Inavolisib (GDC-0077)

Catalog No.S8668 Batch:S866805

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Technical Data

Formula

C18H19F2N5O4
Molecular Weight 407.37 CAS No. 2060571-02-8
Solubility (25°C)* In vitro DMSO 81 mg/mL (198.83 mM)
Water Insoluble
Ethanol Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5% DMSO 95% Corn oil
0.65mg/ml Taking the 1 mL working solution as an example, add 50 μL of 13 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
4.05mg/ml Taking the 1 mL working solution as an example, add 50 μL of 81 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description Inavolisib (GDC-0077, RG6114, RO-7113755) is a potent selective inhibitor of PI3K alpha (PI3Kα) with an IC50 of 0.038 nM. GDC-0077 is >300-fold more selective for PI3K alpha over the other class I PI3K isoforms (beta, delta, and gamma) and >2000-fold more selective over PIK family members. GDC-0077 binds to the ATP binding site of PI3K and inhibits the phosphorylation of PIP2 to PIP3.
Targets
PI3K alpha [1]
(Cell-free assay)
0.038 nM
In vitro

GDC-0077 potently inhibits mutant PI3K pathway signaling and cell viability through unique HER2-dependent mutant p110a degradation.[2]
In vivo

GDC-0077 treatment at the MTD in vivo results in tumor regressions in multiple PIK3CA-mutant xenograft and patient-derived xenograft models.[2]

Protocol (from reference)

Cell Assay:

[2]
  • Cell lines

    HCC1954 cells, HDQ-P1 cells, SW48 cells, MCF7 cells, HCC202 heterozygous cells

  • Concentrations

    10 nM

  • Incubation Time

    24 h

  • Method

    ATP-based cell viability assay in Colon cancer cell lines. Western blot of the p110a protein levels and pAKT signaling in Colon cancer cell lines treated with GDC-0077 for gradient concentrations for 24 hours.
Animal Study:

[2]
  • Animal Models

    Female NCR nude mice inoculated with HCC1954 tumor cells, female NOD-SCID gamma mice inoculated with WHIM20 tumor cells, female NOD-SCID gamma mice inoculated with HCI-003 tumor cells

  • Dosages

    25 mg/kg

  • Administration

    Oral gavage

Selleck's Inavolisib (GDC-0077) has been cited by 4 publications

AKT and EZH2 inhibitors kill TNBCs by hijacking mechanisms of involution [ Nature, 2024, 10.1038/s41586-024-08031-6] PubMed: 39385030
Functional Assessments of Gynecologic Cancer Models Highlight Differences Between Single-Node Inhibitors of the PI3K/AKT/mTOR Pathway and a Pan-PI3K/mTOR Inhibitor, Gedatolisib [ Cancers (Basel), 2024, 16(20)3520] PubMed: 39456616
The Oncogenic PI3K-Induced Transcriptomic Landscape Reveals Key Functions in Splicing and Gene Expression Regulation [ Cancer Res, 2022, 82(12):2269-2280] PubMed: 35442400
PI3K inhibitors in trastuzumab-resistant HER2-positive breast cancer cells with PI3K pathway alterations [ Am J Cancer Res, 2022, 12(7):3067-3082] PubMed: 35968355

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.