Vistusertib (AZD2014)
This product is for research use only, not for human use. We do not sell to patients.
For small sizes, please check our retail website as below: www.invivochem.com
| Size | Price | Stock |
|---|---|---|
| 250mg | $720 | Check With Us |
| 500mg | $1150 | Check With Us |
| 1g | $1725 | Check With Us |
: Cat #: V0195 CAS #: 1009298-59-2 Purity ≥ 98%
Description: Vistusertib (formerly AZD-2014) is a novel, potent, orally bioavailable and ATP competitive inhibitor of mTOR (mammalian target of rapamycin) with potential antitumor activity.
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| Molecular Weight (MW) | 462.54 |
|---|---|
| Molecular Formula | C25H30N6O3 |
| CAS No. | 1009298-59-2 |
| Storage | -20℃ for 3 years in powder formr |
| -80℃ for 2 years in solvent | |
| Solubility In Vitro | DMSO: 38 mg/mL (82.15 mM)r |
| Water: <1 mg/mLr | |
| Ethanol: <1 mg/mL | |
| Solubility In Vivo | 5% DMSO+30% PEG 300+ddH2O: 5mg/mL |
| SMILES Code | O=C(NC)C1=CC=CC(C2=CC=C3C(N4[C@@H](C)COCC4)=NC(N5[C@@H](C)COCC5)=NC3=N2)=C1 |
| Synonyms | AZD2014, AZD-2014, AZD 2014, Vistusertib |
| Protocol | 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. |
|---|---|---|
| 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 Cmax and AUC is observed following single dose and repeat dosing of AZD2014: Cmax 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). |
These protocols are for reference only. InvivoChem does not
independently validate these methods.
| Solvent volume to be added | Mass (the weight of a compound) | |||
|---|---|---|---|---|
| Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
| 1mM | 2.1620 mL | 10.8099 mL | 21.6198 mL | 43.2395 mL |
| 5mM | 0.4324 mL | 2.1620 mL | 4.3240 mL | 8.6479 mL |
| 10mM | 0.2162 mL | 1.0810 mL | 2.1620 mL | 4.3240 mL |
| 20mM | 0.1081 mL | 0.5405 mL | 1.0810 mL | 2.1620 mL |
The molarity calculator equation
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The dilution calculator equation
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Step One: Enter information below
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Average weight of animals g
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Step Two: Enter the in vivo formulation
%DMSO
+
%
+
%Tween 80
+
%ddH2O
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 add
µL
PEG300, mix and clarify, next add
µL
Tween 80,mix and clarify, next add
µL
ddH2O,mix and clarify.
Note:
- (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
- (2) Be sure to add the solvent(s) in order.