Vistusertib (Synonyms: AZD2014)

Cat. No.: HY-15247 Purity: 98.21%: FAQs
Data Sheet SDS COA Handling Instructions

Vistusertib (AZD2014) is an ATP competitive mTOR inhibitor with an IC₅₀ of 2.81 nM. AZD2014 inhibits both mTORC1 and mTORC2 complexes.

For research use only. We do not sell to patients.

Vistusertib Chemical Structure

CAS No. : 1009298-59-2

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10 mM * 1 mL in DMSO	USD 92	In-stock	Estimated Time of Arrival: December 31
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10 mM * 1 mL ready for reconstitution	USD 92	In-stock	Estimated Time of Arrival: December 31
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10 mg	USD 144	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 300	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 26 publication(s) in Google Scholar

21 Publications Citing Use of MCE Vistusertib

: Vistusertib purchased from MCE. 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.

: Vistusertib purchased from MCE. 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.

: Vistusertib purchased from MCE. 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 inhibitors Rapamycin, AZD2014, MLN0128, BEZ235 and 4EGI-1. Images are cropped for clarity from the same exposure of the same membrane.

: Vistusertib purchased from MCE. 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.

: Vistusertib purchased from MCE. 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

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mTOR mTORC1 mTORC2

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

Vistusertib (AZD2014) is an ATP competitive mTOR inhibitor with an IC₅₀ of 2.81 nM. AZD2014 inhibits both mTORC1 and mTORC2 complexes.

IC₅₀ & Target^[1]

mTOR

2.81 nM (IC₅₀)

mTORC1

mTORC2

PI3Kα

3.766 μM (IC₅₀)

Autophagy

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Vistusertib (AZD2014) induces dose-dependent tumor growth inhibition in several xenograft and primary explant models. The antitumor activity of Vistusertib (AZD2014) is associated with modulation of both mTORC1 and mTORC2 substrates, consistent with its mechanism of action. The pharmacokinetics of Vistusertib (AZD2014) in mice is tested upon administration of doses between 7.5 and 15 mg/kg. A dose-dependent increase in C_max and AUC is observed following single dose and repeat dosing of AZD2014: C_max range from 1 to 16 μM and AUC range from 220 to 5,042 μM·h across this dose range. The pharmacodynamic effect of Vistusertib (AZD2014) against an mTORC1 biomarker (phosphorylation of S6) and an mTORC2 biomarker (phosphorylation of AKT) is assessed in SCID mice bearing MCF7 xenografts following administration of 3.75, 7.5, and 15 mg/kg AZD2014. There is a good relationship between the drug plasma concentrations and biomarker levels (estimated p-AKT IC₅₀ of 0.119 μM total, 53% SE, and estimated p-S6 IC₅₀ 0.392 μM, 28.8% SE)^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

Molecular Weight

462.54

Appearance

Solid

Formula

C₂₅H₃₀N₆O₃

CAS No.

1009298-59-2

SMILES

O=C(NC)C1=CC=CC(C2=CC=C3C(N=C(N4[[email protected]@H](C)COCC4)N=C3N5[[email protected]@H](C)COCC5)=N2)=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : ≥ 50 mg/mL (108.10 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.1620 mL	10.8099 mL	21.6198 mL
5 mM	0.4324 mL	2.1620 mL	4.3240 mL
10 mM	0.2162 mL	1.0810 mL	2.1620 mL

*Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

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
2.

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
3.

Add each solvent one by one: 5% DMSO 40% PEG300 5% Tween-80 50% saline
Solubility: 2.5 mg/mL (5.40 mM); Suspended solution; Need ultrasonic
4.

Add each solvent one by one: 5% DMSO 95% (20% SBE-β-CD in saline)
Solubility: 2.5 mg/mL (5.40 mM); Suspended solution; Need ultrasonic

*All of the co-solvents are available by MCE.

Purity & Documentation

Purity: 98.21%

Select Batch:

Data Sheet (279 KB) SDS (251 KB)

COA (248 KB) LCMS (265 KB)

Handling Instructions (2659 KB)

References

[1]. Guichard SM, et al. AZD2014, an inhibitor of mTORC1 and mTORC2, is highly effective in ER+ breast cancer when administered using intermittent or continuous schedules. Mol Cancer Ther. 2015 Nov;14(11):2508-18. [Content Brief]

Cell Assay	MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	Mice^[1] MCF7 experiments: 5×10⁶ MCF7 cells are injected s.c. in a volume of 0.1 mL in male SCID mice and are randomized into control and treatment groups when tumor size reach 0.2 cm³. Vistusertib (AZD2014) is dissolved in captisol, and diluted to a final captisol concentration of 30% (w/v). Vistusertib (AZD2014) is administered by oral gavage (0.1 mL/10 g body weight). The control group receive vehicle only. Tumor volumes (measured by calliper), animal body weight and condition are recorded twice weekly for the duration of the study. The tumor volume is calculated (taking length to be the longest diameter across and width to be the corresponding perpendicular diameter) using the formula: (length×width)×√(length×width)×(π/6). MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. Guichard SM, et al. AZD2014, an inhibitor of mTORC1 and mTORC2, is highly effective in ER+ breast cancer when administered using intermittent or continuous schedules. Mol Cancer Ther. 2015 Nov;14(11):2508-18. [Content Brief]

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Keywords:

Vistusertib1009298-59-2AZD2014AZD 2014AZD-2014mTORAutophagyApoptosisMammalian target of RapamycinInhibitorinhibitorinhibit

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Vistusertib (Synonyms: AZD2014)

Customer Review

21 Publications Citing Use of MCE Vistusertib

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•Related Screening Libraries:

View All mTOR Isoform Specific Products:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

Molarity Calculator

Dilution Calculator

The molarity calculator equation

The dilution calculator equation

Keywords:

Your Recently Viewed Products:

Customer Review

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