Linsitinib (OSI-906)

For research use only. Not for use in humans.

目录号：S1091

CAS No. 867160-71-2

Linsitinib (OSI-906)是一种选择性IGF-1R抑制剂，在无细胞试验中IC50为35 nM；对InsR抑制作用适中，IC50为75 nM，对Abl，ALK，BTK，EGFR， FGFR1/2，PKA等没有抑制活性。Phase 3。

规格

价格

库存

购买数量

10mM (1mL in DMSO)	RMB 1550.54	现货
5mg	RMB 1393.48	现货
10mg	RMB 2226.24	现货
50mg	RMB 5899.91	现货
200mg	RMB 13677.3	现货
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客户使用Selleck生产的Linsitinib (OSI-906)发表文献147篇：

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Nat Commun, 2019, 10(1):518

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Nat Commun, 2019, 10(1):2532

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Cancers (Basel), 2019, 11(9)

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FASEB J, 2019, 33(10):11210-11222

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Cells, 2019, 8(4)

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J Gerontol A Biol Sci Med Sci, 2019, 74(9):1375-1385

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Sci Rep, 2019, 9(1):5309

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Mediators Inflamm, 2019, 2019:5497467

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J Agric Food Chem, 2019, 67(34):9510-9521

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Mol Med Rep, 2019, 19(4):2825-2830

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Exp Ther Med, 2019, 17(3):1663-1669

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Nat Commun, 2018, 9(1):1777

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Genes Dev, 2018, 32(13-14):915-928

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Biomaterials, 2018, 155:64-79

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Cancers (Basel), 2018, 10(9)

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Cell Oncol, 2018, 41(3):283-296

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Endocrinology, 2018, 159(1):285-296

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Front Endocrinol, 2018, 9:178

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Cell Signal, 2018, 52:12-22

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PLoS One, 2018, 13(2):e0191890

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Oncotarget, 2018, 9(10):8810-8822

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Oncotarget, 2018,

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Mol Cell, 2017, 67(3):512-527

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Theranostics, 2017, 7(4):974-986

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Cancer Res, 2017, 77(15):4014-4025

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Oncogene, 2017,

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Br J Pharmacol, 2017, 174(4):328-340

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Diabetologia, 2017, 60(8):1442-1453

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Mol Cancer Ther, 2016,

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产品安全说明书

IGF-1R抑制剂选择性比较

生物活性

产品描述

靶点

IGF-1R ^[1] (Cell-free assay)	Insulin Receptor ^[1] (Cell-free assay)	IRR ^[1] (Cell-free assay)
35 nM	75 nM	75 nM

体外研究

OSI-906 抑制IGF-IR自磷酸化和下游信号蛋白AKT, ERK1/2和S6激酶的激活，IC50为0.028到 0.13 μM。OSI-906通过与C-螺旋相互作用而使靶点蛋白形成中间结构形态。OSI-906作用于肝脏微粒体，具有良好的代谢稳定性。OSI-906浓度为1μM时，完全抑制IR 和IGF-IR磷酸化。OSI-906抑制一些肿瘤细胞系增殖，包括非小细胞肺癌和结肠直肠癌(CRC)肿瘤细胞系，EC50为0.021到 0.810 μM。^[1]

Cell Data

Cell Lines	Assay Type	Incubation Time	Activity Description	PMID
A4-Fuk	M3PhNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		M1zLWmlEPTB;MD6wNlgxPiEQvF2=	MoXDQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6OTZ2ND:nQnNCVkeHUkyvZV4>
KS-1	MmfNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		NUTROnVxUUN3ME2wMlA{QDN3IN88US=>	NVj0WmRnRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7MU[0OE8oRlODTlfFVlww[T5?
TE-11	MkHyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		MWLJR\|UxRTBwMEe4NlIh\|ryP	MXm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFkyPjR2Lze+V2FPT0WUPD;hQi=>
EW-1	MmKxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		Ml\ZTWM2OD1yLkC4OVg2KM7:TR?=	NWf3Uo9[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7MU[0OE8oRlODTlfFVlww[T5?
HMV-II	MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		Mki1TWM2OD1yLkC4PFQ3KM7:TR?=	NUXjNIpXRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7MU[0OE8oRlODTlfFVlww[T5?
COLO-205	MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		MVPJR\|UxRTBwMUC0OVQh\|ryP	MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFkyPjR2Lze+V2FPT0WUPD;hQi=>
ES1	NGfa[m9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		NYLVW491UUN3ME2wMlExPjl4IN88US=>	MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFkyPjR2Lze+V2FPT0WUPD;hQi=>
GDM-1	MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		NXXSWHVpUUN3ME2wMlE{Pjd{IN88US=>	NV6zdWFIRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7MU[0OE8oRlODTlfFVlww[T5?
ML-2	MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		NV7Xc5hJUUN3ME2wMlE2QDl4IN88US=>	MlzKQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6OTZ2ND:nQnNCVkeHUkyvZV4>
Saos-2	NX:3[3RWT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		M3LHXGlEPTB;MD6xOlUzPiEQvF2=	MUe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFkyPjR2Lze+V2FPT0WUPD;hQi=>
NCI-H1355	MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		NEm4cnBKSzVyPUCuNVgyOzVizszN	MnvsQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6OTZ2ND:nQnNCVkeHUkyvZV4>
G-401	NX[xSWZRT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		MWfJR\|UxRTBwMUiyN{DPxE1?	NYjT[nhxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7MU[0OE8oRlODTlfFVlww[T5?
EW-16	MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		NXTlVnAxUUN3ME2wMlE5Pzd5IN88US=>	MmnyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6OTZ2ND:nQnNCVkeHUkyvZV4>
EW-7	NIDMV4VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		M3jGT2lEPTB;MD6xPFg5OSEQvF2=	MVK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFkyPjR2Lze+V2FPT0WUPD;hQi=>
NCI-H727	NW\sd5B{T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		NELVVZFKSzVyPUCuNVk4QTRizszN	MoXZQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6OTZ2ND:nQnNCVkeHUkyvZV4>
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NCI-H1648	NEDOT\|lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		NF\2VGtKSzVyPUSuNlk5OTlizszN	MnPPQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6OTZ2ND:nQnNCVkeHUkyvZV4>
LCLC-103H	MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		MnniTWM2OD12LkOyNVk2KM7:TR?=	NE\Y[Hc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODlzNkS0M{c,W0GQR1XSQE9iRg>?
LS-411N	NE\ablhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		NYTxfWhKUUN3ME20MlQ1QDh3IN88US=>	NWLhdYRnRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7MU[0OE8oRlODTlfFVlww[T5?
NCI-H1092	NVuySm9rT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		M{DGUmlEPTB;ND60OVY5PyEQvF2=	M{PZb\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQTF4NESvK\|5USU6JRWK8M4E,
PANC-10-05	MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		MmSzTWM2OD12Lk[5PFQh\|ryP	MlexQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6OTZ2ND:nQnNCVkeHUkyvZV4>
DK-MG	NVnaSXRIT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		NIm3bJdKSzVyPUSuPFA6OzNizszN	MornQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6OTZ2ND:nQnNCVkeHUkyvZV4>
OVCAR-5	NInlNG9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		NEPidHBKSzVyPUSuPFEzOjZizszN	NVPFU4xLRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7MU[0OE8oRlODTlfFVlww[T5?
CAL-39	MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		MkThTWM2OD12Lki3Olch\|ryP	MojHQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6OTZ2ND:nQnNCVkeHUkyvZV4>
TE-441-T	M{HmVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		NWLtU\|ZyUUN3ME20MlkxPTN5IN88US=>	NFnZZ3M9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODlzNkS0M{c,W0GQR1XSQE9iRg>?
MOLT-16	MlLLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		NWTYNoFiUUN3ME20Mlk2OjV\|IN88US=>	MlzZQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6OTZ2ND:nQnNCVkeHUkyvZV4>
MCF7	MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		M4HCdGlEPTB;NT6xOFUyPyEQvF2=	M2Xud\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQTF4NESvK\|5USU6JRWK8M4E,
CAPAN-1	MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		MmLlTWM2OD13LkK1O\|A4KM7:TR?=	NYjoVohNRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7MU[0OE8oRlODTlfFVlww[T5?
PSN1	MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		NF7LT4tKSzVyPUWuNlczOzVizszN	MljHQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6OTZ2ND:nQnNCVkeHUkyvZV4>
NCI-H292	NELsWZBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		MX\JR\|UxRTVwM{CwOFQh\|ryP	MXu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFkyPjR2Lze+V2FPT0WUPD;hQi=>
CPC-N	MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		NULacmlrUUN3ME21MlM6PDF7IN88US=>	M2T3ZlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQTF4NESvK\|5USU6JRWK8M4E,
DoTc2-4510	M2OwfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		NH[0PFZKSzVyPUWuOFU{PzFizszN	M{PxeVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQTF4NESvK\|5USU6JRWK8M4E,
LB1047-RCC	M4i2O2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7		NWjLSmp5UUN3ME21MlU2QTN\|IN88US=>	NYHRdGt5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7MU[0OE8oRlODTlfFVlww[T5?
MHH-ES-1	M33We2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7		NXX6TZhFUUN3ME21MlU6QTB5IN88US=>	MkGyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6OTZ2ND:nQnNCVkeHUkyvZV4>
NMC-G1	Mnj6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		MmLVTWM2OD13LkewNlI4KM7:TR?=	NFXBWXY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODlzNkS0M{c,W0GQR1XSQE9iRg>?
SW1710	NF7sclNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		MUXJR\|UxRTVwN{S3OVEh\|ryP	MkK3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6OTZ2ND:nQnNCVkeHUkyvZV4>
YAPC	MmHMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		M2P6RmlEPTB;NT63OlIxOSEQvF2=	NF;NNpA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODlzNkS0M{c,W0GQR1XSQE9iRg>?
22RV1	MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		MUHJR\|UxRTVwOECwNVkh\|ryP	MlHEQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6OTZ2ND:nQnNCVkeHUkyvZV4>
COLO-679	M4DrO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7		M2LLUWlEPTB;NT64PFk1QCEQvF2=	NX7RXm9rRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7MU[0OE8oRlODTlfFVlww[T5?
TCCSUP	MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		MlyyTWM2OD13LkmzNlU6KM7:TR?=	M17iPVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQTF4NESvK\|5USU6JRWK8M4E,
C2BBe1	MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		M2LrR2lEPTB;NT65N\|k4KM7:TR?=	MmPlQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6OTZ2ND:nQnNCVkeHUkyvZV4>
TE-15	M13UR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7		MVHJR\|UxRTZwME[2NFUh\|ryP	NIH6emI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODlzNkS0M{c,W0GQR1XSQE9iRg>?
SCLC-21H	NFTpe5ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		MkDxTWM2OD14LkGwPFQ{KM7:TR?=	M122NlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQTF4NESvK\|5USU6JRWK8M4E,
EoL-1-cell	MmDHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		M{LyTmlEPTB;Nj6xOlU3OyEQvF2=	MofTQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6OTZ2ND:nQnNCVkeHUkyvZV4>
NKM-1	M4HibGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		NXTyOJJTUUN3ME22MlE3PzFizszN	M3XxWVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQTF4NESvK\|5USU6JRWK8M4E,
NCI-H1304	MkSxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		NHjib4hKSzVyPU[uNlc1OjhizszN	M{jHblxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQTF4NESvK\|5USU6JRWK8M4E,
NB6	M{fSSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		NGrjVmVKSzVyPU[uNlk3OjJizszN	M3O3VVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQTF4NESvK\|5USU6JRWK8M4E,
NALM-6	NX76XVByT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		M362XmlEPTB;Nj6zN\|I{KM7:TR?=	MonnQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6OTZ2ND:nQnNCVkeHUkyvZV4>
NCI-H522	MljOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		MmnqTWM2OD14LkOzN\|A3KM7:TR?=	MlG5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6OTZ2ND:nQnNCVkeHUkyvZV4>
MV-4-11	MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		MmrsTWM2OD14LkO3NFc6KM7:TR?=	NGS4Toc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODlzNkS0M{c,W0GQR1XSQE9iRg>?
LB2241-RCC	NVXDUnRCT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		MV3JR\|UxRTZwM{i2Olch\|ryP	NWnWTIlQRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7MU[0OE8oRlODTlfFVlww[T5?
NCI-H1417	MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		NWDkfGRGUUN3ME22MlQxQDR5IN88US=>	M36wTVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQTF4NESvK\|5USU6JRWK8M4E,
HT-1197	Mn;6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		MkTuTWM2OD14LkW3NVIzKM7:TR?=	NFfIfYk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODlzNkS0M{c,W0GQR1XSQE9iRg>?
P30-OHK	MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		MYDJR\|UxRTZwNkK3O{DPxE1?	NUn2WHdyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7MU[0OE8oRlODTlfFVlww[T5?
ALL-PO	NV73WFJUT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		NG\vOmZKSzVyPU[uO\|E6OTZizszN	NHu1WFY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODlzNkS0M{c,W0GQR1XSQE9iRg>?
OVCAR-4	M1jLVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		M{fQc2lEPTB;Nj63OVQxPSEQvF2=	M{jTfFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQTF4NESvK\|5USU6JRWK8M4E,
HCC2157	NYT1OVFFT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		MWjJR\|UxRTZwN{e0O\|Uh\|ryP	NYTTTnMzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7MU[0OE8oRlODTlfFVlww[T5?
NCI-H838	NFzzcXpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		NVG2SZJlUUN3ME22Mlk3PDlizszN	MnvsQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6OTZ2ND:nQnNCVkeHUkyvZV4>
NCI-H1299	MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		MofqTWM2OD14Lkm3NFkh\|ryP	Mo\jQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6OTZ2ND:nQnNCVkeHUkyvZV4>
SW954	M3vLSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		M{[3NmlEPTB;Nz6yNFA3QCEQvF2=	NGe5W3Q9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODlzNkS0M{c,W0GQR1XSQE9iRg>?
NCI-H441	NWLG[m5kT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		NFXWUlFKSzVyPUeuN\|QxPjVizszN	M4OwOVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQTF4NESvK\|5USU6JRWK8M4E,
SK-MEL-2	NGDB[oVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		NEXzb4dKSzVyPUeuOFg{PzNizszN	NIrrdVY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODlzNkS0M{c,W0GQR1XSQE9iRg>?
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CAL-54	NE\Dc4RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		NVG5emxsUUN3ME23MlgzQTd5IN88US=>	MnTMQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6OTZ2ND:nQnNCVkeHUkyvZV4>
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HDLM-2	NHnYSZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		MkPITWM2OD1\|MD65O\|I2KM7:TR?=	NF[0dXY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODlzNkS0M{c,W0GQR1XSQE9iRg>?
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LB996-RCC	M1f0V2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7		M4TJXGlEPTB;M{KuNlM2QCEQvF2=	MXK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFkyPjR2Lze+V2FPT0WUPD;hQi=>
NCI-H2009	MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		NI\KNWZKSzVyPUOyMlQ6QDFizszN	NYjLfmRORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7MU[0OE8oRlODTlfFVlww[T5?
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SK-HEP-1	NEnzTGFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		MkfyTWM2OD1\|OD63PFIzKM7:TR?=	M3\Ib\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQTF4NESvK\|5USU6JRWK8M4E,
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MDA-MB-231	MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		MYTJR\|UxRTRyLkm4PVgh\|ryP	MYK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFkyPjR2Lze+V2FPT0WUPD;hQi=>
RPMI-2650	MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		NX\sVoNYUUN3ME20NU4yPTl\|IN88US=>	NGL2Rmk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODlzNkS0M{c,W0GQR1XSQE9iRg>?
KYSE-140	MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		NYLzNG1zUUN3ME20NU45OTJ\|IN88US=>	M4\vc\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQTF4NESvK\|5USU6JRWK8M4E,
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NCI-H661	MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		NWm0RVFpUUN3ME20OE4zQTV6IN88US=>	MmXyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6OTZ2ND:nQnNCVkeHUkyvZV4>
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RD	NXTsc3BNeUiWUzDhd5NigQ>?		MVzxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhWkRiY3XscJM>	NIjPbW09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N\|UyOzl:L3G+
BT-12	M37QOpFJXFNiYYPzZZk>		M3\qfpFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCEVD2xNkBk\Wyucx?=	MXG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-
NB1643	M2j0cZFJXFNiYYPzZZk>		M4rPWpFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCQQkG2OFMh[2WubIO=	MoSxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=
OHS-50	MX\xTHRUKGG\|c3H5		NHXzXZhyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiT1jTMVUxKGOnbHzz	NWDuc4I2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N\|UyOzlpPkK5OFM2OTN7PD;hQi=>
Rh41	NVXzZnRPeUiWUzDhd5NigQ>?		MVnxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhWmh2MTDj[Yxtew>?	MmfLQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=
SJ-GBM2	MnjjdWhVWyCjc4PhfS=>		M{DTRZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCVSj3HRm0zKGOnbHzz	M4HwNFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
SK-N-MC	M{\nW5FJXFNiYYPzZZk>		M3rNNJFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCVSz3OMW1EKGOnbHzz	MlrzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=
NB-EBc1	MVzxTHRUKGG\|c3H5		NUH3S494eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC\|Y4Ll[Y4h\m:{IF7CMWVD[zFiY3XscJM>	Mn7XQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=
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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 Mol Carcinog 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 Cancer Med 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 Cancer Med 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 Oncotarget 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 Mol Cancer H226B and H460 cells were subject to daily treatment with linsitinib (1 μM) for 1-5 days. pS6 / S6; PubMed: 21257723 Clin Cancer Res 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 J Biol Chem 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 Neuro Oncol InsR/IGF1R dual inhibitors, OSI-906 and BMS-754807, dose-dependently inhibited T4105 viability.	26136493

体内研究

OSI-906 作用于IGF-IR驱动的移植瘤鼠模型，抑制肿瘤生长，按 75 mg / kg剂量处理，导致100% TGI和 55% 衰退，按25 mg/kg剂量处理，导致 60% TGI，没有衰退。OSI-906处理犬，大鼠和小鼠，诱导不同的消除半衰期，消除半衰期分别为1.18 小时, 2.64小时和2.14小时。OSI-906按不同剂量单独处理给药雌性Sprague-Dawley 大鼠和雌性CD-1小鼠，每天一次，V_max值与OSI-906 剂量不成比例。OSI-906 按 25 mg/kg剂量处理12天，提高血糖值。OSI-906按75 mg/kg 剂量单独处理IGF-IR-驱动的人全长人类IGF-IR (LISN)移植鼠模型，在4 和24小时间最大程度抑制IGF-IR磷酸化(80%)，血浆药物浓度为26.6-4.77 μM。^[1] OSI-906 按60 mg/kg剂量单独作用于NCI-H292 移植鼠，处理2，4，24小时，抑制糖吸收。OSI-906 作用于NCI-H292移植鼠模型，抑制肿瘤生长。^[2]

激酶实验：^[1]	- 合并蛋白激酶生化实验: 通过以ELISA为基础的检测法(IGF-IR, IR, EGFR 和 KDR)或使用100 µM ATP的放射检测法进行蛋白激酶检测实验。在内部ELISA检测实验中，使用聚 (Glu:Tyr)作为底物，结合到96孔实验板表面，使用辣根过氧化物酶标记的自磷酸化抗体测定磷酸化。使用ABTS作为过氧化物酶底物，通过在405/490 nm处测量吸光度而测定结合的抗体。所有实验使用纯化的重组激酶催化域。在昆虫细胞中，人类IGF-IR或EGFR的重组酶表达作为NH2-末端谷胱甘肽S-转移酶融合蛋白，且在内部纯化。通过抑制百分数对log₁₀药品浓度的S型剂量-反应曲线测定IC50值。进行内部实验需重复进行实验，除非另有说明，取三次测量的最小值。
细胞实验：^[1]	- 合并 Cell lines: MCF7, NCI-H292, Colo-205, HT29, H358, H1703, BxPC3, A673, SW620, DU4475, HepG2 和Hepa-1, RKO 3T3/hulGF-IR, H292 细胞 Concentrations: 0.02-0.8 μM Incubation Time: 3天 Method: 为了测定细胞增殖，细胞接种在含FCS 10%的合适培养基上，在不同浓度OSI-906存在时，温育3天。通过细胞内ATP含量的荧光量化，使用CellTiterGlo测定抑制细胞生长的情况。数据作为衡量最大增殖的一部分，通过在不同浓度 OSI-906存在时的细胞密度除以对照组（只用DMSO处理）细胞密度。 (Only for Reference)
动物实验：^[1]	- 合并 Animal Models: IGF-IR驱动的全长人类IGF-IR (LISN) 移植小鼠模型 Dosages: 25 mg/kg和75 mg/kg Administration: 口服处理，每天一次，持续14天 (Only for Reference)

参考文献

溶解度 (25°C)

体外	DMSO	84 mg/mL (199.29 mM)
	Water	Insoluble
	Ethanol	Insoluble
体内	从左到右依次将纯溶剂加入产品，现配现用(数据来自Selleck实验检测而非文献)： 5%DMSO+40%PEG300+5%Tween80+50%ddH2O	6.25mg/mL

* 溶解度检测是由Selleck技术部门检测的，可能会和文献中提供的溶解度有所差异，这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据 Download Linsitinib (OSI-906) SDF

分子量	421.49
化学式	C₂₆H₂₃N₅O
CAS号	867160-71-2
储存条件	3年-20°C 粉状 2年-80°C 溶于溶剂
别名	N/A

动物体内配方计算器 (澄清溶液)

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）

给药剂量

mg/kg

动物平均体重

每只动物给药体积

动物数量

只

第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）

% DMSO+ % + % Tween 80+ % ddH₂O

计算重置

计算结果:

工作液浓度： mg/ml；

DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；

体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL ddH₂O，混匀澄清。

注意：1. 首先保证母液是澄清的；
2. 一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。

计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

质量

浓度

体积

分子量
=

×

×

*在配置溶液时，请务必参考Selleck产品标签上、SDS / COA（可在Selleck的产品页面获得）批次特异的分子量使用本工具。

稀释计算器

用本工具协助配置特定浓度的溶液，使用的计算公式为：

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入输出 )

C1

V1

C2

V2
×

=

×

在配置溶液时，请务必参考Selleck产品标签上、SDS / COA（可在Selleck的产品页面获得）批次特异的分子量使用本工具。.

连续稀释计算器方程

连续稀释
初始浓度:
稀释倍数:

计算结果

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

分子量计算器

通过输入化合物的化学式来计算其分子量：

注：化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量	浓度	体积	分子量
=	×	×
计算

临床试验信息 (data from https://clinicaltrials.gov, updated on 2022-01-17)

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

技术支持

在订购、运输、储存和使用我们的产品的任何阶段，您遇到的任何问题，均可以通过拨打我们的热线电话400-668-6834，或者技术支持邮箱tech@selleck.cn，直接联系到我们。我们会在24小时内尽快联系您。

操作手册

如果有其他问题，请给我们留言。

常见问题及建议解决方法

问题 1：
Does the inhibitor dissolve in the vehicle (30% PEG400/0.5%Tween 80/5% propylene glycol) or is it a suspension?
回答：
OSI-906 in 30% PEG400/0.5%Tween 80/5% propylene glycol is a suspension.

IGF-1R Signaling Pathway Map

IGF-1R Inhibitors with Unique Features

泛IGF-1R抑制剂

GSK1904529A : Dual IGF-1R/IR inhibitor, IC50=27 nM/25 nM.
活性最高的IGF-1R抑制剂

BMS-754807 : IGF-1R, IC50=1.8 nM; InsR, IC50=1.7 nM.
用于临床的IGF-1R抑制剂

BMS-754807 : Phase II for Breast Cancer.
最新的IGF-1R抑制剂

PQ 401 : Inhibitor of autophosphorylation of IGF-1R domain with IC50 of <1 μM.

研究领域

产品类型

定制您的化合物库

Linsitinib (OSI-906)

客户使用Selleck生产的Linsitinib (OSI-906)发表文献147篇：

产品安全说明书

IGF-1R抑制剂选择性比较

生物活性

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

参考文献

溶解度 (25°C)

化学数据 Download Linsitinib (OSI-906) SDF

动物体内配方计算器 (澄清溶液)

计算器

摩尔浓度计算器

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

稀释计算器

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

连续稀释计算器方程

连续稀释

计算结果

分子量计算器

总分子量：g/mol

摩尔浓度计算器

临床试验信息 (data from https://clinicaltrials.gov, updated on 2022-01-17)

技术支持

常见问题及建议解决方法

IGF-1R Signaling Pathway Map

IGF-1R Inhibitors with Unique Features

相关IGF-1R产品