2. PI3K/Akt/mTOR
  3. PI3K mTOR
  4. SN32976

SN32976 is a potent and selective class I PI3K and mTOR inhibitor with IC50s of 15.1 nM, 461 nM, 110 nM, 134 nM and 194 nM for PI3Kα, PI3Kβ, PI3Kγ, PI3Kδ and mTOR, respectively. SN32976 shows high selectivity among other 442 kinases. SN32976 shows anticancer effects.

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

SN32976 Chemical Structure

SN32976 Chemical Structure

CAS No. : 1246202-11-8

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Based on 1 publication(s) in Google Scholar

SN32976 Related Antibodies

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mTOR mTORC1 mTORC2

  • Biological Activity

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Description

SN32976 is a potent and selective class I PI3K and mTOR inhibitor with IC50s of 15.1 nM, 461 nM, 110 nM, 134 nM and 194 nM for PI3Kα, PI3Kβ, PI3Kγ, PI3Kδ and mTOR, respectively. SN32976 shows high selectivity among other 442 kinases. SN32976 shows anticancer effects[1].

IC50 & Target[1]

PI3Kα

15.1 nM (IC50)

PI3Kβ

461 nM (IC50)

PI3Kγ

110 nM (IC50)

PI3Kδ

134 nM (IC50)

mTOR

194 nM (IC50)

Cellular Effect
Cell Line Type Value Description References
Sf9 IC50
206 nM
Compound: SN32976; 16
Inhibition of recombinant human N-terminal p110delta/p85alpha expressed in baculovirus infected Sf9 insect cells using PIP2 as substrate by HTRF assay
Inhibition of recombinant human N-terminal p110delta/p85alpha expressed in baculovirus infected Sf9 insect cells using PIP2 as substrate by HTRF assay
[PMID: 30850264]
Sf9 IC50
5.3 nM
Compound: SN32976; 16
Inhibition of recombinant human N-terminal p110alpha/p85alpha expressed in baculovirus infected Sf9 insect cells using PIP2 as substrate by HTRF assay
Inhibition of recombinant human N-terminal p110alpha/p85alpha expressed in baculovirus infected Sf9 insect cells using PIP2 as substrate by HTRF assay
[PMID: 30850264]
Sf9 IC50
743 nM
Compound: SN32976; 16
Inhibition of recombinant human N-terminal p110beta/p85alpha expressed in baculovirus infected Sf9 insect cells using PIP2 as substrate by HTRF assay
Inhibition of recombinant human N-terminal p110beta/p85alpha expressed in baculovirus infected Sf9 insect cells using PIP2 as substrate by HTRF assay
[PMID: 30850264]
In Vitro

SN32976 (1-100 nM; for 1 h) inhibits both Thr308 and Ser473 pAKT expression in U-87 MG cells at concentrations as low as 10 nM[1].
The cell lines are PTEN null (U-87 MG, PC3, NZM34), H1047R PIK3CA mutant (HCT116, NZM40), E545K PIK3CA mutant (NCI-H460, MCF7) and PIK3CA amplified (FaDu). SN32976 potently inhibits cell proliferation in all cell lines, with EC50 values ranging from 18.5 nM in NCI-H460 cells to 1787 nM in NZM34 cells[1].

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

SN32976 Related Antibodies

Western Blot Analysis[1]

Cell Line: U-87 MG cells
Concentration: 1 nM, 3 nM, 10 nM, 30 nM, 100 nM
Incubation Time: for 1 h
Result: Inhibited both Thr308 and Ser473 pAKT expression in U-87 MG cells.
In Vivo

SN32976 (37.5-75 mg/kg; po; daily; for 21 days) inhibits tumor growth in U-87 MG tumor xenograft models[1].

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

Animal Model: 6-8 week old female balb/c nude or female balb/c Rag1−/− mice inoculated with U-87 MG cells[1]
Dosage: 37.5 mg/kg; 75 mg/kg
Administration: po; daily; for 21 days
Result: Inhibited tumor growth in U-87 MG tumor xenograft models.
Molecular Weight

581.64

Formula

C24H33F2N9O4S
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=S(CCN(C)C)(N1CCN(C2=NC(N3C4=CC=CC(OC)=C4N=C3C(F)F)=NC(N5CCOCC5)=N2)CC1)=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 : 10 mg/mL (17.19 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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7193 mL 8.5964 mL 17.1928 mL
5 mM 0.3439 mL 1.7193 mL 3.4386 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

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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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    90% Corn Oil

    Solubility: ≥ 1 mg/mL (1.72 mM); Clear solution

    This protocol yields a clear solution of ≥ 1 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 (10.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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mg/kg

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g

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(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:
%
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% 
+
%
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
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 1.7193 mL 8.5964 mL 17.1928 mL 42.9819 mL
5 mM 0.3439 mL 1.7193 mL 3.4386 mL 8.5964 mL
10 mM 0.1719 mL 0.8596 mL 1.7193 mL 4.2982 mL
15 mM 0.1146 mL 0.5731 mL 1.1462 mL 2.8655 mL
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SN32976 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:

SN329761246202-11-8SN 32976SN-32976PI3KmTORPhosphoinositide 3-kinaseMammalian target of Rapamycinclass I PI3KPI3KαPI3KβPI3KγPI3Kδanticancer effectsInhibitorinhibitorinhibit

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