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。

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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131篇：

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Cells, 2019, 8(4)

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Sci Rep, 2019, 9(1):5309

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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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PLoS One, 2018, 13(2):e0191890

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

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

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Cancer Res, 2017, 77(8):1842-1853

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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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Endocrinology, 2017,

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Cancer Med, 2017, 6(6):1353-1361

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Biochimie, 2017, 138:62-69

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Hepatology, 2017, 66(6):2002-2015

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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	M17lOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		NXu3O3RsUUN3ME2wMlAzQDB4IN88US=>	MmHvQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6OTZ2ND:nQnNCVkeHUkyvZV4>
KS-1	NE\PWYVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		M{DG[GlEPTB;MD6wN\|g{PSEQvF2=	NE\nS5Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODlzNkS0M{c,W0GQR1XSQE9iRg>?
TE-11	NXjmTFA2T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		NWLZco1XUUN3ME2wMlA4QDJ{IN88US=>	MkfkQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6OTZ2ND:nQnNCVkeHUkyvZV4>
EW-1	MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		M3jybWlEPTB;MD6wPFU5PSEQvF2=	NV7CcIlPRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7MU[0OE8oRlODTlfFVlww[T5?
HMV-II	NF;yUFNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		MoPRTWM2OD1yLkC4PFQ3KM7:TR?=	NV\VWY9FRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7MU[0OE8oRlODTlfFVlww[T5?
COLO-205	MnvES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		NFPG[GNKSzVyPUCuNVA1PTRizszN	Ml3ZQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6OTZ2ND:nQnNCVkeHUkyvZV4>
ES1	NVLpVoRDT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		NV3xbGY{UUN3ME2wMlExPjl4IN88US=>	M3S4VFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQTF4NESvK\|5USU6JRWK8M4E,
GDM-1	M13rOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		MWHJR\|UxRTBwMUO2O\|Ih\|ryP	M3rlRVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQTF4NESvK\|5USU6JRWK8M4E,
ML-2	NITHVFVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		NVG3bJpKUUN3ME2wMlE2QDl4IN88US=>	MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFkyPjR2Lze+V2FPT0WUPD;hQi=>
Saos-2	NGDKUWpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		M2DOTWlEPTB;MD6xOlUzPiEQvF2=	NIn0d5c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODlzNkS0M{c,W0GQR1XSQE9iRg>?
NCI-H1355	MlrzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		MoHjTWM2OD1yLkG4NVM2KM7:TR?=	MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFkyPjR2Lze+V2FPT0WUPD;hQi=>
G-401	NIniTVVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		Mlm1TWM2OD1yLkG4NlMh\|ryP	NUTidnhtRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7MU[0OE8oRlODTlfFVlww[T5?
EW-16	M1rzN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7		NFXkb2lKSzVyPUCuNVg4PzdizszN	M2K5clxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQTF4NESvK\|5USU6JRWK8M4E,
EW-7	MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		MlvKTWM2OD1yLkG4PFgyKM7:TR?=	NXe1ZVRTRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7MU[0OE8oRlODTlfFVlww[T5?
NCI-H727	M1rSTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		MmPPTWM2OD1yLkG5O\|k1KM7:TR?=	MYm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFkyPjR2Lze+V2FPT0WUPD;hQi=>
LCLC-97TM1	MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		MXPJR\|UxRTBwMkC5OVUh\|ryP	NID4PFI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODlzNkS0M{c,W0GQR1XSQE9iRg>?
NCI-H650	NHziepVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		MmiwTWM2OD1yLkKxN\|g1KM7:TR?=	MoXxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6OTZ2ND:nQnNCVkeHUkyvZV4>
NCI-H2122	MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		Mk\2TWM2OD1yLkKzNlk6KM7:TR?=	MnWxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6OTZ2ND:nQnNCVkeHUkyvZV4>
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DK-MG	MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		NGPvd\|ZKSzVyPUSuPFA6OzNizszN	MljhQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6OTZ2ND:nQnNCVkeHUkyvZV4>
OVCAR-5	NHnZV4ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		MoXUTWM2OD12LkixNlI3KM7:TR?=	MXK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFkyPjR2Lze+V2FPT0WUPD;hQi=>
CAL-39	MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		NFjWcndKSzVyPUSuPFc3PyEQvF2=	MkP6QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6OTZ2ND:nQnNCVkeHUkyvZV4>
TE-441-T	MkftS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		M4LDOWlEPTB;ND65NFU{PyEQvF2=	NWLGWIJsRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7MU[0OE8oRlODTlfFVlww[T5?
MOLT-16	NXe1U5BGT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		MYfJR\|UxRTRwOUWyOVMh\|ryP	NXTiR5pXRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7MU[0OE8oRlODTlfFVlww[T5?
MCF7	NEHnSpdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		NYfJSWZlUUN3ME21MlE1PTF5IN88US=>	NIflR5Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODlzNkS0M{c,W0GQR1XSQE9iRg>?
CAPAN-1	MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		MnzLTWM2OD13LkK1O\|A4KM7:TR?=	MmDTQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6OTZ2ND:nQnNCVkeHUkyvZV4>
PSN1	MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		MUPJR\|UxRTVwMkeyN\|Uh\|ryP	NGK1bWI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODlzNkS0M{c,W0GQR1XSQE9iRg>?
NCI-H292	MmHES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		NG\wRXBKSzVyPUWuN\|AxPDRizszN	MknqQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6OTZ2ND:nQnNCVkeHUkyvZV4>
CPC-N	M2HlXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		NIHlS4dKSzVyPUWuN\|k1OTlizszN	MXe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFkyPjR2Lze+V2FPT0WUPD;hQi=>
DoTc2-4510	NIXu[llIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		NIm4XJVKSzVyPUWuOFU{PzFizszN	Mnq0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6OTZ2ND:nQnNCVkeHUkyvZV4>
LB1047-RCC	Mlv5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		NVW2[4ttUUN3ME21MlU2QTN\|IN88US=>	NIn1fJY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODlzNkS0M{c,W0GQR1XSQE9iRg>?
MHH-ES-1	NXPQN4ZCT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		NX7NW3o4UUN3ME21MlU6QTB5IN88US=>	Mn3SQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6OTZ2ND:nQnNCVkeHUkyvZV4>
NMC-G1	MmjZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		MVjJR\|UxRTVwN{CyNlch\|ryP	M4HPXFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQTF4NESvK\|5USU6JRWK8M4E,
SW1710	MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		MnLaTWM2OD13Lke0O\|UyKM7:TR?=	MYe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFkyPjR2Lze+V2FPT0WUPD;hQi=>
YAPC	M3f6Xmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		Ml;uTWM2OD13Lke2NlAyKM7:TR?=	MkXVQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6OTZ2ND:nQnNCVkeHUkyvZV4>
22RV1	MorMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		NF;WU2tKSzVyPUWuPFAxOTlizszN	Mn3XQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6OTZ2ND:nQnNCVkeHUkyvZV4>
COLO-679	M{DQbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		MX;JR\|UxRTVwOEi5OFgh\|ryP	MnzrQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6OTZ2ND:nQnNCVkeHUkyvZV4>
TCCSUP	M12xUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		NW\rdFM3UUN3ME21Mlk{OjV7IN88US=>	NXX4dnlGRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7MU[0OE8oRlODTlfFVlww[T5?
C2BBe1	MmTNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		M3PHOWlEPTB;NT65N\|k4KM7:TR?=	M3vmSVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQTF4NESvK\|5USU6JRWK8M4E,
TE-15	MlH3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		M17pUmlEPTB;Nj6wOlYxPSEQvF2=	NVryVYFORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7MU[0OE8oRlODTlfFVlww[T5?
SCLC-21H	M1K1VWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		MmfSTWM2OD14LkGwPFQ{KM7:TR?=	NVj0[YY6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7MU[0OE8oRlODTlfFVlww[T5?
EoL-1-cell	M1ntXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		M2f5U2lEPTB;Nj6xOlU3OyEQvF2=	MoLtQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6OTZ2ND:nQnNCVkeHUkyvZV4>
NKM-1	M2rCW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7		MXPJR\|UxRTZwMU[3NUDPxE1?	MVi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFkyPjR2Lze+V2FPT0WUPD;hQi=>
NCI-H1304	NGLOTG1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		MV7JR\|UxRTZwMke0Nlgh\|ryP	MYq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFkyPjR2Lze+V2FPT0WUPD;hQi=>
NB6	MofyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		MljSTWM2OD14LkK5OlIzKM7:TR?=	M37V[\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQTF4NESvK\|5USU6JRWK8M4E,
NALM-6	MnnwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		NGf2bXdKSzVyPU[uN\|MzOyEQvF2=	MWm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFkyPjR2Lze+V2FPT0WUPD;hQi=>
NCI-H522	M3\sOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		MU\JR\|UxRTZwM{OzNFYh\|ryP	MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFkyPjR2Lze+V2FPT0WUPD;hQi=>
MV-4-11	M2HJWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		NXHxXXU1UUN3ME22MlM4ODd7IN88US=>	M2njdVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQTF4NESvK\|5USU6JRWK8M4E,
LB2241-RCC	MmXRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		MmHXTWM2OD14LkO4OlY4KM7:TR?=	MYi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFkyPjR2Lze+V2FPT0WUPD;hQi=>
NCI-H1417	MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		NYi0VHVKUUN3ME22MlQxQDR5IN88US=>	MlfKQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6OTZ2ND:nQnNCVkeHUkyvZV4>
HT-1197	MnTES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		NYHoNotpUUN3ME22MlU4OTJ{IN88US=>	MV68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFkyPjR2Lze+V2FPT0WUPD;hQi=>
P30-OHK	MkjnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		M4XtfWlEPTB;Nj62Nlc4KM7:TR?=	NILxVms9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODlzNkS0M{c,W0GQR1XSQE9iRg>?
ALL-PO	NIDQS2lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		M1W1U2lEPTB;Nj63NVkyPiEQvF2=	NYHBfIJ{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7MU[0OE8oRlODTlfFVlww[T5?
OVCAR-4	MmHNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		NVfOU\|htUUN3ME22Mlc2PDB3IN88US=>	MUW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFkyPjR2Lze+V2FPT0WUPD;hQi=>
HCC2157	MmD5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		MXvJR\|UxRTZwN{e0O\|Uh\|ryP	MVO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFkyPjR2Lze+V2FPT0WUPD;hQi=>
NCI-H838	NYjiN2g3T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		MmGzTWM2OD14Lkm2OFkh\|ryP	MYe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFkyPjR2Lze+V2FPT0WUPD;hQi=>
NCI-H1299	NIDnUYlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		NUflWpQyUUN3ME22Mlk4ODlizszN	NVvTPZBXRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7MU[0OE8oRlODTlfFVlww[T5?
SW954	MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		Mk\3TWM2OD15LkKwNFY5KM7:TR?=	M3HPXlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQTF4NESvK\|5USU6JRWK8M4E,
NCI-H441	MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		M125bWlEPTB;Nz6zOFA3PSEQvF2=	MV[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFkyPjR2Lze+V2FPT0WUPD;hQi=>
SK-MEL-2	MmXXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		MVPJR\|UxRTdwNEizO\|Mh\|ryP	MkL2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6OTZ2ND:nQnNCVkeHUkyvZV4>
KARPAS-45	NWXhNXVJT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		M{nWfGlEPTB;Nz62OVkzQSEQvF2=	NY\CVW1zRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7MU[0OE8oRlODTlfFVlww[T5?
CAL-54	MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		NFLCWlBKSzVyPUeuPFI6PzdizszN	MXu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFkyPjR2Lze+V2FPT0WUPD;hQi=>
KYSE-180	NXK4SWJQT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		NFvYd2hKSzVyPUeuPFg6PDFizszN	Mn3SQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6OTZ2ND:nQnNCVkeHUkyvZV4>
NCI-H187	MlHjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		NYPhe45{UUN3ME23Mlk2QTR5IN88US=>	M1rRRVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQTF4NESvK\|5USU6JRWK8M4E,
RT-112	M1KyXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		M3PFRmlEPTB;OD6wPVY4PyEQvF2=	NFr1TnY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODlzNkS0M{c,W0GQR1XSQE9iRg>?
NCI-H1437	M4\ZPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		NGfKfZJKSzVyPUiuNFk4QTVizszN	NI\XZVI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODlzNkS0M{c,W0GQR1XSQE9iRg>?
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KYSE-520	NYLSVIYxT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		NH3IfIJKSzVyPUS4MlU{OTVizszN	MoPZQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6OTZ2ND:nQnNCVkeHUkyvZV4>
SNG-M	MnqwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		M{PhVWlEPTB;NEmuOFM1KM7:TR?=	MlHoQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6OTZ2ND:nQnNCVkeHUkyvZV4>
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HEK293	NH;vW2VHfW6ldHnvckBie3OjeR?=	NV:xPVlpPjBibXnudy=>	M4mwbWlvcGmkaYTpc44hd2ZiZoXscEBt\W6pdHigTWdHNTFicnXj[ZB1d3JiKIXub45wf25ib4Lp[4lvMSCjdYTvdIhwe3Cqb4L5cIF1cW:wIITyZY5{\mWldHXkJIlvKEiHS{K5N{Bk\WyuczDwdoV1emWjdHXkJIZweiB4MDDtbY5{KG[xbHzve4VlKGK7IFnHSk0yKHO2aX31cIF1cW:wIH3lZZN2emWmIHHmeIVzKDFyIH3pcpMh[nlicYXhcpRqfGG2aY\lJHdme3Sncn6gZoxwfCCjbnHsfZNqeyxiSVO1NEA:KDBwMECyPEDPxE1w	NEHPfII9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Nkm1NVc2Oyd-Mk[5OVE4PTN:L3G+
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HEK293	M4rTfWZ2dmO2aX;uJIF{e2G7	M{LNTVYxKG2rboO=	MmLFTY5pcWKrdHnvckBw\iCodXzsJIxmdme2aDDpcpN2dGmwIILlZ4VxfG:{IDj1cotvd3ewIH;ybYdqdiliYYX0c5Bpd3OyaH;yfYxifGmxbjD0doFve2[nY4Tl[EBqdiCKRVuyPVMh[2WubIOgdJJmfHKnYYTl[EBnd3JiNkCgcYlveyCob3zsc5dm\CCkeTDJS2YuOSC\|dHnteYxifGmxbjDt[YF{fXKnZDDh[pRmeiBzMDDtbY5{KGK7IIH1ZY51cXSjdHn2[UBY\XO2ZYLuJIJtd3RiYX7hcJl{cXNuIFnDOVAhRSByLkCxOkDPxE1w	NYH0TGVERGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[5OVE4PTNpPkK2PVUyPzV\|PD;hQi=>
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Ba/F3	NWfMOZFtTnWwY4Tpc44h[XO\|YYm=		M13tdWlvcGmkaYTpc44hd2ZiZoXscEBt\W6pdHigbY5{fWyrbjDy[YNmeHSxcjCoeY5sdm:5bjDvdolocW5rIITyZY5{\mWldHXkJIlvKEKjL1[zJINmdGy\|IHHzd4V{e2WmIHHzJINmdGxicILvcIln\XKjdHnvckwhUUN3MDC9JFAvOTJ4IN88UU4>	NI\5VWE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Nkm1NVc2Oyd-Mk[5OVE4PTN:L3G+
A673	NVPNTYloeUiWUzDhd5NigQ>?		MlXsdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[\|ohWHKrbXHyfUB{[3KnZX6g[o9zKEF4N{OgZ4VtdHN?	MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-
Saos-2	NVe3UGR1eUiWUzDhd5NigQ>?		M{XSNJFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCVYX;zMVIh[2WubIO=	MYm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-
BT-37	M3TPZ5FJXFNiYYPzZZk>		NVnYU5ZoeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC\|Y4Ll[Y4h\m:{IFLUMVM4KGOnbHzz	MVe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-
RD	M3TRbJFJXFNiYYPzZZk>		MmLjdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[\|ohWHKrbXHyfUB{[3KnZX6g[o9zKFKGIHPlcIx{	M4fSPVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
BT-12	MkLUdWhVWyCjc4PhfS=>		M2LGXJFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCEVD2xNkBk\Wyucx?=	NVTOOXdzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N\|UyOzlpPkK5OFM2OTN7PD;hQi=>
NB1643	MoDOdWhVWyCjc4PhfS=>		MV;xTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhVkJzNkSzJINmdGy\|	MVi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-
OHS-50	NUCwT4dMeUiWUzDhd5NigQ>?		NHfL[GZyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiT1jTMVUxKGOnbHzz	NH\wV2g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N\|UyOzl:L3G+
Rh41	MkCzdWhVWyCjc4PhfS=>		MXzxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhWmh2MTDj[Yxtew>?	NXyxSVJ1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N\|UyOzlpPkK5OFM2OTN7PD;hQi=>
SJ-GBM2	NGPQZ\|FyUFSVIHHzd4F6		MWjxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhW0pvR1LNNkBk\Wyucx?=	NUXaTmtIRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N\|UyOzlpPkK5OFM2OTN7PD;hQi=>
SK-N-MC	NVnRNpBOeUiWUzDhd5NigQ>?		MYjxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhW0tvTj3NR{Bk\Wyucx?=	NXTSWWc1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N\|UyOzlpPkK5OFM2OTN7PD;hQi=>
NB-EBc1	NIXac21yUFSVIHHzd4F6		NIPNRllyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiTlKtSWJkOSClZXzsdy=>	NXywPXhCRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N\|UyOzlpPkK5OFM2OTN7PD;hQi=>
LAN-5	M3vERZFJXFNiYYPzZZk>		NX;zcpc2eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC\|Y4Ll[Y4h\m:{IFzBUk02KGOnbHzz	M2rV[VxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=

... 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、MSDS / 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、MSDS / 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 2020-01-06)

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131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 2020-01-06)

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