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  4. Pro-PTX

Pro-PTX is a Pd-sensitive Paclitaxel (HY-B0015) prodrug with anticancer activity 200 to 700-fold lower than that of the parent compound. Pro-PTX triggers intramolecular cyclization via Pd-catalyzed depropargylation to release active Paclitaxel (HY-B0015) and a non-toxic byproduct. Pro-PTX diffuses efficiently through porous agarose and alginate hydrogel networks, reacts with embedded Pd nanosheets and gets activated. Pro-PTX exhibits significantly reduced 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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Pro-PTX

Pro-PTX Chemical Structure

CAS No. : 3011748-20-9

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Description

Pro-PTX is a Pd-sensitive Paclitaxel (HY-B0015) prodrug with anticancer activity 200 to 700-fold lower than that of the parent compound. Pro-PTX triggers intramolecular cyclization via Pd-catalyzed depropargylation to release active Paclitaxel (HY-B0015) and a non-toxic byproduct. Pro-PTX diffuses efficiently through porous agarose and alginate hydrogel networks, reacts with embedded Pd nanosheets and gets activated. Pro-PTX exhibits significantly reduced 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[1][2].

In Vitro

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; 3 days) co-treatment of A549 cells with Pd hydrogel scaffolds (agarose or alginate) activates the prodrug, resulting in cytotoxicity equivalent to active PTX[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.

Pro-PTX Related Antibodies

Cell Cytotoxicity Assay[1]

Cell Line: human non-small-cell lung carcinoma A549 cells, human glioblastoma U87 cells, human brain vascular pericytes (HBVPs)
Concentration: 0.001-10 μM
Incubation Time: 5 days
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.

Cell Proliferation Assay[1]

Cell Line: human non-small-cell lung carcinoma A549 cells
Concentration: 0.75 μM
Incubation Time: 3 days
Result: Potently inhibited cell proliferation when co-treated with Pd Agarose or Pd Alginate hydrogels, resulting in anticancer activity equivalent to direct treatment with active PTX.

Immunofluorescence[1]

Cell Line: human non-small-cell lung carcinoma A549 cells
Concentration: 0.75 μM
Incubation Time: 48 h
Result: Resulted in clear microtubule accumulation when co-treated with Pd Alginate hydrogels, identical to the pattern observed with active PTX treatment.
In Vivo

Pro-PTX (20 mg/kg; i.p.) activated via Pd-EV-mediated bio-orthogonal catalysis produces a substantial, sustained slowing of xenograft lung tumor growth in BALB/c nu/nu mice[2].
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.

Animal Model: BALB/c nu/nu (6-8-week-old female; subcutaneous xenograft model)[2]
Dosage: 20 mg/kg
Administration: i.p.; 3 doses (2 days and 5 days after first Pd-EV dose, third dose 2 days after second Pd-EV dose)
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.
Animal Model: BALB/c nu/nu (6-8-week-old female)[2]
Dosage: 10-20 mg/kg
Administration: i.p.; twice, separated by 3 days
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.
Molecular Weight

1050.11

Formula

C56H63N3O17
CAS No.
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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Please store the product under the recommended conditions in the Certificate of Analysis.
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References
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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:

Pro-PTX3011748-20-9Drug IntermediateDrug Iintermediatemicrotubule stabilizationhuman brain vascular pericytesU87lung cancernon-small-cell lung carcinomatumor-bearing miceBALB/c nu/nu miceglioblastomaHBVPsA549Inhibitorinhibitorinhibit

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