Linsitinib (OSI-906)

For research use only.

Catalog No.S1091

134 publications

Linsitinib (OSI-906) Chemical Structure

CAS No. 867160-71-2

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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Selleck's Linsitinib (OSI-906) has been cited by 134 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
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MZ2-MEL NWnROWtJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3\HRmlEPTB;Mz65NlA5PiEQvF2= NXfWZZhORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7MU[0OE8oRlODTlfFVlww[T5?
TGW NIDQcXpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYn1Smg4UUN3ME20MlAyOzFzIN88US=> MXK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFkyPjR2Lze+V2FPT0WUPD;hQi=>
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NB13 NH\LeYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1TPNGlEPTB;ND6yOlg5PyEQvF2= NHLpPZU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODlzNkS0M{c,W0GQR1XSQE9iRg>?
NTERA-S-cl-D1 NF7QPJlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX:xN2JTUUN3ME20MlI5PjF3IN88US=> NEP1Omo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODlzNkS0M{c,W0GQR1XSQE9iRg>?
NCI-H1648 NYTuVYpqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXLPb3ZsUUN3ME20MlI6QDF7IN88US=> Mn7OQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6OTZ2ND:nQnNCVkeHUkyvZV4>
LCLC-103H NITNWlBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkDHTWM2OD12LkOyNVk2KM7:TR?= NVfNTohsRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7MU[0OE8oRlODTlfFVlww[T5?
LS-411N MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmHETWM2OD12LkS0PFg2KM7:TR?= MUK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFkyPjR2Lze+V2FPT0WUPD;hQi=>
NCI-H1092 MoTFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{ficWlEPTB;ND60OVY5PyEQvF2= M{TGNFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQTF4NESvK|5USU6JRWK8M4E,
PANC-10-05 MoTSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX\3TYVbUUN3ME20MlY6QDRizszN NInxZWo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODlzNkS0M{c,W0GQR1XSQE9iRg>?
DK-MG NETTUIpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUP3dJh[UUN3ME20MlgxQTN|IN88US=> NWq2e2tSRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7MU[0OE8oRlODTlfFVlww[T5?
OVCAR-5 NVfwdFA5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWTJR|UxRTRwOEGyNlYh|ryP MY[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFkyPjR2Lze+V2FPT0WUPD;hQi=>
CAL-39 NYPjNYdrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFLOU4ZKSzVyPUSuPFc3PyEQvF2= MlTMQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6OTZ2ND:nQnNCVkeHUkyvZV4>
TE-441-T NUDBO5B1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGHEW4pKSzVyPUSuPVA2OzdizszN M2\3[VxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQTF4NESvK|5USU6JRWK8M4E,
MOLT-16 MmnnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1zWTGlEPTB;ND65OVI2OyEQvF2= M3fhdVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQTF4NESvK|5USU6JRWK8M4E,
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CAPAN-1 NE\FNWlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUXJR|UxRTVwMkW3NFch|ryP NWf6TY5FRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7MU[0OE8oRlODTlfFVlww[T5?
PSN1 MnvaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFHFcGVKSzVyPUWuNlczOzVizszN NX3ncFM2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7MU[0OE8oRlODTlfFVlww[T5?
NCI-H292 NGT5S25Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX7JR|UxRTVwM{CwOFQh|ryP NF\TUZQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODlzNkS0M{c,W0GQR1XSQE9iRg>?
CPC-N MkPRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVvDRWR2UUN3ME21MlM6PDF7IN88US=> MYi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFkyPjR2Lze+V2FPT0WUPD;hQi=>
DoTc2-4510 MluxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHiyW2lKSzVyPUWuOFU{PzFizszN NWOxPYFmRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7MU[0OE8oRlODTlfFVlww[T5?
LB1047-RCC NUTxRYw1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4fwZ2lEPTB;NT61OVk{OyEQvF2= MlT5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6OTZ2ND:nQnNCVkeHUkyvZV4>
MHH-ES-1 M4KzPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIraZXJKSzVyPUWuOVk6ODdizszN MV68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFkyPjR2Lze+V2FPT0WUPD;hQi=>
NMC-G1 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHfqZllKSzVyPUWuO|AzOjdizszN NX7LPVJrRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7MU[0OE8oRlODTlfFVlww[T5?
SW1710 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NITSXpFKSzVyPUWuO|Q4PTFizszN MnnxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6OTZ2ND:nQnNCVkeHUkyvZV4>
YAPC MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXnJR|UxRTVwN{[yNFEh|ryP NIThSnM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODlzNkS0M{c,W0GQR1XSQE9iRg>?
22RV1 NUTO[ZZCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF7HTYxKSzVyPUWuPFAxOTlizszN MVq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFkyPjR2Lze+V2FPT0WUPD;hQi=>
COLO-679 MlnyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVjJR|UxRTVwOEi5OFgh|ryP NHfZWmo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODlzNkS0M{c,W0GQR1XSQE9iRg>?
TCCSUP NGPHW2NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYDac2pKUUN3ME21Mlk{OjV7IN88US=> NFvXb4I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODlzNkS0M{c,W0GQR1XSQE9iRg>?
C2BBe1 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlzRTWM2OD13LkmzPVch|ryP NHrBNWY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODlzNkS0M{c,W0GQR1XSQE9iRg>?
TE-15 MmDtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3LleGlEPTB;Nj6wOlYxPSEQvF2= MUS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFkyPjR2Lze+V2FPT0WUPD;hQi=>
SCLC-21H NXTWW3BIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWDJR|UxRTZwMUC4OFMh|ryP NV62VWsxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7MU[0OE8oRlODTlfFVlww[T5?
EoL-1-cell MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MojQTWM2OD14LkG2OVY{KM7:TR?= MXq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFkyPjR2Lze+V2FPT0WUPD;hQi=>
NKM-1 NITDXYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUXiRXlQUUN3ME22MlE3PzFizszN MlP1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6OTZ2ND:nQnNCVkeHUkyvZV4>
NCI-H1304 MnPMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFezSlBKSzVyPU[uNlc1OjhizszN NVTLZpZ7RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7MU[0OE8oRlODTlfFVlww[T5?
NB6 NEj6d4JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MofNTWM2OD14LkK5OlIzKM7:TR?= NUnST2JRRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7MU[0OE8oRlODTlfFVlww[T5?
NALM-6 NWXYN2s5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHvqW3BKSzVyPU[uN|MzOyEQvF2= MV28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFkyPjR2Lze+V2FPT0WUPD;hQi=>
NCI-H522 MkHFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn3TTWM2OD14LkOzN|A3KM7:TR?= M2PJU|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQTF4NESvK|5USU6JRWK8M4E,
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... 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
  • 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 powder
in 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

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Step 2: Enter the in vivo formulation ()
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Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
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Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

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

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

If you have any other enquiries, please leave a message.

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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