Linsitinib (OSI-906)

Catalog No.S1091

For research use only.

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

CAS No. 867160-71-2

Selleck's Linsitinib (OSI-906) has been cited by 147 publications

Purity & Quality Control

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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

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 NYDDfJByT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXfj[nlDUUN3ME2wMlAzQDB4IN88US=> MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFkyPjR2Lze+V2FPT0WUPD;hQi=>
KS-1 M3;uV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3jIXGlEPTB;MD6wN|g{PSEQvF2= NWfORnRrRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7MU[0OE8oRlODTlfFVlww[T5?
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HMV-II MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFrwdJJKSzVyPUCuNFg5PDZizszN NFfXUXE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODlzNkS0M{c,W0GQR1XSQE9iRg>?
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MZ2-MEL Ml\kS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXrTdVEyUUN3ME2zMlkzODh4IN88US=> NFLYe|g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODlzNkS0M{c,W0GQR1XSQE9iRg>?
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GP5d M3TuRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1fuW2lEPTB;ND6wOVM3OiEQvF2= MmG4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6OTZ2ND:nQnNCVkeHUkyvZV4>
BB49-HNC M2m5fWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M13jWmlEPTB;ND6xOVIyOyEQvF2= M3\yRVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQTF4NESvK|5USU6JRWK8M4E,
NB13 NEO0U2JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXTJR|UxRTRwMk[4PFch|ryP NFrKZWQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODlzNkS0M{c,W0GQR1XSQE9iRg>?
NTERA-S-cl-D1 NHTHO5JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYPJR|UxRTRwMki2NVUh|ryP NWP5UFBpRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7MU[0OE8oRlODTlfFVlww[T5?
NCI-H1648 M2DVTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXLJR|UxRTRwMkm4NVkh|ryP NInhN5I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODlzNkS0M{c,W0GQR1XSQE9iRg>?
LCLC-103H MmS2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn7jTWM2OD12LkOyNVk2KM7:TR?= NGrkUYE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODlzNkS0M{c,W0GQR1XSQE9iRg>?
LS-411N NH72S2tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHzhbHhKSzVyPUSuOFQ5QDVizszN MV:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFkyPjR2Lze+V2FPT0WUPD;hQi=>
NCI-H1092 M2fiN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWXJR|UxRTRwNEW2PFch|ryP NUnr[Ww6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7MU[0OE8oRlODTlfFVlww[T5?
PANC-10-05 M3\PTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX\oNWtkUUN3ME20MlY6QDRizszN MWq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFkyPjR2Lze+V2FPT0WUPD;hQi=>
DK-MG MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2rKemlEPTB;ND64NFk{OyEQvF2= M{nNNFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQTF4NESvK|5USU6JRWK8M4E,
OVCAR-5 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHjMNJJKSzVyPUSuPFEzOjZizszN NIfpfVY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODlzNkS0M{c,W0GQR1XSQE9iRg>?
CAL-39 NGXJV4VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH\3TFFKSzVyPUSuPFc3PyEQvF2= NEH2OpQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODlzNkS0M{c,W0GQR1XSQE9iRg>?
TE-441-T MoHUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFTScVBKSzVyPUSuPVA2OzdizszN MmL3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6OTZ2ND:nQnNCVkeHUkyvZV4>
MOLT-16 NGfRVVRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX3JR|UxRTRwOUWyOVMh|ryP M{jNU|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQTF4NESvK|5USU6JRWK8M4E,
MCF7 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkTjTWM2OD13LkG0OVE4KM7:TR?= MWq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFkyPjR2Lze+V2FPT0WUPD;hQi=>
CAPAN-1 NUTGRndjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVXJR|UxRTVwMkW3NFch|ryP M{HwVlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQTF4NESvK|5USU6JRWK8M4E,
PSN1 Mn\HS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGm3eoFKSzVyPUWuNlczOzVizszN NVv0TmFURGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7MU[0OE8oRlODTlfFVlww[T5?
NCI-H292 NUTVUpFOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4jMNWlEPTB;NT6zNFA1PCEQvF2= M2XqSlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQTF4NESvK|5USU6JRWK8M4E,
CPC-N MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFzM[nZKSzVyPUWuN|k1OTlizszN MYi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFkyPjR2Lze+V2FPT0WUPD;hQi=>
DoTc2-4510 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWrIb3dVUUN3ME21MlQ2OzdzIN88US=> MVG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFkyPjR2Lze+V2FPT0WUPD;hQi=>
LB1047-RCC NGm0dWNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2XiT2lEPTB;NT61OVk{OyEQvF2= M{fUNFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQTF4NESvK|5USU6JRWK8M4E,
MHH-ES-1 Mn7VS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV3BW29uUUN3ME21MlU6QTB5IN88US=> NXm5TI1RRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7MU[0OE8oRlODTlfFVlww[T5?
NMC-G1 MlSwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mk\vTWM2OD13LkewNlI4KM7:TR?= M1TBeVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQTF4NESvK|5USU6JRWK8M4E,
SW1710 M4\Gcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml;XTWM2OD13Lke0O|UyKM7:TR?= NUHDTWUyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7MU[0OE8oRlODTlfFVlww[T5?
YAPC Mk[1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXrJR|UxRTVwN{[yNFEh|ryP MmjQQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6OTZ2ND:nQnNCVkeHUkyvZV4>
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COLO-679 M4ryeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVH3NnBsUUN3ME21Mlg5QTR6IN88US=> NXLieYNORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7MU[0OE8oRlODTlfFVlww[T5?
TCCSUP M4HqU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFHwdFBKSzVyPUWuPVMzPTlizszN M2nCSlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQTF4NESvK|5USU6JRWK8M4E,
C2BBe1 M4Tmbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXjvfphNUUN3ME21Mlk{QTdizszN Ml22QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6OTZ2ND:nQnNCVkeHUkyvZV4>
TE-15 NFTpT5ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWDJR|UxRTZwME[2NFUh|ryP NVzEVlE2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7MU[0OE8oRlODTlfFVlww[T5?
SCLC-21H M37QZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX\JR|UxRTZwMUC4OFMh|ryP NWLjOmYyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7MU[0OE8oRlODTlfFVlww[T5?
EoL-1-cell MkjFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWXJR|UxRTZwMU[1OlMh|ryP Mn;KQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6OTZ2ND:nQnNCVkeHUkyvZV4>
NKM-1 MkXBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3y1OmlEPTB;Nj6xOlcyKM7:TR?= NEXOVFY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODlzNkS0M{c,W0GQR1XSQE9iRg>?
NCI-H1304 MmHUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWfJR|UxRTZwMke0Nlgh|ryP MYG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFkyPjR2Lze+V2FPT0WUPD;hQi=>
NB6 M2qzbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoSxTWM2OD14LkK5OlIzKM7:TR?= MlXQQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6OTZ2ND:nQnNCVkeHUkyvZV4>
NALM-6 M2ntVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEDoVHdKSzVyPU[uN|MzOyEQvF2= MXy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFkyPjR2Lze+V2FPT0WUPD;hQi=>
NCI-H522 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXLJR|UxRTZwM{OzNFYh|ryP NH3mdWc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODlzNkS0M{c,W0GQR1XSQE9iRg>?
MV-4-11 M3LE[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4LBPGlEPTB;Nj6zO|A4QSEQvF2= NXLUb2E2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7MU[0OE8oRlODTlfFVlww[T5?
LB2241-RCC M37wSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoOwTWM2OD14LkO4OlY4KM7:TR?= MX:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFkyPjR2Lze+V2FPT0WUPD;hQi=>
NCI-H1417 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV3JR|UxRTZwNEC4OFch|ryP NWrt[5B5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7MU[0OE8oRlODTlfFVlww[T5?
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NCI-H441 MmPNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWjJR|UxRTdwM{SwOlUh|ryP MUm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFkyPjR2Lze+V2FPT0WUPD;hQi=>
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KARPAS-45 MlXBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWXtTGl3UUN3ME23MlY2QTJ7IN88US=> MXi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFkyPjR2Lze+V2FPT0WUPD;hQi=>
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RT-112 NV\sZWI6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1nWc2lEPTB;OD6wPVY4PyEQvF2= MVS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFkyPjR2Lze+V2FPT0WUPD;hQi=>
NCI-H1437 MnPXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2DtfGlEPTB;OD6wPVc6PSEQvF2= Mnq3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6OTZ2ND:nQnNCVkeHUkyvZV4>
SNU-449 MkDGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX3JR|UxRThwMkiyO|Ih|ryP MniwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6OTZ2ND:nQnNCVkeHUkyvZV4>
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HuO-3N1 NIPjbmFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmLJTWM2OD16LkO3PFQ1KM7:TR?= NGfHUHM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODlzNkS0M{c,W0GQR1XSQE9iRg>?
COLO-792 NH7XNm5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mkj0TWM2OD16LkSxOVI4KM7:TR?= NXnaXVY2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7MU[0OE8oRlODTlfFVlww[T5?
MIA-PaCa-2 M1LrNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkXBTWM2OD16Lki1OVA5KM7:TR?= NXrvZY5GRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7MU[0OE8oRlODTlfFVlww[T5?
SK-N-FI M2j5cGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYHJR|UxRTlwMESyOUDPxE1? NXi2d5dRRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7MU[0OE8oRlODTlfFVlww[T5?
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NCI-H28 MlzFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NILWfWhKSzVyPUmuNVA1PjlizszN MWW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFkyPjR2Lze+V2FPT0WUPD;hQi=>
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NCI-H1993 NWjGTIY{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGjqfJNKSzVyPUmuOFQzPjFizszN NVrKZnV[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7MU[0OE8oRlODTlfFVlww[T5?
no-11 M{fOR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkLMTWM2OD17LkS3NVIh|ryP NVLMc4dRRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7MU[0OE8oRlODTlfFVlww[T5?
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NCCIT MlTGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmmxTWM2OD17LkWzNVY6KM7:TR?= M3i5XVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQTF4NESvK|5USU6JRWK8M4E,
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NCI-H1522 NHHzTYlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NImxN5VKSzVyPUGwMlM4ODdizszN NFzRdZo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODlzNkS0M{c,W0GQR1XSQE9iRg>?
NCI-H810 NX\IcoI3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoCxTWM2OD1zMD6zPVA4KM7:TR?= NVmw[W1HRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7MU[0OE8oRlODTlfFVlww[T5?
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MZ1-PC MnfWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEL1TnpKSzVyPUGwMlk2PzFizszN MoTtQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6OTZ2ND:nQnNCVkeHUkyvZV4>
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GI-1 MlfxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV7JR|UxRTFzLki2NVUh|ryP NHz2RoQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODlzNkS0M{c,W0GQR1XSQE9iRg>?
BB65-RCC NVXyUlBqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYfJR|UxRTF{LkC5NVYh|ryP MojsQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6OTZ2ND:nQnNCVkeHUkyvZV4>
NCI-H1651 NGC2S|ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVLVOHU5UUN3ME2xNk4zPDd6IN88US=> M1LzflxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQTF4NESvK|5USU6JRWK8M4E,
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Assay
Methods Test Index PMID
Western blot p-EGFR / EGFR / p-IGF1R / IGF1R / p-IRS1 / IRS1 / p-ERK / ERK / p-AKT / AKT ; p-IGF1R / IGF1R / p-mTOR / mTOR ; cleaved caspase-3 / cleaved PARP ; pSrc(Y416) / Src ; p-STAT3(Y705) / STAT3 ; pS6 / S6 26052929 28440057 26515601 26041671 21257723
Immunofluorescence FoxO1 27535223
Growth inhibition assay Cell 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 (from reference)

Kinase Assay:[1]
  • 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]
  • 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]
  • 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
  • (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):
5%DMSO+40%PEG300+5%Tween80+50%ddH2O
For best results, use promptly after mixing.

6.25mg/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 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1(CC(C1)C2=NC(=C3N2C=CN=C3N)C4=CC5=C(C=C4)C=CC(=N5)C6=CC=CC=C6)O

In vivo Formulation Calculator (Clear solution)

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

mg/kg g μL

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.

Molarity Calculator

Mass Concentration Volume Molecular Weight

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

(data from https://clinicaltrials.gov, updated on 2021-09-06)

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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