2. Cell Cycle/DNA Damage Apoptosis
  3. Topoisomerase Apoptosis Bcl-2 Family
  4. XSJ81

XSJ81 是一种具有口服活性的抗癌剂。XSJ81 显著抑制壶腹癌 (AC) DPC-X3 细胞的增殖，IC50 为 0.655 μM。XSJ81 抑制 DPC-X3 细胞的集落形成，阻滞细胞周期于 G2/M 期，并抑制细胞迁移。XSJ81 在 DPC-X3 细胞中诱导 DNA 损伤和细胞凋亡 (apoptosis)。XSJ81 在 DPC-X3 异种移植瘤的小鼠中展示出显著的抗肿瘤效能。XSJ81 可用于壶腹癌的研究。

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XSJ81

XSJ81 Chemical Structure

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XSJ81 相关抗体

Top Publications Citing Use of Products

查看 Topoisomerase 亚型特异性产品:

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Topoisomerase Topo I Topo II

查看 Bcl-2 Family 亚型特异性产品:

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Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim BNIP3

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

XSJ81 is an orally active anti-cancer agent. XSJ81 significantly inhibits the proliferation of ampullary carcinoma (AC) DPC-X3 cells with an IC50 of 0.655 μM. XSJ81 inhibits the colony formation, arrests cell cycle at the G2/M phase and inhibits the migration in DPC-X3 cells. XSJ81 induces DNA damage and apoptosis in DPC-X3 cells. XSJ81 demonstrates significant anti-tumor efficacy in mice bearing DPC-X3 xenografts. XSJ81 can be used for the study of ampullary carcinoma[1].

IC50 & Target[1]

Topoisomerase I

 

体外研究
(In Vitro)

XSJ81 (0.35-40 μM, 48 h) 显著抑制壶腹癌 (AC) DPC-X3 细胞的增殖，IC50 为 0.655 μM[1]。
XSJ81 (0.35-1.4 μM, 48 h) 以剂量依赖性方式降低 DPC-X3 细胞中 EdU 荧光强度[1]。
XSJ81 (0.003-0.011 μM, 2 周) 以剂量依赖性方式抑制 DPC-X3 细胞的集落形成[1]。
XSJ81 (0.35-1.4 μM, 24-48 h) 使 DPC-X3 细胞阻滞于 G2/M 期，诱导剂量依赖性的细胞凋亡并抑制 DPC-X3 细胞的迁移[1]。
XSJ81 (0.35-1.4 μM, 24 h) 在 DPC-X3 细胞核中诱导剂量依赖性的 γ-H2AX 灶形成[1]。
XSJ81 (200-500 μM, 30 min) 阻断 Topo I 对超螺旋 pBR322 质粒 DNA 的松弛作用，保持质粒处于超螺旋状态，并促进 Topo I 蛋白的蛋白酶体降解[1]。
XSJ81 (100-1000 nM, 0-72 h) 在腺样囊性癌类器官 (ACOs) 中诱导时间和剂量依赖性的细胞毒性[1]。

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

XSJ81 相关抗体:

Cell Cycle Analysis[1]

Cell Line: DPC-X3 cells
Concentration: 0.35, 0.7, 1.4 μM
Incubation Time: 24 h
Result: Down-regulated S-phase marker CCNA1.
Up-regulated G0/G1-phase regulators CNE1 and P53.

Apoptosis Analysis[1]

Cell Line: DPC-X3 cells
Concentration: 0.35, 0.7, 1.4 μM
Incubation Time: 48 h
Result: Induced dose-dependent apoptosis in DPC-X3 cells.
Up-regulated pro-apoptotic protein BAX.
Down-regulated anti-apoptotic protein Bcl-2.
体内研究
(In Vivo)

XSJ81 (100 mg/kg，灌胃给药，单次给药，3-14 天) 在 6 周龄雌性 BALB/c 小鼠中无死亡率[1]。
XSJ81 (5-10 mg/kg，腹腔给药，每 48 小时一次，持续 14 天) 在承载 DPC-X3 异种移植瘤的裸鼠中展示出显著的抗肿瘤效能[1]。

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

Animal Model: DPC-X3 cellular suspensions were subcutaneously injected into the right axillary of the nude mice through orthotopic transplantation procedure to construct the DPC-X3 xenograft model[1]
Dosage: 5 mg/kg and 10 mg/kg
Administration: i.p., once every 48 h, 14 days
Result: Achieved significant tumor growth inhibition.
Showed no significant changes in body weight.
Induced extensive apoptotic areas in tumor tissues.
分子量

604.63

Formula

C30H28N4O8S
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

XSJ81 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:

XSJ81XSJ 81XSJ-81TopoisomeraseApoptosisBcl-2 Familyampullary carcinomaDPC-X3 cellsInhibitorinhibitorinhibit

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