BX517
Based on 2 publication(s) in Google Scholar
BX517 is a potent and selective inhibitor of PDK1 with IC50 of 6 nM.
For research use only. We do not sell to patients.
- Purity: 98.0%
- CAS No.: 850717-64-5
- Formula: C15H14N4O2
- Molecular Weight:282.30
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) BX517
More
Biological Activity
IC50: 6 nM (PDK1)
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| PC-3 | IC50 |
0.1 μM
Compound: BX-517
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Inhibition of AKT phosphorylation in PC3 cells
Inhibition of AKT phosphorylation in PC3 cells
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[PMID: 17544272] |
| PC-3 | IC50 |
100 nM
Compound: 4i, BX-517
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Inhibition of Akt phosphorylation in PC3 cells
Inhibition of Akt phosphorylation in PC3 cells
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[PMID: 17531483] |
BX-517 blocks activation of Akt in tumor cells, is potent with IC50 of 0.1-1.0 μM[1]. BX-517 blocks AKT2 activation in cells with submicromolar potency. BX-517 is 100-fold selective or better against a panel of seven additional Ser/Thr and Tyr kinases[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 850717-64-5
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Appearance Solid
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Molecular Weight 282.30
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Formula C15H14N4O2
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Color Light yellow to khaki
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SMILES
NC(NC1=CC=C(NC(/C2=C(C)\C3=CC=CN3)=O)C2=C1)=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
Publications (2)
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Journal Impact Factor
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Most Recent
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J Plant Physiol
BX517, an inhibitor of the mammalian phospholipid-dependent kinase 1 (PDK1), antagonizes sucrose-induced plant growth and represses the target of rapamycin (TOR) signaling and the cell cycle through WEE1 kinase in Arabidopsis thaliana. [Abstract]2024 Nov 28:304:154386. PMID: 39616729 -
PeerJ
A novel dual MEK/PDK1 inhibitor 9za retards the cell cycle at G0/G1 phase and induces mitochondrial apoptosis in non-small cell lung cancer cells. [Abstract]2020 Oct 2;8:e9981. PMID: 33072436
Solvent & Solubility
DMSO : ≥ 27 mg/mL (95.64 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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)
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 (8.86 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.
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.
Purity & Documentation
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Data Sheet (274 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)
- Portuguese - PT (396 KB)
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Handling Instructions (2659 KB)
References
[1]. Islam I, et al. Indolinone based phosphoinositide-dependent kinase-1 (PDK1) inhibitors. Part 2: optimization of BX-517. Bioorg Med Chem Lett. 2007 Jul 15;17(14):3819-25. [Content Brief]
[2]. Islam I, et al. Indolinone based phosphoinositide-dependent kinase-1 (PDK1) inhibitors. Part 1: design, synthesis and biological activity. Bioorg Med Chem Lett. 2007 Jul 15;17(14):3814-8. [Content Brief]
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 | 3.5423 mL | 17.7117 mL | 35.4233 mL | 88.5583 mL |
| 5 mM | 0.7085 mL | 3.5423 mL | 7.0847 mL | 17.7117 mL | |
| 10 mM | 0.3542 mL | 1.7712 mL | 3.5423 mL | 8.8558 mL | |
| 15 mM | 0.2362 mL | 1.1808 mL | 2.3616 mL | 5.9039 mL | |
| 20 mM | 0.1771 mL | 0.8856 mL | 1.7712 mL | 4.4279 mL | |
| 25 mM | 0.1417 mL | 0.7085 mL | 1.4169 mL | 3.5423 mL | |
| 30 mM | 0.1181 mL | 0.5904 mL | 1.1808 mL | 2.9519 mL | |
| 40 mM | 0.0886 mL | 0.4428 mL | 0.8856 mL | 2.2140 mL | |
| 50 mM | 0.0708 mL | 0.3542 mL | 0.7085 mL | 1.7712 mL | |
| 60 mM | 0.0590 mL | 0.2952 mL | 0.5904 mL | 1.4760 mL | |
| 80 mM | 0.0443 mL | 0.2214 mL | 0.4428 mL | 1.1070 mL |
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