AMG-319

Investigational

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C21H16FN7
Molecular Weight	385.397
Optical Activity	UNSPECIFIED
Defined Stereocenters	1 / 1
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

C[C@H](NC1=C2N=CNC2=NC=N1)C3=CC4=C(C=C(F)C=C4)N=C3C5=NC=CC=C5

InChI

InChIKey=KWRYMZHCQIOOEB-LBPRGKRZSA-N

InChI=1S/C21H16FN7/c1-12(28-21-19-20(25-10-24-19)26-11-27-21)15-8-13-5-6-14(22)9-17(13)29-18(15)16-4-2-3-7-23-16/h2-12H,1H3,(H2,24,25,26,27,28)/t12-/m0/s1

HIDE SMILES / InChI

Description
Sources: https://www.ncbi.nlm.nih.gov/pubmed/25469863 | http://www.amgentrials.com/amgen/trialsummary.aspx?studyid=20101262

AMG-319 is an oral, small molecule inhibitor of PI3Kdelta which is now being tested in phase II for the treatment of head and neck squamous cell carcinoma and in phase I for lymphoid malignancy.

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
PI3-kinase p110-delta subunit 43 Target ID: CHEMBL3130 Sources: https://www.ncbi.nlm.nih.gov/pubmed/25469863	Inhibitor 8297		16.0 nM [IC50]

Conditions

Condition	Modality	Highest Phase	Product
B-cell chronic lymphocytic leukemia 2 Sources: http://www.amgentrials.com/amgen/trialsummary.aspx?studyid=20101262	Primary	Phase I 428	Unknown Approved Use Unknown
Non-Hodgkin's lymphoma 79 Sources: http://www.amgentrials.com/amgen/trialsummary.aspx?studyid=20101262	Primary	Phase I 428	Unknown Approved Use Unknown
Head and neck squamous cell carcinoma 32 Sources: https://clinicaltrials.gov/ct2/show/NCT02540928	Primary	Phase II 1132	Unknown Approved Use Unknown

T_1/2

Value	Dose	Co-administered	Analyte	Population
6.6 h EXPERIMENT https://doi.org/10.1182/blood.V122.21.678.678	400 mg 1 times / day multiple, oral dose: 400 mg route of administration: Oral experiment type: MULTIPLE co-administered:		AMG-319 blood	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

Sourcing

Vendor/Aggregator	ID	URL
1PlusChem LLC	1P00AC3L	https://www.1pchem.com/search?query=1P00AC3L
AChemBlock	H-8702	http://www.achemblock.com/catalogsearch/result/?q=H-8702
Angene	AGN-PC-0WCTJ5	http://www.angenechemical.com/productshow/AGN-PC-0WCTJ5.html
ApexBio Technology	B6013	https://www.apexbt.com/catalogsearch/result/?q=B6013
AstaTech	42355	http://astatechinc.com/CPSResult.php?CRNO=42355
BLD Pharm	BD304678	http://www.bldpharm.com/search/Search.html?keyword=BD304678
BOC Sciences	1608125-21-8	http://www.bocsci.com/description.asp?cas=1608125-21-8
Cayman Chemical	17383	http://www.caymanchem.com/app/template/Product.vm/catalog/17383
Chem Scene	CS-5266	http://www.chemscene.com/goproductList/searchProductList?productObj=CS-5266
ChemShuttle	131671	https://www.chemshuttle.com/catalogsearch/result/?q=131671
Combi-Blocks	QV-9111	http://www.combi-blocks.com/cgi-bin/find.cgi?QV-9111
Excenen	EX-A1028	http://www.excenen.com/searchresultlist.php?id=EX-A1028
KeyOrganics	AS-35220	http://www.keyorganicsinc.com/bionet/catalogsearch/result?q=AS-35220
Lab Network	LN01343955	https://labnetwork.com/frontend-app/p/#!/moleculedetails/LN01343955
Lab Seeker	SC-99783	http://www.labseeker.com/search.php?keywords=SC-99783&category=0
Matrix Scientific	152563	http://www.matrixscientific.com/152563.html
MedChem Express	HY-12948	https://www.medchemexpress.com/search.html?q=HY-12948&ft=&fa=&fp=
MolPort	MolPort-039-137-742	https://www.molport.com/shop/molecule-link/MolPort-039-137-742
MolPort	MolPort-044-561-429	https://www.molport.com/shop/molecule-link/MolPort-044-561-429
Molnova	M12313	https://www.molnova.com/en/serch-list.html?keywords=M12313
MuseChem	I002045	https://www.musechem.com/product/I002045.html
Selleck Chemicals	S7813	http://www.selleckchem.com/search.html?searchDTO.searchParam=S7813
eMolecules	275109663	https://orderbb.emolecules.com/search/#?query=275109663
eMolecules	302072869	https://orderbb.emolecules.com/search/#?query=302072869
eMolecules	53926130	https://orderbb.emolecules.com/search/#?query=53926130
eMolecules	62258245	https://orderbb.emolecules.com/search/#?query=62258245
mcule	MCULE-4632993719	https://mcule.com/MCULE-4632993719/
mcule	MCULE-7252955431	https://mcule.com/MCULE-7252955431/

PubMed

Title	Date	PubMed

Patents

Sample Use Guides

In Vivo Use Guide

25, 50, 100, 200, 300 and 400 mg of AMG-319 were administered by mouth once daily.

Route of Administration: Oral

In Vitro Use Guide

Unknown

Name

Type

Language

AMG-319

Common Name

English

N-((1S)-1-(7-FLUORO-2-(2-PYRIDYL)QUINOLINE-3-YL)ETHYL)-9H-PURINE-6-AMINE

Systematic Name

English

3-QUINOLINEMETHANAMINE, 7-FLUORO-.ALPHA.-METHYL-N-9H-PURIN-6-YL-2-(2-PYRIDINYL)-, (.ALPHA.S)-

Systematic Name

English

J3.391.906I

Code

English

AMG319

Code

English

Code System Code Type Description

EPA CompTox

DTXSID501046373