Cat. No.: HY-156681

Tersolisib

(Synonyms: STX-478; STX-478-101; LY4064809)

1 Cited Publications

Customer Review

Based on 1 publication(s) in Google Scholar

STX-478 (compound 80) is an oral CNS-penetrant allosteric mutant-selective PI3Kα inhibitor. STX-478 shows robust and durable tumor regression and can be used in cancer research.

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

Purity: 99.77%
CAS No.: 2883540-92-7
Formula: C₁₆H₁₂F₅N₅O₂
Molecular Weight:401.29

Storage:

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

Tersolisib Chemical Structure

CAS No.: 2883540-92-7

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- 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

STX-478 (compound 80) is an oral CNS-penetrant allosteric mutant-selective PI3Kα inhibitor. STX-478 shows robust and durable tumor regression and can be used in cancer research^[1].

IC₅₀ & Target

PI3Kα^[1].

All PI3K Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
T47D	IC₅₀	116 nM Compound: 6; STX-478	Antiproliferative activity against human T47D cells assessed as inhibition of cell growth incubated for 72 hrs by CellTiter-Glo assay Antiproliferative activity against human T47D cells assessed as inhibition of cell growth incubated for 72 hrs by CellTiter-Glo assay	[PMID: 38477582]

In Vitro

STX-478 (0-10,000 nM; 1 h) demonstrates selectivity for MCF10A cells harboring the H1047R kinase-domain mutation^[1].

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

Immunofluorescence^[1]

Cell Line:

MCF10A cells
Concentration:

0-10,000 nM
Incubation Time:

1 h
Result:

Targeted the MCF10A cells (with the H1047R kinase domain mutation).

In Vivo

STX-478 (30, 100 mg/kg; p.o.; single daily for 28 days) dose-dependently reduces tumor volume in a CAL-33 xenograft mice model^[1].

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

Animal Model:

Female BALB/c nude mice (CAL-33 xenograft model)^[1].
Dosage:

30, 100 mg/kg
Administration:

Oral administration
Result:

Showed a dose-dependent reduction in tumor volume.

Clinical Trial

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

Chemical Information

CAS No. 2883540-92-7
Appearance Solid
Molecular Weight 401.29
Formula C₁₆H₁₂F₅N₅O₂
Color White to off-white
SMILES

NC1=NC=C(C=N1)NC(N[C@H](C2=C(C3=CC(F)=CC(F)=C3O2)C)C(F)(F)F)=O
Synonyms

STX-478; STX-478-101; LY4064809
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)

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Journal Impact Factor

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

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (249.20 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

2.4920 mL

12.4598 mL

24.9196 mL

5 mM

0.4984 mL

2.4920 mL

4.9839 mL

10 mM

0.2492 mL

1.2460 mL

2.4920 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)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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: ≥ 6.25 mg/mL (15.57 mM); Clear solution

This protocol yields a clear solution of ≥ 6.25 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (62.5 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 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 6.25 mg/mL (15.57 mM); Clear solution

This protocol yields a clear solution of ≥ 6.25 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (62.5 mg/mL) to 900 μL Corn oil, and mix evenly.

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 (273 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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]. JR David St Jean, et al. Urea derivatives which can be used to treat cancer. Patent WO2022265993A1.

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	2.4920 mL	12.4598 mL	24.9196 mL	62.2991 mL
	5 mM	0.4984 mL	2.4920 mL	4.9839 mL	12.4598 mL
	10 mM	0.2492 mL	1.2460 mL	2.4920 mL	6.2299 mL
	15 mM	0.1661 mL	0.8307 mL	1.6613 mL	4.1533 mL
	20 mM	0.1246 mL	0.6230 mL	1.2460 mL	3.1150 mL
	25 mM	0.0997 mL	0.4984 mL	0.9968 mL	2.4920 mL
	30 mM	0.0831 mL	0.4153 mL	0.8307 mL	2.0766 mL
	40 mM	0.0623 mL	0.3115 mL	0.6230 mL	1.5575 mL
	50 mM	0.0498 mL	0.2492 mL	0.4984 mL	1.2460 mL
	60 mM	0.0415 mL	0.2077 mL	0.4153 mL	1.0383 mL
	80 mM	0.0311 mL	0.1557 mL	0.3115 mL	0.7787 mL
	100 mM	0.0249 mL	0.1246 mL	0.2492 mL	0.6230 mL

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Tersolisib

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Orally Active Compound Library

Anti-Breast Cancer Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

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Anti-Cancer Metabolism Compound Library

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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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Anti-Brain Cancer Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

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Posttranslational Modification Library

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Anti-Cancer Compound Library

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Autophagy Compound Library

Anti-Aging Compound Library

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Publications Citing Use of MedChemExpress (MCE) Tersolisib

All PI3K Isoforms

Biological Activity

Chemical Information

Publications (1)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Tersolisib Related Classifications

HY-156681 Related Classifications