Inavolisib (GDC-0077)

Catalog No.S8668 Synonyms: RG6114, RO-7113755

For research use only.

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.

Inavolisib (GDC-0077) Chemical Structure

CAS No. 2060571-02-8

Purity & Quality Control

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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.<sup><a class="sref" href="#s_ref">[2]</a></sup>

In vivo

GDC-0077 treatment at the MTD in vivo results in tumor regressions in multiple PIK3CA-mutant xenograft and patient-derived xenograft models.<sup><a class="sref" href="#s_ref">[2]</a></sup>

Protocol (from reference)

Cell Research:

<sup><a class="sref" href="#s_ref">[2]</a></sup>

  • 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 Research:

<sup><a class="sref" href="#s_ref">[2]</a></sup>

  • 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

Solubility (25°C)

In vitro

DMSO 81 mg/mL
(198.83 mM)
Water Insoluble
Ethanol Insoluble

Chemical Information

Molecular Weight 407.37
Formula

C18H19F2N5O4

CAS No. 2060571-02-8
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC(C(=O)N)NC1=CC2=C(C=C1)C3=NC(=CN3CCO2)N4C(COC4=O)C(F)F

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Molarity Calculator

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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