1. Vitamin D Related/Nuclear Receptor Apoptosis
  2. Orphan Nuclear Receptor Androgen Receptor c-Myc
  3. XY25028

XY25028 是一种口服有效的 LRH-1 抑制剂,IC50 为 0.30 μM。XY25028 可抑制雄激素受体 (AR) 阳性前列腺癌细胞的增殖,抑制 AR 靶基因 KLK2 和 KLK3 的表达。XY25028 可用于去势抵抗性前列腺癌的研究。

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XY25028

XY25028 Chemical Structure

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100 mg   询价  
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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

XY25028 is an orally active LRH-1 inhibitor with an IC50 of 0.30 μM. XY25028 inhibits the proliferation of androgen receptor (AR)-positive prostate cancer cells and suppresses the expression of AR target genes KLK2 and KLK3. XY25028 can be used in the research of castration-resistant prostate cancer[1].

体外研究
(In Vitro)

XY25028 (96 h) 可抑制 22Rv1、C4-2B 和 LNCaP 人前列腺癌细胞系的活力,其 IC50 值分别为 14.46 μM、17.41 μM 和 20.88 μM[1]
XY25028 (10-40 μM; 48 h) 可呈剂量依赖性抑制 22Rv1 人前列腺癌细胞中 KLK2 和 KLK3 的 mRNA 表达[1]
XY25028 (2.5-40 μM; 48 h) 可在处理 48 h 后抑制人前列腺癌细胞 22Rv1 中的 c-Myc 蛋白表达[1]

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

Real Time qPCR[1]

Cell Line: 22Rv1 human prostate cancer cells
Concentration: 10 μM, 20 μM, 40 μM
Incubation Time: 48 h
Result: Significantly reduced KLK3 mRNA levels.

Western Blot Analysis[1]

Cell Line: 22Rv1 human prostate cancer cells
Concentration: 2.5 μM, 5 μM, 10 μM, 20 μM, 40 μM
Incubation Time: 48 h
Result: Significantly reduced c-Myc protein expression at 20 μM and 40 μM compared to vehicle control.
Showed no significant changes in c-Myc protein expression at 2.5 μM, 5 μM, or 10 μM compared to vehicle control.
体内研究
(In Vivo)

XY25028 (50 mg/kg;口服;每日 1 次;连续 16 天) 在 22Rv1 去势抵抗性前列腺癌 (CRPC) 异种移植模型中可产生显著的抗肿瘤功效,肿瘤生长抑制率达 40.7%,且未检测到全身毒性[1]

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

Animal Model: BALB/c-Nude (male, 5 weeks old)[1]
Dosage: 50 mg/kg
Administration: p.o.; once daily; 16 consecutive days
Result: Achieved a tumor growth inhibition (TGI) rate of 40.7%.
Showed no significant body weight changes (a marker of systemic toxicity) throughout the 16-day study period.
分子量

498.66

Formula

C32H38N2O3

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
  • 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.

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产品名称:
XY25028
目录号:
HY-181971
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