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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 of BMS-777607

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
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.

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
3.9 nM [IC50]
1.8 nM [IC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Unknown

Approved Use

Unknown
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
17.6 μM
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
29 μM
10 mg/kg single, oral
dose: 10 mg/kg
route of administration: Oral
experiment type: SINGLE
co-administered:
BMS-777607 blood
Canis lupus
population: UNKNOWN
age: ADULT
sex: MALE
food status: FASTED
8.7 μM
10 mg/kg single, oral
dose: 10 mg/kg
route of administration: Oral
experiment type: SINGLE
co-administered:
BMS-777607 blood
Rattus norvegicus
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
17.6 μM
10 mg/kg single, oral
dose: 10 mg/kg
route of administration: Oral
experiment type: SINGLE
co-administered:
BMS-777607 blood
Mus musculus
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
90 μM × h
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
198 μM × h
10 mg/kg single, oral
dose: 10 mg/kg
route of administration: Oral
experiment type: SINGLE
co-administered:
BMS-777607 blood
Canis lupus
population: UNKNOWN
age: ADULT
sex: MALE
food status: FASTED
37.7 μM × h
10 mg/kg single, oral
dose: 10 mg/kg
route of administration: Oral
experiment type: SINGLE
co-administered:
BMS-777607 blood
Rattus norvegicus
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
90 μM × h
10 mg/kg single, oral
dose: 10 mg/kg
route of administration: Oral
experiment type: SINGLE
co-administered:
BMS-777607 blood
Mus musculus
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
4.5 h
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

Sourcing

Vendor/AggregatorIDURL
PubMed

PubMed

TitleDatePubMed
BMS-777607, a small-molecule met kinase inhibitor, suppresses hepatocyte growth factor-stimulated prostate cancer metastatic phenotype in vitro.
2010-06
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.
2009-03-12
Patents

Sample Use Guides

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
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 Mon Mar 31 21:23:03 GMT 2025
Edited
by admin
on Mon Mar 31 21:23:03 GMT 2025
Record UNII
A3MMS6HDO1
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
BMS-777607
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-
Preferred Name English
ASLAN-002
Code 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
Created by admin on Mon Mar 31 21:23:03 GMT 2025 , Edited by admin on Mon Mar 31 21:23:03 GMT 2025
PRIMARY
FDA UNII
A3MMS6HDO1
Created by admin on Mon Mar 31 21:23:03 GMT 2025 , Edited by admin on Mon Mar 31 21:23:03 GMT 2025
PRIMARY
DRUG BANK
DB12064
Created by admin on Mon Mar 31 21:23:03 GMT 2025 , Edited by admin on Mon Mar 31 21:23:03 GMT 2025
PRIMARY
EPA CompTox
DTXSID50145278
Created by admin on Mon Mar 31 21:23:03 GMT 2025 , Edited by admin on Mon Mar 31 21:23:03 GMT 2025
PRIMARY
NCI_THESAURUS
C74060
Created by admin on Mon Mar 31 21:23:03 GMT 2025 , Edited by admin on Mon Mar 31 21:23:03 GMT 2025
PRIMARY
ChEMBL
CHEMBL460702
Created by admin on Mon Mar 31 21:23:03 GMT 2025 , Edited by admin on Mon Mar 31 21:23:03 GMT 2025
PRIMARY
PUBCHEM
24794418
Created by admin on Mon Mar 31 21:23:03 GMT 2025 , Edited by admin on Mon Mar 31 21:23:03 GMT 2025
PRIMARY
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