2. Apoptosis Anti-infection
  3. IAP Apoptosis HIV
  4. Birinapant

Birinapant (TL32711), a bivalent Smac mimetic, is a potent antagonist for XIAP and cIAP1 with Kds of 45 nM and less than 1 nM, respectively. Birinapant (TL32711) induces the autoubiquitylation and proteasomal degradation of cIAP1 and cIAP2 in intact cells, which results in formation of a RIPK1: caspase-8 complex, caspase-8 activation, and induction of tumor cell death. Birinapant (TL32711) targets TRAF2-associated cIAPs and abrogates TNF-induced NF-κB activation.

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Birinapant Chemical Structure

Birinapant Chemical Structure

CAS No. : 1260251-31-7

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10 mM * 1 mL in DMSO
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Customer Review

Based on 27 publication(s) in Google Scholar

Birinapant Related Antibodies

Top Publications Citing Use of Products

    Birinapant purchased from MedChemExpress. Usage Cited in: Cell. 2019 Jul 25;178(3):585-599.e15.  [Abstract]

    Western blot analysis of polyclonal pools of sgCtrl or sgTRAF2-expressing SK-MEL-23 melanoma cells in the presence or absence of Birinapant, and upon coculture with MART-1 T cell for indicated amounts of time.

    Birinapant purchased from MedChemExpress. Usage Cited in: Front Microbiol. 2018 Sep 19;9:2022.  [Abstract]

    ACH-2 cells are exposed to Birinapant (50 nM) in the presence or absence of PEP005 (5 nM), with TNF-α (10 ng/ml) co-treatment for 24 h, and cell lysates are used for WB analysis.

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    cIAP cIAP-1 cIAP-2 XIAP

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    • Purity & Documentation

    • References

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    Description

    Birinapant (TL32711), a bivalent Smac mimetic, is a potent antagonist for XIAP and cIAP1 with Kds of 45 nM and less than 1 nM, respectively. Birinapant (TL32711) induces the autoubiquitylation and proteasomal degradation of cIAP1 and cIAP2 in intact cells, which results in formation of a RIPK1: caspase-8 complex, caspase-8 activation, and induction of tumor cell death. Birinapant (TL32711) targets TRAF2-associated cIAPs and abrogates TNF-induced NF-κB activation.

    IC50 & Target

    Kd: 45 nM (XIAP), <1 nM (cIAP1)[1]
    In Vitro

    Birinapant (TL32711) (30-10000 nM; 24 hours) significantly decreases the viability of SUM190 cells in a dose-dependent manner[1].
    ? Birinapant (TL32711) (30-1000 nM; 4 hours) shows a significant decrease in cIAP1 levels and enhanced PARP cleavage, and induces apoptosis[1].
    ? Birinapant (TL32711) binds with high affinity to the isolated BIR3 domains of cIAP1, cIAP2, and XIAP and the single BIR domain of ML-IAP and rapidly degrades TRAF2-bound cIAP1 and cIAP2 thereby inhibiting TNF-mediated NF-κB activation[1].

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

    Birinapant Related Antibodies

    Cell Viability Assay[1]

    Cell Line: TRAIL-resistant SUM190 IBC cells
    Concentration: 30, 100, 300, 1000, 10000 nM
    Incubation Time: 24 hours
    Result: Significantly decreased the viability of SUM190 cells in a dose-dependent manner.

    Western Blot Analysis[1]

    Cell Line: SUM190 cells
    Concentration: 30, 300, 1000 nM
    Incubation Time: 4 hours
    Result: Showed a significant decrease in cIAP1 levels and enhanced PARP cleavage.
    In Vivo

    Birinapant (TL32711) (30 mg/kg; i.p.; every third day (*5)) shows antitumor efficacy and are devoid of overt toxicity in preclinical models[2].

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

    Animal Model: Female athymic nude mice (low-passage, patient-derived xenotransplant models of ovarian cancer, colorectal cancer, and melanoma)[2]
    Dosage: 30 mg/kg
    Administration: Intraperitoneal injection; every third day (*5)
    Result: Resulted in inhibition of tumor growth.
    Clinical Trial
    Molecular Weight

    806.94

    Formula

    C42H56F2N8O6
    CAS No.
    Appearance

    Solid

    Color

    Off-white to light yellow

    SMILES

    FC1=CC2=C(C=C1)C(C[C@H]3N(C([C@@H](NC([C@@H](NC)C)=O)CC)=O)C[C@@H](O)C3)=C(C(N4)=C(C[C@H]5N(C([C@@H](NC([C@@H](NC)C)=O)CC)=O)C[C@@H](O)C5)C6=C4C=C(F)C=C6)N2
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 125 mg/mL (154.91 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.2392 mL 6.1962 mL 12.3925 mL
    5 mM 0.2478 mL 1.2392 mL 2.4785 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    • Molarity Calculator

    • Dilution Calculator

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

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    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% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.08 mg/mL (2.58 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 (2.58 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.
    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: 99.70%

    COA (256 KB) HNMR (221 KB) RP-HPLC (114 KB) LCMS (114 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, 6 months; -20°C, 1 month. 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 1.2392 mL 6.1962 mL 12.3925 mL 30.9812 mL
    5 mM 0.2478 mL 1.2392 mL 2.4785 mL 6.1962 mL
    10 mM 0.1239 mL 0.6196 mL 1.2392 mL 3.0981 mL
    15 mM 0.0826 mL 0.4131 mL 0.8262 mL 2.0654 mL
    20 mM 0.0620 mL 0.3098 mL 0.6196 mL 1.5491 mL
    25 mM 0.0496 mL 0.2478 mL 0.4957 mL 1.2392 mL
    30 mM 0.0413 mL 0.2065 mL 0.4131 mL 1.0327 mL
    40 mM 0.0310 mL 0.1549 mL 0.3098 mL 0.7745 mL
    50 mM 0.0248 mL 0.1239 mL 0.2478 mL 0.6196 mL
    60 mM 0.0207 mL 0.1033 mL 0.2065 mL 0.5164 mL
    80 mM 0.0155 mL 0.0775 mL 0.1549 mL 0.3873 mL
    100 mM 0.0124 mL 0.0620 mL 0.1239 mL 0.3098 mL
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    Birinapant 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:

    Birinapant1260251-31-7TL32711TL 32711TL-32711IAPApoptosisHIVHuman immunodeficiency virusInhibitorinhibitorinhibit

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