Paclitaxel [33069-62-4]

Katalog-Nummer HY-B0015-50mg

Size : 50mg

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Paclitaxel est un agent antinéoplasique naturel et stabilise la polymérisation de la tubuline. Paclitaxel peut provoquer à la fois l'arrêt mitotique et la mort cellulaire apoptotique. Paclitaxel induit également l'autophagie.

Paclitaxel ist ein natürlich vorkommendes antineoplastisches Mittel und stabilisiert die tubulinpolymerisation. Paclitaxel kann sowohl einen mitotischen Stillstand als auch apoptotic Zelltod verursachen. Paclitaxel induziert auch autophagy.

Paclitaxel is a naturally occurring antineoplastic agent and stabilizes tubulin polymerization. Paclitaxel can cause both mitotic arrest and apoptotic cell death. Paclitaxel also induces autophagy.

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Paclitaxel Chemische Struktur

CAS. Nr. : 33069-62-4

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Proliferation Assay
WB
Cell Viability Assay
    Paclitaxel (PTX; 3.125, 6.25, 12.5, 25, 50, 100 nM; 48 h) reduces the viability of Hela, SiHa, and C33A cells in a dose-dependent manner.(3.125 nM for Hela cells, 100 nM for SiHa and C33A cells)
    Paclitaxel (PTX; 50 nM; 48 h) increases the expression of Cleaved-caspase-9 and Cleaved-caspase-3 in Hela cells.
    Paclitaxel (25, 50 μM; 24 h) significantly increases the expression of caspase-3 in PK-15 cells.
    Paclitaxel (PTX; 0‑100 nM; 72 h) inhibits the viability of MDA‑MB‑231cells.
    Paclitaxel (CPT; 10-6 -12-10 M; 72 h) demonstrates a strong antitumor activity and an inhibitory of proliferation (IC50 = 6.28 nM) in U937 cells.
    Western blot image and statistical analysis of phosphorylated γH2AX levels in HT-29 cells with different treatments after 48 h. Myricetin and PTX used are 32 μM and 100 nM, respectively.
    The effects of CS1 on polymerized microtubules are also investigated using a cellular tubulin polymer assay. Nocodazole (1 μM) and Paclitaxel (1.5 μM) are used as depolymerization and polymerization controls, respectively.
    Synergistic inhibition of colony formation of ATC cells by E7080 and Paclitaxel. Representative images of colony formation in C643 cells treated with vehicle control (DMSO) or E7080 and Paclitaxel at the indicated concentrations, individually or in combination, are shown in left panel. Quantitative analysis of colony numbers is shown in right panel.
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    Paclitaxel is a naturally occurring antineoplastic agent and stabilizes tubulin polymerization. Paclitaxel can cause both mitotic arrest and apoptotic cell death. Paclitaxel also induces autophagy.

    Traditional Cytotoxic Agents

     

    In Vitro

    Paclitaxel (20 nM; 48 hours) induces programmed cell death and exists a block at the G2/M phase of the cell cycle.
    Paclitaxel (20 nM; 48 hours) induces a consistent increase in the level of p53.

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

    Apoptosis Analysis

    Cell Line: MCF-7, MDA-MB-231 cells
    Concentration: 20 nM
    Incubation Time: 48 hours
    Result: Induced programmed cell death.

    Cell Cycle Analysis

    Cell Line: MCF-7, MDA-MB-231 cells
    Concentration: 20 nM
    Incubation Time: 48 hours
    Result: >60% of MCF-7 cells and 50% of MDA-MB-231 cells were in the G2/M phase following 24 h treament.

    Western Blot Analysis

    Cell Line: MCF-7 cells (harboring wild-type p53)
    Concentration: 20 nM
    Incubation Time: 48 hours
    Result: Induced a consistent increase in the level of p53.
    In Vivo

    Paclitaxel (1-20 mg/kg; i.p.; 1 time/2 days for five cycles) obviously induces liver metastases at the low-Paclitaxel group with little influence on primary tumor growth.

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

    Animal Model: MDA-231 xenograft-bearing mice
    Dosage: 1, 20 mg/kg
    Administration: Intraperitoneal injection; five cycles (1 time/2 days)
    Result: Liver metastases were obviously induced in the low-PTX (1 mg/kg) group with little influence on primary tumor growth compared with high-PTX group.

    853.91

    C47H51NO14

    33069-62-4

    Solid

    White to off-white

    O=C(C1=CC=CC=C1)N[C@@H](C2=CC=CC=C2)[C@H](C(O[C@@H]3C(C)=C([C@@H](OC(C)=O)C([C@@]4(C)[C@]([C@@](CO5)(OC(C)=O)[C@@]5(14)C[C@@H]4O)(14)[C@@H]6OC(C7=CC=CC=C7)=O)=O)C(C)(C)[C@@]6(O)C3)=O)O

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    • Taxus chinensis (Pilger) Rehd.

    Room temperature in continental US; may vary elsewhere.

    4°C, protect from light

    *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

    In Vitro: 

    DMSO : 100 mg/mL (117.11 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : < 0.1 mg/mL (insoluble)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.1711 mL 5.8554 mL 11.7108 mL
    5 mM 0.2342 mL 1.1711 mL 2.3422 mL
    10 mM 0.1171 mL 0.5855 mL 1.1711 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    • Molaritätsrechner

    • Verdünnungsrechner

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.08 mg/mL (2.44 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: 2.08 mg/mL (2.44 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    • Protocol 3

      Add each solvent one by one:  10% DMSO    90% Corn Oil

      Solubility: ≥ 2.08 mg/mL (2.44 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  Corn Oil

      Solubility: 10 mg/mL (11.71 mM); Suspended solution; Need ultrasonic

    • Protocol 2

      Add each solvent one by one:  50% PEG300    50% Saline

      Solubility: 10 mg/mL (11.71 mM); Suspended solution; Need ultrasonic

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

    *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    • [1]. Choi YH, et al. Paclitaxel-induced growth arrest and apoptosis is associated with the upregulation of the Cdk inhibitor, p21WAF1/CIP1, in human breast cancer cells. Oncol Rep. 2012 Dec;28(6):2163-9.  [Content Brief]

      [2]. Dziadyk JM, et al. Paclitaxel-induced apoptosis may occur without a prior G2/M-phase arrest. Anticancer Res. 2004 Jan-Feb;24(1):27-36.  [Content Brief]

      [3]. Li Q, et al. Low doses of paclitaxel enhance liver metastasis of breast cancer cells in the mouse model. FEBS J. 2016 Aug;283(15):2836-52.  [Content Brief]

      [4]. Pan Z, et al. Paclitaxel attenuates Bcl-2 resistance to apoptosis in breast cancer cells through an endoplasmic reticulum-mediated calciumrelease in a dosage dependent manner. Biochem Biophys Res Commun. 2013 Feb 13. pii: S0006-291X(13)00259-3.  [Content Brief]

      [5]. Cadamuro M, et al. Low dose paclitaxel reduces S100A4 nuclear import to inhibit invasion and hematogenous metastasis of cholangiocarcinoma. Cancer Res. 2016 Jun 21.  [Content Brief]

      [6]. Li Q, et al. Low doses of paclitaxel enhance liver metastasis of breast cancer cells in the mouse model. FEBS J. 2016 Jun 16.  [Content Brief]

      [7]. Yilmaz E, et al. Sensory neuron subpopulation-specific dysregulation of intracellular calcium in a rat model of chemotherapy-induced peripheral neuropathy. Neuroscience. 2015 Aug 6;300:210-8.  [Content Brief]

      [8]. Jing C, et al. E7080 enhances the antitumor effects of paclitaxel in anaplastic thyroid cancer. Am J Cancer Res. 2017 Apr 1;7(4):903-912.  [Content Brief]

    • [1]. Choi YH, et al. Paclitaxel-induced growth arrest and apoptosis is associated with the upregulation of the Cdk inhibitor, p21WAF1/CIP1, in human breast cancer cells. Oncol Rep. 2012 Dec;28(6):2163-9.

      [2]. Dziadyk JM, et al. Paclitaxel-induced apoptosis may occur without a prior G2/M-phase arrest. Anticancer Res. 2004 Jan-Feb;24(1):27-36.

      [3]. Li Q, et al. Low doses of paclitaxel enhance liver metastasis of breast cancer cells in the mouse model. FEBS J. 2016 Aug;283(15):2836-52.

      [4]. Pan Z, et al. Paclitaxel attenuates Bcl-2 resistance to apoptosis in breast cancer cells through an endoplasmic reticulum-mediated calciumrelease in a dosage dependent manner. Biochem Biophys Res Commun. 2013 Feb 13. pii: S0006-291X(13)00259-3.

      [5]. Cadamuro M, et al. Low dose paclitaxel reduces S100A4 nuclear import to inhibit invasion and hematogenous metastasis of cholangiocarcinoma. Cancer Res. 2016 Jun 21.

      [6]. Li Q, et al. Low doses of paclitaxel enhance liver metastasis of breast cancer cells in the mouse model. FEBS J. 2016 Jun 16.

      [7]. Yilmaz E, et al. Sensory neuron subpopulation-specific dysregulation of intracellular calcium in a rat model of chemotherapy-induced peripheral neuropathy. Neuroscience. 2015 Aug 6;300:210-8.

      [8]. Jing C, et al. E7080 enhances the antitumor effects of paclitaxel in anaplastic thyroid cancer. Am J Cancer Res. 2017 Apr 1;7(4):903-912.

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.1711 mL 5.8554 mL 11.7108 mL 29.2771 mL
    5 mM 0.2342 mL 1.1711 mL 2.3422 mL 5.8554 mL
    10 mM 0.1171 mL 0.5855 mL 1.1711 mL 2.9277 mL
    15 mM 0.0781 mL 0.3904 mL 0.7807 mL 1.9518 mL
    20 mM 0.0586 mL 0.2928 mL 0.5855 mL 1.4639 mL
    25 mM 0.0468 mL 0.2342 mL 0.4684 mL 1.1711 mL
    30 mM 0.0390 mL 0.1952 mL 0.3904 mL 0.9759 mL
    40 mM 0.0293 mL 0.1464 mL 0.2928 mL 0.7319 mL
    50 mM 0.0234 mL 0.1171 mL 0.2342 mL 0.5855 mL
    60 mM 0.0195 mL 0.0976 mL 0.1952 mL 0.4880 mL
    80 mM 0.0146 mL 0.0732 mL 0.1464 mL 0.3660 mL
    100 mM 0.0117 mL 0.0586 mL 0.1171 mL 0.2928 mL
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    • Cytoskeleton Cell Cycle/DNA Damage Antibody-drug Conjugate/ADC Related Apoptosis Autophagy
    • Microtubule/Tubulin ADC Cytotoxin Apoptosis Autophagy
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    Keywords:

    Paclitaxel33069-62-4Microtubule/TubulinADC CytotoxinApoptosisAutophagyADC PayloadInhibitorinhibitorinhibit

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    Paclitaxel
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