BMS-777607

Investigational

Details

Stereochemistry	ACHIRAL
Molecular Formula	C25H19ClF2N4O4
Molecular Weight	512.893
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CCOC1=C(C(=O)NC2=CC=C(OC3=C(Cl)C(N)=NC=C3)C(F)=C2)C(=O)N(C=C1)C4=CC=C(F)C=C4

InChI

InChIKey=VNBRGSXVFBYQNN-UHFFFAOYSA-N

InChI=1S/C25H19ClF2N4O4/c1-2-35-19-10-12-32(16-6-3-14(27)4-7-16)25(34)21(19)24(33)31-15-5-8-18(17(28)13-15)36-20-9-11-30-23(29)22(20)26/h3-13H,2H2,1H3,(H2,29,30)(H,31,33)

HIDE SMILES / InChI

Molecular Formula	C25H19ClF2N4O4
Molecular Weight	512.893
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Description
Sources: https://www.ncbi.nlm.nih.gov/pubmed/25304900
Curator's Comment: description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/20515943 | https://www.ncbi.nlm.nih.gov/pubmed/26848524 | https://www.ncbi.nlm.nih.gov/pubmed/19260711

BMS 777607 is a substituted 2-aminopyridine shown to inhibit the RON and cMet receptor tyrosine kinases, for the treatment of solid tumors. BMS 777607 demonstrated ligand stimulated and constitutive Met phosphorylation, and inhibition of tumor cell proliferation, in preclinical studies. Preclinical data indicated that BMS 777607 inhibited RON, blocking the conversion of micrometastases to overt metastases by boosting antitumor immunity. Bristol-Myers Squibb conducted a phase I/II trial of BMS 777607 for the treatment of advanced solid tumors in Australia. As at December 2016, no recent reports of development had been identified for preclinical development in Cancer in the USA.

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Hepatocyte growth factor receptor 54 Target ID: CHEMBL3717 Sources: https://www.ncbi.nlm.nih.gov/pubmed/19260711	Inhibitor 8297		3.9 nM [IC50]
Macrophage-stimulating protein receptor 4 Target ID: CHEMBL2689 Sources: https://www.ncbi.nlm.nih.gov/pubmed/19260711	Inhibitor 8297		1.8 nM [IC50]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Advanced solid cancer 28 Sources: https://clinicaltrials.gov/ct2/show/NCT00605618	Primary		Phase II 1132	Unknown Approved Use Unknown

C_max

Value	Dose	Co-administered	Analyte	Population
17.6 μM EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/19260711	10 mg/kg single, oral dose: 10 mg/kg route of administration: Oral experiment type: SINGLE co-administered:		BMS-777607 plasma	Mus musculus population: UNKNOWN age: ADULT sex: UNKNOWN food status: UNKNOWN

AUC

Value	Dose	Co-administered	Analyte	Population
90 μM × h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/19260711	10 mg/kg single, oral dose: 10 mg/kg route of administration: Oral experiment type: SINGLE co-administered:		BMS-777607 plasma	Mus musculus population: UNKNOWN age: ADULT sex: UNKNOWN food status: UNKNOWN

T_1/2

Value	Dose	Co-administered	Analyte	Population
4.5 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/19260711	5 mg/kg single, intravenous dose: 5 mg/kg route of administration: Intravenous experiment type: SINGLE co-administered:		BMS-777607 plasma	Mus musculus population: UNKNOWN age: ADULT sex: UNKNOWN food status: UNKNOWN

Sourcing

Vendor/Aggregator	ID	URL
001 Chemical	DY34086	https://www.001chemical.com/chem/search?q=DY34086
1PlusChem LLC	1P00088T	https://www.1pchem.com/search?query=1P00088T
AChemBlock	10298	http://www.achemblock.com/catalogsearch/result/?q=10298
AK Scientific	SYN5733	https://aksci.com/item_detail.php?cat=SYN5733
AK Scientific	X7495	https://aksci.com/item_detail.php?cat=X7495
AOBIOUS INC	AOB87395	http://aobious.com/aobious/search?search_query=AOB87395
Angene	AGN-PC-0WH9LW	http://www.angenechemical.com/productshow/AGN-PC-0WH9LW.html
ApexBio Technology	A5703	https://www.apexbt.com/catalogsearch/result/?q=A5703
AstaTech	42553	http://astatechinc.com/CPSResult.php?CRNO=42553
BLD Pharm	BD239485	http://www.bldpharm.com/search/Search.html?keyword=BD239485
BOC Sciences	1025720-94-8	http://www.bocsci.com/description.asp?cas=1025720-94-8
Capot Chemical	22433	https://www.capotchem.com/search.do?q=22433
Cayman Chemical	18517	http://www.caymanchem.com/app/template/Product.vm/catalog/18517
Chem Scene	CS-0227	http://www.chemscene.com/goproductList/searchProductList?productObj=CS-0227
ChemShuttle	109739	https://www.chemshuttle.com/catalogsearch/result/?q=109739
ChemShuttle	185593	https://www.chemshuttle.com/catalogsearch/result/?q=185593
Debye Scientific	DA-35016	https://www.debyesci.com/index.php?id=product&ext[cno]=DA-35016
Excenen	EX-A004	http://www.excenen.com/searchresultlist.php?id=EX-A004
Hairui	HR145166	http://www.hairuichem.com/en/product/search.do?q=HR145166
KeyOrganics	AS-17034	http://www.keyorganicsinc.com/bionet/catalogsearch/result?q=AS-17034
Matrix Scientific	146655	http://www.matrixscientific.com/146655.html
MedChem Express	HY-12076	https://www.medchemexpress.com/search.html?q=HY-12076&ft=&fa=&fp=
MolPort	MolPort-016-633-238	https://www.molport.com/shop/molecule-link/MolPort-016-633-238
Molcore	MC34086	http://www.molcore.com/CatMC34086.html
Molnova	M10120	https://www.molnova.com/en/serch-list.html?keywords=M10120
MuseChem	I000168	https://www.musechem.com/product/I000168.html
ShangHai Biochempartner	BCP000298	http://www.biochempartner.com/search_BCP000298
ShangHai Biochempartner	BCP02303	http://www.biochempartner.com/search_BCP02303
TargetMol	T2699	https://www.targetmol.com/search?keyword=T2699
Toronto Research Chemicals	A603310	https://www.trc-canada.com/product-detail/?CatNum=A603310
Toronto Research Chemicals	O575300	https://www.trc-canada.com/product-detail/?CatNum=O575300
eMolecules	32278072	https://orderbb.emolecules.com/search/#?query=32278072
eMolecules	85163690	https://orderbb.emolecules.com/search/#?query=85163690
eNovation Chemicals	D372423	https://www.enovationchem.com/Products.asp?SEARCHTEXT=D372423&searchbtn.x=0&searchbtn.y=0
mcule	MCULE-1077157668	https://mcule.com/MCULE-1077157668/
mcule	MCULE-4005570946	https://mcule.com/MCULE-4005570946/

PubMed

Title	Date	PubMed
Discovery of N-(4-(2-amino-3-chloropyridin-4-yloxy)-3-fluorophenyl)-4-ethoxy-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamide (BMS-777607), a selective and orally efficacious inhibitor of the Met kinase superfamily.	2009 Mar 12	19260711
BMS-777607, a small-molecule met kinase inhibitor, suppresses hepatocyte growth factor-stimulated prostate cancer metastatic phenotype in vitro.	2010 Jun	20515943

Patents

Sample Use Guides

In Vivo Use Guide

U118MG and SF126 cells were implanted stereotactically into the brains of CD1NuNu mice. In the more aggressive tumor SF126 model, treatment was started at day 3 after implantation while treatment in the U118MG model was started on day 7 after implantation. In both models, BMS-777607 treatment (30 or 100 mg/kg, i.p. 2x/day) resulted in a significant decrease of intracranial tumor growth on day 14 after implantation.

Route of Administration: Intraperitoneal

In Vitro Use Guide

Human high-grade glioma cells U118MG and SF126 glioma cells were treated with BMS-777607 at different concentrations (1.56 mkM–50 mkM). Culture medium was replaced or exchanged after 24, 48 and 72 hours. The exposure of U118MG and SF126 glioma cells with 12.5 μM BMS-777607 resulted in significantly reduced cell numbers in MTT assay after 24 hours of treatment.

Substance Class	Chemical Created by `admin` on `Sat Dec 16 04:40:30 UTC 2023` Edited by `admin` on `Sat Dec 16 04:40:30 UTC 2023`
Record UNII	A3MMS6HDO1
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

BMS-777607

Code

English

ASLAN-002

Code

English

3-PYRIDINECARBOXAMIDE, N-(4-((2-AMINO-3-CHLORO-4-PYRIDINYL)OXY)-3-FLUOROPHENYL)-4-ETHOXY-1-(4-FLUOROPHENYL)-1,2-DIHYDRO-2-OXO-

Systematic Name

English

ASLAN002

Code

English

N-(4-((2-AMINO-3-CHLOROPYRIDIN-4-YL)OXY)-3-FLUOROPHENYL)-4-ETHOXY-1-(4-FLUOROPHENYL)-2-OXO-1,2-DIHYDROPYRIDINE-3-CARBOXAMIDE

Systematic Name

English

Code System Code Type Description

CAS

1025720-94-8