CNX-1351
Based on 1 Customer Validation
CNX-1351 is a potent and isoform-selective targeted covalent PI3Kα inhibitor with IC50 of 6.8 nM.
For research use only. We do not sell to patients.
- Purity : 98.87%
- CAS No.: 1276105-89-5
- Formula: C30H35N7O3S
- Molecular Weight:573.71
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
Description
IC50 & Target
[1]|
PI3Kα 6.8 nM (IC50) |
PI3Kβ 166 nM (IC50) |
PI3Kδ 240.3 nM (IC50) |
PI3Kγ 3020 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| MCF7 | GI50 |
54.7 nM
Compound: 3, CNX-1351
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Growth inhibition of human MCF7 cells assessed as cell viability after 96 hrs by Cell Titre Glo assay
Growth inhibition of human MCF7 cells assessed as cell viability after 96 hrs by Cell Titre Glo assay
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[PMID: 23360348] |
| SK-OV-3 | EC50 |
10 nM
Compound: 3, CNX-1351
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Inhibition of PI3Kalpha in human SKOV3 cells assessed as inhibition of Akt Ser473 phosphorylation at 1 to 1000 nM after 1 hr by immunoblot analysis
Inhibition of PI3Kalpha in human SKOV3 cells assessed as inhibition of Akt Ser473 phosphorylation at 1 to 1000 nM after 1 hr by immunoblot analysis
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[PMID: 23360348] |
| SK-OV-3 | GI50 |
77.6 nM
Compound: 3, CNX-1351
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Growth inhibition of human SKOV3 cells assessed as cell viability after 96 hrs by Cell Titre Glo assay
Growth inhibition of human SKOV3 cells assessed as cell viability after 96 hrs by Cell Titre Glo assay
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[PMID: 23360348] |
In Vitro
CNX-1351 is able to potently (EC50<100 nM) and specifically inhibit signaling in PI3Kα-dependent cancer cell lines, and this leads to a potent antiproliferative effect (GI50<100 nM). CNX-1351 inhibits PI3K signaling in SKOV3 cells, with potency (EC50 of 10-100 nM) similar to that of the pan-PI3K inhibitor. To investigate the functional consequence of inhibiting PI3Kα in cells, two cell lines with different PIK3CA activating mutations, SKOV3 ovarian cancer cells (H1047R) and MCF-7 breast cancer cells (E545K), are treated with CNX-1351 and growth is monitored. Both PIK3CA-driven cell lines are growth inhibited by exposure to CNX-1351 for 96 h (GI50 of 78 and 55 nM, respectively)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1276105-89-5
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Appearance Solid
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Molecular Weight 573.71
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Formula C30H35N7O3S
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Color White to yellow
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SMILES
C/C(C)=C/C(CCC(N1CCN(CC2=CC3=NC(C4=CC=CC5=C4C=NN5)=NC(N6CCOCC6)=C3S2)CC1)=O)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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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 : 100 mg/mL (174.30 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.36 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Purity & Documentation
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Data Sheet (277 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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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, 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 | 1.7430 mL | 8.7152 mL | 17.4304 mL | 43.5760 mL |
| 5 mM | 0.3486 mL | 1.7430 mL | 3.4861 mL | 8.7152 mL | |
| 10 mM | 0.1743 mL | 0.8715 mL | 1.7430 mL | 4.3576 mL | |
| 15 mM | 0.1162 mL | 0.5810 mL | 1.1620 mL | 2.9051 mL | |
| 20 mM | 0.0872 mL | 0.4358 mL | 0.8715 mL | 2.1788 mL | |
| 25 mM | 0.0697 mL | 0.3486 mL | 0.6972 mL | 1.7430 mL | |
| 30 mM | 0.0581 mL | 0.2905 mL | 0.5810 mL | 1.4525 mL | |
| 40 mM | 0.0436 mL | 0.2179 mL | 0.4358 mL | 1.0894 mL | |
| 50 mM | 0.0349 mL | 0.1743 mL | 0.3486 mL | 0.8715 mL | |
| 60 mM | 0.0291 mL | 0.1453 mL | 0.2905 mL | 0.7263 mL | |
| 80 mM | 0.0218 mL | 0.1089 mL | 0.2179 mL | 0.5447 mL | |
| 100 mM | 0.0174 mL | 0.0872 mL | 0.1743 mL | 0.4358 mL |
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