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Saracatinib (AZD0530)

Name: Saracatinib (AZD0530)
Brand: Selleck Chemicals
SKU: S1006
Rating: 5 (239 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 239 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	MlzFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?			M4\X[mlEPTB;MD6wOlE1OyEQvF2=	MnLFQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlE4ODl{Lze+V2FPT0WUPD;hQi=>
LAMA-84	NYjMcHdKT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=			MoXTTWM2OD1yLkG1PVkh\|ryP	NFfRTIk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTdyOUKvK\|5USU6JRWK8M4E,
MEG-01	MmPSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?			MYPJR\|UxRTBwMkO2PFgh\|ryP	NI[4VWE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTdyOUKvK\|5USU6JRWK8M4E,
EM-2	NIe5TYVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=			MX7JR\|UxRTBwMk[1JO69VQ>?	MY[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVcxQTJxJ{7TRW5ITVJ:L3G+
TE-15	MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?			Mlq1TWM2OD1yLkK3OFEzKM7:TR?=	MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVcxQTJxJ{7TRW5ITVJ:L3G+
NCI-H1648	MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?			MX;JR\|UxRTBwMkixNVYh\|ryP	MWW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVcxQTJxJ{7TRW5ITVJ:L3G+
TE-12	MmH2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?			MoHQTWM2OD1yLkOyOlgh\|ryP	Mk\PQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlE4ODl{Lze+V2FPT0WUPD;hQi=>
LB996-RCC	Mn\KS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?			MXzJR\|UxRTBwNESxPVYh\|ryP	MljSQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlE4ODl{Lze+V2FPT0WUPD;hQi=>
K-562	M1jQTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7			NG\MOVFKSzVyPUCuOFQ6PjdizszN	MljaQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlE4ODl{Lze+V2FPT0WUPD;hQi=>
D-336MG	Ml7YS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?			M3vVb2lEPTB;MD61NFMxPCEQvF2=	NWT6ZZM1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjF5MEmyM{c,W0GQR1XSQE9iRg>?
NOS-1	NEjIWIVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=			NIG2c41KSzVyPUCuOlA2OjlizszN	NF\Nb3g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTdyOUKvK\|5USU6JRWK8M4E,
EW-24	NYHsR2x4T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=			NHPOeVVKSzVyPUCuOlI3QTNizszN	M{XJU\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyPzB7Mj:nQnNCVkeHUkyvZV4>
BV-173	MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?			Ml33TWM2OD1yLk[1NlQ6KM7:TR?=	MUi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVcxQTJxJ{7TRW5ITVJ:L3G+
NCCIT	M1Lt[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7			NInkfWFKSzVyPUCuO\|MzOThizszN	M3;LTVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyPzB7Mj:nQnNCVkeHUkyvZV4>
NCI-H1436	MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?			NFrablRKSzVyPUCuO\|kxPDlizszN	M3;YZVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyPzB7Mj:nQnNCVkeHUkyvZV4>
BB30-HNC	M3jKVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7			M2PWO2lEPTB;MD64OlIxOyEQvF2=	NELWR449[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTdyOUKvK\|5USU6JRWK8M4E,
TE-8	NGLxXZNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=			M3TFcWlEPTB;MD64O\|I4PSEQvF2=	NH72S5U9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTdyOUKvK\|5USU6JRWK8M4E,
A704	Ml3nS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?			NFLEbHlKSzVyPUCuPFkzOSEQvF2=	MWG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVcxQTJxJ{7TRW5ITVJ:L3G+
TK10	MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?			MUPJR\|UxRTBwOUC2Olkh\|ryP	NGX2d2E9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTdyOUKvK\|5USU6JRWK8M4E,
KS-1	MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?			MljmTWM2OD1zLkG5O\|c6KM7:TR?=	MmDwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlE4ODl{Lze+V2FPT0WUPD;hQi=>
C2BBe1	NFL2fJlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=			MVXJR\|UxRTFwMkC1NFch\|ryP	M{XrUlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyPzB7Mj:nQnNCVkeHUkyvZV4>
RXF393	NIfFNHZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=			NInJd4tKSzVyPUGuNlQ{PiEQvF2=	NG\TR2o9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTdyOUKvK\|5USU6JRWK8M4E,
KGN	NXm1[nQ5T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=			MWnJR\|UxRTFwMke2PFch\|ryP	NFfXZW89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTdyOUKvK\|5USU6JRWK8M4E,
NB69	MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?			NFLhc\|ZKSzVyPUGuN\|c1QTdizszN	NIPyNYw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTdyOUKvK\|5USU6JRWK8M4E,
TE-11	NEjVU2JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=			Mmr3TWM2OD1zLkSzOFE5KM7:TR?=	NXq2b4ZuRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjF5MEmyM{c,W0GQR1XSQE9iRg>?
TE-1	NInHSHJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=			M3WwZ2lEPTB;MT60OFExPSEQvF2=	MnfPQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlE4ODl{Lze+V2FPT0WUPD;hQi=>
ST486	NGrLPZdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=			MUfJR\|UxRTFwNEW4OVIh\|ryP	MVG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVcxQTJxJ{7TRW5ITVJ:L3G+
HOP-62	NGjE[lJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=			M{DaR2lEPTB;MT61NFI1PiEQvF2=	M2e1W\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyPzB7Mj:nQnNCVkeHUkyvZV4>
EW-16	NFGwSHFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=			NVj5PFJjUUN3ME2xMlU2ODh\|IN88US=>	MmfiQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlE4ODl{Lze+V2FPT0WUPD;hQi=>
LB1047-RCC	MmnWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?			MkOxTWM2OD1zLkW1OFU{KM7:TR?=	M17DVFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyPzB7Mj:nQnNCVkeHUkyvZV4>
TE-10	NXjheGpMT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=			NFvadZhKSzVyPUGuOlYzPTJizszN	NHTWW5A9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTdyOUKvK\|5USU6JRWK8M4E,
RL95-2	MmXGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?			MmPGTWM2OD1zLk[2PVAzKM7:TR?=	MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVcxQTJxJ{7TRW5ITVJ:L3G+
DOHH-2	NXjBWVJzT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=			NVHlZVNwUUN3ME2xMlcyPzh{IN88US=>	MlqxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlE4ODl{Lze+V2FPT0WUPD;hQi=>
MFH-ino	MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?			NEjOb3RKSzVyPUGuO\|c5PyEQvF2=	NV;pZXozRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjF5MEmyM{c,W0GQR1XSQE9iRg>?
GB-1	NF36SXdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=			M3S4XmlEPTB;MT63PVg{OyEQvF2=	Mm[0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlE4ODl{Lze+V2FPT0WUPD;hQi=>
SK-N-DZ	NH7wVY9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?=			NFTBUoJKSzVyPUGuPFQ3QDhizszN	NWnVUVhlRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjF5MEmyM{c,W0GQR1XSQE9iRg>?
OS-RC-2	MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?			NXvyZmFGUUN3ME2xMlg5PTd2IN88US=>	NVTiUo9JRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjF5MEmyM{c,W0GQR1XSQE9iRg>?
SW982	NW\vfVJmT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=			MXvJR\|UxRTFwOUKwPVMh\|ryP	NEHueFk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTdyOUKvK\|5USU6JRWK8M4E,
KALS-1	M1Pa[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7			M2noV2lEPTB;MT65PFczOiEQvF2=	NWDMNmFoRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjF5MEmyM{c,W0GQR1XSQE9iRg>?
TGBC24TKB	MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?			MkLITWM2OD1{LkC1PVU5KM7:TR?=	NXjMe5hHRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjF5MEmyM{c,W0GQR1XSQE9iRg>?
GI-1	M4HZWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7			MmDZTWM2OD1{LkG2NFg1KM7:TR?=	M2ThVlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyPzB7Mj:nQnNCVkeHUkyvZV4>
SW962	NIS3eGVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=			MmDSTWM2OD1{LkG3NVc5KM7:TR?=	MojIQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlE4ODl{Lze+V2FPT0WUPD;hQi=>
SW872	NXLsdW1tT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=			MYXJR\|UxRTJwMUi1NFch\|ryP	M2\pPVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyPzB7Mj:nQnNCVkeHUkyvZV4>
NCI-H747	NYnXV5NtT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=			MVHJR\|UxRTJwMkW3NVQh\|ryP	NXHlTJo4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjF5MEmyM{c,W0GQR1XSQE9iRg>?
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KP-N-YS	NEDqW2tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=			MoflTWM2OD1{Mz65NlU2KM7:TR?=	NX31eo4xRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjF5MEmyM{c,W0GQR1XSQE9iRg>?
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A253	NF3PSoJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=			M4j1SWlEPTB;M{WuO\|QzQSEQvF2=	NV76SW1sRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjF5MEmyM{c,W0GQR1XSQE9iRg>?
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SW684	MnvTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?			M4TXUGlEPTB;NEGuPFQ6PSEQvF2=	NUHGW49zRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjF5MEmyM{c,W0GQR1XSQE9iRg>?
DEL	MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?			NVfRVY0xUUN3ME20Nk4xPTJ{IN88US=>	NV\TdGh[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjF5MEmyM{c,W0GQR1XSQE9iRg>?
HT-144	MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?			M3TJbWlEPTB;NEKuNVY4PiEQvF2=	MX68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVcxQTJxJ{7TRW5ITVJ:L3G+
TE-9	Mk\PS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?			MnvFTWM2OD12Mz60OVk3KM7:TR?=	MYq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVcxQTJxJ{7TRW5ITVJ:L3G+
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SK-N-SH	MX;xTHRUKGG\|c3H5			NUTkfnBSeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC\|Y4Ll[Y4h\m:{IGPLMW4uW0hiY3XscJM>	NWX4Tm1TRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N\|UyOzlpPkK5OFM2OTN7PD;hQi=>
OHS-50	NGP4[XFyUFSVIHHzd4F6			MonXdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[\|ohWHKrbXHyfUB{[3KnZX6g[o9zKE:KUz21NEBk\Wyucx?=	M{f1T\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
SJ-GBM2	NHTIVppyUFSVIHHzd4F6			MmLrdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[\|ohWHKrbXHyfUB{[3KnZX6g[o9zKFOMLVfCUVIh[2WubIO=	M{LzTVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
SK-N-MC	Mn31dWhVWyCjc4PhfS=>			MWrxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhW0tvTj3NR{Bk\Wyucx?=	M4nrXFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
LAN-5	NH\pOVNyUFSVIHHzd4F6			NI\NfYxyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiTFHOMVUh[2WubIO=	NYTONXZERGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N\|UyOzlpPkK5OFM2OTN7PD;hQi=>
HEK293	NVrKXnVWTnWwY4Tpc44h[XO\|YYm=	NIfGVXgxNjFidH:gNUB2VQ>?	M3HBcVE3KGi{cx?=	NXPQRlhFUW6qaXLpeIlwdiCxZjDjc4xt[WenbjDJMYlv\HWlZXSgSGRTOiCLNkO4SkBufXSjboSgLJVvc26xd36gc5Jq\2mwKTDwbI9{eGixconsZZRqd25iZYjwdoV{e2WmIHnuJGhGUzJ7MzDj[YxteyCjdDCwMlEhfG9iMTD1UUBi\nSncjCxOkBpenNiYomgW4V{fGW{bjDicI91fGmwZx?=	MmHKQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZzOUGzOlkoRjJ4MUmxN\|Y6RC:jPh?=

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 2022-01-17)

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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