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Rapamycin(Synonyms: 雷帕霉素; 西羅莫司; Sirolimus; AY-22989)

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Rapamycin (Sirolimus) 是一種有效且特異性的 mTOR 抑制劑，作用于 HEK293 細胞，抑制 mTOR，IC50 為 0.1 nM。Rapamycin 與 FKBP12 結合且抑制 mTORC1。Rapamycin 還是一種自噬 (autophagy) 激活劑，免疫抑制劑。
貨號：HY-10219
參數(shù)品牌：MCE
產品參數(shù)
品牌：MCE
型號：HY-10219
起訂量：1
規(guī)格:：10mg
價格:：￥550
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產品詳情

Rapamycin (Sirolimus) 是一種有效且特異性的 mTOR 抑制劑，作用于 HEK293 細胞，抑制 mTOR，IC50 為 0.1 nM。Rapamycin 與 FKBP12 結合且抑制 mTORC1。Rapamycin 還是一種自噬 (autophagy) 激活劑，免疫抑制劑。


生物活性
 Rapamycin (Sirolimus; AY 22989) is a potent and specific mTOR inhibitor with an IC50 of 0.1 nM in HEK293 cells. Rapamycin binds to FKBP12 and specifically acts as an allosteric inhibitor of mTORC1[1]. Rapamycin is an autophagy activator, an immunosuppressant[2].
IC50 & Target[1][2]
mTOR：0.1 nM (IC50, in HEK293 cells )

 


體外研究
(In Vitro)


Rapamycin (12.5-100 nM; 24 hours) treatment exerts modest inhibitory effect on lung cancer cell proliferation in a dose-dependent manner in all cell lines (A549, SPC-A-1, 95D and NCI-H446 cells) tested, achieving about 30-40% reduction in cell proliferation at 100 nM vs. ~10% reduction at 12.5 nM[3].
Lung cancer cell line 95D cells are exposed to Rapamycin (10 nM, 20 nM) and RP-56976 (1 nM, 10 nM) alone or in combination (Rapamycin 20 nM+ RP-56976 10 nM). After 24 hours exposure to Rapamycin or RP-56976 alone does not significantly alter the level of expression or phosphorylation of ERK1/2, whereas cells treated with the combination of Rapamycin with RP-56976 exhibit a marked reduction in the phosphorylation levels of ERK1/2[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[3]

Cell Line: Lung cancer cell lines A549, SPC-A-1, 95D and NCI-H446
Concentration: 12.5 nM, 25 nM, 50 nM, 100 nM
Incubation Time: 24 hours
Result: Treatment exerted modest inhibitory effect on lung cancer cell proliferation in a dose-dependent manner in all cell lines.



體內研究
(In Vivo)


Rapamycin (2.0 mg/kg; intraperitoneal injection; every other day; 28 days) alone has a moderate inhibitory effect. However, the combination of Metformin and Rapamycin exerts a significantly increased inhibition of tumor growth compared with the control group, the Rapamycin monotherapy group and the Metformin monotherapy group[4].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: 24 male nu/nu mice aged 4-5 week old (15-20 g)[4]
Dosage: 2.0 mg/kg
Administration: Intraperitoneal injection; every other day; 28 days
Result: Had a moderate inhibitory effect in monotherapy group. The combination with Metformin exerted a significantly increased inhibition of tumor growth.



Clinical Trial
NCT Number Sponsor Condition Start Date Phase
NCT01885689 City of Hope Medical Center|National Cancer Institute (NCI)
Adult Acute Lymphoblastic Leukemia in Remission|Acute Myeloid Leukemia Arising From Previous Myelodysplastic Syndrome|Adult Acute Myeloid Leukemia in Remission|Myelodysplastic Syndrome|Secondary Myelodysplastic Syndrome|Chronic Myelomonocytic Leukemia|Therapy-Related Myelodysplastic Syndrome
February 10, 2014 Phase 2
NCT04893291 Fondazione Ricerca e Innovazione Cardiovascolare ETS
Coronary Artery Disease|Coronary Artery Stenosis
October 30, 2021 Not Applicable
NCT03582878 Institute for Clinical and Experimental Medicine
Diabetes Mellitus, Type 1
January 1, 2004 Phase 4

分子量
 914.17
CAS 號
 53123-88-9
Formula
 C51H79NO 13
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)


In Vitro: 

DMSO : 125 mg/mL (136.74 mM; Need ultrasonic)

Ethanol : 50 mg/mL (54.69 mM; Need ultrasonic)

配制儲備液
濃度溶劑體積質量 1 mg 5 mg 10 mg
1 mM 1.0939 mL 5.4694 mL 10.9389 mL
5 mM 0.2188 mL 1.0939 mL 2.1878 mL
10 mM 0.1094 mL 0.5469 mL 1.0939 mL
*

請根據(jù)產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，避免反復凍融造成的產品失效。
儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 儲存時，請在 6 個月內使用，-20°C 儲存時，請在 1 個月內使用。

In Vivo:

——為保證實驗結果的可靠性，澄清的儲備液可以根據(jù)儲存條件，適當保存；體內實驗的工作液，建議您現(xiàn)用現(xiàn)配，當天使用； 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% EtOH    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (2.73 mM); Suspended solution

  • 2.

    請依序添加每種溶劑： 10% EtOH    90% (20% SBE-β-CD in saline)

    Solubility: 2.5 mg/mL (2.73 mM); Suspended solution; Need ultrasonic

  • 3.

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

    Solubility: ≥ 2.5 mg/mL (2.73 mM); Suspended solution

  • 4.

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

    Solubility: ≥ 2.08 mg/mL (2.28 mM); Clear solution

  • 5.

    請依序添加每種溶劑： 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.08 mg/mL (2.28 mM); Suspended solution; Need ultrasonic

  • 6.

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

    Solubility: ≥ 2.08 mg/mL (2.28 mM); Clear solution



參考文獻


[1]. Edwards SR, et al. The rapamycin-binding domain of the protein kinase mammalian target of rapamycin is a destabilizing domain. J Biol Chem, 2007, 282(18), 13395-13401.

[2]. Rangaraju S, et al. Rapamycin activates autophagy and improves myelination in explant cultures from neuropathicmice. J Neurosci. 2010 Aug 25;30(34):11388-97.

[3]. Niu H, et al. Rapamycin potentiates cytotoxicity by RP-56976 possibly through downregulation of Survivin in lung cancer cells. J Exp Clin Cancer Res. 2011 Mar 10;30:28.

[4]. Zhang JW, et al. Metformin synergizes with rapamycin to inhibit the growth of pancreatic cancer in vitro and in vivo. Oncol Lett. 2018 Feb;15(2):1811-1816.



Rapamycin(Synonyms: 雷帕霉素; 西羅莫司; Sirolimus; AY-22989)
Rapamycin(Synonyms: 雷帕霉素; 西羅莫司; Sirolimus; AY-22989)

Rapamycin(Synonyms: 雷帕霉素; 西羅莫司; Sirolimus; AY-22989)

分享到微信

×
Rapamycin (Sirolimus) 是一種有效且特異性的 mTOR 抑制劑，作用于 HEK293 細胞，抑制 mTOR，IC50 為 0.1 nM。Rapamycin 與 FKBP12 結合且抑制 mTORC1。Rapamycin 還是一種自噬 (autophagy) 激活劑，免疫抑制劑。
貨號：HY-10219
品牌：MCE
型號：HY-10219
起訂量：1
規(guī)格:：10mg
價格:：￥550
15906629305
在線客服
產品詳情

Rapamycin (Sirolimus) 是一種有效且特異性的 mTOR 抑制劑，作用于 HEK293 細胞，抑制 mTOR，IC50 為 0.1 nM。Rapamycin 與 FKBP12 結合且抑制 mTORC1。Rapamycin 還是一種自噬 (autophagy) 激活劑，免疫抑制劑。


生物活性
 Rapamycin (Sirolimus; AY 22989) is a potent and specific mTOR inhibitor with an IC50 of 0.1 nM in HEK293 cells. Rapamycin binds to FKBP12 and specifically acts as an allosteric inhibitor of mTORC1[1]. Rapamycin is an autophagy activator, an immunosuppressant[2].
IC50 & Target[1][2]
mTOR：0.1 nM (IC50, in HEK293 cells )

 


體外研究
(In Vitro)


Rapamycin (12.5-100 nM; 24 hours) treatment exerts modest inhibitory effect on lung cancer cell proliferation in a dose-dependent manner in all cell lines (A549, SPC-A-1, 95D and NCI-H446 cells) tested, achieving about 30-40% reduction in cell proliferation at 100 nM vs. ~10% reduction at 12.5 nM[3].
Lung cancer cell line 95D cells are exposed to Rapamycin (10 nM, 20 nM) and RP-56976 (1 nM, 10 nM) alone or in combination (Rapamycin 20 nM+ RP-56976 10 nM). After 24 hours exposure to Rapamycin or RP-56976 alone does not significantly alter the level of expression or phosphorylation of ERK1/2, whereas cells treated with the combination of Rapamycin with RP-56976 exhibit a marked reduction in the phosphorylation levels of ERK1/2[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[3]

Cell Line: Lung cancer cell lines A549, SPC-A-1, 95D and NCI-H446
Concentration: 12.5 nM, 25 nM, 50 nM, 100 nM
Incubation Time: 24 hours
Result: Treatment exerted modest inhibitory effect on lung cancer cell proliferation in a dose-dependent manner in all cell lines.



體內研究
(In Vivo)


Rapamycin (2.0 mg/kg; intraperitoneal injection; every other day; 28 days) alone has a moderate inhibitory effect. However, the combination of Metformin and Rapamycin exerts a significantly increased inhibition of tumor growth compared with the control group, the Rapamycin monotherapy group and the Metformin monotherapy group[4].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: 24 male nu/nu mice aged 4-5 week old (15-20 g)[4]
Dosage: 2.0 mg/kg
Administration: Intraperitoneal injection; every other day; 28 days
Result: Had a moderate inhibitory effect in monotherapy group. The combination with Metformin exerted a significantly increased inhibition of tumor growth.



Clinical Trial
NCT Number Sponsor Condition Start Date Phase
NCT01885689 City of Hope Medical Center|National Cancer Institute (NCI)
Adult Acute Lymphoblastic Leukemia in Remission|Acute Myeloid Leukemia Arising From Previous Myelodysplastic Syndrome|Adult Acute Myeloid Leukemia in Remission|Myelodysplastic Syndrome|Secondary Myelodysplastic Syndrome|Chronic Myelomonocytic Leukemia|Therapy-Related Myelodysplastic Syndrome
February 10, 2014 Phase 2
NCT04893291 Fondazione Ricerca e Innovazione Cardiovascolare ETS
Coronary Artery Disease|Coronary Artery Stenosis
October 30, 2021 Not Applicable
NCT03582878 Institute for Clinical and Experimental Medicine
Diabetes Mellitus, Type 1
January 1, 2004 Phase 4

分子量
 914.17
CAS 號
 53123-88-9
Formula
 C51H79NO 13
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)


In Vitro: 

DMSO : 125 mg/mL (136.74 mM; Need ultrasonic)

Ethanol : 50 mg/mL (54.69 mM; Need ultrasonic)

配制儲備液
濃度溶劑體積質量 1 mg 5 mg 10 mg
1 mM 1.0939 mL 5.4694 mL 10.9389 mL
5 mM 0.2188 mL 1.0939 mL 2.1878 mL
10 mM 0.1094 mL 0.5469 mL 1.0939 mL
*

請根據(jù)產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，避免反復凍融造成的產品失效。
儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 儲存時，請在 6 個月內使用，-20°C 儲存時，請在 1 個月內使用。

In Vivo:

——為保證實驗結果的可靠性，澄清的儲備液可以根據(jù)儲存條件，適當保存；體內實驗的工作液，建議您現(xiàn)用現(xiàn)配，當天使用； 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% EtOH    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (2.73 mM); Suspended solution

  • 2.

    請依序添加每種溶劑： 10% EtOH    90% (20% SBE-β-CD in saline)

    Solubility: 2.5 mg/mL (2.73 mM); Suspended solution; Need ultrasonic

  • 3.

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

    Solubility: ≥ 2.5 mg/mL (2.73 mM); Suspended solution

  • 4.

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

    Solubility: ≥ 2.08 mg/mL (2.28 mM); Clear solution

  • 5.

    請依序添加每種溶劑： 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.08 mg/mL (2.28 mM); Suspended solution; Need ultrasonic

  • 6.

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

    Solubility: ≥ 2.08 mg/mL (2.28 mM); Clear solution



參考文獻


[1]. Edwards SR, et al. The rapamycin-binding domain of the protein kinase mammalian target of rapamycin is a destabilizing domain. J Biol Chem, 2007, 282(18), 13395-13401.

[2]. Rangaraju S, et al. Rapamycin activates autophagy and improves myelination in explant cultures from neuropathicmice. J Neurosci. 2010 Aug 25;30(34):11388-97.

[3]. Niu H, et al. Rapamycin potentiates cytotoxicity by RP-56976 possibly through downregulation of Survivin in lung cancer cells. J Exp Clin Cancer Res. 2011 Mar 10;30:28.

[4]. Zhang JW, et al. Metformin synergizes with rapamycin to inhibit the growth of pancreatic cancer in vitro and in vivo. Oncol Lett. 2018 Feb;15(2):1811-1816.



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