U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

Details

Stereochemistry ABSOLUTE
Molecular Formula C25H30N6O3
Molecular Weight 462.5441
Optical Activity UNSPECIFIED
Defined Stereocenters 2 / 2
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of VISTUSERTIB

SMILES

CNC(=O)C1=CC=CC(=C1)C2=CC=C3C(N=C(N=C3N4CCOC[C@@H]4C)N5CCOC[C@@H]5C)=N2

InChI

InChIKey=JUSFANSTBFGBAF-IRXDYDNUSA-N
InChI=1S/C25H30N6O3/c1-16-14-33-11-9-30(16)23-20-7-8-21(18-5-4-6-19(13-18)24(32)26-3)27-22(20)28-25(29-23)31-10-12-34-15-17(31)2/h4-8,13,16-17H,9-12,14-15H2,1-3H3,(H,26,32)/t16-,17-/m0/s1

HIDE SMILES / InChI

Molecular Formula C25H30N6O3
Molecular Weight 462.5441
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 2 / 2
E/Z Centers 0
Optical Activity UNSPECIFIED

Vistusertib (AZ-2014) is a dual inhibitor of mTORC1/mTORC2 which was developed by AstraZeneca for the treatment of cancer. The drug is under clinical development (phase II) in patients with Renal Carcinoma, Squamous Non Small Cell Lung Cancer, Diffuse Large B-Cell Lymphoma, Meningioma, Breast cancer and Gastric cancer, either alone or in combination therapy. Vistusertib penetrates blood-brain barrier.

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
210.0 nM [IC50]
78.0 nM [IC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Unknown

Approved Use

Unknown
Primary
Unknown

Approved Use

Unknown
Primary
Unknown

Approved Use

Unknown
Primary
Unknown

Approved Use

Unknown
Primary
Unknown

Approved Use

Unknown
Primary
Unknown

Approved Use

Unknown
Overview

OverviewOther

Other InhibitorOther SubstrateOther Inducer





Drug as perpetrator​Drug as victimTox targets

Tox targets

TargetModalityActivityMetaboliteClinical evidence
Sourcing

Sourcing

Vendor/AggregatorIDURL
PubMed

PubMed

TitleDatePubMed
Dramatic suppression of colorectal cancer cell growth by the dual mTORC1 and mTORC2 inhibitor AZD-2014.
2014 Jan 10
Transforming growth factor-β (TGF-β) induces the expression of chondrogenesis-related genes through TGF-β receptor II (TGFRII)-AKT-mTOR signaling in primary cultured mouse precartilaginous stem cells.
2014 Jul 18
Inhibition of Bcl-2 potentiates AZD-2014-induced anti-head and neck squamous cell carcinoma cell activity.
2016 Sep 2
Patents

Patents

Sample Use Guides

Renal Carcinoma: patients receive 50mg twice a day. Squamous Non Small Cell Lung Cancer: patients receive study treatment consisting of a single weekly paclitaxel infusion (80 mg/m2) on Day 1 of each week and twice daily 50 mg doses of vistusertib on the first 3 days each week for 6 weeks. Diffuse Large B-Cell Lymphoma: patients receive 125mg of vistusertib twice daily - 2 days on 5 days off in a 28 day cycle. Gastric Adenocarcinoma: patients receive 50mg of vistusertib twice dayly, 3 days on 4 days off of a 7 day cycle + paclitaxel 80mg/m2 given days 1, 8 and 15 of a 28 day cycle.
Route of Administration: Oral
Glioblastoma stem-like cells were treated with vistusertib (2 uM) and radiation to investigate the effects of the drug on the radiosensitivity of cells.
Substance Class Chemical
Created
by admin
on Sat Dec 16 10:31:18 GMT 2023
Edited
by admin
on Sat Dec 16 10:31:18 GMT 2023
Record UNII
0BSC3P4H5X
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
VISTUSERTIB
INN   USAN   WHO-DD  
USAN   INN  
Official Name English
AZD2014
Code English
AZD-2014
Code English
BENZAMIDE, 3-(2,4-BIS((3S)-3-METHYL-4-MORPHOLINYL)PYRIDO(2,3-D)PYRIMIDIN-7-YL)-N-METHYL-
Systematic Name English
Vistusertib [WHO-DD]
Common Name English
VISTUSERTIB [JAN]
Common Name English
3-[2,4-Bis[(3S)-3-methyl-4-morpholinyl]pyrido[2,3-d]pyrimidin-7-yl]-N-methylbenzamide
Systematic Name English
vistusertib [INN]
Common Name English
VISTUSERTIB [USAN]
Common Name English
Classification Tree Code System Code
NCI_THESAURUS C129825
Created by admin on Sat Dec 16 10:31:18 GMT 2023 , Edited by admin on Sat Dec 16 10:31:18 GMT 2023
NCI_THESAURUS C2201
Created by admin on Sat Dec 16 10:31:18 GMT 2023 , Edited by admin on Sat Dec 16 10:31:18 GMT 2023
Code System Code Type Description
SMS_ID
100000174944
Created by admin on Sat Dec 16 10:31:18 GMT 2023 , Edited by admin on Sat Dec 16 10:31:18 GMT 2023
PRIMARY
USAN
EF-07
Created by admin on Sat Dec 16 10:31:18 GMT 2023 , Edited by admin on Sat Dec 16 10:31:18 GMT 2023
PRIMARY
DRUG BANK
DB11925
Created by admin on Sat Dec 16 10:31:18 GMT 2023 , Edited by admin on Sat Dec 16 10:31:18 GMT 2023
PRIMARY
NCI_THESAURUS
C88329
Created by admin on Sat Dec 16 10:31:18 GMT 2023 , Edited by admin on Sat Dec 16 10:31:18 GMT 2023
PRIMARY
ChEMBL
CHEMBL1078983
Created by admin on Sat Dec 16 10:31:18 GMT 2023 , Edited by admin on Sat Dec 16 10:31:18 GMT 2023
PRIMARY
FDA UNII
0BSC3P4H5X
Created by admin on Sat Dec 16 10:31:18 GMT 2023 , Edited by admin on Sat Dec 16 10:31:18 GMT 2023
PRIMARY
PUBCHEM
25262792
Created by admin on Sat Dec 16 10:31:18 GMT 2023 , Edited by admin on Sat Dec 16 10:31:18 GMT 2023
PRIMARY
INN
10158
Created by admin on Sat Dec 16 10:31:18 GMT 2023 , Edited by admin on Sat Dec 16 10:31:18 GMT 2023
PRIMARY
EPA CompTox
DTXSID20143584
Created by admin on Sat Dec 16 10:31:18 GMT 2023 , Edited by admin on Sat Dec 16 10:31:18 GMT 2023
PRIMARY
CAS
1009298-59-2
Created by admin on Sat Dec 16 10:31:18 GMT 2023 , Edited by admin on Sat Dec 16 10:31:18 GMT 2023
PRIMARY
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TARGET -> INHIBITOR
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