S1039

Rapamycin (Sirolimus)

 (Synonyms

Rapamune

)

Technical Data:
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Rapamycin (Sirolimus)
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M.Wt: 914.18
Formula: C51H79NO13
Solubility: DMSO
Purity: >99%
Storage: at -20℃ 2 years
CAS No.: 53123-88-9
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Applications & Customer's Feedback of Rapamycin (Sirolimus):

  • Rapamycin-Sirolimus was purchased from Selleck.Data from Biochem Pharmacol 2011.April;82:216-226.

    Inhibition of mTOR activity may be responsible for sorafenib-induced down-regulation of survivin. H1299 cells were treated with the indicated concentration of RAD001 or Rapamycin for 48 h. Then H1299 cells were incubated with or without 5 mM sorafenib, with or without 5 mM RAD001, and with or without 2 mM rapamycin for 48 h. The indicated protein levels were determined by Western blot analysis. b-Actin protein levels were measured as loading controls.

  • Rapamycin was purchased from Selleck.Data were provided by Dr.Ulrich Bommer of University of Wollongong.

    Rapamycin inhibits growth‐dependent TCTP induction. Cells were serum‐starved for 24h and restimulated with 20% FBS for the indicated times in the presence or absence of rapamycin. The graph shows the relative TCTP signal, corrected for the loading control.

  • Rapamycin was purchased from Selleck.Data from Cancer Cell 2011.June;19:1–13.

    Cooperative Effects of AR and mTOR Inhibition In Vitro and In Vivo (A) In vitro response of Pten null;Ar+ murine (CaP8) and human (LNCaP) prostate cancer cells to AR knockdown (sh-AR) or pharmacological inhibition of AR (MDV3100, 10 mM) with and without rapamycin (R: 1 nM) treatment (Sc, control sh oligo). (B and D) In vivo response to treatments with castration, MDV3100, rapamycin, or their combinations as measured by cell proliferation (Ki67+cells) and (C and D) tumor burden in Pb-Cre+;-PtenL/L and Pb-Cre+;PtenL/L:ArL/Y mutants. Scale bars represent 2 mm (C), 200 mm (D), and 75 mm (D, inset). Error bars represent mean ± SD.

  • Rapamycin was purchased from Selleck.Data from Journal of Lipid Research 2011.September;52:1617-25.

    Rapamycin (RPM) inhibits OA-induced lipogenesis. Male SD rats were divided into three groups, and then treated as follows for seven days: group I (control; Ctrl), normal diet + vehicle; group II (OA), 1% OA diet + vehicle; group III (OA + RPM), 1% OA diet + RPM. (A) Hepatic TG concentrations were determined using the serum triglyceride determination kit. (B) Fixed liver sections were subjected to HE and Oil Red O staining as well as immunohistochemistry assays with SREBP-1 antibody. Representative microphotographs of liver specimens from all groups of rats are shown. (C) The levels of mRNA of the indicated genes involved in lipogenesis were determined by real-time PCR. Each bar represents the mean ± SE of the results obtained from six rats. * P < 0.05, ** P < 0.01, *** P < 0.001.

Novel phosphoinositide 3-kinase/mTOR dual inhibitor, NVP-BGT226, displays potent growth-inhibitory activity against human head and neck cancer cells in vitro and in vivo.  ------Kwang-Yu Chang,Shan-Yin Tsai,et al.Clin Cancer Res. 2011 Nov.17:7116-26.

 

Role of the AMPK/SREBP-1 pathway in the development of orotic acid-induced fatty liver.  ------Eun-Jeong Jung,Sung-Won Kwon,et al.J Lipid Res.2011 Sep;52:1617-25.

 

Cell autonomous role of PTEN in regulating castration-resistant prostate cancer growth.  ------ David J.Mulholland,Linh M.Tran,et al.Cancer Cell. 2011 Jun.19:792-804.

 

Sorafenib induces apoptotic cell death in human non-small cell lung cancer cells by down-regulating mammalian target of rapamycin (mTOR)-dependent survivin expression.  ------Young-Sun Kim,Hyeon-Ok Jin,et al.Biochem Pharmacol. 2011 Aug.82:216-26.


Biological Activity of Rapamycin (Sirolimus):

RAPA administration in two types of fully allogeneic BM transplantation (BMT) systems in which host T cells mediate the rejection of TCD BM grafts (DBAf1 transplanted into C57BLf6 and BALBfc transplanted into C57BLf6). In both instances, RAPA administration prevented the rejection of the donor graft, accelerated post-BMT hematopoietic recovery, and did not compromise recipient survival. [2]
In vitro, rapamycin inhibited the proliferation of primary bone marrow cells induced by IL-3, GM-CSF, KL, or a complex mixture of factors present in cell-conditioned media. Rapamycin also inhibited the multiplication of colony-forming cells in suspension cultures containing IL-3 plus interleukin-1 (IL-1) or interleukin-11 (IL-11) plus KL. [3]



Quality Control:

MSDS
Batch S103903: H-NMR  HPLC  COA
Batch S103904: H-NMR  HPLC  COA
Batch S103905: H-NMR  HPLC  COA


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Customer's Feedback
Arnaud AUTRET, Trinity College
"I would like to confirm you that everything is perfectly fine with ABT and Obatoclax we got from your company. We confirmed their activity in vitro. We notably observed their impact in an apoptotic model and results are similar to those which have been published."

Dongfeng Chen, The Rausing Lab
"Your product U0126(Cat.NO S1102) works well in our experiments. I hope I can get more excellent products from your company in future."

Dr. Alexandra Segref, CECAD Cologne,Germay
"I am very satisfied with your product and costumer service. Bortezomib works very well in our assay, it is comparably cheaper than other inhibitors that we tested is more reliable for our assays. We see a great effect by using 10nM concentration."

R.B. Cambridge
"I have used the chemical that I bought from you(Selleck,PTC-124) and it worked well.So we will eventually be ordering more."

Zhenghe John Wang Assistant Professor, Case Western Reserve University
"We have purchased LBH-589, Saha and MS-275 from you and they all worked well."

Jenny Sun
"We used the LBH-589 in our experiments. The compound is easy to use with excellent reproducibility."

Yu Wang, Harvard University
"The GDC0449 compound worked very well. The results in my hands are equally good as what's been published. Thanks for this great resource for our research."

Philip Seeman, Toronto University
"Your LY404039 compound was well synthesized, its complicated stereochemical structure confirmed by NMR spectroscopy, and was biologically excellent in acting on brain dopamine receptors."

Dung-Fang Lee
"Based on our preliminary data, I found MLN8237 and VX-680 have good effects in inhibiting Aurka-maintaining ESC self-renewal in mouse ES cells."

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