Inavolisib (Synonyms: GDC-0077; RG6114)

Name: Inavolisib
Brand: MedChemExpress
SKU: HY-101562
Rating: 5.0 (3 reviews)

Cat. No.: HY-101562 Purity: 99.96%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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.

For research use only. We do not sell to patients.

Inavolisib Chemical Structure

CAS No. : 2060571-02-8

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 594	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 594	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	USD 257	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 540	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 900	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 1200	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 1590	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 2150	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 3 publication(s) in Google Scholar

3 Publications Citing Use of MCE Inavolisib

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View All PI3K Isoform Specific Products:

View All Isoforms

PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

Biological Activity
Purity & Documentation
References
Customer Review

Description

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]

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.

Clinical Trial

Molecular Weight

407.37

Formula

C₁₈H₁₉F₂N₅O₄

CAS No.

2060571-02-8

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

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)

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)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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
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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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

mg/kg

Animal weight
(per animal)

Dosing volume
(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.

Purity & Documentation

Purity: 99.96%

Select Batch:

Data Sheet (277 KB) SDS (645 KB)

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

Handling Instructions (2659 KB)

References

[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.

Complete Stock Solution Preparation Table

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

Inavolisib Related Classifications

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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Inavolisib (Synonyms: GDC-0077; RG6114)

Customer Review

Inavolisib Related Antibodies

3 Publications Citing Use of MCE Inavolisib

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All PI3K Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Inavolisib Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Inavolisib Related Classifications

Keywords:

Your Recently Viewed Products:

Customer Review

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