Art. -Nr.: HY-101562

Inavolisib

Name: Inavolisib
Brand: MedChemExpress
SKU: HY-101562
Price: 257.00 USD
Availability: InStock
Rating: 5 (11 reviews)

(Synonyms: GDC-0077; RG6114)

11 Cited Publications

Kundenbewertung

Based on 11 publication(s) in Google Scholar

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.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Reinheit : 99.96%
CAS. Nr.: 2060571-02-8
Formel: C₁₈H₁₉F₂N₅O₄
Molecular Weight:407.37

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Inavolisib Chemical Structure

CAS. Nr.: 2060571-02-8

Größe

Preis

Verfügbarkeit

Menge

Amount: USD 0.00

* Bitte wählen Sie Menge, bevor Sie Artikel hinzufügen.

Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (11)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

^[1]

PI3Kα

0.038 nM (IC₅₀)

Alle PI3K Isoform-spezifische Produkte anzeigen :

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]

In Vitro

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.

In Vivo

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.

Related Protocols :

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 2060571-02-8
Appearance Solid
Molecular Weight 407.37
Formel C₁₈H₁₉F₂N₅O₄
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
Synonyms

GDC-0077; RG6114
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (11)

All Cell Proliferation/Viability AssayWB

Sort by:

Journal Impact Factor

Int J Biol Sci

The SGK3/GSK3β/β-catenin signaling promotes breast cancer stemness and confers resistance to alpelisib therapy. [Abstract]

2025 Mar 19;21(6):2462-2475. PMID: 40303291

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.
Clin Transl Med

Genome-wide gain-of-function screening identifies EZH2 mediating resistance to PI3Kα inhibitors in oesophageal squamous cell carcinoma. [Abstract]

2022 May;12(5):e835. PMID: 35604910

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.
Cancer Metab

CD36 inhibition enhances the anti-proliferative effects of PI3K inhibitors in PTEN-loss anti-HER2 resistant breast cancer cells. [Abstract]

2025 Feb 7;13(1):6. PMID: 39920872

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.
Int J Mol Sci

Genomic Characterization of Preclinical Prostate Cancer Cell Line Models. [Abstract]

2024 Jun 1;25(11):6111. PMID: 38892296
Cancer Sci

D-1553: A novel KRASG12C inhibitor with potent and selective cellular and in vivo antitumor activity. [Abstract]

2023 Jul;114(7):2951-2960. PMID: 37158138
Neoplasia

PIK3CA mutant cervical cancer is selectively suppressed by PI3Kα inhibition (Alpelisib/BYL-719 and Inavolisib/GDC-0077) and cooperates with HPV directed T cell therapy. [Abstract]

2026 Jun:76:101305. PMID: 41980433
Cell Signal

Nuclear SIRT6 depletion activates LINE1-cGAS-STING pathway to induce PASMCs senescence in hypoxic pulmonary hypertension. [Abstract]

2026 Mar:139:112351. PMID: 41490817
In Vivo

2026 Sep-Oct;40(5):2663-2669. PMID: 42665384
bioRxiv

2026 Sep 22:2026.09.21.753236. PMID: 42818240
Harvard University

2026.
medRxiv

A Three-subtype Molecular model of Cervical Cancer: Multiple PI3K Pathway inhibitors suppress growth and cooperate with HPV-directed immunotherapy. [Abstract]

2026 Jan 23:2026.01.21.26344562. PMID: 41646800

Lösungsmittel & Löslichkeit

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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

Protocol 3

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.08 mg/mL (5.11 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 4

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.08 mg/mL (5.11 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 5

Add each solvent one by one: 1% DMSO 99% Saline

Solubility: ≥ 0.55 mg/mL (1.35 mM); Clear solution

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (277 KB)
SDS (644 KB)
- English - EN (644 KB)
- Français - FR (644 KB)
- Deutsch - DE (644 KB)
- Norwegian - NO (644 KB)
- Español - ES (644 KB)
- Swedish - SV (644 KB)
- Italian - IT (644 KB)
- Korean - KR (644 KB)
- Portuguese - PT (644 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. R Hong, Abstract PD4-14: GDC-0077 is a selective PI3Kalpha inhibitor that demonstrates robust efficacy in PIK3CA mutant breast cancer models as a single agent and in combination with standard of care therapies. 2017 San Antonio Breast Cancer Symposium.

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Bioz

Keywords

Inavolisib

11 Cited Publications

100 mg Angebot einholen

Subscribe to the

MedChemExpress

Newsletter

Produktname:
Art. -Nr.:
Menge:
MCE Japan Authorized Agent:

Produktname:
CAS. Nr.:
Species:
Reinheit:
Menge:

Inavolisib

Publications Citing Use of MedChemExpress (MCE) Inavolisib

Alle PI3K Isoform-spezifische Produkte anzeigen