC-912Androgen ReceptorApoptosisAR-NTDcell cyclecastration-resistant prostate cancer(CRPC) cellLNCaP95 NOD-SCID miceInhibitorinhibitorinhibit

您最近查看的产品:

Your information is safe with us. * Required Fields.

   产品名称：

  

* 需求量：

* 客户姓名：

 

* Email：

* 电话：

 

* 公司或机构名称：

   留言给我们：

Bulk Inquiry

Inquiry Information

产品名称：
SC912
目录号：
HY-161409
需求量：

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

   产品名称：

  

* Lot #：

* 客户姓名：

 

* Email：

   电话：

 

* 部门：

* 公司或机构名称：

 

   留言给我们：

Request for HNMR Report

We have received your request and will respond to you as soon as possible.

嗨！很高兴为您提供帮助！

尊敬的 MCE 客户您好，
请您选择所在区域，我们将转接对应客服为您服务！

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

热 A B C F G H J L N Q S T X Y Z