BPTES
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货号：A413914
BPTES通过变构调节表现出对谷氨酰胺酶 的强效抑制作用，具有选择性，IC50 为 0.16 μM。
BPTES 化学结构
BPTES 3D分子结构
规格
价格
会员价
库存
数量
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BPTES 纯度/质量文件 产品仅供科研
货号：A413914
标准纯度：
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产品说明书
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BPTES 质控信息
Telaglenastat
+++
99%+
BPTES
++
Glutaminase GLS1 (KGA), IC50: 0.16 μM
98%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。
BPTES 生物活性
靶点
描述
Glutaminase (GLS) is responsible for the hydrolysis of glutamine into glutamate and ammonia. BPTES is a potent and selective allosteric inhibitor of kidney-type GLS （KGS） with an IC50 value of 3.3 ± 0.7 μM[6] [7] [8]
BPTES 动物研究
Dose
Mice: 10 mg/kg[3] [4] [5] [5]
Administration
p.o., i.p., i.v.
Pharmacokinetics
Animal
Rats[5]
Dose
2.0 mg/kg (i.v.)
Administration
i.v.
F
2% (p.o.)
AUC0-inf
636 ± 90 (ng/ml)·h (i.v.)
T1/2
5.3 ± 1.4 h (i.v.)
Tmax
0.7 ± 0.3 h (p.o.)
CL
53 ± 7.6 ml/min/kg (i.v.)
Cmax
40 ± 8.2 ng/ml (p.o.)
Vss
8.8 ± 1.6 L/kg (i.v.)
BPTES 参考文献
[1] Xiang Y, Stine ZE, et al. Targeted inhibition of tumor-specific glutaminase diminishes cell-autonomous tumorigenesis. J Clin Invest. 2015 Jun;125(6):2293-306.
[2] Seltzer MJ, Bennett BD, et al. Inhibition of glutaminase preferentially slows growth of glioma cells with mutant IDH1. Cancer Res. 2010 Nov 15;70(22):8981-7.
[3] Lee JS, Kang JH, et al. Dual targeting of glutaminase 1 and thymidylate synthase elicits death synergistically in NSCLC. Cell Death Dis. 2016 Dec 8;7(12):e2511.
[4] Elgogary A, Xu Q, et al. Combination therapy with BPTES nanoparticles and metformin targets the metabolic heterogeneity of pancreatic cancer. Proc Natl Acad Sci U S A. 2016 Sep 6;113(36):E5328-36.
[5] Yeh TK, Kuo CC, et al. Design, Synthesis, and Evaluation of Thiazolidine-2,4-dione Derivatives as a Novel Class of Glutaminase Inhibitors. J Med Chem. 2017 Jul 13;60(13):5599-5612.
[6] Shukla K, Ferraris DV, Thomas AG, Stathis M, Duvall B, Delahanty G, Alt J, Rais R, Rojas C, Gao P, Xiang Y, Dang CV, Slusher BS, Tsukamoto T. Design, synthesis, and pharmacological evaluation of bis-2-(5-phenylacetamido-1,2,4-thiadiazol-2-yl)ethyl sulfide 3 (BPTES) analogs as glutaminase inhibitors. J Med Chem. 2012 Dec 13;55(23):10551-63. doi: 10.1021/jm301191p. Epub 2012 Nov 30. PMID: 23151085; PMCID: PMC3539823.
[7] Seltzer MJ, Bennett BD, Joshi AD, Gao P, Thomas AG, Ferraris DV, Tsukamoto T, Rojas CJ, Slusher BS, Rabinowitz JD, Dang CV, Riggins GJ. Inhibition of glutaminase preferentially slows growth of glioma cells with mutant IDH1. Cancer Res. 2010 Nov 15;70(22):8981-7. doi: 10.1158/0008-5472.CAN-10-1666. Epub 2010 Nov 2. PMID: 21045145; PMCID: PMC3058858.
[8] Le A, Lane AN, Hamaker M, Bose S, Gouw A, Barbi J, Tsukamoto T, Rojas CJ, Slusher BS, Zhang H, Zimmerman LJ, Liebler DC, Slebos RJ, Lorkiewicz PK, Higashi RM, Fan TW, Dang CV. Glucose-independent glutamine metabolism via TCA cycling for proliferation and survival in B cells. Cell Metab. 2012 Jan 4;15(1):110-21. doi: 10.1016/j.cmet.2011.12.009. PMID: 22225880; PMCID: PMC3345194.
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BPTES 实验方案
计算器
摩尔计算器
总药量计算器
工作液计算器
存储液制备
1mg
5mg
10mg
1 mM
5 mM
10 mM
1.91mL
0.38mL
0.19mL
9.53mL
1.91mL
0.95mL
19.06mL
3.81mL
1.91mL
BPTES 技术信息
搜索
