2. Vitamin D Related/Nuclear Receptor PROTAC Apoptosis
  3. Androgen Receptor PROTACs Apoptosis
  4. ITRI-90

ITRI-90 是一种口服活性的雄激素受体 (AR) PROTAC 降解剂。ITRI-90 通过泛素-蛋白酶体系统有效降解全长 AR (AR-FL) 及其剪接变异体 AR-V7 蛋白，从而抑制 AR 转录活性及其靶基因表达。ITRI-90 能显著抑制前列腺癌细胞的增殖 (包括 Enzalutamide 耐药细胞) 并诱导细胞凋亡 (apoptosis)。ITRI-90 表现出良好的药代动力学特性，并在体内显示出强大的抗肿瘤功效。ITRI-90 可用于前列腺癌的相关研究。

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

我们将采用定制合成服务的方式为您快速提供所需产品和技术服务

ITRI-90

ITRI-90 Chemical Structure

CAS No. : 2798907-16-9

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

ITRI-90 相关抗体

Top Publications Citing Use of Products

查看 PROTACs 亚型特异性产品:

查看所有亚型
von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

ITRI-90 is an orally active androgen receptor (AR) PROTAC degrader. ITRI-90 effectively degrades both full-length AR (AR-FL) and the splice variant AR-V7 protein via the ubiquitin-proteasome system, thereby inhibiting AR transcriptional activity and the target gene expression. ITRI-90 significantly inhibits the proliferation of prostate cancer cells and induces apoptosis, include Enzalutamide-resistant growth cell. ITRI-90 exhibits favorable pharmacokinetic properties and demonstrates potent antitumor efficacy in vivo. ITRI-90 can be used for prostate cancer research[1].

体外研究
(In Vitro)

ITRI-90 (0-20 μM，24 小时) 在 LNCaP、CWR22Rv1 和 VCaP 细胞中降低全长 AR (AR-FL) 和剪接变异体AR-V(ΔLBD) 蛋白水平 (在 CWR22Rv1 和 VCaP 细胞中，对 AR-FL 蛋白的 DC50 分别为 2.12、5.73 和 8.67 nM，对 AR-V 蛋白的 DC50 分别为 4.72 和 0.29 nM)[1]。
ITRI-90 (10 μM，24 小时) 在LNCaP、CWR22Rv1 和 VCaP 细胞中显示出持久的作用时长，可实现较低的给药频率[1]。
ITRI-90 (10 μM，6 或 10 小时) 在 CWR22Rv1 细胞中通过泛素-蛋白酶体依赖性系统降解 AR 蛋白水平[1]。
ITRI-90 (0.1-1 μM，24 小时) 对 AR 及 AR-V7 信号通路下游靶基因表达的抑制效率较低，其在 LNCaP和 CWR22Rv1 细胞中通过靶向 NTD 的蛋白降解或直接阻断配体结合介导 AR 抑制[1]。
ITRI-90 (0.001-100 μM，24 小时或 7 天) 在 LNCaP、CWR22Rv1 和 VCaP 细胞中特异性且有效地抑制癌细胞增殖并诱导细胞凋亡[1]。
ITRI-90 (5 或 10 μM, 处理 1 天) 在短期处理和长期获得性耐药的细胞中均能有效降解由Enzalutamide (HY-70002) 诱导的全长 AR 和截短型 AR V(ΔLBD) 蛋白，从而在 VCaP、C4-2B 和 C4-2B/EnzR 细胞中显著削弱 Enzalutamide 耐药细胞的生长[1]。
ITRI-90 在小鼠肝微粒体中显示出较低的血浆清除率 (6.62 mL/min/kg) 和良好的实际体内暴露量 (AUC/dose = 2502.4)[1]。

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

ITRI-90 相关抗体:

Western Blot Analysis[1]

Cell Line: LNCaP, CWR22Rv1, VCaP cells
Concentration: 0, 0.01, 0.03, 0.1, 0.3, 1, 3, 10 and 20 μM
Incubation Time: 24 h
Result: Effectively reduced AR-FL and AR-V(ΔLBD) proteins in a dose-dependent manner.

Western Blot Analysis[1]

Cell Line: LNCaP, CWR22Rv1, VCaP cells
Concentration: 10 μM
Incubation Time: 24 h
Result: Displayed different kinetics of degradation and sustainability after drug washout at different time.
Achieved AR and AR-V(ΔLBD) degradation by 24 h treatment.
Appeared to sustain low pro tein levels up to 24 h after drug washout.

Western Blot Analysis[1]

Cell Line: CWR22Rv1 and 293T cells
Concentration: 10 μM
Incubation Time: 6 or 10 h
Result: Degradation of AR and AR-V(ΔLBD) was recovered by MG132 and MLN4924 treatment.
Showed AR proteins strongly ubiquitinated.

Cell Proliferation Assay[1]

Cell Line: LNCaP, CWR22Rv1, VCaP cells
Concentration: 0.001, 0.01, 0.1, 1, 10 and 100 μM
Incubation Time: 7 days
Result: Strongly inhibited cell growth by over 90% with IC50s = 6.587, 4.134, 5.454 μM for LNCaP, CWR22Rv1, VCaP cells, respectively.
Activated caspase 3/7 within 24 h.

Real Time qPCR[1]

Cell Line: LNCaP and CWR22Rv1 cells
Concentration: 0.1 and 1μM
Incubation Time: 24 h
Result: Decreased KLK3, NKX3.1 and TMPRSS2 expression in LNCaP and CWR22Rv1 cells.
Reduced CCNA2, CDC20, CDK1, UBE2C, UGT2B17 and EDN2 in CWR22Rv1 cells.

Cell Proliferation Assay [1]

Cell Line: LNCaP, CWR22Rv1, VCaP cells
Concentration: 0.001, 0.01, 0.1, 1, 10 and 100 μM
Incubation Time: 7 days
Result: Strongly inhibited cell growth by over 90% for LNCaP, CWR22Rv1 and VCaP cells with IC50s = 6.587, 4.134 and 5.454 μM.

Apoptosis Analysis[1]

Cell Line: LNCaP, CWR22Rv1, VCaP cells
Concentration: 10 μM
Incubation Time: 24 h
Result: Rapidly activated caspase 3/7.

Western Blot Analysis[1]

Cell Line: VCaP, C4-2B/EnzR cells cells
Concentration: 10 μM
Incubation Time: 24 h
Result: Reversed AR degraders significantly in VCaP cell.
Displayed Enzalutamide resistance as well as elevated AR-FL and AR-V7 in Long-term drug exposure of C4-2B Cells resulted in C4-2B/EnzR cells.
Efficiently reduced both AR-FL and the truncated AR-Vs.

Cell Proliferation Assay[1]

Cell Line: VCaP, EnzR cells
Concentration: 5 and 10 μM
Incubation Time: 24 h
Result: Inhibits VCaP proliferation when combined with Enzalutamide.
Significantly inhibited EnzR cells proliferation.
药代动力学
(Parmacokinetics)
Species Dose Route Indicator value
Mice[1] 10 mg/kg p.o. Tmax 1.5 h
Mice[1] 10 mg/kg p.o. Cmax 3945 ng/mL
体内研究
(In Vivo)

ITRI-90 (10 mg/kg，腹腔注射，每日两次，持续 15 天) 在 CWR22Rv1 移植瘤小鼠模型中能显著抑制肿瘤生长，且在肿瘤消退过程中未观察到明显毒性[1]。
ITRI-90 (100 mg/kg，口服，每日两次，持续 21 天) 是一种口服可用的降解剂，在 CWR22Rv1 移植瘤小鼠模型的肿瘤消退过程中特异性靶向全长 AR(AR-FL) 和 LBD 结构域截短的 AR 变异体 (AR-Vs)[1]。

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

Animal Model: CWR22Rv1 cells (5 × 106) induced-male C.B-17 SCID mice (4-6 weeks)[1]
Dosage: 10 mg/kg
Administration: twice daily for 15 days
Result: Significantly impaired the tumor growth without obvious toxicities[1].
Reached an average tumor growth inhibition (TGI) of 76.64% on day 12[1].
Significantly decreased AR-FL 12 and AR-V protein levels in tumors detected at the final time point[1].
Animal Model: CWR22Rv1 cells (5 × 106) induced-male C.B-17 SCID mice (4-6 weeks)[1]
Dosage: 100 mg/kg
Administration: p.o., twice daily for 21 days
Result: Observed significant tumor suppression with an average TGI of 71.73 % without obvious toxicity[1].
Reduced protein levels of AR-FL and AR Vs in the tumors[1].
分子量

908.04

Formula

C45H56F3N9O6S
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

ITRI-90 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:

ITRI-902798907-16-9ITRI90ITRI 90Androgen ReceptorPROTACsApoptosisAR PROTAC degraderapoptosis Enzalutamide-resistantprostate cancerInhibitorinhibitorinhibit

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：
ITRI-90
目录号：
HY-171808
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