MXC-017
MXC-017 is a blood-brain barrier (BBB)-penetrant apoptosis inducer that directly targets Vimentin (VIM). MXC-017 prevents radiation-induced glioma stem cell (GSC) formation, while promoting G0/G1 cell cycle arrest and apoptosis. MXC-017 exhibits minimal off-target effects and shows no significant cytotoxicity. MXC-017 significantly prolongs median survival when used in combination with radiation therapy in glioblastoma (GBM) mouse models.
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- CAS No.: 3037024-97-5
- Formule: C21H23N3O3S
- Masse moléculaire:397.49
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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Activité biologique
MXC-017 (1-10 μM, 5-7 days) displays no radiosensitizing effect, but prevents radiation-induced induction of marker-positive cells, and dose-dependently reduces sphere formation in HK-374, HK-345 and HK-157 cells with acceleration of GSC exhaustion in HK-374 and HK-217 cells at 10 μM[1].
MXC-017 (1-10 μM, 10 days) significantly reduces GSC frequencies alone or combination with radiation in HK-374, HK-390, HK-217, HK-146, HK-308 and HK-345 cells[1].
MXC-017 (10 µM, 2-5 days) increases the radiation-induced G0/G1 arrest with reduction number of cells in S phase, and significantly increases the proportion of apoptotic cells after 4 Gy irradiation in HK-374 cells[1].
MXC-017 (10 µM, 0.25-24 h) binds to vimentin and prevents decompaction of vimentin intermediate filaments, with no protein levels change in total vimentin and phosphorylation of Ser39, Ser56, or Ser83 in HK-374 cells[1].
MXC-017 (10 µM, 6-24 h) reduces detectable baseline levels of vimentin and preventes the radiation induced increase of the vimentin signal, while no change in total vimentin levels in HK-374 cells [1].
MXC-017 (10 µM, 16-24 h) significantly suppresses the migratory capacity of HK-374 cell with combination of radiation in an independent manner[1].
MXC-017 (10 µM, 48 h) has no off-target effects with no metabolic modulation changes, but induces 357 differentially expressed genes (239 up, 118 down), enriching KRAS activation (pro-inflammatory response) and suppressing E2F/G2M checkpoint, without cellular composition changes in HK-374, HK-390, HK-217 and HK-244 cells[1].
MXC-017 (1-10 µM, 24 h) causes no significant toxicity in NSP cells (up to 2.5 µM), NIH3T3 and EOC20 cells (up to 10 µM), but significant decreases plating efficacy in normal human astrocytes[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HK-374 cells
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Concentration:10 μM, with or without a single dose of 4 Gy irradiation
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Incubation Time:16-24 h
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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.
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Cell Line:HK-374 cells
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Concentration:10 μM, with or without a single dose of 4 Gy irradiation
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Incubation Time:2 or 5 days
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Result:Enhanced the radiation-induced G0/G1 arrest and reduced the number of cells in S phase after 4 Gy irradiation.
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Cell Line:HK-374 cells
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Concentration:10 μM, with or without a single dose of 4 Gy irradiation
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Incubation Time:72 h
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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.
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Cell Line:HK-374 cells
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Concentration:10 μM
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Incubation Time:0.25, 0.5, 1, 2, 4, 6, 24 h
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Result:Did not change the protein levels of total vimentin or phosphorylation of Ser39, Ser56, or Ser83 by using a polyclonal antibody.
MXC-017 (150-900 mg/kg, i.p., once or 5 consecutive days per week for 2 weeks) cause a maximum tolerated dose of 150 mg/kg without clinical signs of toxicity and significant hematological or biochemical abnormalities in C57BL/6 mice model[1].
MXC-017 (150 mg/kg, i.p., 5-days on/2-days off for ＞140 days) significantly reduces the probability for tumor related death in PDOX GBM mice model with combination of radiation[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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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].
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Dosage:50 mg/kg or irradiation (4 or 10 Gy)
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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.
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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.
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Animal Model:Female and male C57BL/6 mice (6-8 weeks old)[1].
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Dosage:Once administration (150, 300, 600, and 900 mg/kg), repeated administration (150, 300, 600 mg/kg)
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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.
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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.
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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].
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Dosage:150 mg/kg, 66 mg/kg (Temozolomide), irradiation
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Administration:i.p., (Temozolomide: p.o.), 5-days on / 2-days off for ＞140 days.
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Result:Significantly reduced the probability for tumor related death compared in PDOX GBM mice model with combination of radiation, outperforming Temozolomide.
Chemical Information
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CAS No. 3037024-97-5
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Masse moléculaire 397.49
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Formule C21H23N3O3S
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SMILES
O=C(NCC1=CC=C(S(=O)(N2CCCCC2)=O)C=C1)N3C4=CC=CC=C4C=C3
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
MXC-017 Related Classifications
HY-174212 Related Classifications
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