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BPTES

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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。

貨號:HY-12683
CAS:314045-39-1
參數(shù)品牌:MCE
產(chǎn)品參數(shù)
品牌:MCE
型號:HY-12683
起訂量:1
規(guī)格::5mg
價格::¥720
我知道了
在線客服
產(chǎn)品詳情

BPTES 

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°C3 years

4°C2 years
In solvent-80°C6 months

-20°C1 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.

配制儲備液
濃度溶劑體積質(zhì)量1 mg5 mg10 mg
1 mM1.9059 mL9.5296 mL19.0592 mL
5 mM0.3812 mL1.9059 mL3.8118 mL
10 mM0.1906 mL0.9530 mL1.9059 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。

In Vivo:

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

  • 1.


    請依序添加每種溶劑: 10% DMSO    40% PEG300    5% Tween-80    45% saline

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


  • 2.


    請依序添加每種溶劑: 10% DMSO    90% corn oil

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


  • 3.


    請依序添加每種溶劑: 2% DMSO    40% PEG300    5% Tween-80    53% saline

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


參考文獻(xiàn)

[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.







BPTES

BPTES

分享到微信

×
BPTES是選擇性的谷氨酰胺酶變構(gòu)抑制劑,IC50 為0.16 μM。

貨號:HY-12683
CAS:314045-39-1
品牌:MCE
型號:HY-12683
起訂量:1
規(guī)格::5mg
價格::¥720
15906629305
在線客服
產(chǎn)品詳情

BPTES 

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°C3 years

4°C2 years
In solvent-80°C6 months

-20°C1 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.

配制儲備液
濃度溶劑體積質(zhì)量1 mg5 mg10 mg
1 mM1.9059 mL9.5296 mL19.0592 mL
5 mM0.3812 mL1.9059 mL3.8118 mL
10 mM0.1906 mL0.9530 mL1.9059 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。

In Vivo:

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

  • 1.


    請依序添加每種溶劑: 10% DMSO    40% PEG300    5% Tween-80    45% saline

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


  • 2.


    請依序添加每種溶劑: 10% DMSO    90% corn oil

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


  • 3.


    請依序添加每種溶劑: 2% DMSO    40% PEG300    5% Tween-80    53% saline

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


參考文獻(xiàn)

[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.







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