Cat. No.: HY-153306

Zovegalisib

(Synonyms: RLY-2608)

1 Cited Publications

Customer Review

Based on 1 publication(s) in Google Scholar

Zovegalisib (RLY-2608) is an orally active first-in-class allosteric mutant-selective inhibitor of PI3Ka with anti-tumor activity. Zovegalisib inhibits tumor growth in PIK3CA-mutant xenograft mice models with minimal impact on insulin.

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

Purity: 98.80%
CAS No.: 2733573-94-7
Formula: C₂₉H₁₄ClF₅N₆O₂
Molecular Weight:608.91

Storage:

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

Zovegalisib Chemical Structure

CAS No.: 2733573-94-7

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

Publications Citing Use of MedChemExpress (MCE) Zovegalisib

Br J Cancer. 2025 Aug;133(2):144-154. [Abstract]

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Cell Proliferation/Viability Assay

Cell Proliferation/Viability Assay

Biological Activity
- Description
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (1)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

All PI3K Isoforms :

In Vitro

Zovegalisib (RLY-2608) (1 nM-100 μM, 5 days) inhibits the proliferation and phosphorylated AKT (pAKT) in PIK3CA mutant cancer cell lines independent of the hotspot mutation^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Zovegalisib (RLY-2608) (25-100 mg/kg, p.o., twice a day for 50 days) inhibits tumors in tumor xenograft mice models with reduced impact on insulin levels^[1].
Zovegalisib (12.5-100 mg/kg, p.o., a single dose for 4 days) demonstrates potent tumor growth inhibition in Balb/c nude female mice bearing HSC-2 tumors^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Tumor xenograft mice models^[1]
Dosage:

25-100 mg/kg
Administration:

p.o., twice a day for 50 days
Result:

Potentiated tumor regression in tumor xenograft mice models.

Clinical Trial

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

Chemical Information

CAS No. 2733573-94-7
Appearance Solid
Molecular Weight 608.91
Formula C₂₉H₁₄ClF₅N₆O₂
Color Light yellow to yellow
SMILES

O=C1N[C@@H](C2=CC(F)=CC=C2Cl)C(C1=C3)=C(NC(C4=CC(F)=CC(C(F)(F)F)=C4)=O)C=C3C5=C(C#N)N6C(C=C5)=NC=N6
Synonyms

RLY-2608
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

Publications (1)

All Cell Proliferation/Viability Assay

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Br J Cancer

Multi-node inhibition targeting mTORC1, mTORC2 and PI3Kα potently inhibits the PI3K/AKT/mTOR pathway in endometrial and breast cancer models. [Abstract]

2025 Aug;133(2):144-154. PMID: 40360883

Zovegalisib purchased from MedChemExpress. Usage Cited in: Br J Cancer. 2025 Aug;133(2):144-154. [Abstract]

Compared to mutant-specific PI3Kα inhibitors (RLY-2608 (Zovegalisib) & STX-478) and PI3Kα inhibitor/degrader inavolisib, the sapanisertib plus serabelisib combination had a substantially lower mean IC₅₀ i.e., 32.0 nM versus 0.89 μM (inavolisib), 6.13 μM (STX-478), 4.85 μM (RLY-2608, Zovegalisib).

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (164.23 mM; ultrasonic and warming and heat to 60°C; 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

1.6423 mL

8.2114 mL

16.4228 mL

5 mM

0.3285 mL

1.6423 mL

3.2846 mL

10 mM

0.1642 mL

0.8211 mL

1.6423 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.

Molarity Calculator

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

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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: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 5 mg/mL (8.21 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.

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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (281 KB)
SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 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)

References

[1]. Andreas Varkaris, et al. Discovery and clinical proof-of-concept of RLY-2608, a first-in-class mutant-selective allosteric PI3Ka inhibitor that decouples anti-tumor activity from hyperinsulinemia. Cancer Discov. 2023 Nov 2. [Content Brief]

[2]. Pazolli E, et al. RLY-2608: the first allosteric mutant-and isoform-selective inhibitor of PI3Kα, is efficacious as a single agent and drives regressions in combination with standard of care therapies in PIK3CA mutant breast cancer models[J]. Cancer Res., 2022, 82.

[3]. Perez C A, et al. First-in-human global multi-center study of RLY-2608, a pan-mutant and isoform-selective PI3Kα inhibitor, as a single agent in patients with advanced solid tumors and in combination with fulvestrant in patients with advanced breast cancer[J]. 2022.

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	1.6423 mL	8.2114 mL	16.4228 mL	41.0570 mL
	5 mM	0.3285 mL	1.6423 mL	3.2846 mL	8.2114 mL
	10 mM	0.1642 mL	0.8211 mL	1.6423 mL	4.1057 mL
	15 mM	0.1095 mL	0.5474 mL	1.0949 mL	2.7371 mL
	20 mM	0.0821 mL	0.4106 mL	0.8211 mL	2.0528 mL
	25 mM	0.0657 mL	0.3285 mL	0.6569 mL	1.6423 mL
	30 mM	0.0547 mL	0.2737 mL	0.5474 mL	1.3686 mL
	40 mM	0.0411 mL	0.2053 mL	0.4106 mL	1.0264 mL
	50 mM	0.0328 mL	0.1642 mL	0.3285 mL	0.8211 mL
	60 mM	0.0274 mL	0.1369 mL	0.2737 mL	0.6843 mL
	80 mM	0.0205 mL	0.1026 mL	0.2053 mL	0.5132 mL
	100 mM	0.0164 mL	0.0821 mL	0.1642 mL	0.4106 mL

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Zovegalisib

Kinase Inhibitor Library

PI3K/Akt/mTOR Compound Library

Stem Cell Signaling Compound Library

Anti-Cancer Compound Library

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Anti-Pancreatic Cancer Compound Library

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Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Anti-Prostate Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Cancer Stem Cells Compound Library

Pain-Related Compound Library

Membrane Protein-targeted Compound Library

Highly Selective Inhibitors Library

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Bioactive Compound Library Max

MCE Bioactive Compound Library

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Clinical Compound Library Plus

Bioactive Compound Library

Anti-Fibrosis Compound Library

Anti-Brain Cancer Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) Zovegalisib

All PI3K Isoforms

Biological Activity

Chemical Information

Publications (1)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Zovegalisib Related Classifications

HY-153306 Related Classifications