Home>>Signaling Pathways>> Ubiquitination/ Proteasome>> Autophagy>>Everolimus (RAD001)

Everolimus (RAD001) (Synonyms: RAD001)

Catalog No.GC13601

A rapamycin derivative

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

Everolimus (RAD001) Chemical Structure

Cas No.: 159351-69-6

Size Price Stock Qty
10mM (in 1mL DMSO)
$48.00
In stock
10mg
$54.00
In stock
25mg
$94.00
In stock
100mg
$274.00
In stock

Tel:(909) 407-4943 Email: sales@glpbio.com

Customer Reviews

Based on customer reviews.

  • GlpBio Citations

    GlpBio Citations
  • Bioactive Compounds Premium Provider

    Bioactive Compounds Premium Provider

Sample solution is provided at 25 µL, 10mM.

Product has been cited by 1 publications

Product Documents

Quality Control & SDS

View current batch:

Protocol

Cell experiment [1]:

Cell lines

MTC cell

Preparation Method

The effects of everolimus and IGF-I on MTC cell viability in vitro were assessed by ATPlite assay on the Wallac Victor™ 1420 Multilabel Counter. Cells were treated after 24 h with or without 10 nM–1 μM everolimus and/or 50 nM IGF-I. Treatments were renewed after the first 24 h of incubation. Cell viability was assessed after 48 h. Results were obtained by determining the mean value of six replicates.

Reaction Conditions

10 nM–1 μM, 24h

Applications

Everolimus dose-dependently reduced cell viability, from –19% at 10 nM to –31% vs. control at 1 μM. In the E-NR MTCs, everolimus did not significantly modify cell viability.

Animal experiment [2]:

Animal models

5‐week‐old NOD/SCID mice

Preparation Method

Everolimus or AZD8055 was dissolved in 30% (w/v) Captisol and given orally to mice at a dose of 5 mg/kg (everolimus) or 20 mg/kg (AZD8055) per day on weekdays from day 2 to day 20. The control mice received the vehicle only.

Dosage form

5 mg/kg, p.o.

Applications

AZD8055 more significantly inhibited the in vivo growth of the ATL‐cell xenografts than did everolimus.

References:

[1]. Gentilin E, et al. Igf-I influences everolimus activity in medullary thyroid carcinoma. Front Endocrinol (Lausanne). 2015 May 5;6:63.

[2].Kawata T, et al, Takaori-Kondo A. Dual inhibition of the mTORC1 and mTORC2 signaling pathways is a promising therapeutic target for adult T-cell leukemia. Cancer Sci. 2018 Jan;109(1):103-111.

Background

Everolimus (RAD001) is an orally active derivative of rapamycin that inhibits the Ser/Thr kinase, mTOR (mammalian target of rapamycin).[1]

In vitro activity of everolimus it displayed that the dose-dependent inhibition of cell growth by everolimus using methylene blue staining after 96 hours of incubation in four different human tumor cell lines, which can be regarded as sensitive (HCT-15, A549) and insensitive (KB-31 and HCT-116).[1] In vitro efficacy test, antiproliferative concentrations of RAD001 resulted in total dephosphorylation of S6K1 and the substrate S6 and a shift in the mobility of 4E-BP1, with IC50 of 0.7 nmol/L and 1,778 nmol/L in both the sensitive murine B16/BL6 melanoma and the insensitive human cervical KB-31,respectively.[2] In vitro study, combination gemcitabine (100 nM) with everolimus (0.05-2 μM) had significantly antiproliferative effect with an arrest of cell cycle at S phase.[3]

In vivo experimental it shown that everolimus is very well tolerated with no obvious clinical signs of toxicity; even when treating for up to 60 mg/kg per day by oral gavage the maximum tolerated dosage was not reached. In vivo efficacy study, daily orally treatment with everolimus (0.5 or 2.5 mg/kg) dose-dependently inhibited growth, and using a higher dose of 5 mg/kg once or twice per week also showed similar antitumor efficacy in the rat CA20498 model.[1] In vivo, treatment with 0.1-10 mg/kg/d RAD001 dose-dependently increased the hemoglobin content but reduced the Tie-2 content and this was significant for VEGF stimulation but not bFGF stimulation.[2]

References:
[1].O'Reilly T, McSheehy PM. Biomarker Development for the Clinical Activity of the mTOR Inhibitor Everolimus (RAD001): Processes, Limitations, and Further Proposals. Transl Oncol. 2010 Apr;3(2):65-79.
[2].Lane HA, et al. mTOR inhibitor RAD001 (everolimus) has antiangiogenic/vascular properties distinct from a VEGFR tyrosine kinase inhibitor. Clin Cancer Res. 2009 Mar 1;15(5):1612-22.
[3].Pinto-Leite R, et al. Everolimus enhances gemcitabine-induced cytotoxicity in bladder-cancer cell lines. J Toxicol Environ Health A. 2012;75(13-15):788-99.

Chemical Properties

Cas No. 159351-69-6 SDF
Synonyms RAD001
Canonical SMILES OCCO[C@H]1[C@H](OC)C[C@H](C[C@H](C)[C@H](CC([C@H](C)/C=C(C)/[C@@H](O)[C@H]2OC)=O)OC([C@@H]3CCCCN3C(C([C@@]4(O)[C@H](C)CC[C@@H](C[C@H](OC)/C(C)=C/C=C/C=C/[C@@H](C)C[C@@H](C)C2=O)O4)=O)=O)=O)CC1
Formula C53H83NO14 M.Wt 958.22
Solubility ≥ 47.911mg/mL in DMSO, ≥ 122 mg/mL in EtOH Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 1.0436 mL 5.218 mL 10.436 mL
5 mM 0.2087 mL 1.0436 mL 2.0872 mL
10 mM 0.1044 mL 0.5218 mL 1.0436 mL
  • Molarity Calculator

  • Dilution Calculator

Mass
=
Concentration
x
Volume
x
MW*
 
 
 
**When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / CoA (available online).

Calculate

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

Reviews

Review for Everolimus (RAD001)

Average Rating: 5 ★★★★★ (Based on Reviews and 30 reference(s) in Google Scholar.)

5 Star
100%
4 Star
0%
3 Star
0%
2 Star
0%
1 Star
0%
Review for Everolimus (RAD001)

GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.

Required fields are marked with *

You may receive emails regarding this submission. Any emails will include the ability to opt-out of future communications.