Discovery of a 2,4-disubstituted pyrrolo[1,2-f][1,2,4]triazine inhibitor (BMS-754807) of insulin-like growth factor receptor (IGF-1R) kinase in clinical development.
This report describes the biological activity, characterization, and SAR leading to 9d (BMS-754807) a small molecule IGF-1R kinase inhibitor in clinical development.
Bristol-Myers Squibb Co, Wallingford, Connecticut 06492, USA.
Mark D
MD
Wittman
Joan M
JM
Carboni
Zheng
Z
Yang
Francis Y
FY
Lee
Melissa
M
Antman
Ricardo
R
Attar
Praveen
P
Balimane
Chiehying
C
Chang
Cliff
C
Chen
Lorell
L
Discenza
David
D
Frennesson
Marco M
MM
Gottardis
Ann
A
Greer
Warren
W
Hurlburt
Walter
W
Johnson
David R
DR
Langley
Aixin
A
Li
Jianqing
J
Li
Peiying
P
Liu
Harold
H
Mastalerz
Arvind
A
Mathur
Krista
K
Menard
Karishma
K
Patel
John
J
Sack
Xiaopeng
X
Sang
Mark
M
Saulnier
Daniel
D
Smith
Kevin
K
Stefanski
George
G
Trainor
Upender
U
Velaparthi
Guifen
G
Zhang
Kurt
K
Zimmermann
Dolatrai M
DM
Vyas
D000818:Animals; D035843:Biomedical Research; D004285:Dogs; D055808:Drug Discovery; D006801:Humans; D051379:Mice; D008958:Models, Molecular; D008968:Molecular Conformation; D047428:Protein Kinase Inhibitors / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology* / Q000627:therapeutic use; D011720:Pyrazoles / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology* / Q000627:therapeutic use; D051381:Rats; D017526:Receptor, IGF Type 1 / Q000037:antagonists & inhibitors* / Q000737:chemistry; D013329:Structure-Activity Relationship; D014227:Triazines / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology* / Q000627:therapeutic use
C545990:BMS 754807; D047428:Protein Kinase Inhibitors; D011720:Pyrazoles; D014227:Triazines; D017526:Receptor, IGF Type 1