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Inavolisib (GDC-0077)

Name: Inavolisib (GDC-0077)
Brand: Selleck Chemicals
SKU: S8668
Rating: 5 (4 reviews)

Synonyms: RG6114, RO-7113755

Catalog No.S8668 Purity:99.84%

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

Batch: Purity: 99.84%

99.84

Inavolisib (GDC-0077) Related Products

Related Targets	p110α p110β p110δ p110γ C2β Vps34	Click to Expand
Related Products	LY294002 3-MA (3-Methyladenine) Dactolisib (BEZ235) Pictilisib (GDC-0941) Wortmannin Buparlisib (BKM120) PI-103 TGX-221 ZSTK474 Omipalisib (GSK2126458) A66 PF-04691502 PIK-75 HCl IC-87114 740 Y-P (PDGFR 740Y-P) AS-605240 Taselisib (GDC 0032) SAR405 Apitolisib (GDC-0980) VPS34-IN1 PIK-90 AZD6482 Gedatolisib (PKI-587) HS-173 AS-252424 Eganelisib (IPI-549) VS-5584 (SB2343) GSK2636771 AZD8186 GSK1059615 Pilaralisib (XL147) TG100-115 CZC24832 Voxtalisib (XL765) XL147 analogue AS-604850 BGT226 (NVP-BGT226) maleate Quercetin Dihydrate VPS34 inhibitor 1 (Compound 19) Samotolisib (LY3023414) Voxtalisib (XL765) Analogue AMG319 Nemiralisib Bimiralisib (PQR309) CH5132799 PKI-402 TG100713 Paxalisib (GDC-0084) SF2523 Serabelisib (TAK-117) GDC-0326 GNE-317 PIK-294 PI-3065 AZD8835 Seletalisib (UCB-5857) leniolisib (CDZ 173) (E)-Akt inhibitor-IV Gallein CAY10505 Selective PI3Kδ Inhibitor 1 (compound 7n) PF-4989216 GNE-477 GNE-493	Click to Expand
Related Compound Libraries	Kinase Inhibitor Library PI3K/Akt Inhibitor Library Apoptosis Compound Library Cell Cycle compound library NF-κB Signaling Compound Library	Click to Expand

Signaling Pathway

PI3K Signaling Pathway

Biological Activity

Description

Targets

PI3K alpha ^[1]
(Cell-free assay)

0.038 nM

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

In Vivo
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]
Animal Research	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

References

Chemical Information & Solubility

Molecular Weight	407.37	Formula	C₁₈H₁₉F₂N₅O₄
CAS No.	2060571-02-8	SDF	--
Smiles	CC(C(=O)N)NC1=CC2=C(C=C1)C3=NC(=CN3CCO2)N4C(COC4=O)C(F)F
Storage (From the date of receipt)	3 years -20°C powder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years -20°C powder		1 month-20°Cin solvent

In vitro
Batch:

DMSO : 81 mg/mL ( (198.83 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molecular Weight Calculator

In vivo Batch: Add solvents to the product individually and in order.					In vivo Formulation Calculator
	Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	4.05mg/ml (9.94mM)	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.	In vivo Formulation Calculator
Clear solution	5% DMSO 1 95% Corn oil	0.7mg/ml (1.72mM)	Taking the 1 mL working solution as an example, add 50 μL of 14 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 1 40%PEG300 2 5%Tween80 3 50%ddH2O	4.05mg/ml (9.94mM)	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 it; 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.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	4.05mg/ml (9.94mM)	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.
Clear solution	5% DMSO 1 95% Corn oil	0.65mg/ml (1.60mM)	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.

Preparing Stock Solutions

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
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Dilution Calculator Molecular Weight Calculator

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

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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