Rapamycin An immunosuppressant macrolide antibiotic and an inhibitor of FRAP

Rapamycin (CAS 53123-88-9)

Rapamycin | CAS 53123-88-9 is rated 5.0 out of 5 by 4.
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Synonym: 23,27-Epoxy-3H-pyrido[2,1-c][1,4]oxaazacyclohentriacontine;AY 22989;Sirolimus
Application: An immunosuppressant macrolide antibiotic and an inhibitor of FRAP
CAS Number: 53123-88-9
Purity: ≥98%
Molecular Weight: 914.17
Molecular Formula: C51H79NO13
* Refer to Certificate of Analysis for lot specific data (including water content).
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Rapamycin is a member of the macrolide immunosuppressant family and a FRAP inhibitor. Rapamycin exhibits binding and inhibitory actions to the FK506 binding protein (FKBP5) proline rotamase via simultaneous binding by FKBP12 and FRAP. FRAP (RAFT1) proteins exhibit homology to PI 4- and PI 3-kinases, which have PI 4-kinase and autophosphorylating activities.The rapamycin/FKBP complex does not inhibit the FRAP PI 4-kinase activity, but does inhibit FRAP autophosphorylation. Rapamycin is unique in its ability to inhibit lymphokine induced cell proliferation at the G1 and S phase as well as an irreversible cellular arrest at the G1 phase in S. cerevisiae cells. It also exhibits selective signal blocking leading to the activation of p70/85 S6 kinase, which is potentially due to the inhibition of FRAP autophosphorylation or protein kinase activity. Angiogenesis inhibition is also exhibited, possibly through the inhibition of the Akt pathway. Rapamycin is an inhibitor of mTOR.


References

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Usage :
Store, as supplied, at -20°C for up to 1 year. Store solutions at -20°C for up to 3 months.
Physical State :
Solid
Solubility :
Soluble in DMSO (25 mg/ml), ethanol (up to 50 mg/ml), chloroform (5 mg/ml), methanol (25 mg/ml), ether, and acetone. Insoluble in water.
Storage :
Store at -20° C
Melting Point :
183-185° C
Boiling Point :
~973.0° C at 760 mmHg (Predicted)
Density :
~1.2 g/cm3 (Predicted)
Refractive Index :
n20D 1.55 (Predicted)
Optical Activity :
α20/D -58.2°
IC50 :
human peripheral blood mononuclear cell proliferation: IC50 = 1 nM; interleukin-2 activation of lymphocytes: IC50 = 5 pM; FK506 binding protein 12: IC50 = 0.1 nM (Homo sapiens); Mus musculus: IC50 = 1 nM (Mus musculus)
Ki Data :
FK506 binding protein 3: Ki= 0.5 nM (Homo sapiens)
pK Values :
pKa: 10.40
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
2
RTECS :
VE6250000
PubChem CID :
5040
Merck Index :
14: 8114
MDL Number :
MFCD00867594
SMILES :
CC1CCC2CC(C(=CC=CC=CC(CC(C(=O)C(C(C(=CC(C(=O)CC(OC(=O)C3CCCCN3C(=O)C(=O)C1(O2)O)C(C)CC4CCC(C(C4)OC)O)C)C)O)OC)C)C)C)OC

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Rapamycin  Product Citations

See how others have used Rapamycin. Click on the entry to view the PubMed entry .

Citations 1 to 10 of 93 total

PMID: # 29524020  Very, N. et al. 2018. Journal of bioenergetics and biomembranes. 50: 213-222.

PMID: # 27545498  Guixé-Muntet, S. et al. 2017. J. Hepatol. 66: 86-94.

PMID: # 28743128  De Cillà, S. et al. 2017. Cellular physiology and biochemistry : international journal of experimental cellular physiology, biochemistry, and pharmacology. 42: 1725-1738.

PMID: # 29020060  Royal, AA. et al. 2017. PLoS ONE. 12: e0186293.

PMID: # 28379541  Aslani, F. et al. 2017. Mol. Hum. Reprod. 23: 370-380.

PMID: # 29040365  Liu, Y. et al. 2017. Acta Biochim. Biophys. Sin. (Shanghai). 1-8.

PMID: # 28486929  Gan, W. et al. 2017. BMC Cell Biol. 18: 22.

PMID: # 27551491  Xia, XJ. et al. 2016. Cell Death Discov. 2: 15065.

PMID: # 27634755  Allain, C. et al. 2016. Cancer Res. 76: 6374-6381.

PMID: # 26935264  Kou, B. et al. 2016. Oncol. Rep. 35: 2880-6.

Citations 1 to 10 of 93 total

溶解药品时要把药品拿出来溶解还是直接在棕色瓶子里溶解,如果在棕色瓶子里溶解的话之后取样瓶子应该会有很多残留吧。药品需要避光保存么?

Asked by: 小静静123
感谢您的提问。这支瓶子是一个4ml的琥珀色玻璃瓶,sc-3504是建议避光保存的。溶解的时候您可以先加入一定体积的溶解液,充分溶解后倒出溶液,再加入溶解液洗瓶,收集洗涤sc-3504瓶子的溶液,并补充至最终的稀释液体积,获得您需要的浓度。更多问题,欢迎通过:电话(+86) 021-60936350、邮箱asia@scbio.cn、或选择网页上Live Chat中的“中文支持”,联系我们的技术支持部门。 Thank you for your inquiry. We do recommend protecting from light. It is packaged in 4 ml amber glass vial. For more detailed information about this question, please contact our Asian Technical Service team at (+86) 021-60936350 or asia@scbio.cn or by live chat on our website.
Answered by: Technical Support 15
Date published: 2017-12-07

一毫克用多少DMSO 溶解不伤害细胞呢?

Asked by: 小静静123
不同的细胞,DMSO溶解指数可能不一样, 具体需要参照相关文献, 或者通过实验摸索到最佳的用量。
Answered by: Technical Support 2
Date published: 2017-12-04

是固体么?怎么加到培养液里?

Asked by: xujie
感谢您的提问。sc-3504是固体的,官网上有溶解度信息,您可以根据您的需要进行溶解,Soluble in DMSO (25 mg/ml), ethanol (up to 50 mg/ml), chloroform (5 mg/ml), methanol (25 mg/ml), ether, and acetone. Insoluble in water. 更多问题,欢迎通过:电话(+86) 021-60936350、邮箱asia@scbio.cn、或选择网页上Live Chat中的“中文支持”,联系我们的技术支持部门。 Thank you for your inquiry. sc-3504 is solid, and here is the solubility information, hope it helps. Soluble in DMSO (25 mg/ml), ethanol (up to 50 mg/ml), chloroform (5 mg/ml), methanol (25 mg/ml), ether, and acetone. Insoluble in water. For more detailed information about this question, please contact our Asian Technical Service team at (+86) 021-60936350 or asia@scbio.cn or by live chat on our website.
Answered by: Technical Support 15
Date published: 2017-11-30

What temperature should aliquotes of Rapamycin be stored?

Asked by: Io5ay
Thank you for your question. We recommend preparing a solution just prior to use. Upon resuspension, Rapamycin should be aliquoted and stored at -20°C. Avoid repeated freeze-thaw cycles. Resuspended product should be stable for 3 months at -20°C when properly stored. Please keep in mind some additives may effect stability.
Answered by: Technical Support
Date published: 2017-03-10

Which isomers are present?

Asked by: Io5ay
Thank you for your question. We do not test for, or characterize the isomer(s) when the Rapamycin chemical is in solid form. However it is expected that it should predominantly contain the trans isomer. Once in solution, the cis and trans isomers are in dynamic equilibrium. The exact ratio of trans and cis varies depending on many factors including solvent, pH and trace metal ions.
Answered by: Technical Support
Date published: 2017-03-10

How long is this item okay to be at ambient temperature?

Asked by: Io5ay
Thank you for your question. Rapamycin can be stored at room temperature for short-term storage conditions. However, we recommend long term storage at -20ºC.
Answered by: Technical Support
Date published: 2017-03-09
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Rated 5 out of 5 by from Rapamycin indirectly impacts O-GlcNAcylation Treatments of normal and colon cancer cells with mTOR regulators including rapamycin modulate O-GlcNAc transferase and O-GlcNAcylation levels. However, deregulation of O-GlcNAcylation affects mTOR signaling activation only in cancer cells. Thus, a crosstalk occurs between O-GlcNAcylation and mTOR signaling.
Date published: 2019-03-26
Rated 5 out of 5 by from Provided all essential information along Provided all essential information along with nominal price
Date published: 2016-01-28
Rated 5 out of 5 by from Cells were pre Cells were pre-treated with rapamycin (sc-3504) for 30 minutes prior to TPO stimulation, then screened for proliferation by BrdU staining and FCM (16123382). -SCBT Publication Review
Date published: 2015-07-02
Rated 5 out of 5 by from Kanayama Kanayama, et. al. (PubMed ID 25609235) used rapamycin (sc-3504) to induce autophagy in the macrophages studied. -SCBT Publication Review
Date published: 2015-07-02
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