Vistusertib
Based on 32 publication(s) in Google Scholar
Vistusertib (AZD2014) is an ATP competitive mTOR inhibitor with an IC50 of 2.81 nM. AZD2014 inhibits both mTORC1 and mTORC2 complexes.
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- Purity : 99.70%
- CAS No.: 1009298-59-2
- 화학식: C25H30N6O3
- 분자량:462.54
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- Protocol
- 순도&문서
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Vistusertib
More- Science. 2017 Dec 1;358(6367):eaan4368. [Abstract]
- Cancer Res. 2025 Nov 21:10.1158/0008-5472.CAN-24-3753. [Abstract]
- Autophagy. 2021 Jun;17(6):1349-1366. [Abstract]
- Nat Commun. 2026 Feb 12;17(1):1214. [Abstract]
- Nat Commun. 2019 Jul 1;10(1):2901. [Abstract]
- Nat Commun. 2017 Jun 8:8:15617. [Abstract]
- Sci Transl Med. 2018 Jul 18;10(450):eaaq1093. [Abstract]
- Theranostics. 2020 Jan 1;10(4):1531-1543. [Abstract]
- Phytomedicine. 2020 Mar:68:153191. [Abstract]
- Environ Int. 2024 Apr:186:108582. [Abstract]
- Oncogene. 2021 Jan;40(3):564-577. [Abstract]
- Cell Rep. 2022 Oct 25;41(4):111553. [Abstract]
- Environ Pollut. 2024 Jan 15:341:122910. [Abstract]
- Mol Cancer Res. 2019 Jan;17(1):42-53. [Abstract]
- Front Pharmacol. 2020 Nov 11:11:580407. [Abstract]
- Arab J Chem. 2024 Mar 26, 105762.
- Molecules. 2020 Apr 23;25(8):1980. [Abstract]
- Cancers (Basel). 2024 Aug 7;16(16):2785. [Abstract]
- Cancers (Basel). 2022 Mar 19;14(6):1575. [Abstract]
- J Cell Mol Med. 2026 Apr;30(7):e71101. [Abstract]
- J Photochem Photobiol B. 2020 Dec:213:112055. [Abstract]
- Microb Pathog. 2026 Apr:213:108349. [Abstract]
- PLoS One. 2025 Jun 17;20(6):e0324443. [Abstract]
- Oncol Lett. 2022 Feb;23(2):70. [Abstract]
- Int J Hematol. 2019 Oct;110(4):490-499. [Abstract]
- bioRxiv. 2026 Jul 3.
- bioRxiv. 2026 Mar 25.
- bioRxiv. 2024 October 25.
- Elife. 2020 Dec 7:9:e61405. [Abstract]
- Oncotarget. 2018 Sep 21;9(74):33995-34008. [Abstract]
- Oncotarget. 2017 Feb 21;8(8):12775-12783. [Abstract]
- Patent. US20160089377A1.
Customer Validation & Images
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Biological Activity
제품 설명
IC50 & Target
[1]|
mTOR 2.81 nM (IC50) |
mTORC1 |
mTORC2 |
PI3Kα 3.766 μM (IC50) |
Autophagy |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| HEK293 | IC50 |
0.0028 μM
Compound: 21, AZD2014
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Inhibition of recombinant FLAG-tagged mTOR (1362 to 2549) (unknown origin) expressed in HEK293 cells
Inhibition of recombinant FLAG-tagged mTOR (1362 to 2549) (unknown origin) expressed in HEK293 cells
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[PMID: 23375793] |
| MDA-MB-468 | IC50 |
0.08 μM
Compound: 21, AZD2014
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Inhibition of mTORC2 in human MDA-MB-468 cells assessed as reduction of AKT phosphorylation at Ser473 after 2 hrs
Inhibition of mTORC2 in human MDA-MB-468 cells assessed as reduction of AKT phosphorylation at Ser473 after 2 hrs
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[PMID: 23375793] |
| MDA-MB-468 | IC50 |
0.2 μM
Compound: 21, AZD2014
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Inhibition of mTORC1 in human MDA-MB-468 cells assessed as reduction of pS6 phosphorylation at Ser235/236 after 2 hrs
Inhibition of mTORC1 in human MDA-MB-468 cells assessed as reduction of pS6 phosphorylation at Ser235/236 after 2 hrs
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[PMID: 23375793] |
In Vitro
The inhibitory effects of Vistusertib (AZD2014) are measured against isolated recombinant mTOR enzyme (IC50 of 2.81 nM) as well as in cellular assays measuring both mTORC1 and mTORC2 activities. In MDAMB468 cells, Vistusertib (AZD2014) decreases the phosphorylation of the mTORC1 substrate ribosomal protein S6 (Ser235/236) with a mean IC50 value of 210 nM and the mTORC2 substrate AKT (Ser473) with a mean IC50 value of 78 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1009298-59-2
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Appearance Solid
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분자량 462.54
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화학식 C25H30N6O3
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Color Yellow to orange
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SMILES
O=C(NC)C1=CC=CC(C2=CC=C3C(N=C(N4[C@@H](C)COCC4)N=C3N5[C@@H](C)COCC5)=N2)=C1
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Synonyms
AZD2014
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 1 year -20°C 6 months
Publications (32)
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Journal Impact Factor
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Most Recent
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Science
2017 Dec 1;358(6367):eaan4368. PMID: 29191878 -
Cancer Res
Single-Cell Lineage Tracing Uncovers Resistance Signatures and Sensitizing Strategies to FLT3 Inhibitors in Acute Myeloid Leukemia. [Abstract]2025 Nov 21:10.1158/0008-5472.CAN-24-3753. PMID: 41270153 -
Autophagy
The anti-cancer drug ABTL0812 induces ER stress-mediated cytotoxic autophagy by increasing dihydroceramide levels in cancer cells. [Abstract]2021 Jun;17(6):1349-1366. PMID: 32397857 -
Nat Commun
Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]2026 Feb 12;17(1):1214. PMID: 41680175 -
Nat Commun
An ErbB2/c-Src axis links bioenergetics with PRC2 translation to drive epigenetic reprogramming and mammary tumorigenesis. [Abstract]2019 Jul 1;10(1):2901. PMID: 31263101 -
Nat Commun
2017 Jun 8:8:15617. PMID: 28593995
Vistusertib purchased from MedChemExpress. Usage Cited in: Nat Commun. 2017 Jun 8:8:15617. [Abstract]
Immunoblot analysis of KRAS protein levels in parental (P) and resistant derivatives (R1 and R2) following 4 h treatment with the corresponding inhibitor AZD2014 (Vistusertib).
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Sci Transl Med
PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]2018 Jul 18;10(450):eaaq1093. PMID: 30021885 -
Theranostics
Response to mTOR and PI3K inhibitors in enzalutamide-resistant luminal androgen receptor triple-negative breast cancer patient-derived xenografts. [Abstract]2020 Jan 1;10(4):1531-1543. PMID: 32042320 -
Phytomedicine
Atractylenolide I inhibits colorectal cancer cell proliferation by affecting metabolism and stemness via AKT/mTOR signaling. [Abstract]2020 Mar:68:153191. PMID: 32135457 -
Environ Int
Evidence of promoting effects of 6:2 Cl-PFESA on hepatocellular carcinoma proliferation in humans: An ideal alternative for PFOS in terms of environmental health?. [Abstract]2024 Apr:186:108582. PMID: 38513556 -
Oncogene
The translational repressor 4E-BP1 regulates RRM2 levels and functions as a tumor suppressor in Ewing sarcoma tumors. [Abstract]2021 Jan;40(3):564-577. PMID: 33191406 -
Cell Rep
2022 Oct 25;41(4):111553. PMID: 36288704 -
Environ Pollut
Environment relevant exposure of perfluorooctanoic acid accelerates the growth of hepatocellular carcinoma cells through mammalian target of rapamycin (mTOR) signal pathway. [Abstract]2024 Jan 15:341:122910. PMID: 37967710 -
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
Vistusertib purchased from MedChemExpress. Usage Cited in: Mol Cancer Res. 2019 Jan;17(1):42-53. [Abstract]
Combination of RAD001 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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Front Pharmacol
CC-223, NSC781406, and BGT226 Exerts a Cytotoxic Effect Against Pancreatic Cancer Cells via mTOR Signaling. [Abstract]2020 Nov 11:11:580407. PMID: 33343350 -
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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 -
Cancers (Basel)
Evaluation of Combined Chemotherapy and Genomic-Driven Targeted Therapy in Patient-Derived Xenografts Identifies New Therapeutic Approaches in Squamous Non-Small-Cell Lung Cancer Patients. [Abstract]2024 Aug 7;16(16):2785. PMID: 39199558 -
Cancers (Basel)
Identification of New Vulnerabilities in Conjunctival Melanoma Using Image-Based High Content Drug Screening. [Abstract]2022 Mar 19;14(6):1575. PMID: 35326726 -
J Cell Mol Med
2026 Apr;30(7):e71101. PMID: 41896195 -
J Photochem Photobiol B
Directly imaging the localisation and photosensitization properties of the pan-mTOR inhibitor, AZD2014, in living cancer cells. [Abstract]2020 Dec:213:112055. PMID: 33142217 -
Microb Pathog
mTORC2-dependent autophagy inhibition regulates the replication of HSV-1 and adenovirus in viral keratitis & conjunctivitis. [Abstract]2026 Apr:213:108349. PMID: 41628839 -
PLoS One
2025 Jun 17;20(6):e0324443. PMID: 40526635 -
Oncol Lett
CRNDE silencing promotes apoptosis and enhances cisplatin sensitivity of colorectal carcinoma cells by inhibiting the Akt/mTORC1-mediated Warburg effect. [Abstract]2022 Feb;23(2):70. PMID: 35069879 -
Int J Hematol
An mTORC1/2 dual inhibitor, AZD2014, acts as a lysosomal function activator and enhances gemtuzumab ozogamicin-induced apoptosis in primary human leukemia cells. [Abstract]2019 Oct;110(4):490-499. PMID: 31286402 -
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Elife
2020 Dec 7:9:e61405. PMID: 33284104 -
Oncotarget
Concomitant targeting of the mTOR/MAPK pathways: novel therapeutic strategy in subsets of RICTOR/KRAS-altered non-small cell lung cancer. [Abstract]2018 Sep 21;9(74):33995-34008. PMID: 30338041
Vistusertib purchased from MedChemExpress. Usage Cited in: Oncotarget. 2018 Sep 21;9(74):33995-34008. [Abstract]
The treatment groups incorporating Selumetinib effectively blocks downstream p-ERK1/2 signaling, AZD2014 has a marked reduction in downstream mTORC1/2 effectors p-AKT, p-S6RP and p-4EBP1, and blockade of RICTOR.
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Oncotarget
2017 Feb 21;8(8):12775-12783. PMID: 28061443
Vistusertib purchased from MedChemExpress. Usage Cited in: Oncotarget. 2017 Feb 21;8(8):12775-12783. [Abstract]
OSI-027, AZD-8055 and AZD-2014 almost completely block MHY1485-induced mTOR activation (p-mTOR/S6K1/Akt Ser473) in skin keratinocytes.
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Vistusertib purchased from MedChemExpress. Usage Cited in: Patent. US20160089377A1.
Western blot of cortical extracts from Cntnap2 mutant or wild-type mice treated with vehicle or various mTOR pathway inhibitors, showing staining for the presence of phosphorylated S6. Individual mice are tested, and are represented in the lanes as follows. Lane 1=Cntnap2+/− mouse 9-10 weeks old treated with vehicle as for AZD2014; Lane 2=Cntnap2+/− mouse 7.3 months old treated with Rapamycin; Lane 3=Cntnap2+/− mouse 6.3 months old treated with Torin 2; Lane 4=Cn
용액&용해도
In Vitro:
DMSO : ≥ 50 mg/mL (108.10 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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)
In Vivo:
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 (5.40 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 (5.40 mM); Suspended solution; Need ultrasonic and warming
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.
In Vivo Dissolution Calculator
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
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
순도&문서
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Data Sheet (279 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
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 | 2.1620 mL | 10.8099 mL | 21.6198 mL | 54.0494 mL |
| 5 mM | 0.4324 mL | 2.1620 mL | 4.3240 mL | 10.8099 mL | |
| 10 mM | 0.2162 mL | 1.0810 mL | 2.1620 mL | 5.4049 mL | |
| 15 mM | 0.1441 mL | 0.7207 mL | 1.4413 mL | 3.6033 mL | |
| 20 mM | 0.1081 mL | 0.5405 mL | 1.0810 mL | 2.7025 mL | |
| 25 mM | 0.0865 mL | 0.4324 mL | 0.8648 mL | 2.1620 mL | |
| 30 mM | 0.0721 mL | 0.3603 mL | 0.7207 mL | 1.8016 mL | |
| 40 mM | 0.0540 mL | 0.2702 mL | 0.5405 mL | 1.3512 mL | |
| 50 mM | 0.0432 mL | 0.2162 mL | 0.4324 mL | 1.0810 mL | |
| 60 mM | 0.0360 mL | 0.1802 mL | 0.3603 mL | 0.9008 mL | |
| 80 mM | 0.0270 mL | 0.1351 mL | 0.2702 mL | 0.6756 mL | |
| 100 mM | 0.0216 mL | 0.1081 mL | 0.2162 mL | 0.5405 mL |
Vistusertib Related Classifications
HY-15247 Related Classifications
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