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  4. 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.

For research use only. We do not sell to patients.

Pro-PTX

Pro-PTX Chemical Structure

CAS No. : 3011748-20-9

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Pro-PTX Related Antibodies

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Description

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[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; 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.

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 mice (6-8-week-old female; subcutaneous lung cancer 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 mice (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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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Pro-PTX Related Classifications

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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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