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Products are for research use only. Not for human use. We do not sell to patients.

Signaling Pathway

Everolimus

HY-10218

(RAD001; SDZ-RAD; Certican; Zortress; Afinitor; RAD 001)

Everolimus
Everolimus Chemical Structure

Everolimus (RAD001) is a mTOR inhibitor of FKBP12 with IC50 of 1.6-2.4 nM.

Price and Availability of Everolimus
Size Price Stock
5 mg $36 In-stock
10 mg $64 In-stock
25 mg $116 In-stock
50 mg $197 In-stock
100 mg $304 In-stock
250 mg $661 In-stock
500 mg $930 In-stock
>1000 mg Get quote
We offer a substantial discount on larger orders.Inquiry for price and availability only. Please place your order via our email or fax.
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Everolimus Data Sheet

View current batch:

Purity: 98.02%

Cell Cycle/DNA Damage

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Biological Activity of Everolimus

Everolimus (RAD001) also known as SDZ-RAD, Certican, Zortress, Afinitorm is MTOR inhibitor with IC50 of 0.63 nM.

Clinical Information

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References on Everolimus

1 . Thompson LA, Kim M, Wenger SD, O'Bryant CL.Everolimus: a new treatment option for advanced pancreatic neuroendocrine tumors.Ann Pharmacother. 2012 Sep;46(9):1212-9. Epub 2012 Sep 4.
Abstract
OBJECTIVE: To present the current clinical evidence on everolimus for use in pancreatic neuroendocrine tumors (pNET). DATA SOURCES: A literature search was performed using PubMed and MEDLINE (1946-March 2012). Search terms were everolimus, RAD001, mTOR inhibitor, and pancreatic neuroendocrine tumors. Abstracts from the American Society of Clinical Oncology 2000-2012 meetings and Food and Drug Administration (FDA) reviews were searched to obtain otherwise unpublished data. The national clinical trials registry was searched for current and future studies of everolimus in pNET. STUDY SELECTION AND DATA EXTRACTION: Clinical studies available in the English language describing the pharmacology, pharmacokinetics, clinical activity, and safety of everolimus in pNET were included. All peer-reviewed, clinically relevant publications were reviewed for inclusion...

2 . Papadimitrakopoulou VA, Soria JC, Jappe A, Jehl V, Klimovsky J, Johnson BE.Everolimus and erlotinib as second- or third-line therapy in patients with advanced non-small-cell lung cancer.J Thorac Oncol. 2012 Oct;7(10):1594-601.
Abstract
INTRODUCTION: : The epidermal growth factor receptor inhibitor erlotinib is an approved treatment for chemotherapy-refractory advanced non-small-cell lung cancer (NSCLC). Because activated epidermal growth factor receptor signals through the phosphatidylinositol 3-kinase/Akt/mammalian target of rapamycin (mTOR) pathway, adding the oral mTOR inhibitor everolimus to erlotinib may improve efficacy by blocking multiple components of the same pathway. We conducted a phase I study to determine feasible dosages of combination therapy with erlotinib and everolimus for previously treated metastatic or unresectable NSCLC. METHODS: : Participants had advanced NSCLC progressing after two or less previous chemotherapy regimens. Feasibility of daily/weekly everolimus plus daily erlotinib was determined using a 6 + 6 dose-escalation design based on the rate of dose-limiting toxicities. Antitumor activity was assessed by the Response Evaluation Criteria In Solid Tumors study...

3 . Manzia TM, Sforza D, Angelico R, Bellini MI, Ciano P, Manuelli M, Toti L, Tisone G.Everolimus and enteric-coated mycophenolate sodium ab initio after liver transplantation: midterm results.Transplant Proc. 2012 Sep;44(7):1942-5.
Abstract
BACKGROUND AND AIM: Everolimus (EVR) use in liver transplantation (OLT) has been prescribed with calcineurin inhibitors (CNIs), steroids, and monoclonal antibodies. The aim of our study was to evaluate the safety, feasibility, and impact on renal function of EVR ab initio, in combination with enteric-coated mycophenolate sodium (EC-MPS) without the use of induction treatment, steroids, or CNIs. PATIENTS AND METHODS: We retrospective analyzed nine consecutive patients who underwent OLT at our institution. The initial dose of EVR (1.5 mg/d) was adjusted to achieve trough levels of 8 to 12 ng/mL. EC-MPS introduced at 1080 mg/d was maintained at the same dose over time...

4 . Schuler W; Sedrani R; Cottens S; Haberlin B; Schulz M; Schuurman H J; Zenke G; Zerwes H G; Schreier M H SDZ RAD, a new rapamycin derivative: pharmacological properties in vitro and in vivo. Transplantation (1997), 64(1), 36-42.
Abstract
BACKGROUND: This report describes the preclinical pharmacological profile of the new rapamycin analog, SDZ RAD, i.e., 40-O-(2-hydroxyethyl)-rapamycin.METHODS: The pharmacological effects of SDZ RAD were assessed in a variety of in vitro and in vivo models, which included an autoimmune disease model as well as kidney and heart allotransplantation models using different rat strain combinations.RESULTS: SDZ RAD has a mode of action that is different from that of cyclosporine or FK506. In contrast to the latter, SDZ RAD inhibits growth factor-driven cell proliferation in general, as demonstrated for the in vitro cell proliferation of a lymphoid cell line and of vascular smooth muscle cells. SDZ ...

5 . Yokomasu, Akira; Yano, Ikuko; Sato, Eriko; Masuda, Satohiro; Katsura, Toshiya; Inui, Ken-ichi. Effect of itraconazole on the pharmacokinetics of everolimus administered by different routes in rats. Biopharmaceutics & Drug Disposition (2009), 30(9), 517-523.
Abstract
The effect of itraconazole on the pharmacokinetics of everolimus was investigated in rats. Ten minutes after an intravenous or intraintestinal administration of itraconazole, everolimus was delivered intravenously (0.2 mg/kg) or intraintestinally (0.5 mg/kg). Blood concentrations of everolimus were measured up to 240 min, and pharmacokinetic parameters were calculated. Intraintestinally administered itraconazole (20 mg/kg) significantly increased the area under the concentration–time curve (AUC) of intraintestinally administered everolimus about 4.5-fold, but even at 50 mg/kg did not affect the AUC of intravenously administered everolimus. However, intravenously administered itraconazole (50...

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