Everolimus
| Code | Size | Price |
|---|
| CDX-E0074-M100 | 100 mg | £487.00 |
Quantity:
| CDX-E0074-M250 | 250 mg | £926.00 |
Quantity:
Prices exclude any Taxes / VAT
Overview
Regulatory Status: RUO
Shipping:
Ambient
Storage:
+4°C
Documents
Further Information
Alternate Names/Synonyms:
42-O-(2-Hydroxyethyl)rapamycin; NVP-RAD001; RAD001; SDZRAD; Zortress; Afinitor; Certican; Votubia
Appearance:
White to off-white solid.
CAS:
159351-69-6
EClass:
32160000
Form (Short):
liquid
GHS Symbol:
GHS08
Handling Advice:
Protect from light and moisture.
Hazards:
H372, H412
InChi:
InChI=1S/C53H83NO14/c1-32-16-12-11-13-17-33(2)44(63-8)30-40-21-19-38(7)53(62,68-40)50(59)51(60)54-23-15-14-18-41(54)52(61)67-45(35(4)28-39-20-22-43(66-25-24-55)46(29-39)64-9)31-42(56)34(3)27-37(6)48(58)49(65-10)47(57)36(5)26-32/h11-13,16-17,27,32,34-36,38-41,43-46,48-49,55,58,62H,14-15,18-26,28-31H2,1-10H3/b13-11+,16-12+,33-17+,37-27+/t32-,34-,35-,36-,38-,39+,40+,41+,43-,44+,45+,46-,48-,49+,53-/m1/s1
InChiKey:
HKVAMNSJSFKALM-GKUWKFKPSA-N
Long Description:
Chemical. CAS: 159351-69-6. Formula: C53H83NO14. MW: 958.2. Isolated from Streptomyces hygroscopicus. 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.
MDL:
MFCD07785165
Molecular Formula:
C53H83NO14
Molecular Weight:
958.2
Package Type:
Vial
Precautions:
P273, P314
Product 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.
Purity:
>99% (HPLC)
Signal word:
Danger
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
Solubility Chemicals:
Soluble in DMSO (50mg/ml), ethanol (50mg/ml), methanol or DMF. Insoluble in water.
Source / Host:
Isolated from Streptomyces hygroscopicus.
Transportation:
Non-hazardous
UNSPSC Category:
Natural Products/Extracts
UNSPSC Number:
12352200
Use & Stability:
Stable for at least 2 years after receipt when stored at -20°C.
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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