2. PI3K/Akt/mTOR Apoptosis
  3. PI3K Apoptosis
  4. Inavolisib

Inavolisib  (Synonyms: GDC-0077; RG6114)

製品番号: HY-101562 純度: 99.96%
COA 取扱説明書 Technical Support

Inavolisib (GDC-0077) is a potent, orally active, and selective PI3Kα inhibitor (IC50=0.038 nM). Inavolisib exerts its activity by binding to the ATP binding site of PI3K, thereby inhibiting the phosphorylation of PIP2 to PIP3. Inavolisib is more selective for mutant versus wild-type PI3Kα. Inavolisib can be used for the study of breast cancer.

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CAS 番号 : 2060571-02-8

容量 価格（税別） 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 594 在庫あり
Solution
10 mM * 1 mL in DMSO USD 594 在庫あり
Solid
1 mg $257 在庫あり
5 mg $540 在庫あり
10 mg $900 在庫あり
25 mg $1200 在庫あり
50 mg $1590 在庫あり
100 mg $2150 在庫あり
200 mg   お問い合わせ  
500 mg   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

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カスタマーレビュー

Based on 7 publication(s) in Google Scholar

Other Forms of Inavolisib:

Inavolisib 関連抗体

Top Publications Citing Use of Products

    Inavolisib purchased from MedChemExpress. Usage Cited in: Int J Biol Sci. 2025 Mar 19;21(6):2462-2475.  [Abstract]

    Dose-response curves for Inavolisib (0.1-100 μM ) in parental and alpelisib-resistant breast cancer cell lines.

    Inavolisib purchased from MedChemExpress. Usage Cited in: Cancer Metab. 2025 Feb 7;13(1):6.  [Abstract]

    The effects of Inavolisib (0-1.1 μM, 72 h) on the proliferation of SK-BR-3 and HCC1569 cells.

    Inavolisib purchased from MedChemExpress. Usage Cited in: Cancer Metab. 2025 Feb 7;13(1):6.  [Abstract]

    The modulated protein levels of SCD-1 and CD36 were assessed by western blotting in SK-BR-3 cells treated with Inavolisib (0.5 μM) for 24 h.

    Inavolisib purchased from MedChemExpress. Usage Cited in: Cancer Metab. 2025 Feb 7;13(1):6.  [Abstract]

    The modulated protein levels of SCD-1 and CD36 were assessed by western blotting in HCC1569 cells treated with Inavolisib (2 μM) for 24 h.

    Inavolisib purchased from MedChemExpress. Usage Cited in: Clin Transl Med. 2022 May;12(5):e835.  [Abstract]

    EZH2 overexpression was conferred in esophageal squamous cell carcinoma (ESCC) cells. EV32 and HE6 cells were treated with GDC-0077 (0.1-10 μM) for 72 hours, and cell proliferation was detected by SRB assay.

    PI3K アイソフォーム固有の製品をすべて表示:

    すべてのアイソフォームを表示
    PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

    • 生物活性

    • 純度とドキュメンテーション

    • 参考文献

    • カスタマーレビュー

    製品説明

    Inavolisib (GDC-0077) is a potent, orally active, and selective PI3Kα inhibitor (IC50=0.038 nM). Inavolisib exerts its activity by binding to the ATP binding site of PI3K, thereby inhibiting the phosphorylation of PIP2 to PIP3. Inavolisib is more selective for mutant versus wild-type PI3Kα. Inavolisib can be used for the study of breast cancer[1].

    IC50 & Target[1]

    PI3Kα

    0.038 nM (IC50)

    Cellular Effect
    Cell Line Type Value Description References
    HCC1954 EC50
    60 nM
    Compound: 32; GDC-0077
    Antiproliferative activity against human HCC1954 cells assessed as reduction in cell viability incubated for 4 days by Celltiter-Glo luminescence assay
    Antiproliferative activity against human HCC1954 cells assessed as reduction in cell viability incubated for 4 days by Celltiter-Glo luminescence assay
    		[PMID: 36455032]
    MCF7 EC50
    30 nM
    Compound: 32; GDC-0077
    Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 4 days by Celltiter-Glo luminescence assay
    Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 4 days by Celltiter-Glo luminescence assay
    		[PMID: 36455032]
    体外実験

    Inavolisib (GDC-0077) is >300-fold more selective for PI3Kα over the other class I PI3K isoforms (β, δ, and γ) and >2000-fold more selective over PIK family members. Inavolisib selectively degrades mutant PI3Kα in a proteasome-dependent fashion resulting in reduction of PI3K pathway activity biomarkers such as pAKT and pPRAS40, inhibition of cell proliferation, and increased apoptosis in human PIK3CA-mutant breast cancer cell lines to a greater extent when compared to PIK3CA wild-type cells[1].

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

    Inavolisib 関連抗体
    体内実験

    Inavolisib (p.o.) results in tumor regressions, induction of apoptosis, and a reduction of pAKT, pPRAS40, and pS6RP in a dose-dependent fashion in PIK3CA-mutant breast cancer xenograft models[1].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    臨床実験
    分子量

    407.37

    分子式

    C18H19F2N5O4
    CAS 番号
    Appearance

    Solid

    Color

    White to yellow

    SMILES

    C[C@@H](C(N)=O)NC1=CC=C(C2=NC(N3[C@H](C(F)F)COC3=O)=CN2CCO4)C4=C1
    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 : 100 mg/mL (245.48 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 2.4548 mL 12.2739 mL 24.5477 mL
    5 mM 0.4910 mL 2.4548 mL 4.9095 mL
    10 mM 0.2455 mL 1.2274 mL 2.4548 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)

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始）

    C1

    ×
    体積 （開始）

    V1

    =
    濃度 （終了）

    C2

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    体積 （終了）

    V2

    体内:

    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:  5% DMSO    40% PEG300    5% Tween-80    50% Saline

      Solubility: ≥ 2.75 mg/mL (6.75 mM); Clear solution

    • Protocol 2

      Add each solvent one by one:  5% DMSO    95% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.75 mg/mL (6.75 mM); Clear solution

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

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    (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.
    純度とドキュメンテーション

    純度: 99.96%

    COA (253 KB) HNMR (283 KB) CNMR (274 KB) RP-HPLC (257 KB) LCMS (109 KB)

    取扱説明書 (2659 KB)
    参考文献

    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 2.4548 mL 12.2739 mL 24.5477 mL 61.3693 mL
    5 mM 0.4910 mL 2.4548 mL 4.9095 mL 12.2739 mL
    10 mM 0.2455 mL 1.2274 mL 2.4548 mL 6.1369 mL
    15 mM 0.1637 mL 0.8183 mL 1.6365 mL 4.0913 mL
    20 mM 0.1227 mL 0.6137 mL 1.2274 mL 3.0685 mL
    25 mM 0.0982 mL 0.4910 mL 0.9819 mL 2.4548 mL
    30 mM 0.0818 mL 0.4091 mL 0.8183 mL 2.0456 mL
    40 mM 0.0614 mL 0.3068 mL 0.6137 mL 1.5342 mL
    50 mM 0.0491 mL 0.2455 mL 0.4910 mL 1.2274 mL
    60 mM 0.0409 mL 0.2046 mL 0.4091 mL 1.0228 mL
    80 mM 0.0307 mL 0.1534 mL 0.3068 mL 0.7671 mL
    100 mM 0.0245 mL 0.1227 mL 0.2455 mL 0.6137 mL
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    Inavolisib Related Classifications

    • Molarity Calculator

    • Dilution Calculator

    The molarity calculator equation

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

    質量   濃度   体積   分子量 *
    = × ×

    The dilution calculator equation

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

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
    × = ×
    C1   V1   C2   V2
    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:

    Inavolisib2060571-02-8GDC-0077 RG6114GDC0077GDC 0077RG6114RG 6114RG-6114PI3KApoptosisPhosphoinositide 3-kinaseInhibitorinhibitorinhibit

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    製品名:
    Inavolisib
    製品番号:
    HY-101562
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