Everolimus An immunosuppresive inhibitor of FRAP (mTOR)

Everolimus (CAS 159351-69-6)

Everolimus | CAS 159351-69-6 is rated 5.0 out of 5 by 1.
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Synonym: 40-O-(2-Hydroxyethyl)rapamycin; 42-O-(2-Hydroxy)ethyl Rapamycin; Afinitor
Application: An immunosuppresive inhibitor of FRAP (mTOR)
CAS Number: 159351-69-6
Purity: ≥98%
Molecular Weight: 958.22
Molecular Formula: C53H83NO14
* Refer to Certificate of Analysis for lot specific data (including water content).
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Everolimus is a macrolide derived from rapamycin (sc-3504) with immunosuppressant properties shown to inhibit cell proliferation induced by growth factors. Macrolides belong to a group of antibiotics that bind to the 50S ribosomal subunit and inhibit protein synthesis. Studies indicate that everolimus is a mTOR (FRAP) inhibitor that displays high affinity toward the intracellular receptor FKBP12. Additionally, the Everolimus-FKBP12 complex decreases the activity of the S6K1 and 4EBP by binding to FRAP.


References

1. Weisblum, B. 1984. Br. Med. Bull. 40: 47-53. PMID: 6442874
2. Dumont, F.J. 2001. Curr Opin Investig Drugs. 2: 1220-1234. PMID: 11717808
3. Nashan, B. 2002. Ther Drug Monit. 24: 53-58. PMID: 11805723
4. Anandappa, G., et al. 2010. Cancer Manag Res. 2: 61-70. PMID: 21188097
5. Patsenker, E., et al. 2010. J Hepatol. [Epub ahead of print]. PMID: 21168455

Physical State :
Solid
Solubility :
Soluble in chloroform, methanol, DMSO (100 mg/ml), water (<1 mg/ml at 25° C), and ethanol (100 mg/ml).
Storage :
Store at -20° C
Melting Point :
110-115° C
Boiling Point :
998.75° C at 760 mmHg (Predicted)
Density :
1.18 g/cm3 (Predicted)
Refractive Index :
n20D 1.55 (Predicted)
IC50 :
Antiangiogenic effects in VEGF-induced HUVEC50 proliferation : IC50 = 0.12 nM; MTOR: IC50 = 0.63 nM; Vascular effects in bFGF-induced HUVEC50 proliferation : IC50 = 0.8 nM
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
2
RTECS :
VE6255000
PubChem CID :
6442177
Merck Index :
14: 3907
MDL Number :
MFCD07785165
SMILES :
C[C@@H]1CC[C@H]2C[C@@H](/C(=C/C=C/C=C/[C@H](C[C@H](C(=O)[C@@H]([C@@H](/C(=C/[C@H](C(=O)C[C@H](OC(=O)[C@@H]3CCCCN3C(=O)C(=O)[C@@]1(O2)O)[C@H](C)C[C@@H]4CC[C@H]([C@@H](C4)OC)OCCO)C)/C)O)OC)C)C)/C)OC

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Certificate of Analysis

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Everolimus  Product Citations

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

Citations 1 to 1 of 1 total

PMID: # 27991928  Mateo, F. et al. 2016. Oncogene.

Citations 1 to 1 of 1 total

What is the appearance of the compound?

Asked by: two2igm05
Thank you for your question. Everolimus, sc-218452, is in white to off-white powder form.
Answered by: Chemical Support 4
Date published: 2017-04-28
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Rated 5 out of 5 by from Patsenker Patsenker, E. et al. (PubMed 21168455) wanted to test the potential of Everolimus, a macrolide derived from Rapamycin, in halting experimental liver fibrosis progression in rats. Everolimus decreased fibrosis up to 70%, improved portal pressure, reduced ascites, and showed potent down-regulation of pro-fibrogenic genes, paralleled by a strong increase in matrix degradation (collagenase) activity. -SCBT Publication Review
Date published: 2015-04-28
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