Everolimus
Based on 119 publication(s) in Google Scholar
Everolimus (RAD001) is a Rapamycin (HY-10219) derivative and a potent, selective, orally active, blood-brain barrier-permeable mTOR1 inhibitor. Everolimus binds to FKBP-12 to generate an immunosuppressive complex. Everolimus inhibits tumor cells proliferation and induces cell apoptosis and autophagy. Everolimus has potent immunosuppressive and anticancer activities.
For research use only. We do not sell to patients.
- Purity: 99.85%
- CAS No.: 159351-69-6
- Formula: C53H83NO14
- Molecular Weight:958.22
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months
Publications Citing Use of MedChemExpress (MCE) Everolimus
More- Signal Transduct Target Ther. 2025 Dec 15;10(1):406. [Abstract]
- Signal Transduct Target Ther. 2021 May 28;6(1):188. [Abstract]
- Nat Med. 2016 Jul;22(7):723-6. [Abstract]
- Nature. 2016 Dec 1;540(7631):119-123. [Abstract]
- Cancer Cell. 2024 Jul 8;42(7):1286-1300.e8. [Abstract]
- Nat Cancer. 2023 Oct;4(10):1508-1525. [Abstract]
- Mil Med Res. 2023 Dec 20;10(1):68. [Abstract]
- Nat Commun. 2025 Dec 15. [Abstract]
- Acta Pharm Sin B. 2020 Jun;10(6):1004-1019. [Abstract]
- Sci Transl Med. 2013 Jul 31;5(196):196ra99. [Abstract]
- Adv Sci (Weinh). 2025 Nov 14:e17330. [Abstract]
- Adv Sci (Weinh). 2024 Aug 23:e2400156. [Abstract]
- Adv Sci (Weinh). 2024 Aug 9:e2404693. [Abstract]
- J Clin Invest. 2017 Sep 1;127(9):3339-3352. [Abstract]
- Exp Hematol Oncol. 2016 Jul 29:5:22. [Abstract]
- J Adv Res. 2025 Oct 16:S2090-1232(25)00818-5. [Abstract]
- Sci Adv. 2023 Jul 21;9(29):eadd9871. [Abstract]
- Mol Ther. 2025 Jan 8;33(1):279-296. [Abstract]
- Cell Rep Med. 2025 Apr 2:102053. [Abstract]
- J Exp Med. 2023 Nov 6;220(11):e20211743. [Abstract]
- Mol Psychiatry. 2025 Jul;30(7):3077-3089. [Abstract]
- Cancer Lett. 2022 Feb 1:526:352-362. [Abstract]
- Cancer Lett. 2021 Jan 1;496:127-133. [Abstract]
- Cancer Lett. 2017 Nov 1:408:43-54. [Abstract]
- Adv Healthc Mater. 2025 Aug 11:e00602. [Abstract]
- Cell Death Dis. 2021 Oct 21;12(11):978. [Abstract]
- Circ Heart Fail. 2024 Apr;17(4):e011110. [Abstract]
- Hepatobiliary Surg Nutr. 2023 Dec 1;12(6):835-853. [Abstract]
- Cell Syst. 2020 Jan 22;10(1):66-81.e11. [Abstract]
- Cell Syst. 2018 Apr 25;6(4):424-443.e7. [Abstract]
- J Transl Med. 2023 Oct 26;21(1):754. [Abstract]
- Biomed Pharmacother. 2023 Oct:166:115397. [Abstract]
- Biomed Pharmacother. 2021 Jan;133:110906. [Abstract]
- PLoS Biol. 2019 May 21;17(5):e3000252. [Abstract]
- Sci Data. 2024 Sep 19;11(1):1024. [Abstract]
- Cell Rep. 2023 Jun 27;42(6):112519. [Abstract]
- Cell Rep. 2022 Aug 16;40(7):111194. [Abstract]
- Br J Cancer. 2023 Oct;129(8):1225-1237. [Abstract]
- Sci Signal. 2021 Jun 22;14(688):eabe6156. [Abstract]
- Epilepsia. 2020 Jun;61(6):1301-1311. [Abstract]
- Elife. 2017 Dec 14;6:e27293. [Abstract]
- Cell Biol Toxicol. 2026 Feb 13;42(1):42. [Abstract]
- Biochem Pharmacol. 2026 Mar 10:249:117889. [Abstract]
- Mol Cancer Ther. 2018 Dec;17(12):2689-2701. [Abstract]
- J Ethnopharmacol. 2026 Feb 28:357:120890. [Abstract]
- Cells. 2019 Jun 18;8(6). pii: E605. [Abstract]
- Drug Des Devel Ther. 2018 Apr 19:12:911-920. [Abstract]
- Nutrients. 2018 Dec 8;10(12). pii: E1950. [Abstract]
- Int J Mol Sci. 2025 Feb 6;26(3):1381. [Abstract]
- Int J Oncol. 2018 Aug;53(2):904-914. [Abstract]
- Cell Mol Neurobiol. 2019 Mar;39(2):241-254. [Abstract]
- Int J Cancer. 2024 Jul 15;155(2):324-338. [Abstract]
- Mol Cancer Res. 2019 Jan;17(1):42-53. [Abstract]
- Molecules. 2025 Jul 26;30(15):3139. [Abstract]
- Molecules. 2020 Apr 23;25(8):1980. [Abstract]
- Molecules. 2018 Mar 23;23(4). pii: E736. [Abstract]
- Molecules. 2017 Dec 12;22(12). pii: E2207. [Abstract]
- Cell Rep Methods. 2026 Jun 15;6(6):101339. [Abstract]
- Cancers (Basel). 2020 Nov 13;12(11):3366. [Abstract]
- ACS Omega. 2025 Oct 29;10(44):52562-52575. [Abstract]
- Cancer Sci. 2018 Jan;109(1):103-111. [Abstract]
- FASEB J. 2026 Apr 15;40(7):e71722. [Abstract]
- FASEB J. 2025 Sep 30;39(18):e71061. [Abstract]
- J Cell Mol Med. 2021 Nov;25(21):10088-10100. [Abstract]
- Transl Oncol. 2022 Jul; 21: 101444. [Abstract]
- Oncol Res. 2022 Jan 31;28(9):873-884. [Abstract]
- Gynecol Oncol. 2020 Dec;159(3):827-838. [Abstract]
- J Neurosci. 2026 Feb 3:e0958252026. [Abstract]
- Sci Rep. 2025 Jan 18;15(1):2415. [Abstract]
- Sci Rep. 2024 Mar 22;14(1):6873. [Abstract]
- Biomedicines. 2021 Dec 10;9(12):1873. [Abstract]
- J Biomed Mater Res A. 2021 Jun;109(6):1015-1026. [Abstract]
- J Pharmacol Exp Ther. 2025 Oct 8;392(11):103744. [Abstract]
- Microbiol Spectr. 2023 Jun 15;11(3):e0530222. [Abstract]
- Front Mol Neurosci. 2021 Nov 26:14:772847. [Abstract]
- Bioengineering (Basel). 2025 Oct 19;12(10):1121. [Abstract]
- Viruses. 2021 Jun 3;13(6):1061. [Abstract]
- Viruses. 2020 Jun 10;12(6):628. [Abstract]
- Exp Cell Res. 2020 Aug 1;393(1):112054. [Abstract]
- Breast Cancer (Dove Med Press). 2026 Mar 4:18:580570. [Abstract]
- Arch Med Res. 2023 Oct 6;54(7):102894. [Abstract]
- Diagnostics (Basel). 2023 Mar 24;13(7):1232. [Abstract]
- Int J Med Sci. 2025 Jan 27;22(4):940-954. [Abstract]
- Hum Cell. 2025 Jul 7;38(5):125. [Abstract]
- Hum Cell. 2024 Oct 22;38(1):4. [Abstract]
- Cancer Med. 2024 Jun;13(12):e7432. [Abstract]
- J Pharm Biomed Anal. 2021 Jul 15:201:114120. [Abstract]
- J Chromatogr B Analyt Technol Biomed Life Sci. 2024 Apr 15:1237:124100. [Abstract]
- Mol Biol Rep. 2022 Jan;49(1):451-461. [Abstract]
- Fish Shellfish Immunol Rep. 2021 Feb 14:2:100006. [Abstract]
- PLoS One. 2024 Nov 1;19(11):e0308647. [Abstract]
- PLoS One. 2016 Jan 28;11(1):e0147682. [Abstract]
- Acta Trop. 2023 Feb:238:106802. [Abstract]
- Acta Trop. 2020 Dec;212:105708. [Abstract]
- Prostate. 2019 Jan;79(1):44-53. [Abstract]
- J Viral Hepat. 2026 Jan;33(1):e70118. [Abstract]
- Biochem Biophys Res Commun. 2020 Nov 26;533(1):1-8. [Abstract]
- Drugs R D. 2026 May 24. [Abstract]
- In Vitro Cell Dev Biol Anim. 2021 May;57(5):510-518. [Abstract]
- Can J Physiol Pharmacol. 2020 Jul;98(7):449-458. [Abstract]
- Int J Clin Exp Pathol. 2017;10(3):3033-3042.
- bioRxiv. 2026 Jun 16.
- bioRxiv. 2026 Mar 18.
- bioRxiv. 2026 Mar 25.
- bioRxiv. 2026 Jan 9.
- bioRxiv. 2026 Jan 5:2026.01.05.697773. [Abstract]
- University of Toronto. 2025.
- bioRxiv. 2025 Nov 24.
- iMetaMed. 2025 Oct 21.
- Res Sq. 2024 Jun 25.
- Res Sq. 2024 Jun 13.
- Research Square Preprint. 2023 May 10.
- Patent. US20210299273A1.
- Preprints. 2021, 2021040399.
- bioRxiv. 2021 Mar 4.
- J Oncol. 2019 Jun 2:2019:8340926. [Abstract]
- University Würzburg. 2019 May.
- Am J Dig Dis (Madison). 2015;2(2):95-99.
- Oncotarget. 2015 Dec 8;6(39):42183-96. [Abstract]
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Biological Activity
|
mTOR 5-6 nM (IC50) |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| CAKI-1 | IC50 |
14 μM
Compound: Everolimus
|
Cytotoxicity against human Caki1 cells after 72 hrs by MTT assay
Cytotoxicity against human Caki1 cells after 72 hrs by MTT assay
|
[PMID: 24445311] |
| COLO 205 | IC50 |
20 μM
Compound: Everolimus
|
Cytotoxicity against human COLO205 cells after 72 hrs by MTT assay
Cytotoxicity against human COLO205 cells after 72 hrs by MTT assay
|
[PMID: 24445311] |
| Cortical neurone | IC50 |
150 pM
Compound: RAD001
|
Inhibition of oversizing of mouse primary cortical neuron harboring TSC1 deletion mutant at 20 nM incubated for 7 days by immunofluorescence assay
Inhibition of oversizing of mouse primary cortical neuron harboring TSC1 deletion mutant at 20 nM incubated for 7 days by immunofluorescence assay
|
[PMID: 31955578] |
| DU-145 | IC50 |
8 μM
Compound: Everolimus
|
Cytotoxicity against human DU145 cells after 72 hrs by MTT assay
Cytotoxicity against human DU145 cells after 72 hrs by MTT assay
|
[PMID: 24445311] |
| HaCaT | CC50 |
28.3 μM
Compound: 37
|
Cytotoxicity against human HaCaT cells
Cytotoxicity against human HaCaT cells
|
[PMID: 33539089] |
| HCT-116 | IC50 |
12 μM
Compound: Everolimus
|
Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay
Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay
|
[PMID: 24445311] |
| HEK293 | IC50 |
5 nM
Compound: Everolimus
|
Inhibition of mTOR in HEK293 cells
Inhibition of mTOR in HEK293 cells
|
[PMID: 32324396] |
| HeLa | CC50 |
28.3 μM
Compound: 37
|
Cytotoxicity against human HeLa cells
Cytotoxicity against human HeLa cells
|
[PMID: 33539089] |
| HOP-62 | IC50 |
19 μM
Compound: Everolimus
|
Cytotoxicity against human HOP62 cells after 72 hrs by MTT assay
Cytotoxicity against human HOP62 cells after 72 hrs by MTT assay
|
[PMID: 24445311] |
| HT-29 | IC50 |
15 μM
Compound: Everolimus
|
Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay
Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay
|
[PMID: 24445311] |
| Huh-7 | CC50 |
>10 μM
Compound: 37
|
Cytotoxicity against human Huh-7 cells
Cytotoxicity against human Huh-7 cells
|
[PMID: 33539089] |
| MCF7 | EC50 |
<1 nM
Compound: Everolimus
|
Cytotoxicity against human MCF7 cells after 5 days by Presto blue reagent-based fluorescence analysis
Cytotoxicity against human MCF7 cells after 5 days by Presto blue reagent-based fluorescence analysis
|
10.1039/C5MD00493D |
| OVCAR-3 | IC50 |
16 μM
Compound: Everolimus
|
Cytotoxicity against human OVCAR3 cells after 72 hrs by MTT assay
Cytotoxicity against human OVCAR3 cells after 72 hrs by MTT assay
|
[PMID: 24445311] |
| SK-HEP1 | IC50 |
12 μM
Compound: Everolimus
|
Cytotoxicity against human SKHEP1 cells after 72 hrs by MTT assay
Cytotoxicity against human SKHEP1 cells after 72 hrs by MTT assay
|
[PMID: 24445311] |
| SQ20B | IC50 |
5.5 μM
Compound: Everolimus
|
Cytotoxicity against human SQ20B cells after 72 hrs by MTT assay
Cytotoxicity against human SQ20B cells after 72 hrs by MTT assay
|
[PMID: 24445311] |
| SQ20B | IC50 |
7.3 μM
Compound: RAD001
|
Cytotoxicity against human SQ20B cells after 72 hrs by MTT assay
Cytotoxicity against human SQ20B cells after 72 hrs by MTT assay
|
[PMID: 24836070] |
Everolimus (RAD001) is an orally active derivative of rapamycin that inhibits the Ser/Thr kinase, mTOR[1]. In both the sensitive murine B16/BL6 melanoma (IC50, 0.7 nM) and the insensitive human cervical KB-31 (IC50, 1,778 nM), antiproliferative concentrations of Everolimus results in total dephosphorylation of S6K1 and the substrate S6 and a shift in the mobility of 4E-BP1, which is indicative of a reduced phosphorylation status[3]. Everolimus exhibits a dose-dependent inhibition in both the total cells and the stem cells from the BT474 cell line and the primary breast cancer cells, albeit with different degrees of growth inhibition. Compare with the total cells, Everolimus is less effective in growth inhibition in the stem cells at all tested concentrations (P<0.001). The IC50 values of Everolimus for BT474 and the primary CSCs are 2,054 and 3,227 nM, or 29 times and 21 times greater than the IC50 values for their corresponding total cells, respectively[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 159351-69-6
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Appearance Solid
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Molecular Weight 958.22
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Formula C53H83NO14
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Color White to off-white
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SMILES
O=C([C@@]1(O)[C@@H](CC[C@@H](C[C@@H](/C(C)=C/C=C/C=C/[C@H](C[C@@H](C)C([C@@H]([C@@H](/C(C)=C/[C@H]2C)O)OC)=O)C)OC)O1)C)C(N3CCCC[C@H]3C(O[C@@H](CC2=O)[C@@H](C[C@H]4C[C@H]([C@H](OCCO)CC4)OC)C)=O)=O
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Synonyms
RAD001; SDZ-RAD
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Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 1 year -20°C 6 months
Publications (119)
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Journal Impact Factor
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Most Recent
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Signal Transduct Target Ther
Selective depletion of tumor-associated SAMHD1 enhances chemotherapeutic efficacy and antitumor immune responses. [Abstract]2025 Dec 15;10(1):406. PMID: 41392286 -
Signal Transduct Target Ther
Cyst(e)ine in nutrition formulation promotes colon cancer growth and chemoresistance by activating mTORC1 and scavenging ROS. [Abstract]2021 May 28;6(1):188. PMID: 34045438 -
Nat Med
Combination inhibition of PI3K and mTORC1 yields durable remissions in mice bearing orthotopic patient-derived xenografts of HER2-positive breast cancer brain metastases. [Abstract]2016 Jul;22(7):723-6. PMID: 27270588 -
Nature
2016 Dec 1;540(7631):119-123. PMID: 27880763 -
Cancer Cell
Anti-tumor efficacy of HRS-4642 and its potential combination with proteasome inhibition in KRAS G12D-mutant cancer. [Abstract]2024 Jul 8;42(7):1286-1300.e8. PMID: 38942026 -
Nat Cancer
PD-1 instructs a tumor-suppressive metabolic program that restricts glycolysis and restrains AP-1 activity in T cell lymphoma. [Abstract]2023 Oct;4(10):1508-1525. PMID: 37723306 -
Mil Med Res
Elevated FBXL6 activates both wild-type KRAS and mutant KRASG12D and drives HCC tumorigenesis via the ERK/mTOR/PRELID2/ROS axis in mice. [Abstract]2023 Dec 20;10(1):68. PMID: 38124228 -
Nat Commun
2025 Dec 15. PMID: 41397976 -
Acta Pharm Sin B
RICTOR/mTORC2 affects tumorigenesis and therapeutic efficacy of mTOR inhibitors in esophageal squamous cell carcinoma. [Abstract]2020 Jun;10(6):1004-1019. PMID: 32642408
Everolimus purchased from MedChemExpress. Usage Cited in: Acta Pharm Sin B. 2020 Jun;10(6):1004-1019. [Abstract]
ECa109 cells stably transfected with control shRNA or RICTOR shRNA were treated with RAD001 (10 μmol/L) or PP242 (2 μmol/L) for 48 h, and total proteins were extracted to analysis the expression of RICTOR, p-AKT (Ser473), AKT, p-PRAS40 (Thr246), PRAS40, p-p70S6K and p70S6K by Western blot (n=5).
Everolimus purchased from MedChemExpress. Usage Cited in: Acta Pharm Sin B. 2020 Jun;10(6):1004-1019. [Abstract]
Total proteins in tumor tissues from nude mice were extracted and the expressions of RICTOR, p-AKT (Ser473), AKT, p-PRAS40 (Thr246), PRAS40, p-p70S6K (Thr389) and p70S6K were evaluated by Western blot (n=5). Values represent the mean±SD.
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Sci Transl Med
mTORC1 inhibition is required for sensitivity to PI3K p110α inhibitors in PIK3CA-mutant breast cancer. [Abstract]2013 Jul 31;5(196):196ra99. PMID: 23903756
Everolimus purchased from MedChemExpress. Usage Cited in: Sci Transl Med. 2013 Jul 31;5(196):196ra99. [Abstract]
Apoptosis and PI3K/Akt/mTOR pathway inhibition in cells treated with BYL719, RAD001, or the combination. Protein lysates from HCC1954 and JIMT-1 cells treated for 18 hours with 0.5 μM BYL719, 1 nM RAD001 or the combination are analyzed by immunoblotting against the indicated proteins. Data are shown as mean ± SEM. p-value is calculated using two-sided student’s t-test.
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Adv Sci (Weinh)
Obesity-Associated TRIM15 Promotes the Proliferation of Esophageal Adenocarcinoma Through the YY2/FOXRED1 Axis. [Abstract]2025 Nov 14:e17330. PMID: 41237333 -
Adv Sci (Weinh)
Novel CAR-T Cells Specifically Targeting SIA-CIgG Demonstrate Effective Antitumor Efficacy in Bladder Cancer. [Abstract]2024 Aug 23:e2400156. PMID: 39178136 -
Adv Sci (Weinh)
Methuosis Inducer SGI-1027 Cooperates with Everolimus to Promote Apoptosis and Pyroptosis by Triggering Lysosomal Membrane Permeability in Renal Cancer. [Abstract]2024 Aug 9:e2404693. PMID: 39119834 -
J Clin Invest
Activin-A enhances mTOR signaling to promote aberrant chondrogenesis in fibrodysplasia ossificans progressiva. [Abstract]2017 Sep 1;127(9):3339-3352. PMID: 28758906 -
Exp Hematol Oncol
Effects of molecularly targeted therapies on murine thymus: highly selective mTOR inhibitors induce reversible thymic involution. [Abstract]2016 Jul 29:5:22. PMID: 27478685 -
J Adv Res
Targeting PLOD2 induces epithelioid differentiation and improves therapeutic response in sarcomatoid renal cell carcinoma. [Abstract]2025 Oct 16:S2090-1232(25)00818-5. PMID: 41109566 -
Sci Adv
Macrophage fusion event as one prerequisite for inorganic nanoparticle-induced antitumor response. [Abstract]2023 Jul 21;9(29):eadd9871. PMID: 37467339 -
Mol Ther
2025 Jan 8;33(1):279-296. PMID: 39521960 -
Cell Rep Med
CAN-Scan: A multi-omic phenotype-driven precision oncology platform identifies prognostic biomarkers of therapy response for colorectal cancer. [Abstract]2025 Apr 2:102053. PMID: 40187357 -
J Exp Med
2023 Nov 6;220(11):e20211743. PMID: 37642941 -
Mol Psychiatry
Phenotypic rescue via mTOR inhibition in neuron-specific Pten knockout mice reveals AKT and mTORC1-site specific changes. [Abstract]2025 Jul;30(7):3077-3089. PMID: 39953287 -
Cancer Lett
Jolkinolide B sensitizes bladder cancer to mTOR inhibitors via dual inhibition of Akt signaling and autophagy. [Abstract]2022 Feb 1:526:352-362. PMID: 34798195 -
Cancer Lett
Palmitic acid negatively regulates tumor suppressor PTEN through T366 phosphorylation and protein degradation. [Abstract]2021 Jan 1;496:127-133. PMID: 33039560 -
Cancer Lett
Everolimus selectively targets vemurafenib resistant BRAFV600E melanoma cells adapted to low pH. [Abstract]2017 Nov 1:408:43-54. PMID: 28826720
Everolimus purchased from MedChemExpress. Usage Cited in: Cancer Lett. 2017 Nov 1:408:43-54. [Abstract]
Western blot analysis of p-p70S6k, p70S6k, p-AKT and AKT after 6 h of treatment with 20 μM Everolimus. Levels of p-p70S6k and p-AKT are quantified by densitometric analysis and a corresponding histogram is constructed as relative to p70S6k or AKT and α-tubulin. The lower panel shows a representative Western blot.
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Adv Healthc Mater
Novel Drug-Testing Platform for Vascular Injury-induced Intimal Hyperplasia Using a Microphysiological System. [Abstract]2025 Aug 11:e00602. PMID: 40787716 -
Cell Death Dis
Everolimus and plicamycin specifically target chemoresistant colorectal cancer cells of the CMS4 subtype. [Abstract]2021 Oct 21;12(11):978. PMID: 34675191 -
Circ Heart Fail
mTOR Inhibition Prolongs Survival and Has Beneficial Effects on Heart Function After Onset of Lamin A/C Gene Mutation Cardiomyopathy in Mice. [Abstract]2024 Apr;17(4):e011110. PMID: 38567527 -
Hepatobiliary Surg Nutr
Influence of immunosuppressive drugs on natural killer cells in therapeutic drug exposure in liver transplantation. [Abstract]2023 Dec 1;12(6):835-853. PMID: 38115918 -
Cell Syst
Torin2 Exploits Replication and Checkpoint Vulnerabilities to Cause Death of PI3K-Activated Triple-Negative Breast Cancer Cells. [Abstract]2020 Jan 22;10(1):66-81.e11. PMID: 31812693 -
Cell Syst
A Library of Phosphoproteomic and Chromatin Signatures for Characterizing Cellular Responses to Drug Perturbations. [Abstract]2018 Apr 25;6(4):424-443.e7. PMID: 29655704 -
J Transl Med
Fasting mimicking diet inhibits tumor-associated macrophage survival and pro-tumor function in hypoxia: implications for combination therapy with anti-angiogenic agent. [Abstract]2023 Oct 26;21(1):754. PMID: 37884960 -
Biomed Pharmacother
Toxic effects of sirolimus and everolimus on the development and behavior of zebrafish embryos. [Abstract]2023 Oct:166:115397. PMID: 37659200 -
Biomed Pharmacother
Combined inhibition of RNA polymerase I and mTORC1/2 synergize to combat oral squamous cell carcinoma. [Abstract]2021 Jan;133:110906. PMID: 33190037 -
PLoS Biol
2019 May 21;17(5):e3000252. PMID: 31112550 -
Sci Data
High-throughput drug screening identifies novel therapeutics for Low Grade Serous Ovarian Carcinoma. [Abstract]2024 Sep 19;11(1):1024. PMID: 39300112 -
Cell Rep
PROX1 induction by autolysosomal activity stabilizes persister-like state of colon cancer via feedback repression of the NOX1-mTORC1 pathway. [Abstract]2023 Jun 27;42(6):112519. PMID: 37224811 -
Cell Rep
S-palmitoylation of PCSK9 induces sorafenib resistance in liver cancer by activating the PI3K/AKT pathway. [Abstract]2022 Aug 16;40(7):111194. PMID: 35977495 -
Br J Cancer
Anti-angiogenic therapy using the multi-tyrosine kinase inhibitor Regorafenib enhances tumor progression in a transgenic mouse model of ß-cell carcinogenesis. [Abstract]2023 Oct;129(8):1225-1237. PMID: 37620408 -
Sci Signal
TSHZ2 is an EGF-regulated tumor suppressor that binds to the cytokinesis regulator PRC1 and inhibits metastasis. [Abstract]2021 Jun 22;14(688):eabe6156. PMID: 34158398 -
Epilepsia
Evaluation of subchronic administration of antiseizure drugs in spontaneously seizing rats. [Abstract]2020 Jun;61(6):1301-1311. PMID: 32420627 -
Elife
2017 Dec 14;6:e27293. PMID: 29239720 -
Cell Biol Toxicol
Linc-ROR orchestrates autophagy suppression and marks gastric cancer via the miR-145-5p/CARMIL1 axis. [Abstract]2026 Feb 13;42(1):42. PMID: 41688632 -
Biochem Pharmacol
PMEPA1 promotes mTOR inhibitor resistance in triple-negative breast cancer: Targeting the TGF-β/PMEPA1 axis as a therapeutic strategy to overcome resistance. [Abstract]2026 Mar 10:249:117889. PMID: 41819443 -
Mol Cancer Ther
ST8SIA1 Regulates Tumor Growth and Metastasis in TNBC by Activating the FAK-AKT-mTOR Signaling Pathway. [Abstract]2018 Dec;17(12):2689-2701. PMID: 30237308 -
J Ethnopharmacol
Paris polyphylla Smith var. yunnanensis-derived saponins potentiate the antitumor activity of GPX4 inhibitors. [Abstract]2026 Feb 28:357:120890. PMID: 41232632 -
Cells
Development of Personalized Therapeutic Strategies by Targeting Actionable Vulnerabilities in Metastatic and Chemotherapy-Resistant Breast Cancer PDXs. [Abstract]2019 Jun 18;8(6). pii: E605. PMID: 31216647 -
Drug Des Devel Ther
Attenuation of everolimus-induced cytotoxicity by a protective autophagic pathway involving ERK activation in renal cell carcinoma cells. [Abstract]2018 Apr 19:12:911-920. PMID: 29719377
Everolimus purchased from MedChemExpress. Usage Cited in: Drug Des Devel Ther. 2018 Apr 19:12:911-920. [Abstract]
786-O and A498 cell lines are treated by RAD001 with different concentrations for 24 hours. Immunoblotting shows that RAD001 induces autophagy indicators including upregulation of LC3-II/I and downregulation of p62 in a dose-dependent manner.
Everolimus purchased from MedChemExpress. Usage Cited in: Drug Des Devel Ther. 2018 Apr 19:12:911-920. [Abstract]
Immunoblotting demonstrates that AZD6244 can effectively restore upregulation of LC3-II/I and downregulation of p62 induced by RAD001 in 786-O and A498 cells.
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Nutrients
Oleuropein, the Main Polyphenol of Olea europaea Leaf Extract, Has an Anti-Cancer Effect on Human BRAF Melanoma Cells and Potentiates the Cytotoxicity of Current Chemotherapies. [Abstract]2018 Dec 8;10(12). pii: E1950. PMID: 30544808
Everolimus purchased from MedChemExpress. Usage Cited in: Nutrients. 2018 Dec 8;10(12). pii: E1950. [Abstract]
Western analysis of protein expression in cells treatmented with or without PLX4032 or RAD001.
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Int J Mol Sci
Discovery of TRPV4-Targeting Small Molecules with Anti-Influenza Effects Through Machine Learning and Experimental Validation. [Abstract]2025 Feb 6;26(3):1381. PMID: 39941149 -
Int J Oncol
Wnt inhibitory factor-1-mediated autophagy inhibits Wnt/β-catenin signaling by downregulating dishevelled-2 expression in non-small cell lung cancer cells. [Abstract]2018 Aug;53(2):904-914. PMID: 29916529 -
Cell Mol Neurobiol
Retinoic Acid-Induced Protein 14 (RAI14) Promotes mTOR-Mediated Inflammation Under Inflammatory Stress and Chemical Hypoxia in a U87 Glioblastoma Cell Line. [Abstract]2019 Mar;39(2):241-254. PMID: 30554401 -
Int J Cancer
Establishment of patient-derived organoids for guiding personalized therapies in breast cancer patients. [Abstract]2024 Jul 15;155(2):324-338. PMID: 38533706 -
Mol Cancer Res
Repurposing of mTOR Complex Inhibitors Attenuates MCL-1 and Sensitizes to PARP Inhibition. [Abstract]2019 Jan;17(1):42-53. PMID: 30201826
Everolimus purchased from MedChemExpress. Usage Cited in: Mol Cancer Res. 2019 Jan;17(1):42-53. [Abstract]
Combination of Everolimus with AZD2281 (left panel) and AZD2014 with AZD2281 (right panel) activates the RIPK1 Ser 166 phosphorylation in Clone A and SF-539 cells respectively.
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Molecules
Therapeutic Drug Monitoring of Everolimus Using Volumetric Absorptive Microsampling and Quantitative Dried Blood Spot Methods with LC-MS/MS in Adult Solid Organ Transplant Recipients: An Analytical and Clinical Comparative Study. [Abstract]2025 Jul 26;30(15):3139. PMID: 40807312 -
Molecules
In Vitro and in Vivo Activity of mTOR Kinase and PI3K Inhibitors Against Leishmania donovani and Trypanosoma brucei. [Abstract]2020 Apr 23;25(8):1980. PMID: 32340370 -
Molecules
Facilitating Anti-Cancer Combinatorial Drug Discovery by Targeting Epistatic Disease Genes. [Abstract]2018 Mar 23;23(4). pii: E736. PMID: 29570606 -
Molecules
Effects of Resveratrol, Lovastatin and the mTOR-Inhibitor RAD-001 on Insulin-Induced Genomic Damage In Vitro. [Abstract]2017 Dec 12;22(12). pii: E2207. PMID: 29231877
Everolimus purchased from MedChemExpress. Usage Cited in: Molecules. 2017 Dec 12;22(12). pii: E2207. [Abstract]
p-AKT level in NRK cells treated with 5 nM RAD-001, 1 μM Resveratrol and their combination for 2 h and analyzed by Western blotting. Blots from 3 independent experiments are used for quantification.
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Cell Rep Methods
Tumor immune microenvironment reconstitution in patient-derived organoids enables therapy modeling for NSCLC. [Abstract]2026 Jun 15;6(6):101339. PMID: 42134319 -
Cancers (Basel)
ShcD Binds DOCK4, Promotes Ameboid Motility and Metastasis Dissemination, Predicting Poor Prognosis in Melanoma. [Abstract]2020 Nov 13;12(11):3366. PMID: 33202906 -
ACS Omega
Association Study of OATP1B3 Polymorphisms on Hepatic Uptake and Drug-Drug Interaction In Vitro. [Abstract]2025 Oct 29;10(44):52562-52575. PMID: 41244417 -
Cancer Sci
Dual inhibition of the mTORC1 and mTORC2 signaling pathways is a promising therapeutic target for adult T-cell leukemia. [Abstract]2018 Jan;109(1):103-111. PMID: 29077243
Everolimus purchased from MedChemExpress. Usage Cited in: Cancer Sci. 2018 Jan;109(1):103-111. [Abstract]
ED-40415 cell lines are treated for 0 and 60 min with control (DMSO), Rapamycin, everolimus, LY294002, PP242 and AZD8055. After treatment, protein lysates are immunoblotted for expression of phosphorylated mTOR S2448 (mTORC1), S2481 (mTORC2), total mTOR, p-Akt S473, total Akt, p-p70S6k, total p70S6k, and actin.
Everolimus purchased from MedChemExpress. Usage Cited in: Cancer Sci. 2018 Jan;109(1):103-111. [Abstract]
HUT-102 cell lines are treated for 0 and 60 min with control (DMSO), Rapamycin, everolimus, LY294002, PP242 and AZD8055. After treatment, protein lysates are immunoblotted for expression of phosphorylated mTOR S2448 (mTORC1), S2481 (mTORC2), total mTOR, p-Akt S473, total Akt, p-p70S6k, total p70S6k, and actin.
Everolimus purchased from MedChemExpress. Usage Cited in: Cancer Sci. 2018 Jan;109(1):103-111. [Abstract]
MT-2 cell lines are treated for 0 and 60 min with control (DMSO), Rapamycin, everolimus, LY294002, PP242 and AZD8055. After treatment, protein lysates are immunoblotted for expression of phosphorylated mTOR S2448 (mTORC1), S2481 (mTORC2), total mTOR, p-Akt S473, total Akt, p-p70S6k, total p70S6k, and actin.
Everolimus purchased from MedChemExpress. Usage Cited in: Cancer Sci. 2018 Jan;109(1):103-111. [Abstract]
ATL-43T cell lines are treated for 0 and 60 min with control (DMSO), Rapamycin, everolimus, LY294002, PP242 and AZD8055. After treatment, protein lysates are immunoblotted for expression of phosphorylated mTOR S2448 (mTORC1), S2481 (mTORC2), total mTOR, p-Akt S473, total Akt, p-p70S6k, total p70S6k, and actin.
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FASEB J
Lansoprazole Enhances Everolimus Efficacy Through DDIT3-Mediated PI3K/AKT/mTOR Pathway Inhibition in Pancreatic Neuroendocrine Neoplasms Proliferation. [Abstract]2026 Apr 15;40(7):e71722. PMID: 41911054 -
FASEB J
Myosin Light Chain Kinase-Mediated Endothelial Hyperpermeability Underlies Temsirolimus-Induced Lung Injury. [Abstract]2025 Sep 30;39(18):e71061. PMID: 40991312 -
J Cell Mol Med
Slight up-regulation of Kir2.1 channel promotes endothelial progenitor cells to transdifferentiate into a pericyte phenotype by Akt/mTOR/Snail pathway. [Abstract]2021 Nov;25(21):10088-10100. PMID: 34592781 -
Transl Oncol
A novel treatment strategy of HER2-targeted therapy in combination with Everolimus for HR+/HER2- advanced breast cancer patients with HER2 mutations. [Abstract]2022 Jul; 21: 101444. PMID: 35523006 -
Oncol Res
2022 Jan 31;28(9):873-884. PMID: 34315564 -
Gynecol Oncol
A first-in-class CDK4 inhibitor demonstrates in vitro, ex-vivo and in vivo efficacy against ovarian cancer. [Abstract]2020 Dec;159(3):827-838. PMID: 32958271 -
J Neurosci
A Time-Sensitive Plasticity Distinguishes the Rapid and Sustained Synaptic Actions of Ketamine from Its (2 R,6 R)-Hydroxynorketamine Metabolite. [Abstract]2026 Feb 3:e0958252026. PMID: 41633835 -
Sci Rep
Steroid hormone receptors, exome sequencing and treatment responsiveness of breast cancer patient-derived xenografts originated in a South American country. [Abstract]2025 Jan 18;15(1):2415. PMID: 39827242 -
Sci Rep
Proteomic profiling reveals that ESR1 mutations enhance cyclin-dependent kinase signaling. [Abstract]2024 Mar 22;14(1):6873. PMID: 38519482 -
Biomedicines
An Orthotopic Model of Uveal Melanoma in Zebrafish Embryo: A Novel Platform for Drug Evaluation. [Abstract]2021 Dec 10;9(12):1873. PMID: 34944689 -
J Biomed Mater Res A
Immunomodulatory property and its regulatory mechanism of double network hydrogel on dendritic cells. [Abstract]2021 Jun;109(6):1015-1026. PMID: 32856407 -
J Pharmacol Exp Ther
Essential roles of mechanistic target of rapamycin in the induction of steroid resistance in group 2 innate lymphoid cells and severe asthma. [Abstract]2025 Oct 8;392(11):103744. PMID: 41172625 -
Microbiol Spectr
In Vitro and In Vivo Evaluation of Synergistic Effects of Everolimus in Combination with Antifungal Agents on Exophiala dermatitidis. [Abstract]2023 Jun 15;11(3):e0530222. PMID: 37140396 -
Front Mol Neurosci
Non-synaptic Cell-Autonomous Mechanisms Underlie Neuronal Hyperactivity in a Genetic Model of PIK3CA-Driven Intractable Epilepsy. [Abstract]2021 Nov 26:14:772847. PMID: 34899181 -
Bioengineering (Basel)
Precision Oncology for High-Grade Gliomas: A Tumor Organoid Model for Adjuvant Treatment Selection. [Abstract]2025 Oct 19;12(10):1121. PMID: 41155119 -
Viruses
M Segment-Based Minigenome System of Severe Fever with Thrombocytopenia Syndrome Virus as a Tool for Antiviral Drug Screening. [Abstract]2021 Jun 3;13(6):1061. PMID: 34205062 -
Viruses
Broad-Spectrum Host-Based Antivirals Targeting the Interferon and Lipogenesis Pathways as Potential Treatment Options for the Pandemic Coronavirus Disease 2019 (COVID-19). [Abstract]2020 Jun 10;12(6):628. PMID: 32532085 -
Exp Cell Res
Network-based analysis with primary cells reveals drug response landscape of acute myeloid leukemia. [Abstract]2020 Aug 1;393(1):112054. PMID: 32376287 -
Breast Cancer (Dove Med Press)
Combined Treatment with Shuyu Pills and Everolimus Suppresses Triple-Negative Breast Cancer Growth via the PI3K/AKT/mTOR Pathway. [Abstract]2026 Mar 4:18:580570. PMID: 41809619 -
Arch Med Res
LZTS3/TAGLN Suppresses Cancer Progression in Human Colorectal Adenocarcinoma Through Regulating Cell Proliferation, Migration, and Actin Cytoskeleton. [Abstract]2023 Oct 6;54(7):102894. PMID: 37806182 -
Diagnostics (Basel)
Application of Drug Testing Platforms in Circulating Tumor Cells and Validation of a Patient-Derived Xenograft Mouse Model in Patient with Primary Intracranial Ependymomas with Extraneural Metastases. [Abstract]2023 Mar 24;13(7):1232. PMID: 37046450 -
Int J Med Sci
NCAPH Promotes the Proliferation of Prostate Cancer Cells Via Modulating the E2F1 Mediated PI3K/AKT/mTOR Axis. [Abstract]2025 Jan 27;22(4):940-954. PMID: 39991770 -
Hum Cell
Establishment and characterization of preclinical model of primary ovarian squamous cell carcinoma. [Abstract]2025 Jul 7;38(5):125. PMID: 40624380 -
Hum Cell
Autophagy activation ameliorates the fibrosis of trabecular meshwork cells induced by TGFβ2 through the promotion of fibrotic proteins degradation. [Abstract]2024 Oct 22;38(1):4. PMID: 39436499 -
Cancer Med
2024 Jun;13(12):e7432. PMID: 38923304 -
J Pharm Biomed Anal
HPLC-DAD-CAD-based approach for the simultaneous analysis of hydrophobic drugs and lipid compounds in liposomes and for cyclodextrin/drug inclusion complexes. [Abstract]2021 Jul 15:201:114120. PMID: 33991808 -
J Chromatogr B Analyt Technol Biomed Life Sci
Simultaneous determination of 11 oral targeted antineoplastic drugs and 2 active metabolites by LC-MS/MS in human plasma and its application to therapeutic drug monitoring in cancer patients. [Abstract]2024 Apr 15:1237:124100. PMID: 38547701 -
Mol Biol Rep
mTOR inhibitor PP242 increases antitumor activity of sulforaphane by blocking Akt/mTOR pathway in esophageal squamous cell carcinoma. [Abstract]2022 Jan;49(1):451-461. PMID: 34731371 -
Fish Shellfish Immunol Rep
Essential role of 4E-BP1 for lymphocyte activation and proliferation in the adaptive immune response of Nile tilapia. [Abstract]2021 Feb 14:2:100006. PMID: 36420486 -
PLoS One
A novel small molecule screening assay using normal human chondrocytes toward osteoarthritis drug discovery. [Abstract]2024 Nov 1;19(11):e0308647. PMID: 39485774 -
PLoS One
2016 Jan 28;11(1):e0147682. PMID: 26821351
Everolimus purchased from MedChemExpress. Usage Cited in: PLoS One. 2016 Jan 28;11(1):e0147682. [Abstract]
CHP-212 and SK-N-AS cells are treated with indicated concentrations of AZD6244, MEK162, Everolimus or AZD8055 or combinations thereof as indicated for 1 hour. Then, cells are lysed and analysed by Western blot. Phosphorylation levels of AKT, ERK and S6 are detected by specific anti-phospho antibodies. Loading is verified by specific antibodies to total AKT, ERK and anti-tubulin.
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Acta Trop
Subcutaneous infection mouse model could be applied into real time monitoring the efficacy of anti-cystic echinococcosis drug in vivo. [Abstract]2023 Feb:238:106802. PMID: 36565837 -
Acta Trop
Tacrolimus, a rapamycin target protein inhibitor, exerts anti-cystic echinococcosis effects both in vitro and in vivo. [Abstract]2020 Dec;212:105708. PMID: 32956634 -
Prostate
NPRL2 enhances autophagy and the resistance to Everolimus in castration-resistant prostate cancer. [Abstract]2019 Jan;79(1):44-53. PMID: 30178500
Everolimus purchased from MedChemExpress. Usage Cited in: Prostate. 2019 Jan;79(1):44-53. [Abstract]
Treatment with sub-dose of Everolimus (10 nM), together with CQ (5 µM) increases the levels of Bax and cleaved PARP, and decreases the levels of Bcl-2 expression in both PC3 and LNPER cells.
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J Viral Hepat
The Differential Effects of Immunosuppressants on Hepatitis E Virus Replication and the Triggered Inflammatory Responses in Macrophages. [Abstract]2026 Jan;33(1):e70118. PMID: 41400072 -
Biochem Biophys Res Commun
Everolimus reduces postoperative arthrofibrosis in rabbits by inducing autophagy-mediated fibroblast apoptosis by PI3K/Akt/mTOR signaling pathway. [Abstract]2020 Nov 26;533(1):1-8. PMID: 32919704 -
Drugs R D
A Combination of the Tryptophan Hydroxylase Inhibitor Telotristat with the mTOR Inhibitor Everolimus as an Effective Strategy Against Neuroendocrine Tumors. [Abstract]2026 May 24. PMID: 42177741 -
In Vitro Cell Dev Biol Anim
Breast cancer organoids from malignant pleural effusion-derived tumor cells as an individualized medicine platform. [Abstract]2021 May;57(5):510-518. PMID: 33950403 -
Can J Physiol Pharmacol
Inhibition of autophagy improves resistance and enhances sensitivity of gastric cancer cells to cisplatin. [Abstract]2020 Jul;98(7):449-458. PMID: 32058824 -
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bioRxiv
The combination of BCL-xL PROTAC and mTOR inhibitor sensitizes pancreatic ductal adenocarcinoma to KRASG12D inhibitor treatment by enhancing apoptosis induction. [Abstract]2026 Jan 5:2026.01.05.697773. PMID: 41542622 -
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J Oncol
2019 Jun 2:2019:8340926. PMID: 31275384 -
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Oncotarget
2015 Dec 8;6(39):42183-96. PMID: 26544513
Everolimus purchased from MedChemExpress. Usage Cited in: Oncotarget. 2015 Dec 8;6(39):42183-96. [Abstract]
KNS-62 and T24 cells are treated with 250 nM AZD6244, 250 nM MEK162, 5 nM of Everolimus, 250 nM AKT8055 or combinations thereof as indicated for 1 hour. Then, cells are lysed and analysed by Western blot.
Solvent & Solubility
DMSO : 50 mg/mL (52.18 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (2.61 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (2.61 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
Tumor cells are plated into 96-well plates at densities ranging from 500 to 5,000/100 μL/well, with repeat experiments being done at an optimal cell number, typically 1,000 to 2,000 per well, and incubated overnight. Cells are exposed to Everolimus and incubated for 4 days and the cell number is determined by methylene blue staining. For this, 50 μL glutaraldehyde [20% (v/v)] is added to the wells incubated for 10 min at room temperature. The culture medium is aspirated, cells are washed with distilled water, and 100 μL methylene blue [0.05% (w/v) in water] is added and incubated for 10 min at 37°C. Stained cells are washed three times with water, 200 μL HCl [3% (v/v)] is added, and the plate shaken at room temperature for 20 min. The absorbance of each well is determined at 650 nm. The IC50 values are calculated using Softmax 2.0 software[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[2]
Everolimus, PTK/ZK, and their respective vehicles are prepared each day just before administration to animals and the administration volume is individually adjusted based on animal body weight. In C57/BL6 mice, Everolimus is administered at doses ranging from 0.1 to 10 mg/kg/d orally (10 mL/kg) and predominantly at 2.5 to 10 mg/kg because these doses provides the maximum effect. PTK/ZK is administered at 50 to 100 mg/kg/d orally.
Rats[2]
Wistar-Furth rats are divided into two equal groups based on body weight and treated either with vehicle or Everolimus (10 mg/kg/d orally in mice and 5 mg/kg three times per week orally in rats). Directly after the first measurement at baseline (day 0), Everolimus or vehicle is administered orally by gavage (10 mL/kg) for up to 7 days maximum with subsequent magnetic resonance measurements made within 30 min of the last dose.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (285 KB)
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SDS (623 KB)
- English - EN (623 KB)
- Français - FR (623 KB)
- Deutsch - DE (623 KB)
- Norwegian - NO (623 KB)
- Español - ES (623 KB)
- Swedish - SV (623 KB)
- Italian - IT (623 KB)
- Korean - KR (623 KB)
- Portuguese - PT (623 KB)
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Handling Instructions (2659 KB)
References
[1]. O'Reilly T, et al. 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. [Content Brief]
[2]. Kawata T, et al. 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. [Content Brief]
[3]. Lane HA, et al. mTOR inhibitor RAD001 (everolimus) has antiangiogenic/vascular properties distinct from a VEGFR tyrosine kinase inhibitor. Clin Cancer Res, 2009, 15(5), 1612-1622. [Content Brief]
[4]. Zhu Y, et al. Antitumor effect of the mTOR inhibitor Everolimus on human breast cancer stem cells in vitro and in vivo. Tumour Biol. 2012 Oct;33(5):1349-62. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.0436 mL | 5.2180 mL | 10.4360 mL | 26.0900 mL |
| 5 mM | 0.2087 mL | 1.0436 mL | 2.0872 mL | 5.2180 mL | |
| 10 mM | 0.1044 mL | 0.5218 mL | 1.0436 mL | 2.6090 mL | |
| 15 mM | 0.0696 mL | 0.3479 mL | 0.6957 mL | 1.7393 mL | |
| 20 mM | 0.0522 mL | 0.2609 mL | 0.5218 mL | 1.3045 mL | |
| 25 mM | 0.0417 mL | 0.2087 mL | 0.4174 mL | 1.0436 mL | |
| 30 mM | 0.0348 mL | 0.1739 mL | 0.3479 mL | 0.8697 mL | |
| 40 mM | 0.0261 mL | 0.1305 mL | 0.2609 mL | 0.6523 mL | |
| 50 mM | 0.0209 mL | 0.1044 mL | 0.2087 mL | 0.5218 mL |