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Details

Stereochemistry ACHIRAL
Molecular Formula C19H13F2N7
Molecular Weight 377.3502
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of JNJ-38877605

SMILES

CN1C=C(C=N1)C2=NN3C(C=C2)=NN=C3C(F)(F)C4=CC5=CC=CN=C5C=C4

InChI

InChIKey=JRWCBEOAFGHNNU-UHFFFAOYSA-N
InChI=1S/C19H13F2N7/c1-27-11-13(10-23-27)16-6-7-17-24-25-18(28(17)26-16)19(20,21)14-4-5-15-12(9-14)3-2-8-22-15/h2-11H,1H3

HIDE SMILES / InChI
Molecular Formula C19H13F2N7
Molecular Weight 377.3502
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: DOI:10.1158/1538-7445.AM10-3628 | https://www.ncbi.nlm.nih.gov/pubmed/25745036

JNJ-38877605 is an orally available, small molecule inhibitor of the proto-oncogene c-Met (hepatocyte growth factor receptor [HGFR]) with potential antineoplastic activity. c-Met inhibitor JNJ-38877605 selectively binds to c-Met, thereby inhibiting c-Met phosphorylation and disrupting c-Met signal transduction pathways. JNJ-38877605 was in Phase I clinical trials. Combined clinical and correlative preclinical studies suggest that renal toxicity of JNJ-38877605 is caused by the formation of species-specific insoluble metabolites. These observations preclude further clinical development of JNJ-38877605.

CNS Activity

Originator

Approval Year

Unknown
149124
Targets

Targets

Primary TargetPharmacologyConditionPotency
Hepatocyte growth factor receptor
56
Target ID: CHEMBL3717
Sources: DOI:10.1158/1538-7445.AM10-3628
Inhibitor
8504
 4.0 nM [IC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Phase I
438
Unknown

Approved Use

Unknown
Primary
Preclinical
Unknown

Approved Use

Unknown
Primary
Preclinical
Unknown

Approved Use

Unknown
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
416 ng/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/25745036
60 mg single, oral
dose: 60 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
JNJ-38877605 plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
177 ng/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/25745036
20 mg 1 times / day multiple, oral
dose: 20 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
JNJ-38877605 plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
416 ng/mL
EXPERIMENT
https://www.ncbi.nlm.nih.gov/pubmed/25745036
60 mg 1 times / day multiple, oral
dose: 60 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
JNJ-38877605 blood
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
937 ng × h/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/25745036
60 mg single, oral
dose: 60 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
JNJ-38877605 plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
523 ng × h/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/25745036
20 mg 1 times / day multiple, oral
dose: 20 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
JNJ-38877605 plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
937 ng × h/mL
EXPERIMENT
https://www.ncbi.nlm.nih.gov/pubmed/25745036
60 mg 1 times / day multiple, oral
dose: 60 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
JNJ-38877605 blood
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
1.6 h
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/25745036
60 mg single, oral
dose: 60 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
JNJ-38877605 plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
1.6 h
EXPERIMENT
https://www.ncbi.nlm.nih.gov/pubmed/25745036
60 mg 1 times / day multiple, oral
dose: 60 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
JNJ-38877605 blood
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
Overview

Overview

CYP3A4CYP2C9CYP2D6hERG
inhibitor
2252

substrate
1946
inhibitor
2438
inhibitor
2507

OverviewOther

Other InhibitorOther SubstrateOther Inducer
P-gp
1741
Drug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
CYP2D6
2546
 inconclusive [IC50 16.933 uM]
CYP3A4
2633
 inconclusive [IC50 21.3174 uM]
P-gp
1932
 inconclusive [IC50 8.1995 uM]
CYP2C9
2497
 yes [IC50 3.0112 uM]
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
CYP3A4
1946
 yes
Sourcing

Sourcing

Vendor/AggregatorIDURL
001 Chemical
DY107053
https://www.001chemical.com/chem/search?q=DY107053
1PlusChem LLC
1P01DOA9
https://www.1pchem.com/search?query=1P01DOA9
AK Scientific
SYN1047
https://aksci.com/item_detail.php?cat=SYN1047
AK Scientific
X7476
https://aksci.com/item_detail.php?cat=X7476
AOBIOUS INC
AOB87321
http://aobious.com/aobious/search?search_query=AOB87321
ApexBio Technology
A5092
https://www.apexbt.com/catalogsearch/result/?q=A5092
AstaTech
C77250
http://astatechinc.com/CPSResult.php?CRNO=C77250
BLD Pharm
BD225171
http://www.bldpharm.com/search/Search.html?keyword=BD225171
BOC Sciences
943540-75-8
http://www.bocsci.com/description.asp?cas=943540-75-8
Capot Chemical
22454
https://www.capotchem.com/search.do?q=22454
Chem Scene
CS-0031
http://www.chemscene.com/goproductList/searchProductList?productObj=CS-0031
ChemShuttle
112407
https://www.chemshuttle.com/catalogsearch/result/?q=112407
Debye Scientific
DB-000659
https://www.debyesci.com/index.php?id=product&ext[cno]=DB-000659
eMolecules
31507610
https://orderbb.emolecules.com/search/#?query=31507610
eNovation Chemicals
D395274
https://www.enovationchem.com/Products.asp?SEARCHTEXT=D395274&searchbtn.x=0&searchbtn.y=0
Excenen
EX-A2081
http://www.excenen.com/searchresultlist.php?id=EX-A2081
Hairui
HR118316
http://www.hairuichem.com/en/product/search.do?q=HR118316
KeyOrganics
AS-16207
http://www.keyorganicsinc.com/bionet/catalogsearch/result?q=AS-16207
Lab Network
LN01331014
https://labnetwork.com/frontend-app/p/#!/moleculedetails/LN01331014
Lab Seeker
SC-48063
http://www.labseeker.com/search.php?keywords=SC-48063&category=0
LabSeeker
SC-48063
http://www.labseeker.com/search.php?keywords=SC-48063&category=0
Matrix Scientific
132610
http://www.matrixscientific.com/132610.html
mcule
MCULE-8471857466
https://mcule.com/MCULE-8471857466/
MedChem Express
HY-50683
https://www.medchemexpress.com/search.html?q=HY-50683&ft=&fa=&fp=
Molcore
MC107053
http://www.molcore.com/CatMC107053.html
MolPort
MolPort-009-679-418
https://www.molport.com/shop/molecule-link/MolPort-009-679-418
ShangHai Biochempartner
BCP01812
http://www.biochempartner.com/search_BCP01812
TargetMol
T6095
https://www.targetmol.com/search?keyword=T6095
Toronto Research Chemicals
J212505
https://www.trc-canada.com/product-detail/?CatNum=J212505
PubMed

PubMed

TitleDatePubMed
The c-Met Tyrosine Kinase Inhibitor JNJ-38877605 Causes Renal Toxicity through Species-Specific Insoluble Metabolite Formation.
2015-05-15
Effectiveness of inhibitor rapamycin, saracatinib, linsitinib and JNJ-38877605 against human prostate cancer cells.
2015
MET inhibitors in combination with other therapies in non-small cell lung cancer.
2012-12
Patents

Patents

08030305
1
08173654
1
08629144
28
20070203136
1
20090098181
1
20100197912
2

Sample Use Guides

In Vivo Use Guide
60 mg once daily (21-day treatment cycle)
Route of Administration: Oral
In Vitro Use Guide
In EBC1, GTL16, NCI-H1993, and MKN45 cells, JNJ-38877605 (500 nM) leads to a significant reduction of phosphorylation of Met.
Substance Class Chemical
Created
by admin
on Mon Mar 31 22:29:47 GMT 2025
Edited
by admin
on Mon Mar 31 22:29:47 GMT 2025
Record UNII
15UDG410PN
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
JNJ-38877605
Common Name English
JNJ-38877605-AAA
Preferred Name English
QUINOLINE, 6-(DIFLUORO(6-(1-METHYL-1H-PYRAZOL-4-YL)-1,2,4-TRIAZOLO(4,3-B)PYRIDAZIN-3-YL)METHYL)-
Systematic Name English
Code System Code Type Description
EPA CompTox
DTXSID20677253
Created by admin on Mon Mar 31 22:29:47 GMT 2025 , Edited by admin on Mon Mar 31 22:29:47 GMT 2025
PRIMARY
SMS_ID
300000045591
Created by admin on Mon Mar 31 22:29:47 GMT 2025 , Edited by admin on Mon Mar 31 22:29:47 GMT 2025
PRIMARY
PUBCHEM
46911863
Created by admin on Mon Mar 31 22:29:47 GMT 2025 , Edited by admin on Mon Mar 31 22:29:47 GMT 2025
PRIMARY
DRUG BANK
DB13113
Created by admin on Mon Mar 31 22:29:47 GMT 2025 , Edited by admin on Mon Mar 31 22:29:47 GMT 2025
PRIMARY
ChEMBL
CHEMBL2133806
Created by admin on Mon Mar 31 22:29:47 GMT 2025 , Edited by admin on Mon Mar 31 22:29:47 GMT 2025
PRIMARY
NCI_THESAURUS
C77893
Created by admin on Mon Mar 31 22:29:47 GMT 2025 , Edited by admin on Mon Mar 31 22:29:47 GMT 2025
PRIMARY
FDA UNII
15UDG410PN
Created by admin on Mon Mar 31 22:29:47 GMT 2025 , Edited by admin on Mon Mar 31 22:29:47 GMT 2025
PRIMARY
CAS
943540-75-8
Created by admin on Mon Mar 31 22:29:47 GMT 2025 , Edited by admin on Mon Mar 31 22:29:47 GMT 2025
PRIMARY
CAS
1072116-03-0
Created by admin on Mon Mar 31 22:29:47 GMT 2025 , Edited by admin on Mon Mar 31 22:29:47 GMT 2025
SUPERSEDED
Related Record Type Details
ALDEHYDE OXIDASE
METABOLIC ENZYME -> SUBSTRATE
HEPATOCYTE GROWTH FACTOR RECEPTOR
TARGET -> INHIBITOR
IC50
Related Record Type Details
Structure of JNJ-38877605 M2.2 Metabolite
METABOLITE TOXIC -> PARENT
May be responsible for renal toxicity
Structure of JNJ-38877605 metabolite 3.2
METABOLITE TOXIC -> PARENT
Structure of JNJ-38877605 N-oxide
METABOLITE -> PARENT
Related Record Type Details
Structure of JNJ-38877605
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