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Linsitinib (OSI-906) IGF-1R/Insulin Receptor inhibitor

Name: Linsitinib (OSI-906)
Brand: Selleck Chemicals
SKU: S1091
Availability: InStock
Rating: 5 (207 reviews)

Cat.No.S1091

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

Chemical Structure

Molecular Weight: 421.49

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Quality Control

Batch: Purity: 99.99%

99.99

Related Targets	EGFR VEGFR PDGFR FGFR c-Met Src MEK CSF-1R FLT3 HER2
Other IGF-1R Inhibitors	BMS-536924 NVP-AEW541 BMS-754807 Picropodophyllin (AXL1717) GSK1904529A AG-1024 NVP-ADW742 NT157 PQ 401 Ginsenoside Rg5

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Incubation Time	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
Click to View More Cell Line Experimental Data

Solubility

In vitro
Batch:

DMSO : 84 mg/mL (199.29 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5.000mg/ml (11.86mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	6.250mg/ml (14.83mM)	Taking the 1 mL working solution as an example, add 50 μL of 125 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to make it clear; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	6.250mg/ml (14.83mM)	Taking the 1 mL working solution as an example, add 50 μL of 125 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	421.49	Formula	C₂₆H₂₃N₅O	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	867160-71-2	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CC1(CC(C1)C2=NC(=C3N2C=CN=C3N)C4=CC5=C(C=C4)C=CC(=N5)C6=CC=CC=C6)O

Mechanism of Action

Targets/IC₅₀/Ki	IGF-1R (Cell-free assay) 35 nM Insulin Receptor (Cell-free assay) 75 nM IRR (Cell-free assay) 75 nM
In vitro	Linsitinib (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. It enables an intermediate conformation of the target protein through interactions with the C-helix and displays favorable metabolic stability in liver microsomes. This compound fully inhibits both IR and IGF-1R phosphorylation at a concentration of 1 μM and 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.
Kinase Assay	Protein kinase biochemical assays
Kinase Assay	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. At a concentration of 1 µM, this compound is profiled versus a panel of kinases using the ProfilerPro^TM Kinase Selectivity Assay Kit.
In vivo	Linsitinib (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. Its administration induces different elimination half-lives in dog, rat and mice, which are 1.18 hours, 2.64 hours and 2.14 hours, respectively. When administered at different single doses once-daily in female Sprague-Dawley rats and female CD-1 mice, it reveals that V_max is not dose-proportional to its dose. This compound elevates blood glucose levels at a dose of 25 mg/kg after 12 days of administration. At a single dose of 75 mg/kg in an IGF-1R-driven full-length human IGF-1R (LISN) xenograft mouse model, it achieves maximal inhibition of IGF-1R phosphorylation (80%) between 4 and 24 hours with plasma drug concentrations of 26.6-4.77 μM. When administered as a single dose of 60 mg/kg in NCI-H292 xenograft mice, it inhibits uptake of glucose at 2, 4, and 24 hours post-treatment in vivo. It also inhibits the growth of tumors in an NCI-H292 xenograft mouse model.
References	[1] https://pubmed.ncbi.nlm.nih.gov/21425998/ [2] https://pubmed.ncbi.nlm.nih.gov/21257723/

Applications

Methods	Biomarkers	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

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

Tech Support

Handling Instructions

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Frequently Asked Questions

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

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

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