VISTUSERTIB

Investigational

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 Search

SMILES

CNC(=O)C1=CC=CC(=C1)C2=NC3=C(C=C2)C(=NC(=N3)N4CCOC[C@@H]4C)N5CCOC[C@@H]5C

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

Description
Sources: https://www.ncbi.nlm.nih.gov/pubmed/23375793|https://www.ncbi.nlm.nih.gov/pubmed/24311635

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.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Mammalian target of Rapamycin (mTORC1) 23 Target ID: CHEMBL2221341 Sources: https://www.ncbi.nlm.nih.gov/pubmed/23375793	Inhibitor 8504		210.0 nM [IC50]
mTORC2 8 Target ID: mTORC2 Sources: https://www.ncbi.nlm.nih.gov/pubmed/23375793	Inhibitor 8504		78.0 nM [IC50]

Conditions

Condition	Modality	Highest Phase	Product
Renal cancer 2 Sources: https://www.ncbi.nlm.nih.gov/pubmed/26364551	Primary	Phase II 1147	Unknown Approved Use Unknown
Meningioma 2 Sources: https://www.ncbi.nlm.nih.gov/pubmed/26219339	Primary	Phase II 1147	Unknown Approved Use Unknown
Squamous non-small cell lung cancer 2 Sources: https://clinicaltrials.gov/ct2/show/NCT02403895	Primary	Phase II 1147	Unknown Approved Use Unknown
Diffuse large B-cell lymphoma 22 Sources: https://www.ncbi.nlm.nih.gov/pubmed/24970801	Primary	Phase II 1147	Unknown Approved Use Unknown
Breast cancer 432 Sources: https://www.ncbi.nlm.nih.gov/pubmed/26358751	Primary	Phase II 1147	Unknown Approved Use Unknown
Gastric adenocarcinoma 12 Sources: https://clinicaltrials.gov/ct2/show/NCT02449655	Primary	Phase II 1147	Unknown Approved Use Unknown

C_max

Value	Dose	Co-administered	Analyte	Population
1840 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/30016392/	75 mg 3 times / week multiple, oral dose: 75 mg route of administration: Oral experiment type: MULTIPLE co-administered: PACLITAXEL	PACLITAXEL	VISTUSERTIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
840 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/30016392/	50 mg 6 times / week multiple, oral dose: 50 mg route of administration: Oral experiment type: MULTIPLE co-administered: PACLITAXEL	PACLITAXEL	VISTUSERTIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
926 ng/mL EXPERIMENT https://ascopubs.org/doi/abs/10.1200/JCO.2017.35.15_suppl.2571	50 mg 2 times / day steady-state, oral dose: 50 mg route of administration: Oral experiment type: STEADY-STATE co-administered: PACLITAXEL	PACLITAXEL	VISTUSERTIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE food status: UNKNOWN

AUC

Value	Dose	Co-administered	Analyte	Population
7543 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/30016392/	75 mg 3 times / week multiple, oral dose: 75 mg route of administration: Oral experiment type: MULTIPLE co-administered: PACLITAXEL	PACLITAXEL	VISTUSERTIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
2602 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/30016392/	50 mg 6 times / week multiple, oral dose: 50 mg route of administration: Oral experiment type: MULTIPLE co-administered: PACLITAXEL	PACLITAXEL	VISTUSERTIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
2821 ng × h/mL EXPERIMENT https://ascopubs.org/doi/abs/10.1200/JCO.2017.35.15_suppl.2571	50 mg 2 times / day steady-state, oral dose: 50 mg route of administration: Oral experiment type: STEADY-STATE co-administered: PACLITAXEL	PACLITAXEL	VISTUSERTIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE food status: UNKNOWN

T_1/2

Value	Dose	Co-administered	Analyte	Population
2.7 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/30016392/	75 mg 3 times / week multiple, oral dose: 75 mg route of administration: Oral experiment type: MULTIPLE co-administered: PACLITAXEL	PACLITAXEL	VISTUSERTIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
1.8 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/30016392/	50 mg 6 times / week multiple, oral dose: 50 mg route of administration: Oral experiment type: MULTIPLE co-administered: PACLITAXEL	PACLITAXEL	VISTUSERTIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
3 h EXPERIMENT https://ascopubs.org/doi/abs/10.1200/JCO.2017.35.15_suppl.2571	50 mg 2 times / day steady-state, oral dose: 50 mg route of administration: Oral experiment type: STEADY-STATE co-administered: PACLITAXEL	PACLITAXEL	VISTUSERTIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE food status: UNKNOWN

F_unbound

Value	Dose	Co-administered	Analyte	Population
5% EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/23375793			VISTUSERTIB plasma	Homo sapiens

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
inhibitor 2252 substrate 1946	inhibitor 2438	inhibitor 2507	inhibitor 2217

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
P-gp 1741 BCRP 910	CYP3A5 446 CYP2C8 810	P-gp 301

Drug as perpetrator

Target	Modality	Activity
CYP3A4 2633	inhibitor 4027 Sources: https://pubchem.ncbi.nlm.nih.gov/bioassay/1645841#sid=363677525	inconclusive [IC50 21.3174 uM]
BCRP 985	inhibitor 4027 Sources: https://pubmed.ncbi.nlm.nih.gov/29790111/	likely
P-gp 1932	inhibitor 4027 Sources: https://pubmed.ncbi.nlm.nih.gov/29790111/	likely
P-gp 1932	inducer 1966 Sources: https://pubmed.ncbi.nlm.nih.gov/29790111/	no
CYP2C9 2497	inhibitor 4027 Sources: https://pubchem.ncbi.nlm.nih.gov/bioassay/1645842#sid=440681558	yes [IC50 10.684 uM]
CYP2D6 2546	inhibitor 4027 Sources: https://pubchem.ncbi.nlm.nih.gov/bioassay/1645840#sid=440681558	yes [IC50 15.0916 uM]

Drug as victim

Target	Modality	Activity
CYP2C8 810	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/25805799/	major
CYP3A5 446	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/25805799/	major
CYP3A4 1946	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/25805799/	minor

Tox targets

Target	Modality	Activity	Metabolite	Clinical evidence
hERG 2263	inhibitor 2237 Sources: https://pubmed.ncbi.nlm.nih.gov/23375793/

Sourcing

Vendor/Aggregator	ID	URL
001 Chemical	DY116169	https://www.001chemical.com/chem/search?q=DY116169
1PlusChem LLC	1P0003OQ	https://www.1pchem.com/search?query=1P0003OQ
AChemBlock	10284	http://www.achemblock.com/catalogsearch/result/?q=10284
AK Scientific	SYN1167	https://aksci.com/item_detail.php?cat=SYN1167
AK Scientific	X3569	https://aksci.com/item_detail.php?cat=X3569
Ambeed	A386287	http://www.ambeed.com/search/Search.html?keyword=A386287
Angene	AGN-PC-0WA7WU	http://www.angenechemical.com/productshow/AGN-PC-0WA7WU.html
AOBIOUS INC	AOB3574	http://aobious.com/aobious/search?search_query=AOB3574
ApexBio Technology	A8373	https://www.apexbt.com/catalogsearch/result/?q=A8373
AstaTech	42554	http://astatechinc.com/CPSResult.php?CRNO=42554
BLD Pharm	BD291524	http://www.bldpharm.com/search/Search.html?keyword=BD291524
BOC Sciences	1009298-59-2	http://www.bocsci.com/description.asp?cas=1009298-59-2
Cayman Chemical	17378	http://www.caymanchem.com/app/template/Product.vm/catalog/17378
ChemShuttle	102702	https://www.chemshuttle.com/catalogsearch/result/?q=102702
Debye Scientific	DA-35312	https://www.debyesci.com/index.php?id=product&ext[cno]=DA-35312
eMolecules	108760546	https://orderbb.emolecules.com/search/#?query=108760546
eMolecules	44786305	https://orderbb.emolecules.com/search/#?query=44786305
eNovation Chemicals	D210870	https://www.enovationchem.com/Products.asp?SEARCHTEXT=D210870&searchbtn.x=0&searchbtn.y=0
eNovation Chemicals	D572836	https://www.enovationchem.com/Products.asp?SEARCHTEXT=D572836&searchbtn.x=0&searchbtn.y=0
Excenen	EX-A155	http://www.excenen.com/searchresultlist.php?id=EX-A155
KeyOrganics	AS-16302	http://www.keyorganicsinc.com/bionet/catalogsearch/result?q=AS-16302
Lab Seeker	SC-62590	http://www.labseeker.com/search.php?keywords=SC-62590&category=0
LabSeeker	SC-62590	http://www.labseeker.com/search.php?keywords=SC-62590&category=0
Matrix Scientific	131592	http://www.matrixscientific.com/131592.html
mcule	MCULE-5509729271	https://mcule.com/MCULE-5509729271/
mcule	MCULE-9455167791	https://mcule.com/MCULE-9455167791/
MedChem Express	HY-15247	https://www.medchemexpress.com/search.html?q=HY-15247&ft=&fa=&fp=
Molcore	MC116169	http://www.molcore.com/CatMC116169.html
Molnova	M10062	https://www.molnova.com/en/serch-list.html?keywords=M10062
MolPort	MolPort-023-293-553	https://www.molport.com/shop/molecule-link/MolPort-023-293-553
MuseChem	I000107	https://www.musechem.com/product/I000107.html
ShangHai Biochempartner	BCP000631	http://www.biochempartner.com/search_BCP000631
ShangHai Biochempartner	BCP05748	http://www.biochempartner.com/search_BCP05748
TargetMol	T1961	https://www.targetmol.com/search?keyword=T1961
Toronto Research Chemicals	A808115	https://www.trc-canada.com/product-detail/?CatNum=A808115
Toronto Research Chemicals	H969900	https://www.trc-canada.com/product-detail/?CatNum=H969900

PubMed

Title	Date	PubMed
Inhibition of Bcl-2 potentiates AZD-2014-induced anti-head and neck squamous cell carcinoma cell activity.	2016-09-02	27343560
Pre-clinical evaluation of AZD-2014, a novel mTORC1/2 dual inhibitor, against renal cell carcinoma.	2015-02-28	25444920
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.	2014-07-18	24946212
Dramatic suppression of colorectal cancer cell growth by the dual mTORC1 and mTORC2 inhibitor AZD-2014.	2014-01-10	24309100
The mTORC1/mTORC2 inhibitor AZD2014 enhances the radiosensitivity of glioblastoma stem-like cells.	2014-01	24311635

Patents

Sample Use Guides

In Vivo Use Guide

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

In Vitro Use Guide

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 `Mon Mar 31 23:18:05 GMT 2025` Edited by `admin` on `Mon Mar 31 23:18:05 GMT 2025`
Record UNII	0BSC3P4H5X
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

VISTUSERTIB

Official Name

English

vistusertib [INN]

Preferred 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 [USAN]

Common Name

English

Classification Tree Code System Code

NCI_THESAURUS

C129825