2. PI3K/Akt/mTOR
  3. PI3K
  4. Taselisib

Taselisib (GDC-0032) is a potent PI3K inhibitor targets PIK3CA mutations, with Kis of 0.12 nM, 0.29 nM, 0.97 nM, and 9.1 nM for PI3Kδ, PI3Kα, PI3Kγ and PI3Kβ, respectively.

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No. CAS : 1282512-48-4

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10 mM * 1 mL in DMSO
ready for reconstitution
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Revisión del cliente

Based on 21 publication(s) in Google Scholar

Taselisib Related Antibodies

Top Publications Citing Use of Products

    Taselisib purchased from MedChemExpress. Usage Cited in: Cell Discov. 2016 Sep 20:2:16030.  [Abstract]

    Effects of combined inhibition of PI3K and STAT3 pathways on PTEN-mutated T-ALL cells. (a) Short-term treatment of Ba/F3-shPTEN-NTRK2-Tel cells with isoform-selective inhibitors and Pan-PI3K inhibitor GDC-0032. Cells are treated with DMSO, BYL719, KIN193, GS-1101, GDC-0032 (1 μM) or JAK–STAT inhibitor AZD-1480 (1 μM) for 3 h (n=3) for each treatment. (b) Immunoblot analysis of P-Akt and p-S6 in PF382 and JURKAT cells. Cells are treated with the same inhibitors as in a. (c) Combination of siNTRK2

    Taselisib purchased from MedChemExpress. Usage Cited in: Br J Cancer. 2016 Jul 26;115(3):303-11.  [Abstract]

    Effect of the combination of CYC065 and Taselisib in vitro. (A) Uterine serous carcinoma-ARK-1 and USC-ARK-2 are treated with the half-maximal inhibitory concentration (IC50) of CYC065, the IC50 of Taselisib (GDC0032) or the combination of the IC50s of the two compounds for 72 h. Cell counting is then carried. The incubation of USC-ARK-1 and USC-ARK-2 cells with the combination of CYC065 and Taselisib is significantly more effective in inhibiting cells’ growth th

    Ver todos los productos específicos de isoformas PI3K:

    Ver todas las isoformas
    PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

    • Actividad biológica

    • Protocolo

    • Pureza y Documentación

    • Referencias

    • Revisión del cliente

    Descripciòn

    Taselisib (GDC-0032) is a potent PI3K inhibitor targets PIK3CA mutations, with Kis of 0.12 nM, 0.29 nM, 0.97 nM, and 9.1 nM for PI3Kδ, PI3Kα, PI3Kγ and PI3Kβ, respectively.

    IC50 & Target[3]

    PI3Kδ

    0.12 nM (Ki)

    PI3Kα

    0.29 nM (Ki)

    PI3Kγ

    0.97 nM (Ki)

    PI3Kβ

    9.1 nM (Ki)

    Cellular Effect
    Cell Line Type Value Description References
    PC-3 EC50
    0.571 μM
    Compound: 11l, GDC-0032
    Cytotoxicity against human PC3 cells
    Cytotoxicity against human PC3 cells
    		[PMID: 23662903]
    PC-3 IC50
    0.031 μM
    Compound: 11l, GDC-0032
    Inhibition of PI3Kalpha in human PC3 cells assessed as reduction of AKT phosphorylation
    Inhibition of PI3Kalpha in human PC3 cells assessed as reduction of AKT phosphorylation
    		[PMID: 23662903]
    In Vitro

    Taselisib (GDC-0032) (100 nM) inhibits AKT/mTOR signaling in PIK3CA mutant cell lines but not in cells with loss or mutation of PTEN; Taselisib (GDC-0032) enhances radiation-induced apoptosis and inhibits growth in head and neck cancer cell lines that are sensitive to its single-agent activiy[1]. Taselisib (GDC-0032) enhances the effects of MEK1/2 inhibition on both BRAFV600E/PTENNull human melanoma cells autochthonous mouse melanomas[2].

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

    Taselisib Related Antibodies
    In Vivo

    Taselisib (GDC-0032) (5 mg/kg, p.o.) potently impairs PI3K signaling and enhances the efficacy of fractionated radiotherapy; Taselisib (GDC-0032) and radiation is more effective than either treatment alone in nude mice implanted with subcutaneous Cal-33 xenografts[1]. The vehicle-treated BRAFV600E/PTENNull melanoma-bearing mice experiencs initial tumor regression after treatment with Taselisib (GDC-0032) (22.5 mg/kg, p.o.)[2].

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

    460.53

    Fòrmula

    C24H28N8O2
    No. CAS
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    CC(C)N1C(C2=CN3C(C(C(OCC3)=C4)=CC=C4C5=CN(C(C)(C(N)=O)C)N=C5)=N2)=NC(C)=N1
    Envío

    Room temperature in continental US; may vary elsewhere.
    Almacenamiento
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 1 year
    -20°C 6 months
    Solvente y solubilidad
    In Vitro: 

    DMSO : 25 mg/mL (54.29 mM; ultrasonic and warming and heat to 60°C; 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 2.1714 mL 10.8571 mL 21.7141 mL
    5 mM 0.4343 mL 2.1714 mL 4.3428 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    • Calculadora de molaridad

    • Calculadora de dilución

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

      Solubility: ≥ 2.5 mg/mL (5.43 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (5.43 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
    Pureza y Documentación

    Purity: 99.75%

    SDS (393 KB)

    COA (257 KB) LCMS (93 KB)

    Instrucciones de manejo (2659 KB)
    Referencias
    Ensayo celular
    [1]

    Cells are seeded in replicates of 6 in 96-well plates with 500 to 5,000 cells/well overnight and then treated with Taselisib (GDC-0032). After 4 days, the media are removed and the cells are fixed with 4% glutaraldehyde for 30 minutes. Fixed cells are stained with 0.1% crystal violet for 2 minutes, then washed, and dissolved in 10% acetic acid.

    MCE no ha confirmado la precisión de estos métodos independientemente. Son solo para referencia.
    Administraciòn de animales
    [1]

    Six-week-old Nu/Nu mice are injected bilaterally with 5×105 cells resuspended in 200 μL of culture media and Matrigel mixed in a 1:1 ratio. After tumors reache approximately 100 to 200 cm3, mice are randomized into treatment arms with 8 to 10 tumors per group. Taselisib (GDC-0032) (5 mg/kg) is dissolved in a vehicle containing 0.5% methylcellulose with 0.2% TWEEN-80 and is administered via daily oral gavage.

    MCE no ha confirmado la precisión de estos métodos independientemente. Son solo para referencia.
    Referencias

    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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.1714 mL 10.8571 mL 21.7141 mL 54.2853 mL
    5 mM 0.4343 mL 2.1714 mL 4.3428 mL 10.8571 mL
    10 mM 0.2171 mL 1.0857 mL 2.1714 mL 5.4285 mL
    15 mM 0.1448 mL 0.7238 mL 1.4476 mL 3.6190 mL
    20 mM 0.1086 mL 0.5429 mL 1.0857 mL 2.7143 mL
    25 mM 0.0869 mL 0.4343 mL 0.8686 mL 2.1714 mL
    30 mM 0.0724 mL 0.3619 mL 0.7238 mL 1.8095 mL
    40 mM 0.0543 mL 0.2714 mL 0.5429 mL 1.3571 mL
    50 mM 0.0434 mL 0.2171 mL 0.4343 mL 1.0857 mL
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    Taselisib 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:

    Taselisib1282512-48-4GDC-0032 RG-7604GDC0032GDC 0032RG7604RG 7604RG-7604PI3KPhosphoinositide 3-kinaseInhibitorinhibitorinhibit

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    Nombre del producto:
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    Cat. No.:
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    SAFETY DATA SHEET (SDS)

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