2. Metabolic Enzyme/Protease Vitamin D Related/Nuclear Receptor
  3. RAR/RXR
  4. XS-060

XS-060 是一种有效的抗癌剂和 RXRα 拮抗剂。 XS-060 通过抑制 pRXRα-PLK1 相互作用显著诱导 RXRα 依赖性有丝分裂停滞。 XS-060 抑制 p-RXRα 与 PLK1 的相互作用，但对 RXRα 与 RARγ 的异二聚化没有影响。 XS-060 抑制 p-RXRα 和 PLK1 在中心体的原位相互作用。

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XS-060 Chemical Structure

XS-060 Chemical Structure

CAS No. : 2787626-06-4

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XS-060 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

XS-060 is a potent anticancer agent and RXRα antagonist. XS-060 significantly induces RXRα-dependent mitotic arrest by inhibiting pRXRα-PLK1 interaction. XS-060 inhibits p-RXRα interaction with PLK1 but has no effect on RXRα heterodimerization with RARγ. XS-060 inhibits the in situ interaction between p-RXRα and PLK1 at the centrosome[1][2].

IC50 & Target

RXRα (Retinoid X receptor alpha)[1]
体外研究
(In Vitro)

XS-060 靶向 RXRα' 的共激活因子结合位点可抑制 pRXRα-PLK1 相互作用，作为抗有丝分裂剂表现出良好的抗肿瘤活性[1]。
XS-060 对 MDA-MB 231 癌细胞具有抗增殖活性，IC50 为 6.880 ± 0.059 μM[1]。

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

XS-060 相关抗体:

Cell Proliferation Assay[1]

Cell Line: MDA-MB 231, A549, and HepG2
Concentration: 5 μM
Incubation Time:
Result: Showed anti-proliferative activity at 5 μM against cancer cells (MDA-MB 231, A549, and HepG2), with cell viability rate (%) of 51.93 ± 4.32, 82.65 ± 2.84, and 48.65 ± 6.45, respectively.
体内研究
(In Vivo)

XS-060 (25 mg/kg, IP or PO, once) 腹腔注射吸收良好，但口服吸收很差[1]。

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

Animal Model: Sprague-Dawley rats (10-14 weeks, 200-220g)[1]
Dosage: 25 mg/kg
Administration: Oral absorption (p.o.) and intraperitoneal injection (i.p.), once, (Pharmacokinetic Analysis)
Result: The oral absorption of XS-060 is very poor, while intraperitoneal injection displayed good absorption[1].
Pharmacokinetic Parameters of XS-060 in Sprague-Dawley rats[1].
XS060 25 mg/kg (i.p.)
Tmax (h) 2.67 ± 1.12
Cmax (μg/L) 1061.50 ± 399.20
AUC0-∞ (μg⋅h/L) 7040.30 ± 1593.52
T1/2 (h) 2.13 ± 0.05
CLz/F (L/(h⋅kg)) 3.67 ± 0.81
Vd, z/F (L/kg) 11.31 ± 2.71
分子量

334.37

Formula

C20H18N2O3
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

XS-060 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:

XS-0602787626-06-4XS060XS 060RAR/RXRRetinoic acid receptorsRetinoid X receptorsMDA-MB 231A549HepG2antitumoranti-mitoticpRXRα-PLK1 interactionInhibitorinhibitorinhibit

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