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

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

製品番号: HY-13898 純度: 99.46%
取扱説明書

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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Taselisib 構造式

Taselisib 構造式

CAS 番号 : 1282512-48-4

容量 価格(税別) 在庫状況 数量
無料サンプル (0.5-1 mg)   今すぐ申し込む  
10 mM * 1 mL in DMSO USD 71 在庫あり
Estimated Time of Arrival: December 31
5 mg USD 70 在庫あり
Estimated Time of Arrival: December 31
10 mg USD 110 在庫あり
Estimated Time of Arrival: December 31
50 mg USD 250 在庫あり
Estimated Time of Arrival: December 31
100 mg USD 450 在庫あり
Estimated Time of Arrival: December 31
200 mg USD 750 在庫あり
Estimated Time of Arrival: December 31
500 mg   お問い合わせ  
1 g   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

カスタマーレビュー

Based on 13 publication(s) in Google Scholar

Top Publications Citing Use of Products

    Taselisib 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

    Taselisib 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
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    製品説明

    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

    PI3Kδ

    0.12 nM (Ki)

    PI3Kα

    0.29 nM (Ki)

    PI3Kγ

    0.97 nM (Ki)

    PI3Kβ

    9.1 nM (Ki)

    体外実験

    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].

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

    体内実験

    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].

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

    臨床実験
    分子量

    460.53

    分子式

    C₂₄H₂₈N₈O₂

    CAS 番号

    1282512-48-4

    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

    輸送条件

    Room temperature in continental US; may vary elsewhere.

    保管条件
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    溶剤 & 溶解度
    体外: 

    DMSO : 50 mg/mL (108.57 mM; Need ultrasonic)

    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
    10 mM 0.2171 mL 1.0857 mL 2.1714 mL
    *Please refer to the solubility information to select the appropriate solvent.
    体内:
    • 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

    • 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

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

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

    *All of the co-solvents are provided by MCE.
    参考文献
    細胞実験
    [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 はこれらの方法の精度を確認していません。 こちらは参照専用です。

    動物実験
    [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 はこれらの方法の精度を確認していません。 こちらは参照専用です。

    参考文献

    純度: 99.46%

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    Keywords:

    TaselisibGDC-0032 RG-7604GDC0032GDC 0032RG7604RG 7604RG-7604PI3KPhosphoinositide 3-kinaseInhibitorinhibitorinhibit

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    製品名:
    Taselisib
    製品番号:
    HY-13898
    数量:
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