1. PI3K/Akt/mTOR
  2. PI3K

GDC-0032 (Synonyms: Taselisib; RG-7604)

Cat. No.: HY-13898 Purity: 99.75%
Handling Instructions

GDC-0032 is a potent β-sparing small molecule inhibitor of PI3K, with Ki values of 0.29 nM, 0.91 nM, 0.97 nM for PI3Kα, PI3Kβ and PI3Kγ, respectively.

For research use only. We do not sell to patients.
GDC-0032 Chemical Structure

GDC-0032 Chemical Structure

CAS No. : 1282512-48-4

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 106 In-stock
5 mg USD 96 In-stock
10 mg USD 144 In-stock
50 mg USD 360 In-stock
100 mg USD 576 In-stock
200 mg USD 1056 In-stock
500 mg   Get quote  
1 g   Get quote  

* Please select Quantity before adding items.

    GDC-0032 purchased from MCE. Usage Cited in: Br J Cancer. 2016 Jul 26;115(3):303-11.

    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

    GDC-0032 purchased from MCE. Usage Cited in: Cell Discov. 2016 Sep 20;2:16030.

    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
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    GDC-0032 is a potent β-sparing small molecule inhibitor of PI3K, with Ki values of 0.29 nM, 0.91 nM, 0.97 nM for PI3Kα, PI3Kβ and PI3Kγ, respectively.

    IC50 & Target[3]

    PI3Kδ

    0.12 nM (Ki)

    PI3Kα

    0.29 nM (Ki)

    PI3Kγ

    0.97 nM (Ki)

    PI3Kβ

    9.1 nM (Ki)

    In Vitro

    GDC-0032 (100 nM) inhibits AKT/mTOR signaling in PIK3CA mutant cell lines but not in cells with loss or mutation of PTEN; 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]. GDC-0032 enhances the effects of MEK1/2 inhibition on both BRAFV600E/PTENNull human melanoma cells autochthonous mouse melanomas[2].

    In Vivo

    GDC-0032 (5 mg/kg, p.o.) potently impairs PI3K signaling and enhances the efficacy of fractionated radiotherapy; 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 GDC-0032 (22.5 mg/kg, p.o.)[2].

    Clinical Trial
    References
    Preparing Stock Solutions
    Concentration Volume 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
    10 mM 0.2171 mL 1.0857 mL 2.1714 mL
    Please refer to the solubility information to select the appropriate solvent.
    Cell Assay
    [1]

    GDC-0032 is dissolved in DMSO.

    Cells are seeded in replicates of 6 in 96-well plates with 500 to 5,000 cells/well overnight and then treated with 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 has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [1]

    GDC-0032 is dissolved in sterile water, 0.5% methyl-cellulose, and 0.2% Tween-80.

    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. 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 has not independently confirmed the accuracy of these methods. They are for reference only.

    References

    Purity: 99.75%

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    Product Name:
    GDC-0032
    Cat. No.:
    HY-13898
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