1. PI3K/Akt/mTOR
  2. PDK-1
  3. BX517

BX517 is a potent and selective inhibitor of PDK1 with IC50 of 6 nM.

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

BX517 Chemical Structure

BX517 Chemical Structure

CAS No. : 850717-64-5

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 88 In-stock
Solution
10 mM * 1 mL in DMSO USD 88 In-stock
Solid
5 mg USD 80 In-stock
10 mg USD 110 In-stock
25 mg USD 190 In-stock
50 mg USD 350 In-stock
100 mg USD 550 In-stock
200 mg   Get quote  
500 mg   Get quote  

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products

1 Publications Citing Use of MCE BX517

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

BX517 is a potent and selective inhibitor of PDK1 with IC50 of 6 nM.

IC50 & Target

IC50: 6 nM (PDK1)

In Vitro

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.

Molecular Weight

282.30

Formula

C15H14N4O2

CAS No.
Appearance

Solid

Color

Light yellow to khaki

SMILES

NC(NC1=CC=C(NC(/C2=C(C)\C3=CC=CN3)=O)C2=C1)=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 : ≥ 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.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.5423 mL 17.7117 mL 35.4233 mL
5 mM 0.7085 mL 3.5423 mL 7.0847 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: ≥ 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.
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

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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BX517 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.

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Product Name:
BX517
Cat. No.:
HY-13842
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