Linsitinib (OSI-906)

Catalog No.S1091

Linsitinib (OSI-906) Chemical Structure

Molecular Weight(MW): 421.49

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.

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Cited by 59 Publications

Purity & Quality Control

Choose Selective IGF-1R Inhibitors

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

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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
A4-Fuk MmrtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3vN[2lEPTB;MD6wNlgxPiEQvF2= M{\IR3NCVkeHUh?=
KS-1 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGjBSWdKSzVyPUCuNFM5OzVizszN MmPVV2FPT0WU
TE-11 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXfJR|UxRTBwMEe4NlIh|ryP NGO0dYVUSU6JRWK=
EW-1 M3m4PWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnH5TWM2OD1yLkC4OVg2KM7:TR?= NGj3[plUSU6JRWK=
HMV-II MnjoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYq5V3J{UUN3ME2wMlA5QDR4IN88US=> NWrWZpRTW0GQR1XS
COLO-205 NIO0U3dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1zsTmlEPTB;MD6xNFQ2PCEQvF2= MXvTRW5ITVJ?
ES1 Mn7BS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGrHXmRKSzVyPUCuNVA3QTZizszN NEDoW3RUSU6JRWK=
GDM-1 NFL4U2ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV\JR|UxRTBwMUO2O|Ih|ryP M4HkW3NCVkeHUh?=
ML-2 M362TGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVzJR|UxRTBwMUW4PVYh|ryP NWLzflRGW0GQR1XS
Saos-2 MonsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWHJR|UxRTBwMU[1NlYh|ryP MVTTRW5ITVJ?
NCI-H1355 MnTzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MW\JR|UxRTBwMUixN|Uh|ryP MWfTRW5ITVJ?
G-401 MlTjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXewToFsUUN3ME2wMlE5OjNizszN M{n6c3NCVkeHUh?=
EW-16 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYHJR|UxRTBwMUi3O|ch|ryP NI\yTnRUSU6JRWK=
EW-7 M1r4SGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVnJR|UxRTBwMUi4PFEh|ryP M373d3NCVkeHUh?=
NCI-H727 M4jSTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVOxT2E{UUN3ME2wMlE6Pzl2IN88US=> NYXWPJRtW0GQR1XS
LCLC-97TM1 M4nmV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnLzTWM2OD1yLkKwPVU2KM7:TR?= MkHyV2FPT0WU
NCI-H650 Mln0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NES1VldKSzVyPUCuNlE{QDRizszN NHfWd4RUSU6JRWK=
NCI-H2122 NGfkWZpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUHJR|UxRTBwMkOyPVkh|ryP M3\MbnNCVkeHUh?=
SK-N-DZ MoTzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MU\JR|UxRTBwMkO2PVgh|ryP MWLTRW5ITVJ?
HT-29 NVfrU3M3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV30[YM3UUN3ME2wMlI1OjR6IN88US=> M1vNVnNCVkeHUh?=
LB771-HNC NH3OTFBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYL3U2F5UUN3ME2wMlI2QTF3IN88US=> M3vqSXNCVkeHUh?=
HT-144 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mnz4TWM2OD1yLkK2NVkyKM7:TR?= MkHDV2FPT0WU
LAN-6 NHfrfFVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3;4[WlEPTB;MD6yOlM1QCEQvF2= M1vQOnNCVkeHUh?=
EW-18 M3XBcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVHmR4ZFUUN3ME2wMlI4ODBzIN88US=> Mki3V2FPT0WU
LS-1034 MkPuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3PMeGlEPTB;MD6yO|E{OiEQvF2= MnfXV2FPT0WU
EW-11 NEXZXoJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHTme|JKSzVyPUCuNlg1OzJizszN NV:y[YV6W0GQR1XS
SNU-C1 NWrMd255T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWjJR|UxRTBwMkmzNVMh|ryP M4j5XHNCVkeHUh?=
RS4-11 NVnMWZlkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NETOW3pKSzVyPUCuN|M4PThizszN M3Hoe3NCVkeHUh?=
ES4 MlvnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUnJR|UxRTBwNEGwN|gh|ryP NH7sU3RUSU6JRWK=
COLO-320-HSR NIrHZWtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVXJR|UxRTBwNEGzOlgh|ryP MnjhV2FPT0WU
NB10 MmDYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGPFPVJKSzVyPUCuOFU1OzdizszN M{PLcHNCVkeHUh?=
BFTC-905 MmrZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYrNb4pSUUN3ME2wMlQ3PzV6IN88US=> M{e1OXNCVkeHUh?=
A375 NIfUSXFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGPLNGtKSzVyPUCuOFc3OTdizszN NYO0cXNsW0GQR1XS
SJRH30 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1;aRmlEPTB;MD61NFgzOiEQvF2= NF\oc5lUSU6JRWK=
NOS-1 MnzyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFrteFRKSzVyPUCuOVIzPjdizszN NYG4SpFVW0GQR1XS
SIG-M5 NU[yRVhMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVrJR|UxRTBwNUO1OVch|ryP MXzTRW5ITVJ?
DOK Mli5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml\zTWM2OD1yLkW1OkDPxE1? Mlf6V2FPT0WU
NB69 M3zQ[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF3lVFFKSzVyPUCuOVgzPTdizszN MojwV2FPT0WU
SK-NEP-1 M4jMOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXvJR|UxRTBwNkCyN|Yh|ryP M4PT[nNCVkeHUh?=
SK-MM-2 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVjJR|UxRTBwNkW0PVEh|ryP M1HGbHNCVkeHUh?=
NCI-H358 NWjaXFNLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXfJR|UxRTBwNkewPFIh|ryP M4nEcHNCVkeHUh?=
RH-1 NWTacXhLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEO3[VZKSzVyPUCuO|Q5PTlizszN Mlq0V2FPT0WU
NH-12 NFTuNXNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWrWb4RjUUN3ME2wMlc3ODR4IN88US=> MVLTRW5ITVJ?
TE-12 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlSyTWM2OD1yLke2OFg3KM7:TR?= MnO5V2FPT0WU
COLO-668 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIjteFFKSzVyPUCuPFQ3PjZizszN M3jXeXNCVkeHUh?=
PANC-08-13 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX;JR|UxRTBwOE[zO|ch|ryP NUPUfm83W0GQR1XS
HCC2998 NULWOYdST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2OxeGlEPTB;MD64PFI3OyEQvF2= MWXTRW5ITVJ?
ABC-1 M2PrR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn60TWM2OD1yLkmwN|UzKM7:TR?= NXW0N5J2W0GQR1XS
ES6 NHP3eHFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVvFd2tOUUN3ME2wMlkyODZ4IN88US=> MlXpV2FPT0WU
SNU-387 NGTZN3lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4rxe2lEPTB;MD65PVM6OyEQvF2= M1XFNHNCVkeHUh?=
CMK MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnS1TWM2OD1yLkm5PVI6KM7:TR?= M173[3NCVkeHUh?=
SJSA-1 NUXZT4FMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmTCTWM2OD1zLkCzOlU{KM7:TR?= M{DmUHNCVkeHUh?=
SIMA MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIjBRmdKSzVyPUGuNFY5OjVizszN NHy2U2VUSU6JRWK=
ES3 NH;SR45Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NY[5c5hqUUN3ME2xMlEzOjl5IN88US=> NGDLXmNUSU6JRWK=
IGROV-1 NEXkdZhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUe3V4ZMUUN3ME2xMlE2PDR2IN88US=> NXT4SotlW0GQR1XS
MEL-JUSO MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV7FOIJyUUN3ME2xMlE2PzV7IN88US=> M3[zOXNCVkeHUh?=
T84 M1v2eWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlvOTWM2OD1zLkKwPVE1KM7:TR?= M4\wUnNCVkeHUh?=
CAL-85-1 M3K0e2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWrJR|UxRTFwMkOxN|gh|ryP Mmj1V2FPT0WU
RD MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3znXGlEPTB;MT6yOlQ2PSEQvF2= NWjTXnY2W0GQR1XS
TE-8 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGXHSWJKSzVyPUGuN|E1PjJizszN Moe2V2FPT0WU
L-363 M3i2Omdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH\2NXhKSzVyPUGuN|QzODhizszN M1fKTHNCVkeHUh?=
EKVX MnPZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX;neGpLUUN3ME2xMlM1PTZ6IN88US=> M{mxfXNCVkeHUh?=
SK-MEL-3 Mof4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml:4TWM2OD1zLkS4OVU3KM7:TR?= NH;NXlRUSU6JRWK=
TGBC24TKB MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3\UZWlEPTB;MT61NFE6OyEQvF2= MWXTRW5ITVJ?
NCI-H1770 NVjIb2NDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3HPNGlEPTB;MT61NVEyOyEQvF2= MlL0V2FPT0WU
HuH-7 NET1OYNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUTpPGZoUUN3ME2xMlYxODl6IN88US=> M1fzbnNCVkeHUh?=
HL-60 NFPTNHBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHu0[mtKSzVyPUGuOlY6OjhizszN MX3TRW5ITVJ?
TE-1 NFnpbY5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXjJR|UxRTFwN{C5OFUh|ryP MY\TRW5ITVJ?
LC-2-ad MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWHJR|UxRTFwN{O4PFch|ryP MlLVV2FPT0WU
LB647-SCLC MofTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3i0O2lEPTB;MT63OlU5OyEQvF2= NF[yTZZUSU6JRWK=
NCI-H2171 NWjLeXhtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX\MdJRnUUN3ME2xMlc4PzF4IN88US=> MVvTRW5ITVJ?
SK-PN-DW MojVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEO0coJKSzVyPUGuPVEzQThizszN M2HLe3NCVkeHUh?=
MC-IXC MnvnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2r3RmlEPTB;MT65PFk5KM7:TR?= NV\hTVFrW0GQR1XS
LS-513 M3LmW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUnJR|UxRTJwMEWzNFUh|ryP MmXGV2FPT0WU
EW-3 MmnkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MorZTWM2OD1{LkC5PFQ1KM7:TR?= MUPTRW5ITVJ?
OPM-2 M{fwfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2rIeWlEPTB;Mj6xNFIh|ryP MYPTRW5ITVJ?
LP-1 NWLHVnY6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF[2eo5KSzVyPUKuNlU5ODdizszN NFLXN2VUSU6JRWK=
LU-134-A M13CbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGTiW4lKSzVyPUKuNlc4KM7:TR?= NWHpO|hCW0GQR1XS
CP66-MEL Mn;VS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{fVOGlEPTB;Mj6yPVAyPCEQvF2= MX;TRW5ITVJ?
HCC1143 M17nOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoLsTWM2OD1{LkS1N|Y5KM7:TR?= NVzUOWN3W0GQR1XS
LOXIMVI NHz6TodIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{HENmlEPTB;Mj62NFIyKM7:TR?= NHnxVFdUSU6JRWK=
TE-10 NHfOTmFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIjKbFZKSzVyPUKuO|A5OzhizszN NHLJdoRUSU6JRWK=
NCI-H1882 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWXJR|UxRTJwN{WyNlch|ryP NXPnSHB4W0GQR1XS
CHP-126 MnLlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHv0fo9KSzVyPUKuO|Y{OTdizszN MVjTRW5ITVJ?
NCI-H1623 M3S0V2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3;XWGlEPTB;Mj65NlAzPCEQvF2= M{\Qd3NCVkeHUh?=
GB-1 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWPJR|UxRTJwOUO0NFQh|ryP M{S3XnNCVkeHUh?=
RCC10RGB NWTCSHZ[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1rpZWlEPTB;Mj65OVI5OSEQvF2= NETGb2RUSU6JRWK=
NCI-H2141 NFPqXplIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVfI[Y4{UUN3ME2yMlk3QDl4IN88US=> MoToV2FPT0WU
GI-ME-N M{[2[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFPEclNKSzVyPUOuNFA2PjVizszN NVny[nU2W0GQR1XS
NCI-H526 M1XUcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn3OTWM2OD1|LkC0NFg2KM7:TR?= NHrZc4xUSU6JRWK=
NCI-H747 NVTHNHQzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV[xfHlsUUN3ME2zMlA1QTl{IN88US=> M{Tqd3NCVkeHUh?=
SNU-423 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1HlbWlEPTB;Mz6yNFMyOyEQvF2= NHjVSnlUSU6JRWK=
A427 MoDFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4GzWGlEPTB;Mz6yOVY6QSEQvF2= MVXTRW5ITVJ?
CAL-12T NVPR[2lqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2\Bc2lEPTB;Mz60NFcyOyEQvF2= MXLTRW5ITVJ?
LU-99A NV;UVFY{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHjCT49KSzVyPUOuOFcyODVizszN M4rT[HNCVkeHUh?=
MS-1 NHTqU4ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHfQT4pKSzVyPUOuOVM1OjlizszN M33zfHNCVkeHUh?=
SK-LU-1 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4XJOGlEPTB;Mz63OlI6PSEQvF2= NWn0[49TW0GQR1XS
SW837 M1PWO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkfzTWM2OD1|Lke2N|M{KM7:TR?= NGjzUVBUSU6JRWK=
ES8 NV73OYhuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmfQTWM2OD1|LkizPFc4KM7:TR?= Ml7DV2FPT0WU
MZ2-MEL M2jXfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mk\0TWM2OD1|LkmyNFg3KM7:TR?= MVLTRW5ITVJ?
TGW Mo\1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWf6[XpvUUN3ME20MlAyOzFzIN88US=> NV7aSlVbW0GQR1XS
GP5d Mor1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{m5V2lEPTB;ND6wOVM3OiEQvF2= MmK1V2FPT0WU
BB49-HNC MnrOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NETTfINKSzVyPUSuNVUzOTNizszN Mn7oV2FPT0WU
NB13 M2S2fmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV7peHhWUUN3ME20MlI3QDh5IN88US=> Ml\JV2FPT0WU
NTERA-S-cl-D1 NFHJdldIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGXkUIFKSzVyPUSuNlg3OTVizszN MYrTRW5ITVJ?
NCI-H1648 M3v1[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUPJR|UxRTRwMkm4NVkh|ryP NHuwNmdUSU6JRWK=
LCLC-103H NUXDTJpuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmPZTWM2OD12LkOyNVk2KM7:TR?= MlfSV2FPT0WU
LS-411N NVzaWnJKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFfqR|NKSzVyPUSuOFQ5QDVizszN MoHqV2FPT0WU
NCI-H1092 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGXLOVVKSzVyPUSuOFU3QDdizszN NXfUfXJFW0GQR1XS
PANC-10-05 NXLwZog2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWHlfWduUUN3ME20MlY6QDRizszN NEDROXZUSU6JRWK=
DK-MG MmrkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NU\hWY51UUN3ME20MlgxQTN|IN88US=> Ml7iV2FPT0WU
OVCAR-5 MmnyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmPPTWM2OD12LkixNlI3KM7:TR?= Mk\3V2FPT0WU
CAL-39 M1LuN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVvJR|UxRTRwOEe2O{DPxE1? NYLrNWtrW0GQR1XS
TE-441-T M1rRTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV3JSpdsUUN3ME20MlkxPTN5IN88US=> Ml;pV2FPT0WU
MOLT-16 NHm1Z4FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1HVSmlEPTB;ND65OVI2OyEQvF2= MkHEV2FPT0WU
MCF7 Mk\HS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkHpTWM2OD13LkG0OVE4KM7:TR?= NYXo[oxZW0GQR1XS
CAPAN-1 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWL6cmtVUUN3ME21MlI2PzB5IN88US=> M{Gzc3NCVkeHUh?=
PSN1 M3rER2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3OzbGlEPTB;NT6yO|I{PSEQvF2= NEnoTnVUSU6JRWK=
NCI-H292 MkLoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkLpTWM2OD13LkOwNFQ1KM7:TR?= NH;NW4NUSU6JRWK=
CPC-N MkD4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUnJR|UxRTVwM{m0NVkh|ryP MmjWV2FPT0WU
DoTc2-4510 NEXnZmRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{XzTmlEPTB;NT60OVM4OSEQvF2= MVTTRW5ITVJ?
LB1047-RCC MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn\zTWM2OD13LkW1PVM{KM7:TR?= MVrTRW5ITVJ?
MHH-ES-1 Mlr2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYDJR|UxRTVwNUm5NFch|ryP MWPTRW5ITVJ?
NMC-G1 NUXJZXJ2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGD5RY1KSzVyPUWuO|AzOjdizszN NIPDN5NUSU6JRWK=
SW1710 NIrSdlBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV\JR|UxRTVwN{S3OVEh|ryP M2HyNnNCVkeHUh?=
YAPC M174[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFvJS3hKSzVyPUWuO|YzODFizszN MojZV2FPT0WU
22RV1 M{P0Smdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3HFfmlEPTB;NT64NFAyQSEQvF2= M1foXnNCVkeHUh?=
COLO-679 M4XJR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MknxTWM2OD13Lki4PVQ5KM7:TR?= M4e2WnNCVkeHUh?=
TCCSUP NVfpZXVjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MonrTWM2OD13LkmzNlU6KM7:TR?= M4[0TXNCVkeHUh?=
C2BBe1 MofIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXzJR|UxRTVwOUO5O{DPxE1? MUXTRW5ITVJ?
TE-15 Ml\BS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHiyU5FKSzVyPU[uNFY3ODVizszN MomwV2FPT0WU
SCLC-21H NXrxOnBCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEe0b4FKSzVyPU[uNVA5PDNizszN NVv3XW5{W0GQR1XS
EoL-1-cell M4nGVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXLUUHNOUUN3ME22MlE3PTZ|IN88US=> NVnHfllYW0GQR1XS
NKM-1 M16wT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFPLWGRKSzVyPU[uNVY4OSEQvF2= NIn4SlFUSU6JRWK=
NCI-H1304 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVPJR|UxRTZwMke0Nlgh|ryP NXLxNWpTW0GQR1XS
NB6 NIDGNHdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUTTVlBxUUN3ME22MlI6PjJ{IN88US=> MU\TRW5ITVJ?
NALM-6 NYq4UJp3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFnXVWFKSzVyPU[uN|MzOyEQvF2= NXfLeox4W0GQR1XS
NCI-H522 NU\rdpNwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{LGN2lEPTB;Nj6zN|MxPiEQvF2= MV7TRW5ITVJ?
MV-4-11 NWq1NWE5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn7pTWM2OD14LkO3NFc6KM7:TR?= NYW2bmhQW0GQR1XS
LB2241-RCC M2O1[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoriTWM2OD14LkO4OlY4KM7:TR?= M1rw[nNCVkeHUh?=
NCI-H1417 NYjVcYV4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml\aTWM2OD14LkSwPFQ4KM7:TR?= MnjZV2FPT0WU
HT-1197 NGXmVWlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnywTWM2OD14LkW3NVIzKM7:TR?= NV\rU4VyW0GQR1XS
P30-OHK NGHXZ41Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlLXTWM2OD14Lk[yO|ch|ryP MkD1V2FPT0WU
ALL-PO MmXOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2PaOGlEPTB;Nj63NVkyPiEQvF2= NXHw[|hLW0GQR1XS
OVCAR-4 NEK0OpBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHTaeoJKSzVyPU[uO|U1ODVizszN M37ZbXNCVkeHUh?=
HCC2157 NEXK[3VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYCwTXdFUUN3ME22Mlc4PDd3IN88US=> M2XoTHNCVkeHUh?=
NCI-H838 NXP5dZF{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVjJR|UxRTZwOU[0PUDPxE1? M1Pzc3NCVkeHUh?=
NCI-H1299 NYPaSZc6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlvyTWM2OD14Lkm3NFkh|ryP NFzCTJFUSU6JRWK=
SW954 M33UZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXf5Z|VsUUN3ME23MlIxODZ6IN88US=> M2rUPXNCVkeHUh?=
NCI-H441 NEDnZ2xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXzJR|UxRTdwM{SwOlUh|ryP MlTIV2FPT0WU
SK-MEL-2 MlS5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEDlfZZKSzVyPUeuOFg{PzNizszN M{fyfXNCVkeHUh?=
KARPAS-45 NIPxbHlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlXGTWM2OD15Lk[1PVI6KM7:TR?= MmTEV2FPT0WU
CAL-54 M13CcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NU\JcFNSUUN3ME23MlgzQTd5IN88US=> NHH0bpBUSU6JRWK=
KYSE-180 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYP6fY1{UUN3ME23Mlg5QTRzIN88US=> Ml73V2FPT0WU
NCI-H187 Mk\YS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4\2[GlEPTB;Nz65OVk1PyEQvF2= NXTNdYpQW0GQR1XS
RT-112 M3TpfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWHJR|UxRThwMEm2O|ch|ryP MnvXV2FPT0WU
NCI-H1437 NXzaRYpGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXjJR|UxRThwMEm3PVUh|ryP MXzTRW5ITVJ?
SNU-449 M3TIemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWHJR|UxRThwMkiyO|Ih|ryP M1i0bnNCVkeHUh?=
HCC1187 NFrNS5NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFnsUFRKSzVyPUiuNlk{QTFizszN MVfTRW5ITVJ?
NCI-H2030 NGrwVJlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWnJR|UxRThwM{e3NVQh|ryP MYHTRW5ITVJ?
HuO-3N1 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoLaTWM2OD16LkO3PFQ1KM7:TR?= NXfVSZlKW0GQR1XS
COLO-792 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NILyeGFKSzVyPUiuOFE2OjdizszN MnLOV2FPT0WU
MIA-PaCa-2 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXfJR|UxRThwOEW1NFgh|ryP NWr5PXBtW0GQR1XS
SK-N-FI M2CzbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYHJR|UxRTlwMESyOUDPxE1? NFnsfGFUSU6JRWK=
MMAC-SF MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3n3b2lEPTB;OT6wPVc2OSEQvF2= NUi2PZZIW0GQR1XS
NCI-H28 NEG1eZFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn7ETWM2OD17LkGwOFY6KM7:TR?= M1PP[XNCVkeHUh?=
ETK-1 NFvFW3VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlX5TWM2OD17LkK5PVc1KM7:TR?= MlzLV2FPT0WU
NCI-H1993 NHrU[oFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoSyTWM2OD17LkS0NlYyKM7:TR?= NIrD[FZUSU6JRWK=
no-11 M2DISmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEHJfpVKSzVyPUmuOFcyOiEQvF2= MXvTRW5ITVJ?
ChaGo-K-1 MmDpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3HJOGlEPTB;OT61NVU5OyEQvF2= MWLTRW5ITVJ?
NCCIT M{i4bmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEHOW4tKSzVyPUmuOVMyPjlizszN MmXTV2FPT0WU
SAS NETBSoRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF32coJKSzVyPUGwMlI1QCEQvF2= MYjTRW5ITVJ?
A673 M3[3ZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGHIUmZKSzVyPUGwMlM4ODRizszN M3HMZ3NCVkeHUh?=
NCI-H1522 M3LkZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUDNT3B4UUN3ME2xNE4{PzB5IN88US=> MUTTRW5ITVJ?
NCI-H810 NHO2RpZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYDJR|UxRTFyLkO5NFch|ryP MV\TRW5ITVJ?
IST-MES1 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlXETWM2OD1zMD60OVY1KM7:TR?= MkfFV2FPT0WU
GR-ST NX7JW4h[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkXQTWM2OD1zMD61NFI1KM7:TR?= M1vGS3NCVkeHUh?=
SUP-T1 NUPzc3Y5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYfOXVRuUUN3ME2xNE44OzF5IN88US=> M4LBfnNCVkeHUh?=
NB5 NYDWSms5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEXyVFJKSzVyPUGwMlkxOjJizszN NFKxdVFUSU6JRWK=
MZ1-PC MnKyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1PVfGlEPTB;MUCuPVU4OSEQvF2= MlmxV2FPT0WU
SK-CO-1 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYHJR|UxRTFyLkm5N|Eh|ryP NUXnc4NVW0GQR1XS
Capan-2 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVqyfohXUUN3ME2xNU4{OTl6IN88US=> NFPoUJZUSU6JRWK=
697 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MknZTWM2OD1zMT62O|U4KM7:TR?= M{LOUHNCVkeHUh?=
REH M13ZW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYrJR|UxRTFzLke0OVEh|ryP NFG2eoZUSU6JRWK=
GI-1 NVLOXXdjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFexdI5KSzVyPUGxMlg3OTVizszN NH\Leo1USU6JRWK=
BB65-RCC Ml\oS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVK0RZZxUUN3ME2xNk4xQTF4IN88US=> M2rjVHNCVkeHUh?=
NCI-H1651 NI[1NXJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGTFZ3NKSzVyPUGyMlI1PzhizszN M3;zcHNCVkeHUh?=
NCI-H1618 NF;2O|RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3HFPWlEPTB;MUKuN|k4PiEQvF2= MmHPV2FPT0WU
NCI-H2081 NF24[YFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXzOfohbUUN3ME2xNk43OTRzIN88US=> NF;XXXZUSU6JRWK=
GCIY MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmLYTWM2OD1zMj63NlE{KM7:TR?= M2\aVHNCVkeHUh?=
NY M13wR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVLQR45OUUN3ME2xN{4xPjR|IN88US=> MUDTRW5ITVJ?
PANC-03-27 NYPtfHBVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnLSTWM2OD1zMz6wPFA4KM7:TR?= MmO0V2FPT0WU
BHY NH\HXmNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4jJXWlEPTB;MUOuNlEzOSEQvF2= Mn;1V2FPT0WU
SK-OV-3 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVS4V2V1UUN3ME2xN{4{PzZ|IN88US=> MYHTRW5ITVJ?
5637 NEiyT|lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmDJTWM2OD1zMz63O|U6KM7:TR?= NInhbI9USU6JRWK=
LC-1F M4LYZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmXPTWM2OD1zND6wN|U3KM7:TR?= M1zJW3NCVkeHUh?=
SNB75 NEL5TY1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mlu0TWM2OD1zND6wN|g{KM7:TR?= NVXOVXFEW0GQR1XS
CHP-212 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4\mWmlEPTB;MUSuNFQ3PCEQvF2= MVTTRW5ITVJ?
HT-1376 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4HhWmlEPTB;MUSuNVEzPiEQvF2= NIjXeXpUSU6JRWK=
MONO-MAC-6 NXn0[YJxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2TBPGlEPTB;MUSuNVUxOiEQvF2= MknKV2FPT0WU
CA46 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUPJR|UxRTF2LkG4Nlch|ryP M4HDO3NCVkeHUh?=
SCC-15 Mk\iS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4jzcGlEPTB;MUSuOVU5OyEQvF2= M1i3NHNCVkeHUh?=
ATN-1 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mo\uTWM2OD1zND62OlI4KM7:TR?= MlLNV2FPT0WU
NCI-H2405 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYjJR|UxRTF2LkixOVch|ryP NHf3b3dUSU6JRWK=
NCI-H716 M1;Xc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYTyS5RZUUN3ME2xOE45PDl|IN88US=> NIjMTmhUSU6JRWK=
SW620 NUn2fJZoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4f0fGlEPTB;MUSuPVAyPCEQvF2= M4f2VHNCVkeHUh?=
NCI-H226 NIXPRZFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1uwZWlEPTB;MUSuPVA5PSEQvF2= NHjJZmxUSU6JRWK=
SW962 NGiyVJdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIDmSJNKSzVyPUG0Mlk1OzJizszN NIHiPItUSU6JRWK=
KYSE-150 NELxNndIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NY\WN3Y{UUN3ME2xOE46PTVizszN NYH5PYtEW0GQR1XS
OCUB-M NUe0OYRkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV7jTJdJUUN3ME2xOE46QDh|IN88US=> M2njOnNCVkeHUh?=
ES7 MmrjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXrEWG55UUN3ME2xOU4xQTh2IN88US=> MX\TRW5ITVJ?
SW1463 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlH3TWM2OD1zNT60NlI{KM7:TR?= NXXN[5dHW0GQR1XS
CAKI-1 NF;YenlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoX0TWM2OD1zNT61N|Q3KM7:TR?= MkTQV2FPT0WU
MKN28 NH62ZpBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVHOTVVKUUN3ME2xOU42PDd7IN88US=> M1\mR3NCVkeHUh?=
SW13 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGDUdnpKSzVyPUG1MlYyQCEQvF2= M4TUcHNCVkeHUh?=
A3-KAW MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NY\uOYJGUUN3ME2xOU46Pjl5IN88US=> NEW1T4lUSU6JRWK=
LU-65 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVTJR|UxRTF3Lkm3Olgh|ryP NEjpO4hUSU6JRWK=
Calu-1 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV;JR|UxRTF4LkCzOlgh|ryP MY\TRW5ITVJ?
ST486 M2W5Xmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYTqXFU4UUN3ME2xOk4xPDNzIN88US=> NWrRNFBJW0GQR1XS
BB30-HNC NHvkWZVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHG2T2RKSzVyPUG2MlEzPDZizszN NHq5OpVUSU6JRWK=
EGI-1 MoXWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYDJR|UxRTF4LkS0OkDPxE1? NUfINlJ4W0GQR1XS
SH-4 NVPHdm5FT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWn3d5JCUUN3ME2xOk41PzNzIN88US=> M4D4eXNCVkeHUh?=
MN-60 NYPkZnBJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYLJR|UxRTF5LkKyPVch|ryP MkPmV2FPT0WU
MPP-89 NWXRPZV1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{[0UWlEPTB;MUeuNlQ2QSEQvF2= MXfTRW5ITVJ?
A2780 NFLEOWNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV7m[nBzUUN3ME2xO{41OTN7IN88US=> Mo\CV2FPT0WU
Daoy M2HrT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF7nUpBKSzVyPUG3MlQ3QTVizszN NHTObY9USU6JRWK=
NCI-H2126 NXjIeIxvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX\0PG5IUUN3ME2xO{41PzdzIN88US=> M1TmdXNCVkeHUh?=
NCI-H1563 NVS0XIVHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX7JR|UxRTF5LkS5NVch|ryP MX\TRW5ITVJ?
8-MG-BA M17ZO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX\JR|UxRTF5Lk[2OFgh|ryP MoH3V2FPT0WU
786-0 MlXmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHPoUFBKSzVyPUG3Mlg{PTNizszN M3XrXnNCVkeHUh?=
AM-38 M1LWN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGTkS|FKSzVyPUG3Mlk{ODZizszN MWPTRW5ITVJ?
COLO-824 MmTPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVLJR|UxRTF6LkS0N|Yh|ryP M1zxbHNCVkeHUh?=
SK-MEL-30 NFWxdJJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{C3OmlEPTB;MUiuOVA5OiEQvF2= M{Pq[nNCVkeHUh?=
CESS NVKybIFoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGLScnNKSzVyPUG4Mlc3ODlizszN MlrwV2FPT0WU
BL-70 MlnxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXTJR|UxRTF6LkixOVYh|ryP NG\lfWhUSU6JRWK=
NCI-H2170 MoD5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUHE[XhRUUN3ME2xPE46OTd7IN88US=> M3j3eHNCVkeHUh?=
HT-3 MmLOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmSyTWM2OD1zOD65PFMh|ryP MVrTRW5ITVJ?
BOKU M1\vZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnPTTWM2OD1zOT6wN|gyKM7:TR?= Mom0V2FPT0WU
HPAF-II Mli4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIXtVZZKSzVyPUG5MlMxOTVizszN M4fJbHNCVkeHUh?=
KGN NHjYbZFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYDJTlJ7UUN3ME2xPU41PzZ3IN88US=> NW\4UHFUW0GQR1XS
MC-CAR MmfQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3fkOGlEPTB;MUmuOlMyOyEQvF2= NXHVfoR{W0GQR1XS
BHT-101 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEDU[pRKSzVyPUG5Mlc4PyEQvF2= NYfteW46W0GQR1XS
SW1783 NHXLcJpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVLJR|UxRTF7Lke4NFYh|ryP Ml3sV2FPT0WU
KP-N-YN M4XOTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF7WXYtKSzVyPUKwMlAzPjJizszN NUTkV|M{W0GQR1XS
LU-165 NX\Nd|ZFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXe2TnhtUUN3ME2yNE42PTdzIN88US=> NY\WeVNCW0GQR1XS
GOTO NGPvXXNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV7WXplmUUN3ME2yNE43PDVzIN88US=> NX\xNZB3W0GQR1XS
EFM-19 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFy4WolKSzVyPUKxMlA4OTZizszN MmnLV2FPT0WU
CTV-1 NWjKTVI3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NELMXWJKSzVyPUKxMlExPTRizszN M4TQWHNCVkeHUh?=
HEL M2HCWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXTjZ3JoUUN3ME2yNU41OjF4IN88US=> NHvBfIxUSU6JRWK=
SNU-C2B NUS2Ull5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWfJR|UxRTJzLkSyOkDPxE1? M1jWenNCVkeHUh?=
ECC4 NEHzfHNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MojPTWM2OD1{MT63NFch|ryP NWixcWpEW0GQR1XS
NEC8 MoC4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NILOV4dKSzVyPUKxMlg{PjhizszN M{\BZ3NCVkeHUh?=
KMOE-2 NIjROWZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{SzOWlEPTB;MkGuPFkzOSEQvF2= NV;0ZoZ2W0GQR1XS
NCI-H524 M3LZe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGi0PGxKSzVyPUKyMlA5ODhizszN MkflV2FPT0WU
WSU-NHL MlHoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mm\NTWM2OD1{Mj6xOVc4KM7:TR?= NHXKWW9USU6JRWK=
SF126 MkD3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVLJR|UxRTJ{LkK0Olkh|ryP MkjtV2FPT0WU
HOP-92 Mnr3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4fRWmlEPTB;MkKuN|E3PyEQvF2= NF\V[29USU6JRWK=
CTB-1 M2\0ZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUPJR|UxRTJ{LkS2O|ch|ryP NFfieIxUSU6JRWK=
KYSE-270 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3rRSWlEPTB;MkKuPVM2PyEQvF2= MUHTRW5ITVJ?
SK-MEL-24 NETzVZhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH7nN45KSzVyPUKzMlE5PyEQvF2= M3;OVHNCVkeHUh?=
Calu-3 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWHJR|UxRTJ|LkKxNlgh|ryP MYLTRW5ITVJ?
GAMG NVS5VpNTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUfrcIptUUN3ME2yN{4zOzZ5IN88US=> M3nWW3NCVkeHUh?=
SW1573 NV\pOm55T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3L1UWlEPTB;MkOuO|QyPSEQvF2= MU\TRW5ITVJ?
MHH-NB-11 NVy0RZNGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVfJR|UxRTJ2LkCxPVQh|ryP MUnTRW5ITVJ?
TK10 NELWV3pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUSzPIdzUUN3ME2yOE42ODF|IN88US=> NHLiPVZUSU6JRWK=
LB373-MEL-D MlXsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M13PZ2lEPTB;MkSuOlA3PCEQvF2= NFPHd3JUSU6JRWK=
KALS-1 NW\5[VF7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MY\JR|UxRTJ2LkezNlch|ryP MVjTRW5ITVJ?
HUTU-80 NETGPGRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYrJR|UxRTJ3LkiwN|Ih|ryP NF7X[FhUSU6JRWK=
HuP-T3 NFPEUppIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVnt[3hHUUN3ME2yOk4yPjd2IN88US=> MY\TRW5ITVJ?
OE19 NWDodIxtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYTJR|UxRTJ4LkKxOVMh|ryP MU\TRW5ITVJ?
J82 NFfmSHZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlXHTWM2OD1{Nj6yOFcyKM7:TR?= NXLBdlQ3W0GQR1XS
DU-4475 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHH3OGFKSzVyPUK2MlM5OTlizszN NH7PRoFUSU6JRWK=
DMS-53 NX\HT3Y2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MW\JR|UxRTJ4LkWxN|gh|ryP MULTRW5ITVJ?
COLO-741 NIDXT3FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4Cz[GlEPTB;Mk[uPFM1PCEQvF2= MU\TRW5ITVJ?
SW48 MlfKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUPJR|UxRTJ4Lki4NkDPxE1? NX\lbJJpW0GQR1XS
IGR-1 M4Pie2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF7XSodKSzVyPUK2Mlk{OzRizszN MUPTRW5ITVJ?
639-V NFzSV2dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV73eVQ3UUN3ME2yO{4xOjR3IN88US=> Mmf0V2FPT0WU
LK-2 NXjjOI5VT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{LhXGlEPTB;MkeuOFE1OSEQvF2= M1K5c3NCVkeHUh?=
NCI-H2347 MnLFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlroTWM2OD1{Nz65Olk6KM7:TR?= MWXTRW5ITVJ?
NCI-H2228 M4\Jc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXS1bmNJUUN3ME2yPE4xQTB3IN88US=> M2HFd3NCVkeHUh?=
LS-123 M4C2O2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF\kSZNKSzVyPUK4MlEzPjJizszN MmX1V2FPT0WU
U031 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3m2ZmlEPTB;MkiuNlUzKM7:TR?= MorvV2FPT0WU
NCI-H1792 NFvXdZRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmLLTWM2OD1{OD60O|IyKM7:TR?= NVjRbY05W0GQR1XS
NCI-H2087 NVTBRXlQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{DpNWlEPTB;MkiuO|U2OiEQvF2= MYnTRW5ITVJ?
NCI-H2342 NXeweIRzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXfBbmczUUN3ME2yPU42OjB6IN88US=> MWrTRW5ITVJ?
SW626 MmjjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlPHTWM2OD1{OT63OVYh|ryP MkLYV2FPT0WU
LB2518-MEL M2PwN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUHJR|UxRTJ7LkixOUDPxE1? M{LNV3NCVkeHUh?=
RXF393 MkDYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MonBTWM2OD1|MD6wPVUzKM7:TR?= MWfTRW5ITVJ?
LC4-1 NFvBfY9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4XTUGlEPTB;M{CuN|A6OiEQvF2= MnHmV2FPT0WU
NCI-H1694 M1vsSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVXTelFGUUN3ME2zNE43PjJ2IN88US=> Mn;kV2FPT0WU
K5 NHLaTHBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2SzTWlEPTB;M{CuPVcxOiEQvF2= M1PJU3NCVkeHUh?=
HDLM-2 NGDEcI1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXHSbZptUUN3ME2zNE46PzJ3IN88US=> M4rMW3NCVkeHUh?=
BCPAP NUC5e3U5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnrDTWM2OD1|MT64N|c6KM7:TR?= M13ONHNCVkeHUh?=
BC-3 NGXiRW9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH3vRnZKSzVyPUOyMlE1ODNizszN NUDUR|BJW0GQR1XS
LB996-RCC M3\jb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF3SSZpKSzVyPUOyMlI{PThizszN Mor0V2FPT0WU
NCI-H2009 NUjYT4dQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlXFTWM2OD1|Mj60PVgyKM7:TR?= MVXTRW5ITVJ?
HTC-C3 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXXWO2J7UUN3ME2zN{44PTF7IN88US=> MV3TRW5ITVJ?
LAMA-84 M2nT[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3vO[mlEPTB;M{SuOFQxPyEQvF2= MXvTRW5ITVJ?
CCRF-CEM MkjkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEftOHlKSzVyPUO0MlU4OTVizszN MoXNV2FPT0WU
AN3-CA NXjuNYxOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3vIRWlEPTB;M{WuNFU3QCEQvF2= MW\TRW5ITVJ?
NCI-H1734 NUDRdJRlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWPuZZFLUUN3ME2zOU4zPTZzIN88US=> MlXmV2FPT0WU
Ca-Ski NFTCeo9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF;STmtKSzVyPUO1MlQyODFizszN MYrTRW5ITVJ?
U-266 NHfvVIdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2r5W2lEPTB;M{WuOlEyPCEQvF2= MYXTRW5ITVJ?
SBC-5 NXjYRmQ{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkXrTWM2OD1|NT63O|gyKM7:TR?= NYHPeYR5W0GQR1XS
GT3TKB MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEXhUoxKSzVyPUO3MlEyPSEQvF2= MoLMV2FPT0WU
MDA-MB-175-VII M2DSWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2X3N2lEPTB;M{euNlI1QCEQvF2= MVnTRW5ITVJ?
PFSK-1 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWi1TnY5UUN3ME2zO{4zPDN3IN88US=> M2TEVXNCVkeHUh?=
IMR-5 NW\1[FdXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUHmPFR1UUN3ME2zO{4zPDh5IN88US=> MWHTRW5ITVJ?
Daudi MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFPhUlFKSzVyPUO3MlM2QTdizszN M4r3TXNCVkeHUh?=
A498 M2TUNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkHvTWM2OD1|Nz63NlE5KM7:TR?= MkjwV2FPT0WU
SCC-4 NFn2eFJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4POUmlEPTB;M{euO|g1OyEQvF2= NHvheHRUSU6JRWK=
COLO-680N M2rvZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4\Ob2lEPTB;M{iuNlg5PSEQvF2= MnvxV2FPT0WU
SK-MES-1 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX;JR|UxRTN6LkOyNVUh|ryP MljaV2FPT0WU
SR MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmnxTWM2OD1|OD61OFk2KM7:TR?= M1n4SnNCVkeHUh?=
LNCaP-Clone-FGC MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXjJR|UxRTN6LkW2N|ch|ryP Mn\RV2FPT0WU
SK-HEP-1 NFjVZolIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXjJR|UxRTN6Lke4NlIh|ryP M1fpNXNCVkeHUh?=
BPH-1 NXX4OphiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXHpT2h[UUN3ME2zPE45OzJ7IN88US=> M3PPfXNCVkeHUh?=
NCI-H1755 MnHRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1jJc2lEPTB;M{muOVgyPyEQvF2= NGTVdGRUSU6JRWK=
LXF-289 NIjLfnhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYLJR|UxRTN7LkiwPFQh|ryP M{DwVHNCVkeHUh?=
SW1088 NU[yOotqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmH2TWM2OD12MD6yNVA4KM7:TR?= Mmf1V2FPT0WU
MOLT-4 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYHJR|UxRTRyLkK5NFEh|ryP MX7TRW5ITVJ?
AsPC-1 NHXiV4tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mly3TWM2OD12MD60OVg{KM7:TR?= NESzWodUSU6JRWK=
HOP-62 MmLnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1PqNWlEPTB;NECuOlU3QCEQvF2= MlnqV2FPT0WU
A172 M1XH[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFXEe3FKSzVyPUSwMlg2OTFizszN Mo[4V2FPT0WU
SN12C NIe4O2ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3PoW2lEPTB;NECuPVM5PSEQvF2= Mk\vV2FPT0WU
MDA-MB-231 NXr2c3JvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWHEcWhOUUN3ME20NE46QDl6IN88US=> NHSyUFdUSU6JRWK=
RPMI-2650 MnT5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGfoNIlKSzVyPUSxMlE2QTNizszN MU\TRW5ITVJ?
KYSE-140 M2S0WGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYPJR|UxRTRzLkixNlMh|ryP M4nwSnNCVkeHUh?=
KINGS-1 Mn7xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3Ow[WlEPTB;NEKuOFY6PyEQvF2= MoHEV2FPT0WU
HSC-3 NG\Z[ZpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2CwOmlEPTB;NEKuOlY3OSEQvF2= NUnxS29uW0GQR1XS
PC-14 MoXmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NETlUGtKSzVyPUSzMlE5QDJizszN MWrTRW5ITVJ?
COR-L105 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX3FOWFqUUN3ME20N{43PTB{IN88US=> NYnLc2ZlW0GQR1XS
BE-13 NH3tOJNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M37VSWlEPTB;NESuNlM4OSEQvF2= MlX5V2FPT0WU
NCI-H661 M4PGN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NU\WflVSUUN3ME20OE4zQTV6IN88US=> NHzwS4tUSU6JRWK=
IST-MEL1 MmLZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGXtTVZKSzVyPUS0MlM2QTlizszN NYCzNm9NW0GQR1XS
HCC1806 MlHNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3:yV2lEPTB;NESuOVg4OyEQvF2= NILJOG9USU6JRWK=
COLO-800 M4jm[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXW2e2FxUUN3ME20OE45PDV|IN88US=> NULqe2dCW0GQR1XS
IST-SL2 NUjGO2JPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWq4UpdTUUN3ME20OU4yOjR5IN88US=> MUHTRW5ITVJ?
8305C NILGTItIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYXJR|UxRTR3LkOwPUDPxE1? MmfEV2FPT0WU
UACC-62 NH\NW4lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MluzTWM2OD12Nj6yPFc2KM7:TR?= NF\NOnBUSU6JRWK=
COR-L23 NV;Wb3FYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYTJR|UxRTR5LkG5PUDPxE1? NUm4WXRFW0GQR1XS
EFE-184 M{XHfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mnj5TWM2OD12Nz6zPFgh|ryP NEjjPVhUSU6JRWK=
DMS-114 M3nuXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWrHcGU2UUN3ME20O{41OTR7IN88US=> M4HhfnNCVkeHUh?=
KYSE-520 M3X4SGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV65dG5iUUN3ME20PE42OzF3IN88US=> NFPqOGtUSU6JRWK=
SNG-M NHfzc5dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3;pfWlEPTB;NEmuOFM1KM7:TR?= MmLJV2FPT0WU
A2058 NH64fo9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVfJR|UxRTR7LkS4PFUh|ryP NY\FVnoxW0GQR1XS

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-EGFR / EGFR / p-IGF1R / IGF1R / p-IRS1 / IRS1 / p-ERK / ERK / p-AKT / AKT; 

PubMed: 26052929     


Effects of linsitinib on EGFR and IGF1R Signaling Pathways. H1975, AR1, AR2 and AR3 cells were treated with control DMSO or linsitinib (2 and 5 μM) for 24 hours. Cell lysates were subjected to Western blot analysis. IGF1R-IRS-1-AKT phosphorylation was effectively inhibited by linsitinib in afatinib resistance cells whereas IRS-1-AKT phosphorylation was up-regulated by linsitinib in H1975 parental cells.

p-IGF1R / IGF1R / p-mTOR / mTOR ; 

PubMed: 28440057     


Linsitinib inhibits the activation of ERK and PI3K pathways. After treatment of Linsitinib at 0.1 or 1.0 μmol/L for 72 h, the phosphorylation of insulin‐like growth factor‐1 receptor (IGF‐1R), ERK1/2, and AKT/mTOR pathways were analyzed in TE‐13, TE‐1, and KYSE‐510 cell lines by western blot.

cleaved caspase-3 / cleaved PARP; 

PubMed: 28440057     


Reduced apoptosis in Linsitinib-resistant esophageal squamous cell carcinoma cells. After treatment of Linsitinib at 0.1 or 1.0 μmol/L for 72 h, cleaved PARP and activated Caspase‐3 were examined in TE-13, TE-1, and KYSE-510 cells by western blot. Tubulin was used as a loading control.

pSrc(Y416) / Src; 

PubMed: 26515601     


A549, H226Br, and H1975 cells were treated with 1 or 2 μM linsitinib (diluted in RPMI 1640 medium containing 10% FBS) for 12 or 24 h. Before harvest, cells were further stimulated with 10% FBS for 20 min. Cells were lysed with modified RIPA buffer and the protein expression was determined by Western blot analysis.

p-STAT3(Y705) / STAT3 ; 

PubMed: 26041671     


H226B and H460 cells were subject to daily treatment with linsitinib (1 μM) for 1-5 days.

pS6 / S6; 

PubMed: 21257723     


Western blot of NCI-H292 cells following 30 minutes of exposure to OSI-906 shows target inhibition of pIGF-1R and pIR at all doses as well as inhibition of downstream targets pAKT and pS6.

26052929 28440057 26515601 26041671 21257723
Immunofluorescence
FoxO1; 

PubMed: 27535223     


After starvation, control or βIRKO β-cell lines were treated with insulin (10 nm) in combination with high glucose (450 mg/dL), in the presence or absence of PI3K inhibitor LY294002, insulin receptor, and IGF1 receptor dual inhibitor OSI-906, Akt inhibitor MK2206, or MEK1/2 inhibitor U0126 for 30 min.  A, representative pictures of β-cells immunostained for FoxO1 (red) and DAPI (blue). The scale bar indicates 20 μm.

27535223
Growth inhibition assay
Cell viability; 

PubMed: 26136493     


InsR/IGF1R dual inhibitors, OSI-906 and BMS-754807, dose-dependently inhibited T4105 viability.

26136493
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]

Protocol

Kinase Assay:[1]
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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:[1]
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  • 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.
    (Only for Reference)
Animal Research:[1]
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  • Animal Models: IGF-1R-driven full-length human IGF-1R (LISN) xenograft mouse model
  • Formulation: 25 mM tartaric acid
  • Dosages: 25 mg / kg and 75 mg / kg
  • Administration: Orally administrated at once-daily oral dose for 14 days
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 84 mg/mL (199.29 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
30% PEG 400+0.5% Tween 80+5% Propylene glycol
For best results, use promptly after mixing.
30mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 421.49
Formula

C26H23N5O

CAS No. 867160-71-2
Storage powder
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02546544 Completed Drug: Linsitinib 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 Drug: ASP7487 Velcade Dexamethasone Multiple Myeloma University Health Network Toronto|Multiple Myeloma Research Consortium|Astellas Pharma Inc September 2012 Phase 1|Phase 2
NCT01529684 Completed Drug: radio-labeled OSI-906|Drug: OSI-906 Advanced Solid Tumors|Pharmacokinetics of 14C-OSI-906 Astellas Pharma Global Development Inc.|Astellas Pharma Inc March 19 2012 Phase 1
NCT01221077 Completed Drug: OSI-906|Drug: Erlotinib|Drug: Placebo NSCLC|Non Small Cell Lung Cancer Astellas Pharma Inc April 8 2011 Phase 2

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

Tel: +1-832-582-8158 Ext:3

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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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID