1. Vitamin D Related/Nuclear Receptor Apoptosis
  2. Orphan Nuclear Receptor Androgen Receptor c-Myc
  3. XY25026

XY25026 是一种口服有效的 LRH-1 抑制剂,其 IC50 为 0.28 μM。XY25026 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,并可抑制异种移植模型中的肿瘤生长。XY25026 可用于去势抵抗性前列腺癌的研究。

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XY25026

XY25026 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
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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

XY25026 is an orally active LRH-1 inhibitor with an IC50 of 0.28 μM. XY25026 inhibits the proliferation of androgen receptor (AR)-positive prostate cancer cells, suppresses the expression of AR target genes KLK2 and KLK3, and inhibits tumor growth in xenograft models. XY25026 is applicable to the research of castration-resistant prostate cancer[1].

体外研究
(In Vitro)

XY25026 可在无细胞 AlphaScreen 实验中强效抑制人源 LRH-1 LBD 与 SRC1 共激活因子肽段的相互作用,其 IC50 为 280 nM[1]
XY25026 (96 h) 可抑制人前列腺癌细胞系 22Rv1、C4-2B 和 LNCaP 的增殖,其 IC50 值分别为 13.29 μM、14.56 μM 和 15.89 μM[1]
XY25026 (0-40 μM; 48 h) 可在人前列腺癌细胞 22Rv1 中抑制 AR 靶基因 KLK2、KLK3 以及致癌蛋白 c-Myc 的表达[1]

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

Real Time qPCR[1]

Cell Line: 22Rv1 cells
Concentration: 0, 10, 20 and 40 μM
Incubation Time: 48 h
Result: Suppressed expression of AR target genes KLK2 and KLK3.

Western Blot Analysis[1]

Cell Line: 22Rv1 cells
Concentration: 0, 2.5, 5, 10, 20 and 40 μM
Incubation Time: 48 h
Result: Inhibited the expression of c-Myc.
药代动力学
(Parmacokinetics)
Species Dose Route Cmax Tmax AUC0-t AUC0-∞ T1/2 CL F
Rat[1] 1 mg/kg i.v. 578 ng/mL 0.083 h 343 ng·h/mL 346 ng·h/mL 1.28 h 3071 mL/h/kg /
Rat[1] 5 mg/kg p.o. 37.1 ng/mL 0.833 h 94.6 ng·h/mL 98.5 ng·h/mL 1.63 h / 5.69 %
体内研究
(In Vivo)

XY25026 (50-100 mg/kg;口服;每日一次;连续 16 天) 在 22Rv1 去势抵抗性前列腺癌异种移植模型中可分别达到 31.5% 和 44.6%的肿瘤生长抑制率,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; 100 mg/kg
Administration: p.o.; once daily; 16 days
Result: Achieved a tumor growth inhibition (TGI) rate of 31.5%.
Achieved a tumor growth inhibition (TGI) rate of 44.6%.
Showed no significant body weight changes (a marker of systemic toxicity) throughout the study.
分子量

470.60

Formula

C30H34N2O3

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:
XY25026
目录号:
HY-181970
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