Saracatinib (AZD0530)

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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Biological Activity

Description 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.
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
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>
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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?=
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 (Km). 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)

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.

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
2 years -80°C in solvent
Smiles CN1CCN(CC1)CCOC2=CC3=C(C(=C2)OC4CCOCC4)C(=NC=N3)NC5=C(C=CC6=C5OCO6)Cl

In vivo Formulation Calculator (Clear solution)

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

mg/kg g μL

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

Mass Concentration Volume Molecular Weight

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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