2. PI3K/Akt/mTOR
  3. PI3K mTOR
  4. NSC781406

NSC781406 is a highly potent PI3K and mTOR inhibitor with an IC50 of 2 nM for PI3Kα.

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

NSC781406 Chemical Structure

NSC781406 Chemical Structure

CAS No. : 1676893-24-5

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 166 In-stock
Solution
10 mM * 1 mL in DMSO USD 166 In-stock
Solid
1 mg USD 40 In-stock
5 mg USD 120 In-stock
10 mg USD 192 In-stock
25 mg USD 346 In-stock
50 mg USD 520 In-stock
100 mg USD 795 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 2 publication(s) in Google Scholar

NSC781406 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

View All mTOR Isoform Specific Products:

View All Isoforms
mTOR mTORC1 mTORC2

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

NSC781406 is a highly potent PI3K and mTOR inhibitor with an IC50 of 2 nM for PI3Kα.

IC50 & Target[1]

PI3Kα

2 nM (IC50)

PI3Kγ

2.7 nM (IC50)

PI3Kβ

9.4 nM (IC50)

PI3Kδ

14 nM (IC50)

mTOR

5.4 nM (IC50)

In Vitro

NSC781406 demonstrates potent PI3K inhibition (PI3Kα IC50=2.0 nM) that translates into BEL-7404 cells proliferation inhibition (IC50=20 nM). NSC781406 displays reasonable liver microsome stability. NSC781406 demonstrates cytotoxic activities against leukemia, non-small cell, lung cancer, colon cancer, central nervous system cancer, melanoma, ovarian cancer, renal cancer, prostate cancer, and breast cancer. It is potent against 60 cancer cell lines with a mean GI50 value of 65 nM, and with a GI50 value less than 10 nM against four cancer cell lines[1].

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

NSC781406 Related Antibodies
In Vivo

In the xenograft models, treatment with 30 mg/kg of NSC781406 results in statistically significant antitumor activity, with a mean reduction in relative tumor volume ratio of 52%. Sorafenib displays an inhibition ratio of 44% at 50 mg/kg. NSC781406 is well tolerated at 30 mg/kg, with no observed mortality or significant reduction of body weight[1].

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

627.68

Formula

C29H27F2N5O5S2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

FC1=CC(F)=CC=C1S(=O)(NC2=CC(C3=CC=C(N=CC=C4C#CCN5CCN(S(C)(=O)=O)CC5)C4=C3)=CN=C2OC)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 150 mg/mL (238.98 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 1.5932 mL 7.9658 mL 15.9317 mL
5 mM 0.3186 mL 1.5932 mL 3.1863 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

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: 3.75 mg/mL (5.97 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 3.75 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (37.5 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: ≥ 3.75 mg/mL (5.97 mM); Clear solution

    This protocol yields a clear solution of ≥ 3.75 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 (37.5 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
References
Kinase Assay
[1]

IC50 values for inhibition of the PI3K is measured. PI-103 is used as the reference compound. The compounds (NSC781406) are tested in duplicate for 10 concentrations, 100 nM or 500 nM as the top concentration. All reagents are diluted in kinase buffer.Three-fold, ten-point serial compound (NSC781406) dilutions are performed in kinase buffer[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay
[1]

Cytotoxic effects are tested in the human lung adenocarcinoma cells A549, human colon cancer cells HCT-116, human breast cancer cells MDA-MB-231 and human hepatocellular carcinoma cells BEL-7404. These four tumor cells are diluted to a density of 40,000–50,000 cells/mL in logarithmic phase. After the cells are treated with compounds (NSC781406) for 72 h, MTT solution (5 mg/mL, 20 μL) is added another 4h at 37°C. IC50 values are determined by a nonlinear regression analysis[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

Mice: NSC781406 is orally administered once a day 30 mg/kg for 14 consecutive days or with sorafenib at 50 mg/kg. The relative tumor volume to vehicle-treated control mice is monitored[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.5932 mL 7.9658 mL 15.9317 mL 39.8292 mL
5 mM 0.3186 mL 1.5932 mL 3.1863 mL 7.9658 mL
10 mM 0.1593 mL 0.7966 mL 1.5932 mL 3.9829 mL
15 mM 0.1062 mL 0.5311 mL 1.0621 mL 2.6553 mL
20 mM 0.0797 mL 0.3983 mL 0.7966 mL 1.9915 mL
25 mM 0.0637 mL 0.3186 mL 0.6373 mL 1.5932 mL
30 mM 0.0531 mL 0.2655 mL 0.5311 mL 1.3276 mL
40 mM 0.0398 mL 0.1991 mL 0.3983 mL 0.9957 mL
50 mM 0.0319 mL 0.1593 mL 0.3186 mL 0.7966 mL
60 mM 0.0266 mL 0.1328 mL 0.2655 mL 0.6638 mL
80 mM 0.0199 mL 0.0996 mL 0.1991 mL 0.4979 mL
100 mM 0.0159 mL 0.0797 mL 0.1593 mL 0.3983 mL
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NSC781406 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:

NSC7814061676893-24-5NSC 781406NSC-781406PI3KmTORPhosphoinositide 3-kinaseMammalian target of RapamycinInhibitorinhibitorinhibit

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