2. Vitamin D Related/Nuclear Receptor
  3. Androgen Receptor
  4. UT-143

UT-143 是一种具有口服活性的选择性雄激素受体 (AR) 不可逆共价拮抗剂。UT-143 可抑制 AR 阳性前列腺癌细胞的增殖，降低大鼠雄激素靶组织重量，并抑制 AR 阳性异种移植瘤的生长。UT-143 可用于前列腺癌的研究。

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UT-143

UT-143 Chemical Structure

CAS No. : 2698320-33-9

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UT-143 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

UT-143 is an orally active, selective irreversible covalent antagonist of androgen receptor (AR). UT-143 inhibits the proliferation of AR-positive prostate cancer cells, reduces the weight of androgen target tissues in rats, and suppresses the growth of AR-positive xenograft tumors. UT-143 can be used for the research of prostate cancer[1].

体外研究
(In Vitro)

UT-143 (10 µM; 16 h) 可显著降低 22RV1 前列腺癌细胞中全基因组染色质的可及性，将可及区域数量从 36141 个减少至 10302 个[1]。
UT-143 抑制雄激素受体转录激活，IC50 值为 0.15 μM[1]。

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

UT-143 相关抗体:
药代动力学
(Parmacokinetics)
Species Dose Route T1/2
Rat[1] 20 mg/kg p.o. >12 h
体内研究
(In Vivo)

UT-143 (20 mg/kg；口服；每日一次；连续 13 天) 可强效抑制正常雄性 Sprague-Dawley 大鼠的雄激素依赖性前列腺及精囊生长，且不会改变大鼠的体重或非靶器官重量[1]。
UT-143 (60 mg/kg；口服；每日一次；连续 18 天) 可强效抑制雄性免疫健全 NSG 小鼠体内 AR 阳性 LNCaP-AR 前列腺癌异种移植瘤的生长，肿瘤生长抑制率超过 95%[1]。

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

Animal Model: Sprague-Dawley (male)[1]
Dosage: 20 mg/kg
Administration: p.o.; daily; 13 days
Result: Reduced prostate weight to ~200 mg (vehicle control ~400 mg, P<0.01).
Reduced seminal vesicle weight to ~200 mg (vehicle control ~400 mg, P<0.01).
Had no effect on body weight, lean mass, fat mass, or the weights of the heart, kidney, spleen, and thymus.
Animal Model: NSG (male)[1]
Dosage: 60 mg/kg
Administration: p.o.; daily; 18 days
Result: Achieved greater than 95% tumor growth inhibition, with tumor volume showing a net decrease from baseline over the treatment period.
分子量

462.38

Formula

C20H17F3N6O4
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

UT-143 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:

UT-1432698320-33-9UT143UT 143Androgen ReceptorC327androgen receptor22RV1 prostate cancer cellsSprague-Dawley ratsprostate cancer cellsC406LNCaP-AR prostate cancer xenograftsAR-V7NSG miceSRC-3Inhibitorinhibitorinhibit

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HY-181427
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