Pro-PTX
Pro-PTX is a Pd-sensitive Paclitaxel (HY-B0015) prodrug with anticancer activity. Pro-PTX triggers intramolecular cyclization via Pd-catalyzed depropargylation to release active Paclitaxel (HY-B0015) and a non-toxic byproduct. Pro-PTX exhibits low cytotoxicity and antiproliferative activity in cancer cells and non-cancerous human cerebrovascular pericytes. Pro-PTX is applicable for research related to non-small cell lung cancer, glioblastoma and lung cancer.
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- CAS No.: 3011748-20-9
- Formule: C56H63N3O17
- Masse moléculaire:1050.11
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Pro-PTX (0.001-10 μM; 5 days) exhibits low cytotoxicity in A549 (EC50 = 1.75 μM), U87 (EC50 = 0.54 μM), and HBVPs (EC50 = 4.4 μM), with activity only observed at concentrations ≥1 μM[1].
Pro-PTX (100 μM; 10 h) is completely converted to active PTX after incubation with polymer-supported Pd catalyst in PBS at 37 °C[1].
Pro-PTX (0.75 μM; 48 h) co-treatment of A549 cells with Pd Alginate hydrogels activates the prodrug, resulting in microtubule stabilization identical to that induced by active PTX[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:human non-small-cell lung carcinoma A549 cells, human glioblastoma U87 cells, human brain vascular pericytes (HBVPs)
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Concentration:0.001-10 μM
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Incubation Time:5 days
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Result:Reduced cell viability only at concentrations ≥1 μM in A549 cells, with an EC50 value of 1.75 μM.
Reduced cell viability only at concentrations ≥1 μM in U87 cells, with an EC50 value of 0.54 μM.
Showed negligible antiproliferative effect at most tested concentrations in HBVPs, with an EC50 value of 4.4 μM.
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Cell Line:human non-small-cell lung carcinoma A549 cells
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Concentration:0.75 μM
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Incubation Time:48 h
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Result:Resulted in clear microtubule accumulation when co-treated with Pd Alginate hydrogels, identical to the pattern observed with active PTX treatment.
Pro-PTX (10-20 mg/kg; i.p.; twice separated by 3 days) is well-tolerated in healthy BALB/c nu/nu mice with no evidence of hepatocellular or renal toxicity[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nu/nu mice (6-8-week-old female; subcutaneous lung cancer xenograft model)[2]
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Dosage:20 mg/kg
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Administration:i.p.; 3 doses (2 days and 5 days after first Pd-EV dose, third dose 2 days after second Pd-EV dose)
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Result:Stopped tumor growth and temporarily reduced tumor size after the first treatment cycle.
Maintained significantly slower tumor growth rate than control groups for the duration of the study.
Reduced final tumor growth significantly relative to non-treated, pro-PTX-only, and Pd-EV-only control groups.
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Animal Model:BALB/c nu/nu mice (6-8-week-old female)[2]
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Dosage:10-20 mg/kg
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Administration:i.p.; twice, separated by 3 days
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Result:Exhibited weight evolution comparable to non-treated control mice.
Showed no significant differences in plasma levels of ALP, ALT, GGT, BA, ALB, BUN, and CHOL compared to non-treated control mice, with all values within established mouse reference intervals.
Chemical Information
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CAS No. 3011748-20-9
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Masse moléculaire 1050.11
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Formule C56H63N3O17
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SMILES
CC1=C([C@@H](OC(C)=O)C([C@@]2(C)[C@]([C@@](CO3)(OC(C)=O)[C@@]3([H])C[C@@H]2O)([H])[C@@H]4OC(C5=CC=CC=C5)=O)=O)C(C)(C)[C@@]4(O)C[C@@H]1OC([C@H](OC(N(CCN(C(OCC#C)=O)C)C)=O)[C@@H](NC(C6=CC=CC=C6)=O)C7=CC=CC=C7)=O
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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
[1]. Pérez-López AM, et al. Bioorthogonal Uncaging of Cytotoxic Paclitaxel through Pd Nanosheet-Hydrogel Frameworks. J Med Chem. 2020;63(17):9650-9659. [Content Brief]
[2]. Sancho-Albero M, et al. Extracellular Vesicles-Mediated Bio-Orthogonal Catalysis in Growing Tumors. Cells. 2024;13(8):691. Published 2024 Apr 16. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pro-PTX Related Classifications
HY-177482 Related Classifications
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