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Saracatinib (AZD0530)

Name: Saracatinib (AZD0530)
Brand: Selleck Chemicals
SKU: S1006
Rating: 5 (237 reviews)

Catalog No.S1006

For research use only.

Saracatinib (AZD0530) is a potent Src inhibitor with IC50 of 2.7 nM in cell-free assays, and potent to c-Yes, Fyn, Lyn, Blk, Fgr and Lck; less active for Abl and EGFR (L858R and L861Q). Saracatinib induces autophagy. Phase 2/3.

Saracatinib (AZD0530) Chemical Structure

CAS No. 379231-04-6

Selleck's Saracatinib (AZD0530) has been cited by 237 publications

Purity & Quality Control

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Src Signaling Pathway Map

Biological Activity

Description

Features

The 1st Src inhibitor to show inhibition of the Src pathway in human tumor tissue.

Targets

c-Src ^[2] (Cell-free assay)	LCK ^[2] (Cell-free assay)	c-YES ^[2] (Cell-free assay)	EGFR (L861Q) ^[2] (Cell-free assay)	Lyn ^[2] (Cell-free assay)	Click to View More Targets
2.7 nM	<4 nM	4 nM	4 nM	5 nM	Click to View More Targets

In vitro

Saracatinib also potently inhibits other Src tyrosine kinase family members including c-Yes, Fyn, Lyn, Blk, Fgr, and Lck with IC50 from 4-10 nM. Saracatinib sensitively inhibits Src Y530F NIH 3T3 with IC50 of 80 nM. Saracatinib signiﬁcantly impairs the invasion of HT1080 cells through a 3-dimensional collagen matrix and completely inhibits EGF-induced cell scattering in NBT-II bladder cancer cells. ^[1] Saracatinib potent inhibits Src activation in DU145 and PC3 cells, which through inhibition of Y419 phosphorylation. Saracatinib inhibits the growth of prostate cancer including PC3, DU145, CWR22Rv1 and LNCaP, while Saracatinib shows low activity in LAPC-4, PZ-HPV7 and RWPE-1 cells. Saracatinib induces cell cycle arrest at G1/S but not caspase 3 cleavages. Saracatinib also significantly inhibits DU145 and PC3 migration in the Boyden chamber. ^[2] Saracatinib gives a potent and sustained blockage of AKT and enhances the sensitivity to irradiation in A549 and Calu-6 cells. ^[3] Saracatinib inhibits osteoclast in activity, resorption and formation. Saracatinib also reversibly prevents osteoclast precursor migration. ^[4]

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	Formulation	Activity Description	PMID

CTV-1	MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?			NFuy[HpKSzVyPUCuNFYyPDNizszN	M2LzOlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyPzB7Mj:nQnNCVkeHUkyvZV4>
LAMA-84	Ml;vS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?			MVzJR\|UxRTBwMUW5PUDPxE1?	Mn;kQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlE4ODl{Lze+V2FPT0WUPD;hQi=>
MEG-01	M1f2S2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7			MUfJR\|UxRTBwMkO2PFgh\|ryP	NELWS4g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTdyOUKvK\|5USU6JRWK8M4E,
EM-2	MnHIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?			NUGwRoVTUUN3ME2wMlI3PSEQvF2=	NXnMWG45RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjF5MEmyM{c,W0GQR1XSQE9iRg>?
TE-15	M1\VbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7			M1\VeWlEPTB;MD6yO\|QyOiEQvF2=	M{\YclxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyPzB7Mj:nQnNCVkeHUkyvZV4>
NCI-H1648	NFTTWo9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?=			NH7qSWNKSzVyPUCuNlgyOTZizszN	M3HoO\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyPzB7Mj:nQnNCVkeHUkyvZV4>
TE-12	NIjkW5pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=			M13hVGlEPTB;MD6zNlY5KM7:TR?=	MWe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVcxQTJxJ{7TRW5ITVJ:L3G+
LB996-RCC	NVjGbolPT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=			M2XnUGlEPTB;MD60OFE6PiEQvF2=	M4XaZlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyPzB7Mj:nQnNCVkeHUkyvZV4>
K-562	NHrIZ\|FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=			NXqzUZNIUUN3ME2wMlQ1QTZ5IN88US=>	MnrQQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlE4ODl{Lze+V2FPT0WUPD;hQi=>
D-336MG	NWKze\|R3T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=			MXzJR\|UxRTBwNUCzNFQh\|ryP	NVy4PYF5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjF5MEmyM{c,W0GQR1XSQE9iRg>?
NOS-1	MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?			M4fkdWlEPTB;MD62NFUzQSEQvF2=	MmXtQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlE4ODl{Lze+V2FPT0WUPD;hQi=>
EW-24	M2jwSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7			M{TEcWlEPTB;MD62NlY6OyEQvF2=	NV;QWHp[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjF5MEmyM{c,W0GQR1XSQE9iRg>?
BV-173	MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?			NVL6e\|VDUUN3ME2wMlY2OjR7IN88US=>	MX[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVcxQTJxJ{7TRW5ITVJ:L3G+
NCCIT	M{nSUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7			NUGzT3VKUUN3ME2wMlc{OjF6IN88US=>	MnKwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlE4ODl{Lze+V2FPT0WUPD;hQi=>
NCI-H1436	MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?			NIr1WVFKSzVyPUCuO\|kxPDlizszN	NYXPXopSRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjF5MEmyM{c,W0GQR1XSQE9iRg>?
BB30-HNC	MnjhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?			MkDRTWM2OD1yLki2NlA{KM7:TR?=	M1HudVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyPzB7Mj:nQnNCVkeHUkyvZV4>
TE-8	Mn22S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?			NWXIT4VEUUN3ME2wMlg4Ojd3IN88US=>	MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVcxQTJxJ{7TRW5ITVJ:L3G+
A704	Mn\US5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?			MmjtTWM2OD1yLki5NlEh\|ryP	NEDVUpk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTdyOUKvK\|5USU6JRWK8M4E,
TK10	M{Pi[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7			NV\LcGY6UUN3ME2wMlkxPjZ7IN88US=>	MWS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVcxQTJxJ{7TRW5ITVJ:L3G+
KS-1	NILCdHJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=			NX7BfohXUUN3ME2xMlE6Pzd7IN88US=>	M3Xub\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyPzB7Mj:nQnNCVkeHUkyvZV4>
C2BBe1	NFfpSFdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=			NWjUUHVCUUN3ME2xMlIxPTB5IN88US=>	MoThQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlE4ODl{Lze+V2FPT0WUPD;hQi=>
RXF393	MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?			Mle1TWM2OD1zLkK0N\|Yh\|ryP	NVTFXW9QRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjF5MEmyM{c,W0GQR1XSQE9iRg>?
KGN	NX:5fnFST3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=			NYDMe217UUN3ME2xMlI4Pjh5IN88US=>	MmrhQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlE4ODl{Lze+V2FPT0WUPD;hQi=>
NB69	NWHBPFRnT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=			Ml3vTWM2OD1zLkO3OFk4KM7:TR?=	NF6yO\|M9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTdyOUKvK\|5USU6JRWK8M4E,
TE-11	NGmyNmFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=			MlvSTWM2OD1zLkSzOFE5KM7:TR?=	M4rrWlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyPzB7Mj:nQnNCVkeHUkyvZV4>
TE-1	NYTSeJpmT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=			NFjzNIRKSzVyPUGuOFQyODVizszN	M4DLT\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyPzB7Mj:nQnNCVkeHUkyvZV4>
ST486	MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?			MYnJR\|UxRTFwNEW4OVIh\|ryP	NVT1SlZwRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjF5MEmyM{c,W0GQR1XSQE9iRg>?
HOP-62	M1TtZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7			M{WyXWlEPTB;MT61NFI1PiEQvF2=	M2G0UlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyPzB7Mj:nQnNCVkeHUkyvZV4>
EW-16	M2CzdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7			NFzuWoxKSzVyPUGuOVUxQDNizszN	NVTrNmgxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjF5MEmyM{c,W0GQR1XSQE9iRg>?
LB1047-RCC	NFTTTJFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=			MW\JR\|UxRTFwNUW0OVMh\|ryP	MnrIQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlE4ODl{Lze+V2FPT0WUPD;hQi=>
TE-10	Ml7DS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?			M3XGT2lEPTB;MT62OlI2OiEQvF2=	MoDyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlE4ODl{Lze+V2FPT0WUPD;hQi=>
RL95-2	NHrKTVhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=			MUTJR\|UxRTFwNk[5NFIh\|ryP	MlWyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlE4ODl{Lze+V2FPT0WUPD;hQi=>
DOHH-2	Ml3JS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?			Mlr3TWM2OD1zLkexO\|gzKM7:TR?=	NF;iXnA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTdyOUKvK\|5USU6JRWK8M4E,
MFH-ino	NFqyW5RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=			MnXHTWM2OD1zLke3PFch\|ryP	NV3JSHhwRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjF5MEmyM{c,W0GQR1XSQE9iRg>?
GB-1	MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?			M1v5dGlEPTB;MT63PVg{OyEQvF2=	NFrRd3E9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTdyOUKvK\|5USU6JRWK8M4E,
SK-N-DZ	M2HEbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7			M1\sZ2lEPTB;MT64OFY5QCEQvF2=	Ml;EQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlE4ODl{Lze+V2FPT0WUPD;hQi=>
OS-RC-2	NWXwSYlST3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=			MVjJR\|UxRTFwOEi1O\|Qh\|ryP	M4DmcFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyPzB7Mj:nQnNCVkeHUkyvZV4>
SW982	NGn0bHZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=			M2PhbmlEPTB;MT65NlA6OyEQvF2=	Mkm2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlE4ODl{Lze+V2FPT0WUPD;hQi=>
KALS-1	M2X3VGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7			NG\qRm5KSzVyPUGuPVg4OjJizszN	MY[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVcxQTJxJ{7TRW5ITVJ:L3G+
TGBC24TKB	Mo[1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?			NUnCR\|JIUUN3ME2yMlA2QTV6IN88US=>	NHO1dY09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTdyOUKvK\|5USU6JRWK8M4E,
GI-1	M4DTXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7			NIXjbmRKSzVyPUKuNVYxQDRizszN	NVLQZnQ3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjF5MEmyM{c,W0GQR1XSQE9iRg>?
SW962	M33Pb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7			NF;6bGVKSzVyPUKuNVcyPzhizszN	M3PvblxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyPzB7Mj:nQnNCVkeHUkyvZV4>
SW872	NUnYNnlQT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=			MlznTWM2OD1{LkG4OVA4KM7:TR?=	NEnZfXc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTdyOUKvK\|5USU6JRWK8M4E,
NCI-H747	MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?			MWHJR\|UxRTJwMkW3NVQh\|ryP	MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVcxQTJxJ{7TRW5ITVJ:L3G+
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BB65-RCC	MnTPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?			MUnJR\|UxRTdwOUS5NFQh\|ryP	M2LRSlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyPzB7Mj:nQnNCVkeHUkyvZV4>
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GDM-1	NHzwb5NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=			NIfiNXRKSzVyPUiuPVczQTJizszN	NY\yNpdGRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjF5MEmyM{c,W0GQR1XSQE9iRg>?
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EoL-1-cell	M{[4Tmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7			NIDLTmJKSzVyPUmuN\|AyQTJizszN	MYK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVcxQTJxJ{7TRW5ITVJ:L3G+
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D-283MED	Mo\SS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?			MXvJR\|UxRTFyLkmxO\|Yh\|ryP	M4e3OlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyPzB7Mj:nQnNCVkeHUkyvZV4>
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RPMI-8402	NV7aZ\|R6T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=			NYXidFdIUUN3ME2xNU4yPzhizszN	M374N\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyPzB7Mj:nQnNCVkeHUkyvZV4>
NCI-H1355	NFHwbotIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=			M{\1fmlEPTB;MUGuNVgxPiEQvF2=	M37l[VxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyPzB7Mj:nQnNCVkeHUkyvZV4>
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RPMI-6666	M2\vTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7			MYHJR\|UxRTF{Lkm1Olch\|ryP	NVTrXYR3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjF5MEmyM{c,W0GQR1XSQE9iRg>?
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LB771-HNC	NHm3NpFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=			NFuwfWhKSzVyPUG0Mlc5QThizszN	MmXzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlE4ODl{Lze+V2FPT0WUPD;hQi=>
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NCI-H2126	MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?			M3nPcmlEPTB;MUmuOVEh\|ryP	M3XvflxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyPzB7Mj:nQnNCVkeHUkyvZV4>
HH	Mo\pS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?			MXvJR\|UxRTJyLkCwPVkh\|ryP	M4fBTFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyPzB7Mj:nQnNCVkeHUkyvZV4>
MPP-89	M{DtSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7			NF3B[WlKSzVyPUKzMlIzQDlizszN	NVHKOJU2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjF5MEmyM{c,W0GQR1XSQE9iRg>?
IST-MEL1	NFjyXWtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=			MW\JR\|UxRTJ\|Lki2OVgh\|ryP	MXm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVcxQTJxJ{7TRW5ITVJ:L3G+
KP-N-YS	NETBWmxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=			MVnJR\|UxRTJ\|LkmyOVUh\|ryP	MXi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVcxQTJxJ{7TRW5ITVJ:L3G+
EC-GI-10	NGHzdnRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=			MX\JR\|UxRTJ2LkW5PFkh\|ryP	NUfSdY91RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjF5MEmyM{c,W0GQR1XSQE9iRg>?
EKVX	M3zIe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7			M2fIdGlEPTB;Mk[uNFIxOyEQvF2=	NVfLSo9uRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjF5MEmyM{c,W0GQR1XSQE9iRg>?
TGBC1TKB	MmnzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?			M2robGlEPTB;Mk[uOFM1KM7:TR?=	NIi1N4g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTdyOUKvK\|5USU6JRWK8M4E,
Daudi	MnjCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?			NVziPI0{UUN3ME2yO{4xPzd\|IN88US=>	MkDBQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlE4ODl{Lze+V2FPT0WUPD;hQi=>
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COLO-320-HSR	NWrkZ\|J6T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=			NEmx[5ZKSzVyPUK4MlA{PzNizszN	M2PpO\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyPzB7Mj:nQnNCVkeHUkyvZV4>
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NCI-H209	MkDkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?			NVH2SmRoUUN3ME2zOU4yPDRizszN	MUS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVcxQTJxJ{7TRW5ITVJ:L3G+
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GOTO	MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?			MmDuTWM2OD1\|Nz6zNlI1KM7:TR?=	M3XWeFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyPzB7Mj:nQnNCVkeHUkyvZV4>
SW684	MljES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?			NVXWS3RRUUN3ME20NU45PDl3IN88US=>	MnnqQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlE4ODl{Lze+V2FPT0WUPD;hQi=>
DEL	NXfpV2RUT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=			MlLnTWM2OD12Mj6wOVIzKM7:TR?=	NXTaWZFJRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjF5MEmyM{c,W0GQR1XSQE9iRg>?
HT-144	M4PzdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7			NE\JVW1KSzVyPUSyMlE3PzZizszN	NIrFW\|g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTdyOUKvK\|5USU6JRWK8M4E,
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KARPAS-45	M2\yemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7			MWXJR\|UxRTR2LkO5NlUh\|ryP	M1PaXVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyPzB7Mj:nQnNCVkeHUkyvZV4>
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OHS-50	NXz5T3R5eUiWUzDhd5NigQ>?			NXrnNoNReUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC\|Y4Ll[Y4h\m:{IF;IV{02OCClZXzsdy=>	MVK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-
SJ-GBM2	NGnHXlByUFSVIHHzd4F6			NVTMR5BQeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC\|Y4Ll[Y4h\m:{IGPKMWdDVTJiY3XscJM>	Mmi2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=
SK-N-MC	NHPlWJJyUFSVIHHzd4F6			NX3QbnBxeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC\|Y4Ll[Y4h\m:{IGPLMW4uVUNiY3XscJM>	MYS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-
LAN-5	NIPPdpdyUFSVIHHzd4F6			MVvxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhVEGQLUWgZ4VtdHN?	NHm1SpA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N\|UyOzl:L3G+
HEK293	M3qwbGZ2dmO2aX;uJIF{e2G7	NVHXeHl5OC5zIITvJFEhfU1?	Ml\PNVYhcHK\|	MoDiTY5pcWKrdHnvckBw\iClb3zsZYdmdiCLLXnu[JVk\WRiRFTSNkBKPjN6RjDteZRidnRiKIXub45wf25ib4Lp[4lvMSCyaH;zdIhwenmuYYTpc44h\XiycnXzd4VlKGmwIFjFT\|I6OyClZXzsd{BifCByLkGgeI8hOSC3TTDh[pRmeiBzNjDodpMh[nliV3XzeIVzdiCkbH;0eIlv\w>?	M1THWFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4MUmxN\|Y6Lz5{NkG5NVM3QTxxYU6=

Click to View More Cell Line Experimental Data

Assay

Methods	Test Index	PMID

Western blot	pY576-FAK / pY861-FAK / FAK ; pY418 Src / Src / pY410 CAS / CAS / Py421 Cortactin / Cortactin ; p-Akt / p-mTOR / Akt / mTOR / p-S6 / S6 / p-AMPKα / AMPKα	20551056 20505783 20811583
Growth inhibition assay	Cell number	24349321

In vivo

Saracatinib shows great tumor growth inhibition in Src3T3 allografts and a moderate growth delay in Calu-6, MDA-MB-231, AsPc-1 and BT474C xenografts. ^[1] Saracatinib shows great antitumor activity in orthotopic DU145 xenograft mice at a dose of 25mg/kg (orally administered, daily). ^[2]

Protocol (from reference)

Kinase Assay: ^[1]	Kinase Assay: IC50 of tyrosine kinase activity is measured by an enzyme-linked immunosorbent assay (ELISA) with recombinant catalytic domains of a panel of receptor and non-receptor tyrosine kinases (in some cases only part of the catalytic domain is used). Saracatinib dose ranges from 0.001-10 mM. Speciﬁcity assays against a panel of serine/threonine kinases are performed using a ﬁlter capture assay with ³²P. Brieﬂy, multidrop 384 plates containing 0.5 μL Saracatinib or controls (DMSO) alone or pH 3.0 buffer controls) are incubated with 15 μL of enzyme plus peptide/protein substrate for 5 min before the reaction is initiated by the addition of 10 μL of 20 mM Mg-ATP. For all enzymes the ﬁnal concentration is approximated to the Michaelis constant (K_m). Assays are carried out for 30min at room temperature before termination by the addition of 5 μL orthophosphoric acid. After mixing, the well contents are harvested onto a P81 Uniﬁlter plate, using orthophosphoric acid as the wash buffer. Then IC50 is calculated.
Cell Research: ^[1]	Cell lines: PC3, DU145, CWR22Rv1, LNCaP, LAPC-4, PZ-HPV7 and RWPE-1 cells Concentrations: 62.5 nM - 16 mM Incubation Time: 1, 3 and 5 days Method: Cells are seeded at a density of 2× 10³ in 96-well plates and incubated overnight. Then Saracatinib (62.5 nM-16 mM) is added to the cells. After 1, 3 and 5 days, culture medium is removed followed by addition of 0.2 mL DMSO per well and continuous shaking of plates at 200 rotations per minute for 15min. Then IC50 is measured by MTT metho (Only for Reference)
Animal Research: ^[1]	Animal Models: CB17 mice are implanted with DU145 cells. Dosages: 25 mg/kg Administration: Orally administered daily (Only for Reference)

References

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Solubility (25°C)

In vitro	DMSO	35 mg/mL warmed (64.57 mM)
	Ethanol	31 mg/mL (57.19 mM)
	Water	Insoluble
In vivo	Add solvents to the product individually and in order (Data is from Selleck tests instead of citations): 2% DMSO+30% PEG 300+ddH2O For best results, use promptly after mixing. Click to purchase: PEG300	5mg/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	542.03
Formula	C₂₇H₃₂ClN₅O₅
CAS No.	379231-04-6
Storage	3 years	-20°C	powder
Storage	2 years	-80°C	in solvent
Smiles	CN1CCN(CC1)CCOC2=CC3=C(C(=C2)OC4CCOCC4)C(=NC=N3)NC5=C(C=CC6=C5OCO6)Cl

Download Saracatinib (AZD0530) SDF

In vivo Formulation Calculator (Clear solution)

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

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Dilution Calculator Molecular Weight Calculator

Clinical Trial Information

NCT Number	Recruitment	Interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT04598919	Recruiting	Drug: Saracatinab\|Drug: Placebo	Idiopathic Pulmonary Fibrosis (IPF)	National Jewish Health\|Yale University\|Icahn School of Medicine at Mount Sinai\|AstraZeneca\|National Center for Advancing Translational Science (NCATS)	November 12 2020	Phase 1\|Phase 2
NCT04307953	Recruiting	Drug: AZD0530 Difumarate\|Drug: Matching placebo	Fibrodysplasia Ossificans Progressiva	VU University Medical Center\|Royal National Orthopaedic Hospital NHS Trust\|Klinikum Garmisch-Patenkirchen\|University of Oxford\|Brigham and Women''s Hospital\|AstraZeneca\|Innovative Medicines Initiative	August 5 2020	Phase 2
NCT02085603	Completed	Drug: Saracatinib\|Drug: Placebo	Cancer	Sheffield Teaching Hospitals NHS Foundation Trust\|AstraZeneca	March 2014	Phase 2
NCT01864655	Completed	Drug: saracatinib\|Drug: Placebo	Alzheimer''s Disease	Stephen M. Strittmatter\|National Institute of Neurological Disorders and Stroke (NINDS)\|Yale University	July 2013	Phase 1
NCT01000896	Withdrawn	Drug: AZD0530\|Drug: Carboplatin\|Drug: paclitaxel	Cancer\|Non Small Cell Lung Cancer\|Epithelial Ovarian Cancer	AstraZeneca	January 2010	Phase 1

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

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Frequently Asked Questions

Question 1:
What is the half-life of Saracatinib?

Answer:
Based on the following paper, the half-life of Saracatinib in vivo is around 40hours and it reaches its peak lever around 2-4 hours after dosing: http://clincancerres.aacrjournals.org/content/16/19/4876.long

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