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135篇：

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Cells, 2019, 8(4)

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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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Oncotarget, 2018,

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

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Clin Cancer Res, 2017, 23(11):2795-2805

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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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Sci Rep, 2017, 7(1):2364

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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	M4rkSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		NWT1eW5zUUN3ME2wMlAzQDB4IN88US=>	MYO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFkyPjR2Lze+V2FPT0WUPD;hQi=>
KS-1	NFnzbYFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		Mnu1TWM2OD1yLkCzPFM2KM7:TR?=	NYjUVYF2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7MU[0OE8oRlODTlfFVlww[T5?
TE-11	NYfGVWQ{T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		MVTJR\|UxRTBwMEe4NlIh\|ryP	NID2cmE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODlzNkS0M{c,W0GQR1XSQE9iRg>?
EW-1	MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		NEW3OFhKSzVyPUCuNFg2QDVizszN	M3;WV\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQTF4NESvK\|5USU6JRWK8M4E,
HMV-II	NGf0ZYlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		Ml;oTWM2OD1yLkC4PFQ3KM7:TR?=	NGLp[pM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODlzNkS0M{c,W0GQR1XSQE9iRg>?
COLO-205	M2DuNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		NXPFd4djUUN3ME2wMlExPDV2IN88US=>	MnjaQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6OTZ2ND:nQnNCVkeHUkyvZV4>
ES1	MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		MX;JR\|UxRTBwMUC2PVYh\|ryP	MX:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFkyPjR2Lze+V2FPT0WUPD;hQi=>
GDM-1	MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		NYSz[297UUN3ME2wMlE{Pjd{IN88US=>	MoLyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6OTZ2ND:nQnNCVkeHUkyvZV4>
ML-2	MlL0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		MV3JR\|UxRTBwMUW4PVYh\|ryP	MnexQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6OTZ2ND:nQnNCVkeHUkyvZV4>
Saos-2	NEf5N4JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		M3voO2lEPTB;MD6xOlUzPiEQvF2=	MWG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFkyPjR2Lze+V2FPT0WUPD;hQi=>
NCI-H1355	NVj0OJZpT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		MmPITWM2OD1yLkG4NVM2KM7:TR?=	MlLNQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6OTZ2ND:nQnNCVkeHUkyvZV4>
G-401	MnXES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		MWfJR\|UxRTBwMUiyN{DPxE1?	NXjzOmltRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7MU[0OE8oRlODTlfFVlww[T5?
EW-16	NHn1RVBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		MkDJTWM2OD1yLkG4O\|c4KM7:TR?=	Mm[4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6OTZ2ND:nQnNCVkeHUkyvZV4>
EW-7	MkHVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		MVvJR\|UxRTBwMUi4PFEh\|ryP	NIj0VIo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODlzNkS0M{c,W0GQR1XSQE9iRg>?
NCI-H727	NITicHlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		M{WybGlEPTB;MD6xPVc6PCEQvF2=	MmDOQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6OTZ2ND:nQnNCVkeHUkyvZV4>
LCLC-97TM1	NFLU[WdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		NUW1W5JxUUN3ME2wMlIxQTV3IN88US=>	NIK3dng9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODlzNkS0M{c,W0GQR1XSQE9iRg>?
NCI-H650	NF\vN4JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		M1yz[WlEPTB;MD6yNVM5PCEQvF2=	Ml;RQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6OTZ2ND:nQnNCVkeHUkyvZV4>
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NCI-H1092	NVvLS2hTT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		NXTzTXl5UUN3ME20MlQ2Pjh5IN88US=>	MlfLQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6OTZ2ND:nQnNCVkeHUkyvZV4>
PANC-10-05	NHToU2JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		NGPyZmdKSzVyPUSuOlk5PCEQvF2=	MmizQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6OTZ2ND:nQnNCVkeHUkyvZV4>
DK-MG	MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		NGrGTG5KSzVyPUSuPFA6OzNizszN	NYPiWYhjRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7MU[0OE8oRlODTlfFVlww[T5?
OVCAR-5	NFnDNpRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		MYjJR\|UxRTRwOEGyNlYh\|ryP	NGDG[nE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODlzNkS0M{c,W0GQR1XSQE9iRg>?
CAL-39	MnrqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		NF;kVYpKSzVyPUSuPFc3PyEQvF2=	M3G2XlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQTF4NESvK\|5USU6JRWK8M4E,
TE-441-T	M2D5U2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7		MkTITWM2OD12LkmwOVM4KM7:TR?=	M{C1[\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQTF4NESvK\|5USU6JRWK8M4E,
MOLT-16	NVzZZopYT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		NWn3e\|A4UUN3ME20Mlk2OjV\|IN88US=>	NV;rbYJ[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7MU[0OE8oRlODTlfFVlww[T5?
MCF7	M{LKSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		NGDWXYFKSzVyPUWuNVQ2OTdizszN	M1LlOVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQTF4NESvK\|5USU6JRWK8M4E,
CAPAN-1	MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		NFzleoVKSzVyPUWuNlU4ODdizszN	NHz6R5A9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODlzNkS0M{c,W0GQR1XSQE9iRg>?
PSN1	MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		MoHaTWM2OD13LkK3NlM2KM7:TR?=	M1LOdlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQTF4NESvK\|5USU6JRWK8M4E,
NCI-H292	NYHKW5VNT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		M1TacmlEPTB;NT6zNFA1PCEQvF2=	M1roT\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQTF4NESvK\|5USU6JRWK8M4E,
CPC-N	NULDNIV7T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		M2LqWmlEPTB;NT6zPVQyQSEQvF2=	MUW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFkyPjR2Lze+V2FPT0WUPD;hQi=>
DoTc2-4510	MnPLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		M{\ibGlEPTB;NT60OVM4OSEQvF2=	NH3mcVI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODlzNkS0M{c,W0GQR1XSQE9iRg>?
LB1047-RCC	NHi5WnpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		NXXnemkxUUN3ME21MlU2QTN\|IN88US=>	MYK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFkyPjR2Lze+V2FPT0WUPD;hQi=>
MHH-ES-1	M4LpVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		MUHJR\|UxRTVwNUm5NFch\|ryP	NHn3bHo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODlzNkS0M{c,W0GQR1XSQE9iRg>?
NMC-G1	M2jIXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		MmG3TWM2OD13LkewNlI4KM7:TR?=	MkmwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6OTZ2ND:nQnNCVkeHUkyvZV4>
SW1710	MmHTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		M2[zRmlEPTB;NT63OFc2OSEQvF2=	MV:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFkyPjR2Lze+V2FPT0WUPD;hQi=>
YAPC	NVvHOFhXT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		MVfJR\|UxRTVwN{[yNFEh\|ryP	MnyyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6OTZ2ND:nQnNCVkeHUkyvZV4>
22RV1	M3\E[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		NWn2fXV4UUN3ME21MlgxODF7IN88US=>	MmPlQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6OTZ2ND:nQnNCVkeHUkyvZV4>
COLO-679	MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		MnSwTWM2OD13Lki4PVQ5KM7:TR?=	MlXaQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6OTZ2ND:nQnNCVkeHUkyvZV4>
TCCSUP	NITnblJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		MWnJR\|UxRTVwOUOyOVkh\|ryP	MkG5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6OTZ2ND:nQnNCVkeHUkyvZV4>
C2BBe1	NH7OU\|NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		M2nJcmlEPTB;NT65N\|k4KM7:TR?=	MlH4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6OTZ2ND:nQnNCVkeHUkyvZV4>
TE-15	MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		NF60T2FKSzVyPU[uNFY3ODVizszN	NW\vRnJ7RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7MU[0OE8oRlODTlfFVlww[T5?
SCLC-21H	MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		MXHJR\|UxRTZwMUC4OFMh\|ryP	M3;UZlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQTF4NESvK\|5USU6JRWK8M4E,
EoL-1-cell	NYO2UXFlT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		MmLBTWM2OD14LkG2OVY{KM7:TR?=	NWrDcJpKRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7MU[0OE8oRlODTlfFVlww[T5?
NKM-1	MmXLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		NIG2bmpKSzVyPU[uNVY4OSEQvF2=	NYLHZnB[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7MU[0OE8oRlODTlfFVlww[T5?
NCI-H1304	M4LMd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7		NYrrVZR1UUN3ME22MlI4PDJ6IN88US=>	M17YN\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQTF4NESvK\|5USU6JRWK8M4E,
NB6	MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		M4HvfWlEPTB;Nj6yPVYzOiEQvF2=	NUT3T49TRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7MU[0OE8oRlODTlfFVlww[T5?
NALM-6	NIrvOHBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		NWfPWohZUUN3ME22MlM{OjNizszN	MXK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFkyPjR2Lze+V2FPT0WUPD;hQi=>
NCI-H522	NF:3WGRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		NHjuUnRKSzVyPU[uN\|M{ODZizszN	M2Xr[FxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQTF4NESvK\|5USU6JRWK8M4E,
MV-4-11	NYDUcGZXT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		NHPMRYNKSzVyPU[uN\|cxPzlizszN	NWjTNWhmRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7MU[0OE8oRlODTlfFVlww[T5?
LB2241-RCC	MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		MlfUTWM2OD14LkO4OlY4KM7:TR?=	NWjjXnBWRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7MU[0OE8oRlODTlfFVlww[T5?
NCI-H1417	NV34O2xvT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		NGTUbIdKSzVyPU[uOFA5PDdizszN	M{HVVlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQTF4NESvK\|5USU6JRWK8M4E,
HT-1197	M331VWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		MoXrTWM2OD14LkW3NVIzKM7:TR?=	NU\kcXZXRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7MU[0OE8oRlODTlfFVlww[T5?
P30-OHK	M{D0emdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		M1r6eWlEPTB;Nj62Nlc4KM7:TR?=	NVzlU4JRRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7MU[0OE8oRlODTlfFVlww[T5?
ALL-PO	MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		M3TNcGlEPTB;Nj63NVkyPiEQvF2=	NGD6UIM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODlzNkS0M{c,W0GQR1XSQE9iRg>?
OVCAR-4	MmTZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		MWPJR\|UxRTZwN{W0NFUh\|ryP	M4HxOlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQTF4NESvK\|5USU6JRWK8M4E,
HCC2157	M{LBOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		NH3KcoxKSzVyPU[uO\|c1PzVizszN	MVi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFkyPjR2Lze+V2FPT0WUPD;hQi=>
NCI-H838	M2HZWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		MoP3TWM2OD14Lkm2OFkh\|ryP	M{Dsd\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQTF4NESvK\|5USU6JRWK8M4E,
NCI-H1299	NFHISFVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		M1XHb2lEPTB;Nj65O\|A6KM7:TR?=	MYG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFkyPjR2Lze+V2FPT0WUPD;hQi=>
SW954	MlXyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		Mne5TWM2OD15LkKwNFY5KM7:TR?=	NYjvbHNVRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7MU[0OE8oRlODTlfFVlww[T5?
NCI-H441	NUjGWFBLT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		MV\JR\|UxRTdwM{SwOlUh\|ryP	Mn:wQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6OTZ2ND:nQnNCVkeHUkyvZV4>
SK-MEL-2	MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		MXrJR\|UxRTdwNEizO\|Mh\|ryP	NGSyOnU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODlzNkS0M{c,W0GQR1XSQE9iRg>?
KARPAS-45	MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		MUHJR\|UxRTdwNkW5Nlkh\|ryP	NGPDe4Q9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODlzNkS0M{c,W0GQR1XSQE9iRg>?
CAL-54	M1HGOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		NGTsZ3pKSzVyPUeuPFI6PzdizszN	NWKxTVJKRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7MU[0OE8oRlODTlfFVlww[T5?
KYSE-180	MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		M1m0dWlEPTB;Nz64PFk1OSEQvF2=	NVPOTph6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7MU[0OE8oRlODTlfFVlww[T5?
NCI-H187	M{[4cGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		NYXPZ2JtUUN3ME23Mlk2QTR5IN88US=>	MlX4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6OTZ2ND:nQnNCVkeHUkyvZV4>
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MDA-MB-175-VII	NH22[GdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		NXe1d\|RnUUN3ME2zO{4zOjR6IN88US=>	M3HKdlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQTF4NESvK\|5USU6JRWK8M4E,
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Daudi	M3fDVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		M1vONGlEPTB;M{euN\|U6PyEQvF2=	NGnmeo49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODlzNkS0M{c,W0GQR1XSQE9iRg>?
A498	NVK2VFU4T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		NWWzOmhRUUN3ME2zO{44OjF6IN88US=>	NW\lbZpQRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7MU[0OE8oRlODTlfFVlww[T5?
SCC-4	MlLGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		NH;3UIhKSzVyPUO3Mlc5PDNizszN	MUW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFkyPjR2Lze+V2FPT0WUPD;hQi=>
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SK-HEP-1	M1zVSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		NXvj[og6UUN3ME2zPE44QDJ{IN88US=>	NFTZZZI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODlzNkS0M{c,W0GQR1XSQE9iRg>?
BPH-1	M37hfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		NULadJo1UUN3ME2zPE45OzJ7IN88US=>	MXK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFkyPjR2Lze+V2FPT0WUPD;hQi=>
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LXF-289	MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		NGjhXVJKSzVyPUO5MlgxQDRizszN	NUPYd4JlRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7MU[0OE8oRlODTlfFVlww[T5?
SW1088	MnfkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		MYTJR\|UxRTRyLkKxNFch\|ryP	M{fpb\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQTF4NESvK\|5USU6JRWK8M4E,
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HOP-62	Mk\pS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		NFLuRmtKSzVyPUSwMlY2PjhizszN	M{TGV\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQTF4NESvK\|5USU6JRWK8M4E,
A172	NFjmeJJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		M1;xWGlEPTB;NECuPFUyOSEQvF2=	NYnRU\|ZFRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7MU[0OE8oRlODTlfFVlww[T5?
SN12C	Mmf0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		Mn;ETWM2OD12MD65N\|g2KM7:TR?=	NEjoR4g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODlzNkS0M{c,W0GQR1XSQE9iRg>?
MDA-MB-231	MlzkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		MXPJR\|UxRTRyLkm4PVgh\|ryP	NX:0Nnl1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7MU[0OE8oRlODTlfFVlww[T5?
RPMI-2650	MnPhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		M4TIXWlEPTB;NEGuNVU6OyEQvF2=	NG\wd2k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODlzNkS0M{c,W0GQR1XSQE9iRg>?
KYSE-140	MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		MYrJR\|UxRTRzLkixNlMh\|ryP	MVW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFkyPjR2Lze+V2FPT0WUPD;hQi=>
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HSC-3	NW\LTZpKT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		MX\JR\|UxRTR{Lk[2OlEh\|ryP	NGHkbm89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODlzNkS0M{c,W0GQR1XSQE9iRg>?
PC-14	MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		M33ObWlEPTB;NEOuNVg5OiEQvF2=	M{PtSlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQTF4NESvK\|5USU6JRWK8M4E,
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NCI-H661	MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		MnL5TWM2OD12ND6yPVU5KM7:TR?=	NHL4c3Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODlzNkS0M{c,W0GQR1XSQE9iRg>?
IST-MEL1	MofZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		MknqTWM2OD12ND6zOVk6KM7:TR?=	MnPwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6OTZ2ND:nQnNCVkeHUkyvZV4>
HCC1806	Mm\ZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		M3H4NmlEPTB;NESuOVg4OyEQvF2=	NVPRfW1GRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7MU[0OE8oRlODTlfFVlww[T5?
COLO-800	NHPaNFZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		MofaTWM2OD12ND64OFU{KM7:TR?=	NVvFRoNoRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7MU[0OE8oRlODTlfFVlww[T5?
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BT-12	M3n1NZFJXFNiYYPzZZk>		MVPxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhSlRvMUKgZ4VtdHN?	NVztO4tIRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N\|UyOzlpPkK5OFM2OTN7PD;hQi=>
NB1643	NUXOelVmeUiWUzDhd5NigQ>?		M3vqRpFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCQQkG2OFMh[2WubIO=	MYW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-
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Rh41	MoXQdWhVWyCjc4PhfS=>		NInIfphyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiUni0NUBk\Wyucx?=	NEfXXIc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N\|UyOzl:L3G+
SJ-GBM2	NHvncY5yUFSVIHHzd4F6		MmjWdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[\|ohWHKrbXHyfUB{[3KnZX6g[o9zKFOMLVfCUVIh[2WubIO=	MkDOQIEhfGG{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、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 2021-01-06)

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135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 2021-01-06)

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