2. Apoptosis
  3. Bcl-2 Family
  4. Navitoclax

Navitoclax (ABT-263) est un protéine de la famille Bcl-2 puissant et actif par voie orale qui se lie à de multiples protéines anti-apoptotiques de la famille Bcl-2, telles que Bcl-xL, Bcl-2 et Bcl-w, avec un Ki inférieur à 1 nM.

Navitoclax (ABT-263) ist ein wirksamer und oral wirksamer Proteininhibitor der Bcl-2-Familie, der an mehrere antiapoptotische Proteine ​​der Bcl-2-Familie wie Bcl-xL, Bcl-2 und Bcl-w mit einem Ki von weniger bindet als 1 nM.

Navitoclax (ABT-263) is a potent and orally active Bcl-2 family protein inhibitor that binds to multiple anti-apoptotic Bcl-2 family proteins, such as Bcl-xL, Bcl-2 and Bcl-w, with a Ki of less than 1 nM.

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

Navitoclax Chemical Structure

Navitoclax Chemical Structure

CAS No. : 923564-51-6

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 75 In-stock
Solution
10 mM * 1 mL in DMSO USD 75 In-stock
Solid
1 mg USD 25 In-stock
5 mg USD 50 In-stock
10 mg USD 70 In-stock
50 mg USD 180 In-stock
100 mg USD 250 In-stock
500 mg USD 800 In-stock
1 g   Get quote  
5 g   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 89 publication(s) in Google Scholar

Other Forms of Navitoclax:

Navitoclax Related Antibodies

Top Publications Citing Use of Products

87 Publications Citing Use of MCE Navitoclax

Proliferation Assay
WB

    Navitoclax purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2018 Sep 24;9(10):986.  [Abstract]

    Cells are treated with 25 nM siRNA for 48 hours followed by 1 μM ABT-263 for 36 hours.

    Navitoclax purchased from MedChemExpress. Usage Cited in: ACS Med Chem Lett. 2015 Jun 22;6(8):948-52.  [Abstract]

    Combination treatment. (a) Comparison of AZD-8055 and ABT-263 treatment in all cell lines. Red indicates sensitivity, while blue indicates resistance. (b) Depiction of synergism where the values shown are excess over Bliss Independence, a prediction of inhibition without synergism. Increased synergism is evident by an increased number, shown in red, while negative numbers in blue represent an antagonistic effect.

    View All Bcl-2 Family Isoform Specific Products:

    View All Isoforms
    Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Navitoclax (ABT-263) is a potent and orally active Bcl-2 family protein inhibitor that binds to multiple anti-apoptotic Bcl-2 family proteins, such as Bcl-xL, Bcl-2 and Bcl-w, with a Ki of less than 1 nM[1].

    IC50 & Target[1]

    Bcl-W

    1 nM (Ki)

    Bcl-xL

    1 nM (Ki)

    Bcl-2

    1 nM (Ki)

    In Vitro

    Navitoclax (ABT-263) is active against approximately one-half of the cell lines of the PPTP in vitro panel. The median IC50 for all of the lines in the panel is 1.91 μM[1]. Navitoclax in combination with chemotherapy agents leads most ovarian cancer cell lines a synergistic response, and enhances the caspase activation in both SK-OV-3 and IGROV-1 cell lines[2].

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

    Navitoclax Related Antibodies
    In Vivo

    Navitoclax (100 mg/kg; orally; 21-day treatment) enhances the activity of OSI-744 in vivo. As a single agent, 100 mg/kg Navitoclax alone dosed daily has no significant antitumor activity, whereas daily dosing of OSI-744 at 50 mg/kg results in significant tumor stasis (%TGI=52) during a 21-day treatment period. Notably, the combination of Navitoclax and OSI-744 dosed daily for 21 consecutive days results in 98% TGI and durable tumor regressions in 100% of treated tumor-bearing mice[3].

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

    Animal Model: Mice with NCI-H1650 model[3]
    Dosage: 100 mg/kg
    Administration: Orally; daily; for 21 consecutive days
    Result: As a single agent, 100 mg/kg alone dosed daily had no significant antitumor activity. Notably, the combination with OSI-744 resulted in 98% TGI and durable tumor regressions in 100% of treated tumor-bearing mice.
    Clinical Trial
    Molecular Weight

    974.61

    Formula

    C47H55ClF3N5O6S3
    CAS No.
    Appearance

    Solid

    Color

    White to light yellow

    SMILES

    O=S(C1=CC(S(NC(C2=CC=C(N3CCN(CC4=C(CCC(C)(C4)C)C5=CC=C(Cl)C=C5)CC3)C=C2)=O)(=O)=O)=CC=C1N[C@H](CCN6CCOCC6)CSC7=CC=CC=C7)(C(F)(F)F)=O
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMF : ≥ 100 mg/mL (102.61 mM)

    DMSO : 75 mg/mL (76.95 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.0261 mL 5.1303 mL 10.2605 mL
    5 mM 0.2052 mL 1.0261 mL 2.0521 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • Molarity Calculator

    • Dilution Calculator

    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 In Vitro approach 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% Ethanol    60% Phosal 50 PG    30% PEG400

      Solubility: 7.5 mg/mL (7.70 mM); Clear solution; Need ultrasonic

    • Protocol 2

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

      Solubility: 2.08 mg/mL (2.13 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 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.
    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).
    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.
    Purity & Documentation

    Purity: 99.97% ee.: 99.92%

    COA (252 KB) HNMR (233 KB) LCMS (122 KB) Elemental Analysis Report (109 KB)

    Handling Instructions (2659 KB)
    References

    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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO / DMF 1 mM 1.0261 mL 5.1303 mL 10.2605 mL 25.6513 mL
    5 mM 0.2052 mL 1.0261 mL 2.0521 mL 5.1303 mL
    10 mM 0.1026 mL 0.5130 mL 1.0261 mL 2.5651 mL
    15 mM 0.0684 mL 0.3420 mL 0.6840 mL 1.7101 mL
    20 mM 0.0513 mL 0.2565 mL 0.5130 mL 1.2826 mL
    25 mM 0.0410 mL 0.2052 mL 0.4104 mL 1.0261 mL
    30 mM 0.0342 mL 0.1710 mL 0.3420 mL 0.8550 mL
    40 mM 0.0257 mL 0.1283 mL 0.2565 mL 0.6413 mL
    50 mM 0.0205 mL 0.1026 mL 0.2052 mL 0.5130 mL
    60 mM 0.0171 mL 0.0855 mL 0.1710 mL 0.4275 mL
    DMF 80 mM 0.0128 mL 0.0641 mL 0.1283 mL 0.3206 mL
    100 mM 0.0103 mL 0.0513 mL 0.1026 mL 0.2565 mL
    • No file chosen (Maximum size is: 1024 Kb)
    • If you have published this work, please enter the PubMed ID.
    • Your name will appear on the site.

    Navitoclax Related Classifications

    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:

    Navitoclax923564-51-6ABT-263ABT263ABT 263Bcl-2 FamilyInhibitorinhibitorinhibit

    Your Recently Viewed Products:

    Inquiry Online

    Your information is safe with us. * Required Fields.

    Product Name

    		  

    Salutation

    Applicant Name *

    		 

    Email Address *

    Phone Number *

    		 

    Organization Name *

    Department *

    		 

    Requested quantity *

    Country or Region *

    		      

    Remarks

    Bulk Inquiry

    Inquiry Information

    Product Name:
    Navitoclax
    Cat. No.:
    HY-10087
    Quantity:
    MCE Japan Authorized Agent:

    Customer Review

    Thank You for Your Feedback!

    Request for HNMR Report

    Please fill out this form to request the QC report. We will send it to your Email address shortly.

    Your information is safe with us. * Required Fields.

    Product Name

    		  

    Lot #

    Applicant Name *

    		 

    Email Address *

    Phone Number

    		 

    Department *

    Organization Name *

    		 

    Country or Region *

    Remarks

    Request for HNMR Report

    We have received your request and will respond to you as soon as possible.