The Discovery of OSI-906, a Small-molecule Inhibitor of the Insulin-like Growth Factor-1 and Insulin Receptors - Accounts in Drug Discovery Case Studies in Medicinal Chemistry - page 92

Table 4.12 Kinases which were not inhibited by greater than 50% by OSI-906
at a concentration of 1 mM when profiled using the ProfilerPro t
Kinase Selectivity Assay Kit (Caliper Life Sciences).

ABL c-TAK1 MAPKAPK3 PKC-e

AKT1 DCAMKL2 MARK1 PKC-Z

AKT2 DYRK1a MARK2 PKC-g

AKT3 EGFR MET PKC-y

AMPK Erk1 MSK1 PKC-z

Arg Erk2 MSK2 PKD1

AurA Fer MST2 PKD2

AurC FGFR1 NEK2 PKD3

BMX FGFR2 p38a PKG1-b

BRSK1 FGFR3 p38-b2 PKGa

BRSK2 FGFR4 p38-d PRAK

BTK FLT3 p38-g ROCK2

CAMK2 Flt3(D835Y) p70S6K RSK1

CAMK4 FYN PAK2 RSK2

CaMKII-b GSK3-b PDGFR-a RSK3

CaMKII-g Hck PIM1 SGK1

CDK2 HGK PIM2 SGK2

CHK1 IKK-b PKA SGK3

CHK2 IRAK4 PKC-a SRC

CK1d KDR PKCb2 SYK

c-Raf LCK PKC-b1 TSSK1

CSNK1A1 MAPKAPK2 PKC-d TSSK2

Table 4.13 Selectivity profile of OSI-906 against a panel of kinases (IC 50
values).

Kinase IC 50 (mM) Kinase IC 50 (mM) Kinase IC 50 (mM)

IGF-IR 0.035 IRAK4 410 RON 410

IR 0.075 JAK2 410 ROS1 410

IRR 0.075 KDR 410 SRC 410

Abl 410 Lck 410 TEK 410

ALK 410 LYN A 410 MEK1 410

BTK 410 LYN B 410 PAK3 410

EGFR 410 MET 410 TAOK2 410

EPHA1 410 TRKA 410 AKT1 410

EPHB1 410 PDGFR-a/-b410 AKT2 410

FES 410 FAK 410 Aurora A 410

FGFR-1/-2 410 BRK 410 Aurora B 410

FYN 410 RET 410 PDK1 410

PKA 410 PIM1 410 PLK1 410

PKC-a 10 CDK1 410 P38a 410

ROCK1 410 DYRK3 410 ERK1 410

p70S6K 410 GSK3a 410 CAMK1D 410