2. Apoptosis
  3. Apoptosis
  4. MXC-017

MXC-017 是一种可穿透血脑屏障的的凋亡 (apoptosis) 诱导剂，可直接靶向 glioma stem cells (GSCs)。MXC-017 可阻止放射诱导的 GSC 形成但增加 G0/G1 细胞停滞和细胞凋亡 (apoptosis)。MXC-017 具有极小的脱靶效应，且浓度高至 10 µM 时无显著细胞毒性。MXC-017 显著延长了患者来源的原位异种移植 (PDOX) 胶质母细胞瘤 (GBM) 小鼠模型中联合放射治疗的中位生存期。

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MXC-017 Chemical Structure

MXC-017 Chemical Structure

CAS No. : 3037024-97-5

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MXC-017 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

MXC-017 is a BBB-penetrable apoptosis inducer, directly targeting glioma stem cells (GSCs). MXC-017 prevents radiation-induced GSC formation but increases G0/G1 arrest and apoptosis. MXC-017 has minimal off-target effects with no significant cell toxicity up to 10 µM. MXC-017 significantly extends median survival in patient-derived orthotopic xenograft (PDOX) glioblastoma (GBM) mice models with combination of radiation[1].

体外研究
(In Vitro)

MXC-017 (1-10 μM，5-7 天) 未表现出放射增敏作用，但可阻止放射诱导的标志物阳性细胞的诱导，并以剂量依赖性方式减少 HK-374、HK-345 和 HK-157 细胞中的球体形成，同时加速 HK-374 和 HK-217 细胞中 GSC 的耗竭 (10 μM) [1]。
MXC-017 (1-10 μM，10 天) 单独使用或与放射联用均可显著降低 HK-374、HK-390、HK-217、HK-146、HK-308 和 HK-345 细胞中的 GSC 频率[1]。
MXC-017 (10 µM，2-5 天) 在 4 Gy 放射诱导后，可增加 HK-374 细胞中放射诱导的 G0/G1 停滞，减少 S 期细胞数量，并显著增加凋亡细胞比例[1]。
MXC-017 (10 µM，0.25-24 小时) 可与 HK-374 细胞中波形蛋白结合，阻止波形蛋白中间丝的分解，同时不影响总波形蛋白的蛋白水平以及 Ser39、Ser56 或 Ser83 的磷酸化[1]。
MXC-017 (10 µM，6-24 小时) 可降低 HK-374 细胞中可检测的基线波形蛋白水平，并阻止放射诱导的波形蛋白信号增强，同时不影响总波形蛋白的水平[1]。
MXC-017 (10 µM，16-24 小时) 与放射联用时，以独立的方式显著抑制 HK-374 细胞的迁移能力[1]。
MXC-017 (10 µM，48 小时) 没有脱靶效应，也没有代谢调节变化，但诱导了 357 个差异表达基因 (239 个上调，118 个下调)，且这些基因富集于 KRAS 通路激活 (促炎反应) 和 E2F/G2M 检查点抑制，而不改变 HK-374、HK-390、HK-217 和 HK-244 细胞中的细胞组成[1]。
MXC-017 (1-10 µM，24 小时) 对 NSP 细胞 (高达 2.5 µM) 、NIH3T3 和 EOC20 细胞 (高达 10 µM) 无显著毒性，但会显著降低正常人星形胶质细胞的接种效率[1]。

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

MXC-017 相关抗体:

Cell Migration Assay [1]

Cell Line: HK-374 cells
Concentration: 10 μM, with or without a single dose of 4 Gy irradiation
Incubation Time: 16-24 h
Result: Significantly reduced the migratory capacity of GBM cells with little cells penetrating through the membrane.
Displayed Markedly impaired migration compared to untreated or radiation-only controls.

Cell Cycle Analysis[1]

Cell Line: HK-374 cells
Concentration: 10 μM, with or without a single dose of 4 Gy irradiation
Incubation Time: 2 or 5 days
Result: Enhanced the radiation-induced G0/G1 arrest and reduced the number of cells in S phase after 4 Gy irradiation.

Apoptosis Analysis[1]

Cell Line: HK-374 cells
Concentration: 10 μM, with or without a single dose of 4 Gy irradiation
Incubation Time: 72 h
Result: Did not induce apoptosis with 4 Gy irradiation or treatment alone.
Significantly reduced the viable cell population and increased the proportion of apoptotic cells in combination with 4 Gy irradiation.

Western Blot Analysis[1]

Cell Line: HK-374 cells
Concentration: 10 μM
Incubation Time: 0.25, 0.5, 1, 2, 4, 6, 24 h
Result: Did not change the protein levels of total vimentin or phosphorylation of Ser39, Ser56, or Ser83 by using a polyclonal antibody.
体内研究
(In Vivo)

MXC-017 (50 mg/kg，腹腔注射，给药 5 天/停药 2 天，共 2 周，4 或 10 Gy 放射) 显著延长了 PDOX GBM 小鼠模型中的中位生存期，并有效消除了植入的 HK-374 细胞，同时对正常脑组织损伤极小[1]。
MXC-017 (150-900 mg/kg，腹腔注射，每周一次或连续 5 天，共 2 周) 在 C57BL/6 小鼠模型中，最大耐受剂量为 150 mg/kg，未出现临床毒性症状，也未出现显著的血液学或生化异常[1]。
MXC-017 (150 mg/kg，腹腔注射，给药 5 天/停药 2 天，共＞140 天) 与放射疗法相结合，显著降低了 PDOX GBM 小鼠模型的肿瘤相关死亡的概率[1]。

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

Animal Model: Female and male NSG mice (6-8 weeks old) were implanted into the right striatum of the brains with HK-374 cells (2 × 105 cells/mouse)[1].
Dosage: 50 mg/kg or irradiation (4 or 10 Gy)
Administration: i.p., 5-days on/2-days off for 2 weeks after implanting HK-374 cells 3 days, and then collected brain and tumors samples.
Result: Reduced the number of spheres formation and significantly decreased the GSC frequency by MXC-017 treatment alone and in combination with 4 Gy radiation.
Significantly increased the median survival from 34 to 60 days in PDOX GBM mice model with combination of 10 Gy radiation.
Effectively eliminated implanted HK-374 cells in combination with 10 Gy radiation.
Caused tumor-free in long-term surviving PDOX GBM mice at the time of euthanasia in combination with 10 Gy radiation.
Did not change the proportions of the cell types in PDOX GBM mice model.
Effectively eliminated nestin-positive human tumor cells without loss of olig2-positive oligodendrocytes in the contralateral (non-tumor-bearing) hemisphere in combination with 10 Gy radiation.
Animal Model: Female and male C57BL/6 mice (6-8 weeks old)[1].
Dosage: Once administration (150, 300, 600, and 900 mg/kg), repeated administration (150, 300, 600 mg/kg)
Administration: i.p., once in pairs (1 male/1 female) or 5 consecutive days per week in groups (3 male/ 3 female) for 2 weeks.
Result: Caused no signs of toxicity with once administration up to 900 mg/kg.
Caused no clinical signs of toxicity and no significant hematological or biochemical abnormalities with repeated administration up to 600 mg/kg.
Caused mild toxicity with perivascular inflammation and superficial vasculitis at 150 mg/kg and acute pneumonia at 600 mg/kg in the lungs with repeated administration.
Caused focal interstitial inflammation in the kidney cortex at 300 mg/kg with repeated administration.
Caused focal lobular inflammation and hepatocellular necrosis in liver at 600 mg/kg with repeated administration.
Animal Model: Female and male NSG mice (6-8 weeks old) were implanted into the right striatum of the brains with 17 different PDOXs cells [1].
Dosage: 150 mg/kg, 66 mg/kg (Temozolomide), irradiation
Administration: i.p., (Temozolomide: p.o.), 5-days on / 2-days off for ＞140 days.
Result: Significantly reduced the probability for tumor related death compared in PDOX GBM mice model with combination of radiation, outperforming Temozolomide.
分子量

397.49

Formula

C21H23N3O3S
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

MXC-017 相关分类

  • 摩尔计算器

  • 稀释计算器

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  • Do most proteins show cross-species activity?

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Keywords:

MXC-0173037024-97-5MXC017MXC 017ApoptosisAnticancerRadiationVimentinGlioma stem cellsGSCsHK-374 cellsPDOX GBM modelInhibitorinhibitorinhibit

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