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BPTES是選擇性的谷氨酰胺酶變構(gòu)抑制劑,IC50 為0.16 μM。
生物活性
BPTES is an allosteric and selective glutaminase inhibitor with an IC50 of 0.16 μM.
IC50 & Target
Glutaminase
體外研究(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
體內(nèi)研究(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
分子量:524.68
Formula:C24H24N6O2S3
CAS 號:314045-39-1
運(yùn)輸條件:Room temperature in continental US; may vary elsewhere.
儲存方式:
Powder | -20°C | 3 years |
---|---|---|
4°C | 2 years | |
In solvent | -80°C | 6 months |
-20°C | 1 month |
溶解性數(shù)據(jù)
DMSO : 100 mg/mL (190.59 mM; Need ultrasonic)
H2O : ≥ 0.1 mg/mL (0.19 mM)
* "≥" means soluble, but saturation unknown.
濃度溶劑體積質(zhì)量 | 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 |
請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液;一旦配成溶液,請分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 儲存時,請?jiān)?6 個月內(nèi)使用,-20°C 儲存時,請?jiān)?1 個月內(nèi)使用。
請根據(jù)您的實(shí)驗(yàn)動物和給藥方式選擇適當(dāng)?shù)娜芙夥桨浮R韵氯芙夥桨付颊埾劝凑?nbsp;In Vitro 方式配制澄清的儲備液,再依次添加助溶劑:
——為保證實(shí)驗(yàn)結(jié)果的可靠性,澄清的儲備液可以根據(jù)儲存條件,適當(dāng)保存;體內(nèi)實(shí)驗(yàn)的工作液,建議您現(xiàn)用現(xiàn)配,當(dāng)天使用; 以下溶劑前顯示的百
分比是指該溶劑在您配制終溶液中的體積占比;如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象,可以通過加熱和/或超聲的方式助溶
參考文獻(xiàn)
BPTES是選擇性的谷氨酰胺酶變構(gòu)抑制劑,IC50 為0.16 μM。
生物活性
BPTES is an allosteric and selective glutaminase inhibitor with an IC50 of 0.16 μM.
IC50 & Target
Glutaminase
體外研究(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
體內(nèi)研究(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
分子量:524.68
Formula:C24H24N6O2S3
CAS 號:314045-39-1
運(yùn)輸條件:Room temperature in continental US; may vary elsewhere.
儲存方式:
Powder | -20°C | 3 years |
---|---|---|
4°C | 2 years | |
In solvent | -80°C | 6 months |
-20°C | 1 month |
溶解性數(shù)據(jù)
DMSO : 100 mg/mL (190.59 mM; Need ultrasonic)
H2O : ≥ 0.1 mg/mL (0.19 mM)
* "≥" means soluble, but saturation unknown.
濃度溶劑體積質(zhì)量 | 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 |
請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液;一旦配成溶液,請分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 儲存時,請?jiān)?6 個月內(nèi)使用,-20°C 儲存時,請?jiān)?1 個月內(nèi)使用。
請根據(jù)您的實(shí)驗(yàn)動物和給藥方式選擇適當(dāng)?shù)娜芙夥桨浮R韵氯芙夥桨付颊埾劝凑?nbsp;In Vitro 方式配制澄清的儲備液,再依次添加助溶劑:
——為保證實(shí)驗(yàn)結(jié)果的可靠性,澄清的儲備液可以根據(jù)儲存條件,適當(dāng)保存;體內(nèi)實(shí)驗(yàn)的工作液,建議您現(xiàn)用現(xiàn)配,當(dāng)天使用; 以下溶劑前顯示的百
分比是指該溶劑在您配制終溶液中的體積占比;如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象,可以通過加熱和/或超聲的方式助溶
參考文獻(xiàn)