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BX517(PDK1 inhibitor2) (Synonyms: PDK1 Inhibitor II)

Catalog No.GC15615

BX517(PDK1 inhibitor2) is a potent and selective inhibitor of PDK1 with IC50 of 6 nM.

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BX517(PDK1 inhibitor2) Chemical Structure

Cas No.: 850717-64-5

Size Price Stock Qty
10mM (in 1mL DMSO)
$62.00
In stock
5mg
$56.00
In stock
10mg
$77.00
In stock
25mg
$133.00
In stock
50mg
$245.00
In stock
100mg
$385.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

BX-517 is a potent and selective inhibitor of PDK1 that binds to the ATP binding pocket

of the protein (IC50 = 6 nM). BX-517 also blocks activation of Akt in tumor cells with 10-fold more potent (IC50 = 0.1–1.0 μM) than its analogs tested at the highest dose tested (10 μM). [1] The phosphoinositide-dependent kinase-1 (PDK1) is a Ser/Thr kinase that is a crucial activator of a range of protein kinases in the AGC kinase super-family that play key roles in the progression of cancer and for the activation of Akt, S6 kinase, and protein kinase C. [2]

References:
1.  Islam I, Brown G, Bryant J 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. 
2.  Islam I, Bryant J, Chou YL etc. 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.

Chemical Properties

Cas No. 850717-64-5 SDF
Synonyms PDK1 Inhibitor II
Chemical Name (Z)-N-(3-(1-(1H-pyrrol-2-yl)ethylidene)-2-hydroxy-3H-indol-5-yl)carbamimidic acid
Canonical SMILES C/C(C1=CC=CN1)=C(C(O)=N2)\C3=C2C=CC(NC(O)=N)=C3
Formula C15H14N4O2 M.Wt 282.3
Solubility ≥ 8.55mg/mL in DMSO 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.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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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
10 mM 0.3542 mL 1.7712 mL 3.5423 mL
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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.

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