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BPTES 

Cat. No.: HY-12683 Purity: 98.50%
Data Sheet SDS Handling Instructions

BPTES is an allosteric and selective glutaminase inhibitor, used in cancer treatment.

For research use only. We do not sell to patients.
BPTES Chemical Structure

BPTES Chemical Structure

CAS No. : 314045-39-1

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO $104 In-stock
5 mg $90 In-stock
10 mg $115 In-stock
50 mg $370 In-stock
100 mg   Get quote  
200 mg   Get quote  

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

BPTES is an allosteric and selective glutaminase inhibitor, used in cancer treatment.

In Vitro

BPTES (10 µM) exhibits inhibition of PDAC cell proliferation[1]. BPTES preferentially slows growth of mutant IDH1 cells without inducing apoptosis. BPTES (10 µM) reduces glutaminase activity in both WT and mutant IDH1 expressing cells, diminishes glutamate and α-KG levels, and increases glycolytic intermediates while leaving total 2-HG levels unaffected[2]. BPTES (10 µM) shows a clear synergistic anti-cancer effect with 10 μM of 5-FU in A549 and EKVX cell lines, and results in a growth reduction response not only in EKVX and A549 but also in most of the NSCLC cell lines[3]. BPTES (10 µM) effectively reduces the levels of the metabolites of the TCA cycle, with no changes in the levels of metabolites in glycolysis and the pentose phosphate pathway. BPTES treatment reduces about 30% ATP production under normoxia, and an additional 10% reduction of ATP production is observed under hypoxia in EKVX[4].

In Vivo

BPTES-NPs (BPTES nanoparticles, 1.2 mg BPTES in 100 µL nanoparticles, i.v.) significantly attenuates tumor growth in the patient-derived pancreatic orthotopic tumor model[1].

References
Preparing Stock Solutions
Concentration Volume Mass 1 mg 5 mg 10 mg
1 mM 1.9059 mL 9.5296 mL 19.0592 mL
5 mM 0.3812 mL 1.9059 mL 3.8118 mL
10 mM 0.1906 mL 0.9530 mL 1.9059 mL
Please refer to the solubility information to select the appropriate solvent.
Kinase Assay
[2]

D54 cells are seeded in a T75 flask at 5×105 cells, and IDH1 expression is induced with doxycycline 48 hrs before assaying. Cells are collected and resuspended in PBS, 0.1% Triton X-100, and Halt-Protease Inhibitor. Cells are lysed for 30 min on ice and centrifuged for 30 min at 12000 rpm at 4°C. Protein concentration is measured using the BCA Assay. Varying amounts of protein are added to IDH activity assay buffer (33 mM Tris, pH 7.6, 0.33 mM EDTA, 0.1 mM NADP+, 1.33 mM MnCl2, and 1.3 mM isocitrate), and changes in absorbance at 340 nm after 5 min is documented for each protein amount. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay
[2]

BPTES is dissolved in DMSO.

Cells are plated at a density of 500 cells/well in a 96-well black clear bottom plate. At 24 hrs, media is changed to the appropriate media (DMEM with 4.5 g/L, 1.5 g/L or 0.1 g/L glucose, 10% FBS, pencillin/streptomycin, and 4 mM glutamine with or without doxycyline). 48 hours after plating, compounds or DMSO are added. Media and alamarBlue is added to a volume of 200 µL in each well. Fluorescence is measured at 48 hrs or 72 hrs (EGCG) using a Victor3 plate-reader. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

Four-week-old female Foxn1nuathymic nude mice are used for the assay. Freshly resected pancreatic tumor samples obtained from patients at the time of surgery are propagated from mouse to mouse as a live tumor bank. Once a tumor volume of 50 mm3 is reached (4 wk postimplantation), mice are treated with 12.5 mg/kg BPTES by intraperitoneal injection, 200 mg/kg CB-839 twice per d by oral gavage, 54 mg/kg BPTES-NPs (1.2 mg BPTES in 100 µL nanoparticles per mouse) by intravenous injection, blank-NPs (100 µL per mouse) by intravenous injection, 25 mg/kg gemcitabine intraperitoneally, 250 mg/kg metformin intraperitoneally daily, or a combination of BPTES-NPs with gemcitabine or metformin. BPTES-NPs are injected once every 3 d for a total of six injections over 16 d. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

524.68

Formula

C₂₄H₂₄N₆O₂S₃

CAS No.

314045-39-1

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: 52 mg/mL (Need ultrasonic and warming)

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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BPTES
Cat. No.:
HY-12683
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