2. PI3K/Akt/mTOR
  3. PI3K
  4. STX-478

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.

STX-478 Chemical Structure

STX-478 Chemical Structure

CAS No. : 2883540-92-7

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Solution
10 mM * 1 mL in DMSO In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of STX-478:

STX-478 Related Antibodies

Top Publications Citing Use of Products

View All PI3K Isoform Specific Products:

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PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

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].
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.

STX-478 Related Antibodies

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.
Molecular Weight

401.29

Formula

C16H12F5N5O2
CAS No.
Appearance

Solid

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
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 : 125 mg/mL (311.50 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 2.4920 mL 12.4598 mL 24.9196 mL
5 mM 0.4984 mL 2.4920 mL 4.9839 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)

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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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C2

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V2

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:  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.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • 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

mg/kg

Animal weight
(per animal)

g

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: 99.63% ee.: 100.00%

SDS (251 KB)

COA (248 KB) HNMR (253 KB) NP-HPLC (244 KB) LCMS (94 KB)

Handling Instructions (2659 KB)
References

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.

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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STX-478 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:

STX-4782883540-92-7STX478STX 478PI3KPhosphoinositide 3-kinasecancertumorMCF10AH1047RInhibitorinhibitorinhibit

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