NSC781406 |
| Catalog No.GC33014 |
A dual inhibitor of PI3K and mTOR
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1676893-24-5
Sample solution is provided at 25 µL, 10mM.
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NSC781406 is a highly potent PI3K and mTOR inhibitor with an IC50 of 2 nM for PI3Kα.
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].
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].
[1]. Chen Y, et al. Discovery of benzenesulfonamide derivatives as potent PI3K/mTOR dual inhibitors with in vivo efficacies against hepatocellular carcinoma. Bioorg Med Chem. 2016 Mar 1;24(5):957-66.
Kinase experiment: | 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]. |
Cell experiment: | 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]. |
Animal experiment: | 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]. |
References: [1]. Chen Y, et al. Discovery of benzenesulfonamide derivatives as potent PI3K/mTOR dual inhibitors with in vivo efficacies against hepatocellular carcinoma. Bioorg Med Chem. 2016 Mar 1;24(5):957-66. | |
| Cas No. | 1676893-24-5 | SDF | |
| Canonical 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 | ||
| Formula | C29H27F2N5O5S2 | M.Wt | 627.68 |
| Solubility | DMSO : ≥ 150 mg/mL (238.98 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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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 |
| 10 mM | 0.1593 mL | 0.7966 mL | 1.5932 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 9 reference(s) in Google Scholar.)
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