Linsitinib (OSI-906)

Linsitinib (OSI-906) is a selective inhibitor of IGF-1R with IC50 of 35 nM in cell-free assays; modestly potent to InsR with IC50 of 75 nM, and no activity towards Abl, ALK, BTK, EGFR, FGFR1/2, PKA etc. Phase 3.

Linsitinib (OSI-906) Chemical Structure

Linsitinib (OSI-906) Chemical Structure

CAS: 867160-71-2

Selleck's Linsitinib (OSI-906) has been cited by 185 publications

Purity & Quality Control

Batch: Purity: 99.99%
99.99

Products often used together with Linsitinib (OSI-906)

Osimertinib (AZD9291)


Linsitinib and Osimertinib combination use inhibits the viability of AXL-low expressing EGFR mutated NSCLC cell lines, including HCC4006/HCC827/H3255 cells.

Wang R, et al. Nat Commun. 2020 Sep 14;11(1):4607.

Gefitinib


Gefitinib inhibits HIF-1α and VEGF expression in HCC827 cells, and linsitinib inhibits VEGF production in H1975 cells.

Yeo CD, et al. Exp Lung Res. 2017 Feb;43(1):29-37.

Lapatinib


Linsitinib and Lapatinib combination use markedly inhibit the growth of xenografts in the KYSE450 xenograft model in nude mice.

Kang J, et al. Int J Mol Sci. 2022 Sep 8;23(18):10382.

Afatinib


Linsitinib and Afatinib combination treatment shows more than additive effects on tumor growth in H1975 xenograft.

Lee Y, et al. Mol Carcinog. 2016 May;55(5):991-1001.

Aspirin


Linsitinib and Aspirin inhibit stem-cell-like colon cancer cells growth, decrease expression of CD133, CD44, and CD24, and also increase CDX2 and PTEN gene expression.

Guo Y, et al. Saudi J Biol Sci. 2022 Feb;29(2):872-877.

Linsitinib (OSI-906) Related Products

Signaling Pathway

Choose Selective IGF-1R Inhibitors

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
A4-Fuk Growth Inhibition Assay IC50=0.02806 μM SANGER
KS-1 Growth Inhibition Assay IC50=0.03835 μM SANGER
TE-11 Growth Inhibition Assay IC50=0.07822 μM SANGER
EW-1 Growth Inhibition Assay IC50=0.08585 μM SANGER
HMV-II Growth Inhibition Assay IC50=0.08846 μM SANGER
COLO-205 Growth Inhibition Assay IC50=0.10454 μM SANGER
ES1 Growth Inhibition Assay IC50=0.10696 μM SANGER
GDM-1 Growth Inhibition Assay IC50=0.13672 μM SANGER
ML-2 Growth Inhibition Assay IC50=0.15896 μM SANGER
Saos-2 Growth Inhibition Assay IC50=0.16526 μM SANGER
NCI-H1355 Growth Inhibition Assay IC50=0.18135 μM SANGER
G-401 Growth Inhibition Assay IC50=0.1823 μM SANGER
EW-16 Growth Inhibition Assay IC50=0.18777 μM SANGER
EW-7 Growth Inhibition Assay IC50=0.18881 μM SANGER
NCI-H727 Growth Inhibition Assay IC50=0.19794 μM SANGER
LCLC-97TM1 Growth Inhibition Assay IC50=0.20955 μM SANGER
NCI-H650 Growth Inhibition Assay IC50=0.21384 μM SANGER
NCI-H2122 Growth Inhibition Assay IC50=0.23299 μM SANGER
SK-N-DZ Growth Inhibition Assay IC50=0.23698 μM SANGER
HT-29 Growth Inhibition Assay IC50=0.24248 μM SANGER
LB771-HNC Growth Inhibition Assay IC50=0.25915 μM SANGER
HT-144 Growth Inhibition Assay IC50=0.26191 μM SANGER
LAN-6 Growth Inhibition Assay IC50=0.26348 μM SANGER
EW-18 Growth Inhibition Assay IC50=0.27001 μM SANGER
LS-1034 Growth Inhibition Assay IC50=0.27132 μM SANGER
EW-11 Growth Inhibition Assay IC50=0.28432 μM SANGER
SNU-C1 Growth Inhibition Assay IC50=0.29313 μM SANGER
RS4-11 Growth Inhibition Assay IC50=0.33758 μM SANGER
ES4 Growth Inhibition Assay IC50=0.41038 μM SANGER
COLO-320-HSR Growth Inhibition Assay IC50=0.41368 μM SANGER
NB10 Growth Inhibition Assay IC50=0.45437 μM SANGER
BFTC-905 Growth Inhibition Assay IC50=0.46758 μM SANGER
A375 Growth Inhibition Assay IC50=0.47617 μM SANGER
SJRH30 Growth Inhibition Assay IC50=0.50822 μM SANGER
NOS-1 Growth Inhibition Assay IC50=0.52267 μM SANGER
SIG-M5 Growth Inhibition Assay IC50=0.53557 μM SANGER
DOK Growth Inhibition Assay IC50=0.556 μM SANGER
NB69 Growth Inhibition Assay IC50=0.58257 μM SANGER
SK-NEP-1 Growth Inhibition Assay IC50=0.60236 μM SANGER
SK-MM-2 Growth Inhibition Assay IC50=0.65491 μM SANGER
NCI-H358 Growth Inhibition Assay IC50=0.67082 μM SANGER
RH-1 Growth Inhibition Assay IC50=0.74859 μM SANGER
NH-12 Growth Inhibition Assay IC50=0.76046 μM SANGER
TE-12 Growth Inhibition Assay IC50=0.76486 μM SANGER
COLO-668 Growth Inhibition Assay IC50=0.84666 μM SANGER
PANC-08-13 Growth Inhibition Assay IC50=0.86377 μM SANGER
HCC2998 Growth Inhibition Assay IC50=0.88263 μM SANGER
ABC-1 Growth Inhibition Assay IC50=0.90352 μM SANGER
ES6 Growth Inhibition Assay IC50=0.91066 μM SANGER
SNU-387 Growth Inhibition Assay IC50=0.99393 μM SANGER
CMK Growth Inhibition Assay IC50=0.99929 μM SANGER
SJSA-1 Growth Inhibition Assay IC50=1.03653 μM SANGER
SIMA Growth Inhibition Assay IC50=1.06825 μM SANGER
ES3 Growth Inhibition Assay IC50=1.12297 μM SANGER
IGROV-1 Growth Inhibition Assay IC50=1.15444 μM SANGER
MEL-JUSO Growth Inhibition Assay IC50=1.15759 μM SANGER
T84 Growth Inhibition Assay IC50=1.20914 μM SANGER
CAL-85-1 Growth Inhibition Assay IC50=1.23138 μM SANGER
RD Growth Inhibition Assay IC50=1.26455 μM SANGER
TE-8 Growth Inhibition Assay IC50=1.31462 μM SANGER
L-363 Growth Inhibition Assay IC50=1.34208 μM SANGER
EKVX Growth Inhibition Assay IC50=1.34568 μM SANGER
SK-MEL-3 Growth Inhibition Assay IC50=1.48556 μM SANGER
TGBC24TKB Growth Inhibition Assay IC50=1.50193 μM SANGER
NCI-H1770 Growth Inhibition Assay IC50=1.51113 μM SANGER
HuH-7 Growth Inhibition Assay IC50=1.60098 μM SANGER
HL-60 Growth Inhibition Assay IC50=1.66928 μM SANGER
TE-1 Growth Inhibition Assay IC50=1.70945 μM SANGER
LC-2-ad Growth Inhibition Assay IC50=1.73887 μM SANGER
LB647-SCLC Growth Inhibition Assay IC50=1.76583 μM SANGER
NCI-H2171 Growth Inhibition Assay IC50=1.77716 μM SANGER
SK-PN-DW Growth Inhibition Assay IC50=1.91298 μM SANGER
MC-IXC Growth Inhibition Assay IC50=1.9898 μM SANGER
LS-513 Growth Inhibition Assay IC50=2.05305 μM SANGER
EW-3 Growth Inhibition Assay IC50=2.09844 μM SANGER
OPM-2 Growth Inhibition Assay IC50=2.102 μM SANGER
LP-1 Growth Inhibition Assay IC50=2.25807 μM SANGER
LU-134-A Growth Inhibition Assay IC50=2.277 μM SANGER
CP66-MEL Growth Inhibition Assay IC50=2.29014 μM SANGER
HCC1143 Growth Inhibition Assay IC50=2.45368 μM SANGER
LOXIMVI Growth Inhibition Assay IC50=2.6021 μM SANGER
TE-10 Growth Inhibition Assay IC50=2.70838 μM SANGER
NCI-H1882 Growth Inhibition Assay IC50=2.75227 μM SANGER
CHP-126 Growth Inhibition Assay IC50=2.76317 μM SANGER
NCI-H1623 Growth Inhibition Assay IC50=2.92024 μM SANGER
GB-1 Growth Inhibition Assay IC50=2.93404 μM SANGER
RCC10RGB Growth Inhibition Assay IC50=2.95281 μM SANGER
NCI-H2141 Growth Inhibition Assay IC50=2.96896 μM SANGER
GI-ME-N Growth Inhibition Assay IC50=3.00565 μM SANGER
NCI-H526 Growth Inhibition Assay IC50=3.04085 μM SANGER
NCI-H747 Growth Inhibition Assay IC50=3.04992 μM SANGER
SNU-423 Growth Inhibition Assay IC50=3.20313 μM SANGER
A427 Growth Inhibition Assay IC50=3.25699 μM SANGER
CAL-12T Growth Inhibition Assay IC50=3.40713 μM SANGER
LU-99A Growth Inhibition Assay IC50=3.47105 μM SANGER
MS-1 Growth Inhibition Assay IC50=3.53429 μM SANGER
SK-LU-1 Growth Inhibition Assay IC50=3.76295 μM SANGER
SW837 Growth Inhibition Assay IC50=3.76333 μM SANGER
ES8 Growth Inhibition Assay IC50=3.83877 μM SANGER
MZ2-MEL Growth Inhibition Assay IC50=3.92086 μM SANGER
TGW Growth Inhibition Assay IC50=4.01311 μM SANGER
GP5d Growth Inhibition Assay IC50=4.05362 μM SANGER
BB49-HNC Growth Inhibition Assay IC50=4.15213 μM SANGER
NB13 Growth Inhibition Assay IC50=4.26887 μM SANGER
NTERA-S-cl-D1 Growth Inhibition Assay IC50=4.28615 μM SANGER
NCI-H1648 Growth Inhibition Assay IC50=4.29819 μM SANGER
LCLC-103H Growth Inhibition Assay IC50=4.32195 μM SANGER
LS-411N Growth Inhibition Assay IC50=4.44885 μM SANGER
NCI-H1092 Growth Inhibition Assay IC50=4.45687 μM SANGER
PANC-10-05 Growth Inhibition Assay IC50=4.6984 μM SANGER
DK-MG Growth Inhibition Assay IC50=4.80933 μM SANGER
OVCAR-5 Growth Inhibition Assay IC50=4.81226 μM SANGER
CAL-39 Growth Inhibition Assay IC50=4.8767 μM SANGER
TE-441-T Growth Inhibition Assay IC50=4.90537 μM SANGER
MOLT-16 Growth Inhibition Assay IC50=4.95253 μM SANGER
MCF7 Growth Inhibition Assay IC50=5.14517 μM SANGER
CAPAN-1 Growth Inhibition Assay IC50=5.25707 μM SANGER
PSN1 Growth Inhibition Assay IC50=5.27235 μM SANGER
NCI-H292 Growth Inhibition Assay IC50=5.30044 μM SANGER
CPC-N Growth Inhibition Assay IC50=5.39419 μM SANGER
DoTc2-4510 Growth Inhibition Assay IC50=5.45371 μM SANGER
LB1047-RCC Growth Inhibition Assay IC50=5.55933 μM SANGER
MHH-ES-1 Growth Inhibition Assay IC50=5.59907 μM SANGER
NMC-G1 Growth Inhibition Assay IC50=5.70227 μM SANGER
SW1710 Growth Inhibition Assay IC50=5.74751 μM SANGER
YAPC Growth Inhibition Assay IC50=5.76201 μM SANGER
22RV1 Growth Inhibition Assay IC50=5.80019 μM SANGER
COLO-679 Growth Inhibition Assay IC50=5.88948 μM SANGER
TCCSUP Growth Inhibition Assay IC50=5.93259 μM SANGER
C2BBe1 Growth Inhibition Assay IC50=5.9397 μM SANGER
TE-15 Growth Inhibition Assay IC50=6.06605 μM SANGER
SCLC-21H Growth Inhibition Assay IC50=6.10843 μM SANGER
EoL-1-cell Growth Inhibition Assay IC50=6.16563 μM SANGER
NKM-1 Growth Inhibition Assay IC50=6.1671 μM SANGER
NCI-H1304 Growth Inhibition Assay IC50=6.27428 μM SANGER
NB6 Growth Inhibition Assay IC50=6.29622 μM SANGER
NALM-6 Growth Inhibition Assay IC50=6.3323 μM SANGER
NCI-H522 Growth Inhibition Assay IC50=6.33306 μM SANGER
MV-4-11 Growth Inhibition Assay IC50=6.37079 μM SANGER
LB2241-RCC Growth Inhibition Assay IC50=6.38667 μM SANGER
NCI-H1417 Growth Inhibition Assay IC50=6.40847 μM SANGER
HT-1197 Growth Inhibition Assay IC50=6.57122 μM SANGER
P30-OHK Growth Inhibition Assay IC50=6.6277 μM SANGER
ALL-PO Growth Inhibition Assay IC50=6.71916 μM SANGER
OVCAR-4 Growth Inhibition Assay IC50=6.75405 μM SANGER
HCC2157 Growth Inhibition Assay IC50=6.77475 μM SANGER
NCI-H838 Growth Inhibition Assay IC50=6.9649 μM SANGER
NCI-H1299 Growth Inhibition Assay IC50=6.9709 μM SANGER
SW954 Growth Inhibition Assay IC50=7.20068 μM SANGER
NCI-H441 Growth Inhibition Assay IC50=7.34065 μM SANGER
SK-MEL-2 Growth Inhibition Assay IC50=7.48373 μM SANGER
KARPAS-45 Growth Inhibition Assay IC50=7.65929 μM SANGER
CAL-54 Growth Inhibition Assay IC50=7.82977 μM SANGER
KYSE-180 Growth Inhibition Assay IC50=7.88941 μM SANGER
NCI-H187 Growth Inhibition Assay IC50=7.95947 μM SANGER
RT-112 Growth Inhibition Assay IC50=8.09677 μM SANGER
NCI-H1437 Growth Inhibition Assay IC50=8.09795 μM SANGER
SNU-449 Growth Inhibition Assay IC50=8.28272 μM SANGER
HCC1187 Growth Inhibition Assay IC50=8.29391 μM SANGER
NCI-H2030 Growth Inhibition Assay IC50=8.37714 μM SANGER
HuO-3N1 Growth Inhibition Assay IC50=8.37844 μM SANGER
COLO-792 Growth Inhibition Assay IC50=8.41527 μM SANGER
MIA-PaCa-2 Growth Inhibition Assay IC50=8.85508 μM SANGER
SK-N-FI Growth Inhibition Assay IC50=9.0425 μM SANGER
MMAC-SF Growth Inhibition Assay IC50=9.09751 μM SANGER
NCI-H28 Growth Inhibition Assay IC50=9.10469 μM SANGER
ETK-1 Growth Inhibition Assay IC50=9.29974 μM SANGER
NCI-H1993 Growth Inhibition Assay IC50=9.44261 μM SANGER
no-11 Growth Inhibition Assay IC50=9.4712 μM SANGER
ChaGo-K-1 Growth Inhibition Assay IC50=9.51583 μM SANGER
NCCIT Growth Inhibition Assay IC50=9.53169 μM SANGER
SAS Growth Inhibition Assay IC50=10.248 μM SANGER
A673 Growth Inhibition Assay IC50=10.3704 μM SANGER
NCI-H1522 Growth Inhibition Assay IC50=10.3707 μM SANGER
NCI-H810 Growth Inhibition Assay IC50=10.3907 μM SANGER
IST-MES1 Growth Inhibition Assay IC50=10.4564 μM SANGER
GR-ST Growth Inhibition Assay IC50=10.5024 μM SANGER
SUP-T1 Growth Inhibition Assay IC50=10.7317 μM SANGER
NB5 Growth Inhibition Assay IC50=10.9022 μM SANGER
MZ1-PC Growth Inhibition Assay IC50=10.9571 μM SANGER
SK-CO-1 Growth Inhibition Assay IC50=10.9931 μM SANGER
Capan-2 Growth Inhibition Assay IC50=11.3198 μM SANGER
697 Growth Inhibition Assay IC50=11.6757 μM SANGER
REH Growth Inhibition Assay IC50=11.7451 μM SANGER
GI-1 Growth Inhibition Assay IC50=11.8615 μM SANGER
BB65-RCC Growth Inhibition Assay IC50=12.0916 μM SANGER
NCI-H1651 Growth Inhibition Assay IC50=12.2478 μM SANGER
NCI-H1618 Growth Inhibition Assay IC50=12.3976 μM SANGER
NCI-H2081 Growth Inhibition Assay IC50=12.6141 μM SANGER
GCIY Growth Inhibition Assay IC50=12.7213 μM SANGER
NY Growth Inhibition Assay IC50=13.0643 μM SANGER
PANC-03-27 Growth Inhibition Assay IC50=13.0807 μM SANGER
BHY Growth Inhibition Assay IC50=13.2121 μM SANGER
SK-OV-3 Growth Inhibition Assay IC50=13.3763 μM SANGER
5637 Growth Inhibition Assay IC50=13.7759 μM SANGER
LC-1F Growth Inhibition Assay IC50=14.0356 μM SANGER
SNB75 Growth Inhibition Assay IC50=14.0383 μM SANGER
CHP-212 Growth Inhibition Assay IC50=14.0464 μM SANGER
HT-1376 Growth Inhibition Assay IC50=14.1126 μM SANGER
MONO-MAC-6 Growth Inhibition Assay IC50=14.1502 μM SANGER
CA46 Growth Inhibition Assay IC50=14.1827 μM SANGER
SCC-15 Growth Inhibition Assay IC50=14.5583 μM SANGER
ATN-1 Growth Inhibition Assay IC50=14.6627 μM SANGER
NCI-H2405 Growth Inhibition Assay IC50=14.8157 μM SANGER
NCI-H716 Growth Inhibition Assay IC50=14.8493 μM SANGER
SW620 Growth Inhibition Assay IC50=14.9014 μM SANGER
NCI-H226 Growth Inhibition Assay IC50=14.9085 μM SANGER
SW962 Growth Inhibition Assay IC50=14.9432 μM SANGER
KYSE-150 Growth Inhibition Assay IC50=14.955 μM SANGER
OCUB-M Growth Inhibition Assay IC50=14.9883 μM SANGER
ES7 Growth Inhibition Assay IC50=15.0984 μM SANGER
SW1463 Growth Inhibition Assay IC50=15.4223 μM SANGER
CAKI-1 Growth Inhibition Assay IC50=15.5346 μM SANGER
MKN28 Growth Inhibition Assay IC50=15.5479 μM SANGER
SW13 Growth Inhibition Assay IC50=15.618 μM SANGER
A3-KAW Growth Inhibition Assay IC50=15.9697 μM SANGER
LU-65 Growth Inhibition Assay IC50=15.9768 μM SANGER
Calu-1 Growth Inhibition Assay IC50=16.0368 μM SANGER
ST486 Growth Inhibition Assay IC50=16.0431 μM SANGER
BB30-HNC Growth Inhibition Assay IC50=16.1246 μM SANGER
EGI-1 Growth Inhibition Assay IC50=16.446 μM SANGER
SH-4 Growth Inhibition Assay IC50=16.4731 μM SANGER
MN-60 Growth Inhibition Assay IC50=17.2297 μM SANGER
MPP-89 Growth Inhibition Assay IC50=17.2459 μM SANGER
A2780 Growth Inhibition Assay IC50=17.4139 μM SANGER
Daoy Growth Inhibition Assay IC50=17.4695 μM SANGER
NCI-H2126 Growth Inhibition Assay IC50=17.4771 μM SANGER
NCI-H1563 Growth Inhibition Assay IC50=17.4917 μM SANGER
8-MG-BA Growth Inhibition Assay IC50=17.6648 μM SANGER
786-0 Growth Inhibition Assay IC50=17.8353 μM SANGER
AM-38 Growth Inhibition Assay IC50=17.9306 μM SANGER
COLO-824 Growth Inhibition Assay IC50=18.4436 μM SANGER
SK-MEL-30 Growth Inhibition Assay IC50=18.5082 μM SANGER
CESS Growth Inhibition Assay IC50=18.7609 μM SANGER
BL-70 Growth Inhibition Assay IC50=18.8156 μM SANGER
NCI-H2170 Growth Inhibition Assay IC50=18.9179 μM SANGER
HT-3 Growth Inhibition Assay IC50=18.983 μM SANGER
BOKU Growth Inhibition Assay IC50=19.0381 μM SANGER
HPAF-II Growth Inhibition Assay IC50=19.3015 μM SANGER
KGN Growth Inhibition Assay IC50=19.4765 μM SANGER
MC-CAR Growth Inhibition Assay IC50=19.6313 μM SANGER
BHT-101 Growth Inhibition Assay IC50=19.777 μM SANGER
SW1783 Growth Inhibition Assay IC50=19.7806 μM SANGER
KP-N-YN Growth Inhibition Assay IC50=20.0262 μM SANGER
LU-165 Growth Inhibition Assay IC50=20.5571 μM SANGER
GOTO Growth Inhibition Assay IC50=20.6451 μM SANGER
EFM-19 Growth Inhibition Assay IC50=21.0716 μM SANGER
CTV-1 Growth Inhibition Assay IC50=21.1054 μM SANGER
HEL Growth Inhibition Assay IC50=21.4216 μM SANGER
SNU-C2B Growth Inhibition Assay IC50=21.426 μM SANGER
ECC4 Growth Inhibition Assay IC50=21.707 μM SANGER
NEC8 Growth Inhibition Assay IC50=21.8368 μM SANGER
KMOE-2 Growth Inhibition Assay IC50=21.8921 μM SANGER
NCI-H524 Growth Inhibition Assay IC50=22.0808 μM SANGER
WSU-NHL Growth Inhibition Assay IC50=22.1577 μM SANGER
SF126 Growth Inhibition Assay IC50=22.2469 μM SANGER
HOP-92 Growth Inhibition Assay IC50=22.3167 μM SANGER
CTB-1 Growth Inhibition Assay IC50=22.4677 μM SANGER
KYSE-270 Growth Inhibition Assay IC50=22.9357 μM SANGER
SK-MEL-24 Growth Inhibition Assay IC50=23.187 μM SANGER
Calu-3 Growth Inhibition Assay IC50=23.2128 μM SANGER
GAMG Growth Inhibition Assay IC50=23.2367 μM SANGER
SW1573 Growth Inhibition Assay IC50=23.7415 μM SANGER
MHH-NB-11 Growth Inhibition Assay IC50=24.0194 μM SANGER
TK10 Growth Inhibition Assay IC50=24.5013 μM SANGER
LB373-MEL-D Growth Inhibition Assay IC50=24.6064 μM SANGER
KALS-1 Growth Inhibition Assay IC50=24.7327 μM SANGER
HUTU-80 Growth Inhibition Assay IC50=25.8032 μM SANGER
HuP-T3 Growth Inhibition Assay IC50=26.1674 μM SANGER
OE19 Growth Inhibition Assay IC50=26.2153 μM SANGER
J82 Growth Inhibition Assay IC50=26.2471 μM SANGER
DU-4475 Growth Inhibition Assay IC50=26.3819 μM SANGER
DMS-53 Growth Inhibition Assay IC50=26.5138 μM SANGER
COLO-741 Growth Inhibition Assay IC50=26.8344 μM SANGER
SW48 Growth Inhibition Assay IC50=26.882 μM SANGER
IGR-1 Growth Inhibition Assay IC50=26.9334 μM SANGER
639-V Growth Inhibition Assay IC50=27.0245 μM SANGER
LK-2 Growth Inhibition Assay IC50=27.4141 μM SANGER
NCI-H2347 Growth Inhibition Assay IC50=27.9699 μM SANGER
NCI-H2228 Growth Inhibition Assay IC50=28.0905 μM SANGER
LS-123 Growth Inhibition Assay IC50=28.1262 μM SANGER
U031 Growth Inhibition Assay IC50=28.252 μM SANGER
NCI-H1792 Growth Inhibition Assay IC50=28.4721 μM SANGER
NCI-H2087 Growth Inhibition Assay IC50=28.7552 μM SANGER
NCI-H2342 Growth Inhibition Assay IC50=29.5208 μM SANGER
SW626 Growth Inhibition Assay IC50=29.756 μM SANGER
LB2518-MEL Growth Inhibition Assay IC50=29.815 μM SANGER
RXF393 Growth Inhibition Assay IC50=30.0952 μM SANGER
LC4-1 Growth Inhibition Assay IC50=30.3092 μM SANGER
NCI-H1694 Growth Inhibition Assay IC50=30.6624 μM SANGER
K5 Growth Inhibition Assay IC50=30.9702 μM SANGER
HDLM-2 Growth Inhibition Assay IC50=30.9725 μM SANGER
BCPAP Growth Inhibition Assay IC50=31.8379 μM SANGER
BC-3 Growth Inhibition Assay IC50=32.1403 μM SANGER
LB996-RCC Growth Inhibition Assay IC50=32.2358 μM SANGER
NCI-H2009 Growth Inhibition Assay IC50=32.4981 μM SANGER
HTC-C3 Growth Inhibition Assay IC50=33.7519 μM SANGER
LAMA-84 Growth Inhibition Assay IC50=34.4407 μM SANGER
CCRF-CEM Growth Inhibition Assay IC50=34.5715 μM SANGER
AN3-CA Growth Inhibition Assay IC50=35.0568 μM SANGER
NCI-H1734 Growth Inhibition Assay IC50=35.2561 μM SANGER
Ca-Ski Growth Inhibition Assay IC50=35.4101 μM SANGER
U-266 Growth Inhibition Assay IC50=35.6114 μM SANGER
SBC-5 Growth Inhibition Assay IC50=35.7781 μM SANGER
GT3TKB Growth Inhibition Assay IC50=37.115 μM SANGER
MDA-MB-175-VII Growth Inhibition Assay IC50=37.2248 μM SANGER
PFSK-1 Growth Inhibition Assay IC50=37.2435 μM SANGER
IMR-5 Growth Inhibition Assay IC50=37.2487 μM SANGER
Daudi Growth Inhibition Assay IC50=37.3597 μM SANGER
A498 Growth Inhibition Assay IC50=37.7218 μM SANGER
SCC-4 Growth Inhibition Assay IC50=37.7843 μM SANGER
COLO-680N Growth Inhibition Assay IC50=38.2885 μM SANGER
SK-MES-1 Growth Inhibition Assay IC50=38.3215 μM SANGER
SR Growth Inhibition Assay IC50=38.5495 μM SANGER
LNCaP-Clone-FGC Growth Inhibition Assay IC50=38.5637 μM SANGER
SK-HEP-1 Growth Inhibition Assay IC50=38.7822 μM SANGER
BPH-1 Growth Inhibition Assay IC50=38.8329 μM SANGER
NCI-H1755 Growth Inhibition Assay IC50=39.5817 μM SANGER
LXF-289 Growth Inhibition Assay IC50=39.8084 μM SANGER
SW1088 Growth Inhibition Assay IC50=40.2107 μM SANGER
MOLT-4 Growth Inhibition Assay IC50=40.2901 μM SANGER
AsPC-1 Growth Inhibition Assay IC50=40.4583 μM SANGER
HOP-62 Growth Inhibition Assay IC50=40.6568 μM SANGER
A172 Growth Inhibition Assay IC50=40.8511 μM SANGER
SN12C Growth Inhibition Assay IC50=40.9385 μM SANGER
MDA-MB-231 Growth Inhibition Assay IC50=40.9898 μM SANGER
RPMI-2650 Growth Inhibition Assay IC50=41.1593 μM SANGER
KYSE-140 Growth Inhibition Assay IC50=41.8123 μM SANGER
KINGS-1 Growth Inhibition Assay IC50=42.4697 μM SANGER
HSC-3 Growth Inhibition Assay IC50=42.6661 μM SANGER
PC-14 Growth Inhibition Assay IC50=43.1882 μM SANGER
COR-L105 Growth Inhibition Assay IC50=43.6502 μM SANGER
BE-13 Growth Inhibition Assay IC50=44.2371 μM SANGER
NCI-H661 Growth Inhibition Assay IC50=44.2958 μM SANGER
IST-MEL1 Growth Inhibition Assay IC50=44.3599 μM SANGER
HCC1806 Growth Inhibition Assay IC50=44.5873 μM SANGER
COLO-800 Growth Inhibition Assay IC50=44.8453 μM SANGER
IST-SL2 Growth Inhibition Assay IC50=45.1247 μM SANGER
8305C Growth Inhibition Assay IC50=45.309 μM SANGER
UACC-62 Growth Inhibition Assay IC50=46.2875 μM SANGER
COR-L23 Growth Inhibition Assay IC50=47.199 μM SANGER
EFE-184 Growth Inhibition Assay IC50=47.388 μM SANGER
DMS-114 Growth Inhibition Assay IC50=47.4149 μM SANGER
KYSE-520 Growth Inhibition Assay IC50=48.5315 μM SANGER
SNG-M Growth Inhibition Assay IC50=49.434 μM SANGER
A2058 Growth Inhibition Assay IC50=49.4885 μM SANGER
HEK293 Function assay 60 mins Inhibition of full length IGF-1 receptor (unknown origin) autophosphorylation transfected in HEK293 cells pretreated for 60 mins followed by IGF-1 stimulation measured after 10 mins by quantitative Western blot analysis, IC50 = 0.0028 μM. 26951753
Ba/F3 Function assay Inhibition of full length IGF-1 receptor (unknown origin) transfected in Ba/F3 cells assessed as cell proliferation, IC50 = 0.0076 μM. 26951753
HEK293 Function assay 60 mins Inhibition of full length insulin receptor (unknown origin) autophosphorylation transfected in HEK293 cells pretreated for 60 mins followed by IGF-1 stimulation measured after 10 mins by quantitative Western blot analysis, IC50 = 0.016 μM. 26951753
A431 Function assay Inhibition of IGF1R intracellular phosphorylation in human A431 cells by ELISA, IC50 = 0.018 μM. 20346655
3T3 Function assay Inhibition of human IGF1R expressed in mouse 3T3 cells by ELISA based assay, IC50 = 0.024 μM. 21251824
NIH 3T3 Function assay 2 hrs Inhibition of full length human IGF-1R overexpressed in mouse NIH 3T3 cells assessed as IGF1-induced protein phosphorylation incubated for 2 hrs prior to IGF1 induction measured after 15 mins by ELISA, IC50 = 0.024 μM. 24900721
Ba/F3 Function assay Inhibition of full length insulin receptor (unknown origin) transfected in Ba/F3 cells assessed as cell proliferation, IC50 = 0.126 μM. 26951753
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells 29435139
Saos-2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells 29435139
BT-37 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells 29435139
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells 29435139
BT-12 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells 29435139
NB1643 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells 29435139
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells 29435139
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells 29435139
SJ-GBM2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells 29435139
NB-EBc1 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells 29435139
LAN-5 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells 29435139
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Biological Activity

Description Linsitinib (OSI-906) is a selective inhibitor of IGF-1R with IC50 of 35 nM in cell-free assays; modestly potent to InsR with IC50 of 75 nM, and no activity towards Abl, ALK, BTK, EGFR, FGFR1/2, PKA etc. Phase 3.
Targets
IGF-1R [1]
(Cell-free assay)
Insulin Receptor [1]
(Cell-free assay)
IRR [1]
(Cell-free assay)
35 nM 75 nM 75 nM
In vitro
In vitro OSI-906 inhibits IGF-1R autophosphorylation and activation of the downstream signaling proteins Akt, ERK1/2 and S6 kinase with IC50 of 0.028 to 0.13 μM. OSI-906 enables an intermediate conformation of the target protein through interactions with the C-helix. OSI-906 displays favorable metabolic stability in liver microsomes. OSI-906 fully inhibits both IR and IGF-1R phosphorylation at a concentration of 1 μM. OSI-906 inhibits proliferation of several tumor cell lines including non-small-cell lung cancer and colorectal cancer (CRC) tumor cell line with EC50 of 0.021 to 0.810 μM. [1]
Kinase Assay Protein kinase biochemical assays
Protein kinase assays are either performed in-house by ELISA-based assay methods (IGF-1R, IR, EGFR and KDR) or at Upstate Inc. by a radiometric method with ATP at 100 µM concentration. In-house ELISA assays use poly(Glu:Tyr) as the substrate bound to the surface of 96-well assay plates and phosphorylation is detected using an antiphosphotyrosine antibody conjugated to horseradish peroxidase. The bound antibody is quantified using ABTS as the peroxidase substrate by measuring absorbance at 405 / 490 nm. All assays use purified recombinant kinase catalytic domains. Recombinant enzymes of human IGF-1R or EGFR are expressed as an NH2-terminal glutathione S-transferase fusion protein in insect cells and are purified in house. IC50 values are determined from the sigmoidal dose–response plot of percent inhibition versus log10 compound concentration. A minimum of three measurements, performed in duplicate, are carried out with in-house assays unless otherwise indicated. OSI-906 at a concentration of 1 µM is profiled versus a panel of kinases using the ProfilerProTM Kinase Selectivity Assay Kit.
Cell Research Cell lines MCF7, NCI-H292, Colo-205, HT29, H358, H1703, BxPC3, A673, SW620, DU4475, HepG2 and Hepa-1, RKO 3T3/hulGF-IR and H292 cells
Concentrations 0.02-0.8 μM
Incubation Time 3 days
Method For assays of cell proliferation, cells are seeded into 96-well plates in appropriate media containing FCS 10% and incubated for 3 days in the presence of OSI-906 at various concentrations. Inhibition of cell growth is determined by luminescent quantitation of intracellular ATP content using CellTiterGlo. Data is presented as a fraction of maximal proliferation, calculated by dividing the cellular density in the presence of varying concentrations of OSI-906 by the cellular density of control cells treated with vehicle (DMSO) only.
Experimental Result Images Methods Biomarkers Images PMID
Western blot pS6 / S6 p-STAT3(Y705) / STAT3 pSrc(Y416) / Src cleaved caspase-3 / cleaved PARP p-IGF1R / IGF1R / p-mTOR / mTOR p-EGFR / EGFR / p-IGF1R / IGF1R / p-IRS1 / IRS1 / p-ERK / ERK / p-AKT / AKT 21257723
Immunofluorescence FoxO1 27535223
Growth inhibition assay Cell viability 26136493
In Vivo
In vivo OSI-906 inhibits tumor growth in an IGF-1R-driven xenograft mouse model, with 100% TGI and 55% regression at a dose of 75 mg/kg and 60% TGI and no regression at a dose of 25 mg/kg. OSI-906 administration induces different elimination half-lives of itself in dog, rat and mice, the elimination half-lives are 1.18 hours, 2.64 hours and 2.14 hours, respectively. OSI-906 administration at different single dose once-daily in femal Sprague-Dawley rat and femal CD-1 mouse reveal that the Vmax is not dose-proportional to OSI-906 dose. OSI-906 elevates the blood glucose levels at a dose of 25 mg/kg after 12 days administration. OSI-906 administration at a single dose of 75 mg/kg in IGF-1R-driven full-length human IGF-1R (LISN) xenograft mouse model achieve maximal inhibition of IGF-1R phosphorylation (80%) between 4 and 24 hours with plasma drug concentrations of 26.6-4.77 μM. [1] OSI-906 administered as a single dose of at 60 mg/kg in NCI-H292 xenografts mice inhibits uptake of glucose at 2, 4, and 24 hours post-treatment in vivo. OSI-906 inhibits the growth of tumors in NCI-H292 xenograft mouse model. [2]
Animal Research Animal Models IGF-1R-driven full-length human IGF-1R (LISN) xenograft mouse model
Dosages 25 mg / kg and 75 mg / kg
Administration Orally administrated at once-daily oral dose for 14 days
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02546544 Completed
Relapsed Ewing Sarcoma|Refractory Ewing Sarcoma
University of Oxford|European Organisation for Research and Treatment of Cancer - EORTC|European Commission|Astellas Pharma Inc|Oxford University Hospitals NHS Trust
March 2014 Phase 2
NCT01672736 Terminated
Multiple Myeloma
University Health Network Toronto|Multiple Myeloma Research Consortium|Astellas Pharma Inc
September 2012 Phase 1|Phase 2
NCT01529684 Completed
Advanced Solid Tumors|Pharmacokinetics of 14C-OSI-906
Astellas Pharma Global Development Inc.|Astellas Pharma Inc
March 19 2012 Phase 1
NCT01221077 Completed
NSCLC|Non Small Cell Lung Cancer
Astellas Pharma Inc
April 8 2011 Phase 2

Chemical Information & Solubility

Molecular Weight 421.49 Formula

C26H23N5O

CAS No. 867160-71-2 SDF Download Linsitinib (OSI-906) SDF
Smiles CC1(CC(C1)C2=NC(=C3N2C=CN=C3N)C4=CC5=C(C=C4)C=CC(=N5)C6=CC=CC=C6)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 84 mg/mL ( (199.29 mM); Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Frequently Asked Questions

Question 1:
Does the inhibitor dissolve in the vehicle (30% PEG400/0.5%Tween 80/5% propylene glycol) or is it a suspension?

Answer:
OSI-906 in 30% PEG400/0.5%Tween 80/5% propylene glycol is a suspension.

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