BPTES is an allosteric and selective glutaminase inhibitor with an IC₅₀ of 0.16 μM.

Glutaminase^[1]

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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

524.68

C₂₄H₂₄N₆O₂S₃

314045-39-1

Room temperature in continental US; may vary elsewhere.

DMSO : 100 mg/mL (190.59 mM; Need ultrasonic)

H₂O : ≥ 0.1 mg/mL (0.19 mM)

* “≥” means soluble, but saturation unknown.

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

• 1.

  请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

  Solubility: 2.5 mg/mL (4.76 mM); Suspended solution; Need ultrasonic

  此方案可获得 2.5 mg/mL (4.76 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

  将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

• 2.

  请依序添加每种溶剂： 10% DMSO    90% corn oil

  Solubility: ≥ 2.08 mg/mL (3.96 mM); Clear solution

  此方案可获得 ≥ 2.08 mg/mL (3.96 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

  以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

• 3.

  请依序添加每种溶剂： 2% DMSO    40% PEG300    5% Tween-80    53% saline

  Solubility: 2 mg/mL (3.81 mM); Suspended solution; Need ultrasonic

• [1]. Elgogary A, et al. Combination therapy with BPTES nanoparticles and targets the metabolic heterogeneity of pancreatic cancer. Proc Natl Acad Sci U S A. 2016 Sep 6;113(36):E5328-36.

  [2]. Meghan J. Seltzer, et al. Inhibition of glutaminase preferentially slows growth of glioma cells with mutant IDH1. Cancer Res. 2010 Nov 15; 70(22): 8981-8987.

  [3]. Lee JS, et al. Glutaminase 1 inhibition reduces thymidine synthesis in NSCLC. Biochem Biophys Res Commun. 2016 Aug 26;477(3):374-82

  [4]. Lee JS, et al. Dual targeting of glutaminase 1 and thymidylate synthase elicits death synergistically in NSCLC. Cell Death Dis. 2016 Dec 8;7(12):e2511.

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, and 4 mM glutamine). 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.

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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 LY 188011 intraperitoneally, or a combination of BPTES-NPs with LY 188011. BPTES-NPs are injected once every 3 d for a total of six injections over 16 d.

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

• [1]. Elgogary A, et al. Combination therapy with BPTES nanoparticles and targets the metabolic heterogeneity of pancreatic cancer. Proc Natl Acad Sci U S A. 2016 Sep 6;113(36):E5328-36.

  [2]. Meghan J. Seltzer, et al. Inhibition of glutaminase preferentially slows growth of glioma cells with mutant IDH1. Cancer Res. 2010 Nov 15; 70(22): 8981-8987.

  [3]. Lee JS, et al. Glutaminase 1 inhibition reduces thymidine synthesis in NSCLC. Biochem Biophys Res Commun. 2016 Aug 26;477(3):374-82

  [4]. Lee JS, et al. Dual targeting of glutaminase 1 and thymidylate synthase elicits death synergistically in NSCLC. Cell Death Dis. 2016 Dec 8;7(12):e2511.