Chemodex

Everolimus

CHF 530.00
In stock
CDX-E0074-M100100 mgCHF 530.00
CDX-E0074-M250250 mgCHF 1'017.00
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Product Details
Synonyms 42-O-(2-Hydroxyethyl)rapamycin; NVP-RAD001; RAD001; SDZRAD; Zortress; Afinitor; Certican; Votubia
Product Type Chemical
Properties
Formula

C53H83NO14

MW 958.2
Merck Index 14: 3907
CAS 159351-69-6
RTECS VE6255000
Source/Host Chemicals Isolated from Streptomyces hygroscopicus.
Purity Chemicals ≥99% (HPLC)
Appearance White to off-white solid.
Solubility Soluble in DMSO (50mg/ml), ethanol (50mg/ml), methanol or DMF. Insoluble in water.
Identity Determined by IR.
Other Product Data

Click here for Original Manufacturer Product Datasheet
Our product description may differ slightly from the original manufacturers product datasheet.

InChi Key HKVAMNSJSFKALM-GKUWKFKPSA-N
Smiles OCCO[C@@H]1CC[C@@H](C[C@H]([C@@H]2CC([C@@H](/C=C([C@H]([C@H](C([C@@H](C[C@@H](/C=C/C=C/C=C([C@H](C[C@@H]3CC[C@H]([C@@](O3)(C(C(N4CCCC[C@H]4C(O2)=O)=O)=O)O)C)OC)\C)C)C)=O)OC)O)\C)C)=O)C)C[C@H]1OC
Shipping and Handling
Shipping AMBIENT
Short Term Storage +4°C
Long Term Storage -20°C
Handling Advice Protect from light and moisture.
Use/Stability Stable for at least 2 years after receipt when stored at -20°C.
Documents
MSDS Inquire
Product Specification Sheet
Datasheet Download PDF
Description

Macrolide antibiotic, inhibiting bacterial protein synthesis. Potent immunosuppressant. Binds with high affinity to the FK506 binding protein-12 (FKBP-12) to generate an immunosuppressive complex that inhibits the activation of the mammalian target of rapamycin (mTOR). More selective for the mTORC1 protein complex, with little impact on the mTORC2 complex, compared to Rapamycin. Anticancer agent. Inhibition of mTOR reduces the activity of effectors downstream, which leads to a blockage in the progression of cells from G1 into S phase, and subsequently inducing cell growth arrest, apoptosis and autophagy, resulting in reduction of cell proliferation, angiogenesis and glucose uptake. Inhibits tumor proliferation in vitro and in vivo.

Product References

(1) H.J. Schuurman, et al.; Transplantation 64, 32 (1997) | (2) W. Schuler, et al.; Transplantation 64, 36 (1997) | (3) P. Neuhaus, et al.; Liver Transpl. 7, 473 (2001) (Review) | (4) B. Nashan; Expert Opin. Investig. Drugs. 11, 1845 (2002) (Review) | (5) I. Beuvink, et al.; Cell 120, 747 (2005) | (6) J.K. Patel & J.A. Kobashigawa; Expert Opin. Pharmacother. 7, 1347 (2006) (Review) | (7) P. Smolewski; Anticancer Drugs 17, 487 (2006) (Review) | (8) K. Zitzmann, et al.; Neuroendocrinology 85, 54 (2007) | (9) Z. Zeng, et al.; Blood 109, 3509 (2007) | (10) R. Bianco, et al.; Br. J. Cancer 98, 923 (2008) | (11) A.I. Sanchez-Fructuoso; Expert Opin. Drug Metab. Toxicol. 4, 807 (2008) (Review) | (12) H.A. Lane, et al.; Clin. Cancer Res. 15, 1612 (2009) | (13) D. Lebwohl, et al.; Ann. N. Y. Acad. Sci. 1291, 14 (2013) (Review) | (14) U. Saran, et al.; Clin. Sci. 129, 895 (2015) (Review) | (15) Morviducci, et al.; Diabetes Res. Clin. Pract. (Epub ahead of print) (2018) (Review)

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