Saracatinib (AZD0530)

For research use only.

Catalog No.S1006

199 publications

Saracatinib (AZD0530) Chemical Structure

CAS No. 379231-04-6

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.

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Selleck's Saracatinib (AZD0530) has been cited by 199 publications

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Choose Selective Src Inhibitors

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)
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 NHz6SnBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NULr[3o2UUN3ME2wMlA3OTR|IN88US=> MVzTRW5ITVJ?
LAMA-84 Ml;rS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHXldmtKSzVyPUCuNVU6QSEQvF2= M{fxXXNCVkeHUh?=
MEG-01 NWmwWXJzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmG5TWM2OD1yLkKzOlg5KM7:TR?= NUXhUldOW0GQR1XS
EM-2 M2fleGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmP3TWM2OD1yLkK2OUDPxE1? NWOzXlR7W0GQR1XS
TE-15 NEKzT2JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1\QUGlEPTB;MD6yO|QyOiEQvF2= M2\4bnNCVkeHUh?=
NCI-H1648 NFLK[Y1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3rBNWlEPTB;MD6yPFEyPiEQvF2= MYfTRW5ITVJ?
TE-12 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFzwV21KSzVyPUCuN|I3QCEQvF2= NX;B[|hYW0GQR1XS
LB996-RCC NGTy[oJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{jkcWlEPTB;MD60OFE6PiEQvF2= M3y5V3NCVkeHUh?=
K-562 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXfJR|UxRTBwNES5Olch|ryP M33rW3NCVkeHUh?=
D-336MG MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2S0W2lEPTB;MD61NFMxPCEQvF2= M3jnRnNCVkeHUh?=
NOS-1 MnXKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV7Kd|JDUUN3ME2wMlYxPTJ7IN88US=> MWfTRW5ITVJ?
EW-24 NGrmWVJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVfmRYFGUUN3ME2wMlYzPjl|IN88US=> MXTTRW5ITVJ?
BV-173 MmfQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3;j[2lEPTB;MD62OVI1QSEQvF2= Ml3FV2FPT0WU
NCCIT MmHMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVvJR|UxRTBwN{OyNVgh|ryP NEP2eoNUSU6JRWK=
NCI-H1436 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnHmTWM2OD1yLke5NFQ6KM7:TR?= NHnuRWJUSU6JRWK=
BB30-HNC M{LBNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFnwOnNKSzVyPUCuPFYzODNizszN MVfTRW5ITVJ?
TE-8 NGDhcYFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWXmemxXUUN3ME2wMlg4Ojd3IN88US=> NVnsWnFOW0GQR1XS
A704 MnfNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX;JR|UxRTBwOEmyNUDPxE1? MWDTRW5ITVJ?
TK10 M{TEU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV7JR|UxRTBwOUC2Olkh|ryP M3XrXnNCVkeHUh?=
KS-1 NX3N[5RXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWXZb4U1UUN3ME2xMlE6Pzd7IN88US=> MoKwV2FPT0WU
C2BBe1 MlroS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2LKVWlEPTB;MT6yNFUxPyEQvF2= NVHCc|ZQW0GQR1XS
RXF393 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{TYbGlEPTB;MT6yOFM3KM7:TR?= NEnRfXFUSU6JRWK=
KGN NFTKW|VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3OwVmlEPTB;MT6yO|Y5PyEQvF2= NXzkS5RwW0GQR1XS
NB69 NIKwSm9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEnmcmRKSzVyPUGuN|c1QTdizszN NYDWbWpWW0GQR1XS
TE-11 Mo\sS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4\USWlEPTB;MT60N|QyQCEQvF2= MUDTRW5ITVJ?
TE-1 NGDWN|RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUPJPIdpUUN3ME2xMlQ1OTB3IN88US=> MXPTRW5ITVJ?
ST486 NVTLdnNpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1LxfGlEPTB;MT60OVg2OiEQvF2= NUDRcpJlW0GQR1XS
HOP-62 Mli4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnzrTWM2OD1zLkWwNlQ3KM7:TR?= MkPqV2FPT0WU
EW-16 MnTSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVHJR|UxRTFwNUWwPFMh|ryP NW\SXVV7W0GQR1XS
LB1047-RCC Mn\pS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVntfnZRUUN3ME2xMlU2PDV|IN88US=> MoDvV2FPT0WU
TE-10 NIruS2JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHG5eVhKSzVyPUGuOlYzPTJizszN M3fQ[3NCVkeHUh?=
RL95-2 NX[1T4piT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoT1TWM2OD1zLk[2PVAzKM7:TR?= M1rEVXNCVkeHUh?=
DOHH-2 NH3t[pZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlTSTWM2OD1zLkexO|gzKM7:TR?= NXHJSIc1W0GQR1XS
MFH-ino M4LZ[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoXRTWM2OD1zLke3PFch|ryP M{XpXnNCVkeHUh?=
GB-1 NFO0cmlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVjJR|UxRTFwN{m4N|Mh|ryP MYrTRW5ITVJ?
SK-N-DZ M3\1Smdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGDnR2FKSzVyPUGuPFQ3QDhizszN NEH5SYFUSU6JRWK=
OS-RC-2 M2XSXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYfJR|UxRTFwOEi1O|Qh|ryP NWjJT2JnW0GQR1XS
SW982 MonuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{O0bWlEPTB;MT65NlA6OyEQvF2= Mo[5V2FPT0WU
KALS-1 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{DZPWlEPTB;MT65PFczOiEQvF2= NE\xV2VUSU6JRWK=
TGBC24TKB NXX6eJJzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml7aTWM2OD1{LkC1PVU5KM7:TR?= MYfTRW5ITVJ?
GI-1 NF;EXJRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mmq4TWM2OD1{LkG2NFg1KM7:TR?= MlHMV2FPT0WU
SW962 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXvJR|UxRTJwMUexO|gh|ryP M3PJcnNCVkeHUh?=
SW872 NEHkbXBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIHXV5NKSzVyPUKuNVg2ODdizszN MoPJV2FPT0WU
NCI-H747 M1y4Smdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXrOU5FXUUN3ME2yMlI2PzF2IN88US=> M2LHTHNCVkeHUh?=
MZ1-PC MnjFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3THc2lEPTB;Mj6yPVM2PiEQvF2= MlrNV2FPT0WU
MSTO-211H NWPrcGQ4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mnm4TWM2OD1{LkO1O|I{KM7:TR?= NY\tbVNqW0GQR1XS
BL-70 NIDHWmlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF;UOIxKSzVyPUKuOFc1OjJizszN MWPTRW5ITVJ?
SW954 M1HXTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4rM[WlEPTB;Mj61O|QxQCEQvF2= MUTTRW5ITVJ?
SNB75 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1vqcGlEPTB;Mj62PFU6PCEQvF2= NH\NdY9USU6JRWK=
IST-SL2 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUnLdWVkUUN3ME2yMlczOzd7IN88US=> MoTNV2FPT0WU
GCIY Mn7VS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmTQTWM2OD1{Lki3NFA2KM7:TR?= NGjkUXVUSU6JRWK=
KU812 Ml3TS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIHVSm5KSzVyPUOuNFUzQTlizszN MlnYV2FPT0WU
LXF-289 MlS2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX;JR|UxRTNwMUKxNFkh|ryP MoDYV2FPT0WU
ETK-1 NVL5O4hlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXfJR|UxRTNwMkC3Olch|ryP MXLTRW5ITVJ?
SF126 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHHOeopKSzVyPUOuN|EyPzRizszN M1zO[3NCVkeHUh?=
LC-2-ad MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{HibmlEPTB;Mz61OVch|ryP NYL6VoViW0GQR1XS
KNS-42 MnfFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWiyPXBnUUN3ME2zMlY2KM7:TR?= Mlr6V2FPT0WU
OVCAR-4 Mli4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MonWTWM2OD1|LkezOFM{KM7:TR?= NV35XYhDW0GQR1XS
PF-382 MnLoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MW\JR|UxRTNwOEO2PVgh|ryP MXLTRW5ITVJ?
SH-4 MoS0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIXIZ|FKSzVyPUSuNlUzPTlizszN M3n0XnNCVkeHUh?=
KM12 MkDkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1XVcWlEPTB;ND6zNlQyPiEQvF2= NYfIO4t4W0GQR1XS
NB5 MlrZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXXqemI5UUN3ME20MlQyQDZ2IN88US=> M3TZcnNCVkeHUh?=
KURAMOCHI NVTvPFIyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYHJR|UxRTRwNkWyOVYh|ryP MmHhV2FPT0WU
Becker M1zhe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWLKTopbUUN3ME20MlY3PDF4IN88US=> NYLBepVSW0GQR1XS
MV-4-11 NHzsRVRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIPHUZZKSzVyPUSuPFE{PDRizszN MlzFV2FPT0WU
KINGS-1 M13HOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYnXSI1PUUN3ME20MlgzOzd|IN88US=> M{H2RXNCVkeHUh?=
LS-123 NIXvVG9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIPmd4NKSzVyPUWuOFk3QDRizszN M3zDOHNCVkeHUh?=
SF268 M1z2[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHn6b5BKSzVyPUWuOlEzPjJizszN M4ryNnNCVkeHUh?=
A388 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXPJR|UxRTVwNkO2Olch|ryP NGnrdJJUSU6JRWK=
NMC-G1 M{\4Z2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWPJR|UxRTZwMEG4NVEh|ryP MnrIV2FPT0WU
CGTH-W-1 M3vPZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4DJPGlEPTB;Nj6wNlA4PSEQvF2= MVXTRW5ITVJ?
ES4 NI\wbG9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX\JR|UxRTZwNUOwO|Qh|ryP MV\TRW5ITVJ?
SR MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYTJR|UxRTZwNUi4NFch|ryP MYjTRW5ITVJ?
BB49-HNC NUG2TGllT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYS5W3F2UUN3ME22Mlc{OjB4IN88US=> NITQR4RUSU6JRWK=
KLE NWrPRW84T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVTJR|UxRTZwN{izO|ch|ryP MonjV2FPT0WU
HUTU-80 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NI\rOGFKSzVyPU[uPVg1PjZizszN MYnTRW5ITVJ?
SNU-C2B NFTWdppIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWDwSI57UUN3ME23MlgzPzN5IN88US=> NFvNR|VUSU6JRWK=
BB65-RCC NF3EOWJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXnJR|UxRTdwOUS5NFQh|ryP NHL6[lZUSU6JRWK=
QIMR-WIL MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2SyWWlEPTB;OD60NlgxQCEQvF2= M4H1bHNCVkeHUh?=
GDM-1 MlPnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MorQTWM2OD16Lkm3NlkzKM7:TR?= M{nSOHNCVkeHUh?=
LC4-1 Ml36S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYf1O4drUUN3ME25MlAxQTFzIN88US=> Mo[2V2FPT0WU
MLMA MoX3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXrJR|UxRTlwMUWwNFYh|ryP NHrjb2dUSU6JRWK=
EoL-1-cell NEm5XmVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWf0UoNmUUN3ME25MlMxOTl{IN88US=> MnPmV2FPT0WU
BOKU M2i5cGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlzVTWM2OD17Lkm2OFY3KM7:TR?= NX7rWGEyW0GQR1XS
EVSA-T NXvERXRHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2X1VWlEPTB;MUCuOlU3QCEQvF2= M4fDSnNCVkeHUh?=
D-283MED MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYXJR|UxRTFyLkmxO|Yh|ryP NFyyS2NUSU6JRWK=
NB1 MoKwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYPwOlVGUUN3ME2xNU4xOjR{IN88US=> NFPJcVdUSU6JRWK=
RPMI-8402 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYO4bFlvUUN3ME2xNU4yPzhizszN M3nZNHNCVkeHUh?=
NCI-H1355 NIjyUnFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkTlTWM2OD1zMT6xPFA3KM7:TR?= NFWwZnBUSU6JRWK=
NB7 MkDCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYXJR|UxRTFzLkOyPVch|ryP M4XE[XNCVkeHUh?=
RPMI-6666 NFLhOWhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4Hk[mlEPTB;MUKuPVU3PyEQvF2= M1jjSnNCVkeHUh?=
697 M4fWXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVjJR|UxRTF|LkK3NFEh|ryP NE[wTYVUSU6JRWK=
CTB-1 M2nWPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWLOXXpxUUN3ME2xN{42QTR6IN88US=> M{HvdXNCVkeHUh?=
VA-ES-BJ NXHNfolHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn;RTWM2OD1zMz65NlM1KM7:TR?= NHLud5ZUSU6JRWK=
BE-13 NUPndoZpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX3JR|UxRTF2LkO5NVUh|ryP NVPrU|JJW0GQR1XS
SKM-1 MlO2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1HHb2lEPTB;MUSuOFQ6QSEQvF2= NWLrUXV6W0GQR1XS
TE-6 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIfHSoFKSzVyPUG0Mlc2QTFizszN MUHTRW5ITVJ?
LB771-HNC NFfqVGpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{j5[GlEPTB;MUSuO|g6QCEQvF2= NFPJ[plUSU6JRWK=
ECC4 M4P0bmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NI\neZNKSzVyPUG3MlAzPzdizszN NEnSWo9USU6JRWK=
ES3 Mln1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkfTTWM2OD1zNz60OlU2KM7:TR?= MmjqV2FPT0WU
LB647-SCLC M{H5[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NE\NUpZKSzVyPUG3MlQ6PDlizszN MnHKV2FPT0WU
NB10 NGeyOVFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mki1TWM2OD1zOD61NlU3KM7:TR?= MUfTRW5ITVJ?
L-540 M2D5OWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXGxbZpEUUN3ME2xPE45OTB7IN88US=> NWrrb4o1W0GQR1XS
NCI-H2126 NIq4NXZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUDJR|UxRTF7LkWxJO69VQ>? NVe2UXVSW0GQR1XS
HH MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXv1UGRWUUN3ME2yNE4xODl7IN88US=> MVrTRW5ITVJ?
MPP-89 M2no[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3nSb2lEPTB;MkOuNlI5QSEQvF2= MknEV2FPT0WU
IST-MEL1 MoDxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1rWb2lEPTB;MkOuPFY2QCEQvF2= MoDOV2FPT0WU
KP-N-YS Mk\GS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYHJR|UxRTJ|LkmyOVUh|ryP MonNV2FPT0WU
EC-GI-10 NH34dVZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF\RVldKSzVyPUK0MlU6QDlizszN MYHTRW5ITVJ?
EKVX MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYPJR|UxRTJ4LkCyNFMh|ryP M1TUOnNCVkeHUh?=
TGBC1TKB NWnzOJgyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnKwTWM2OD1{Nj60N|Qh|ryP NU\1VZN2W0GQR1XS
Daudi MknMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXm3XJVnUUN3ME2yO{4xPzd|IN88US=> NEewU2ZUSU6JRWK=
ALL-PO M{C0ZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmnnTWM2OD1{Nz6wPFEh|ryP M3LTfnNCVkeHUh?=
NB6 MmDSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3fteWlEPTB;MkeuOFg5KM7:TR?= NWKyeJFlW0GQR1XS
ES6 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYPJR|UxRTJ5LkmxNlMh|ryP MmfhV2FPT0WU
COLO-320-HSR NIPu[mlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWjJR|UxRTJ6LkCzO|Mh|ryP Mn\iV2FPT0WU
K5 NF3QfYZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUjJR|UxRTJ6LkGyPFch|ryP M3rkcXNCVkeHUh?=
ES1 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEfpPYNKSzVyPUK4Mlc4PzNizszN NVKxPHd[W0GQR1XS
LC-1F NWPBNHR1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVX6OJU6UUN3ME2yPU44OzR4IN88US=> M1i4Z3NCVkeHUh?=
SCLC-21H NEP6eHZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWDHdYFRUUN3ME2zNE44OzF5IN88US=> MnXVV2FPT0WU
SK-PN-DW NHTNXJNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHjxUmdKSzVyPUOyMlU2QThizszN NVnsWodDW0GQR1XS
D-247MG NVjufVJNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHGyVZFKSzVyPUOyMlk4PzNizszN NF35fIRUSU6JRWK=
TE-5 NVLXUpIzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUTPUG5LUUN3ME2zN{4xOzZ{IN88US=> M2fN[HNCVkeHUh?=
MONO-MAC-6 NIDTWJdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2HvSmlEPTB;M{OuOVA1QCEQvF2= NGPpU45USU6JRWK=
LB2518-MEL NWLXb453T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVTJR|UxRTN|Lke2OlYh|ryP NXflbnFSW0GQR1XS
LOXIMVI M4OzOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1H4eGlEPTB;M{OuO|kzQCEQvF2= MX7TRW5ITVJ?
NCI-H209 NGjmcndIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn[4TWM2OD1|NT6xOFQh|ryP NYTE[FhIW0GQR1XS
A253 Mn7hS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFzieHNKSzVyPUO1Mlc1OjlizszN M33vWHNCVkeHUh?=
HCC1599 M1;w[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX3OR5JLUUN3ME2zOk44ODV|IN88US=> Ml\xV2FPT0WU
EB-3 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHrvdm1KSzVyPUO2Mlk2OThizszN MXfTRW5ITVJ?
GOTO NH7G[3BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUnqWFNyUUN3ME2zO{4{OjJ2IN88US=> NYDINW9EW0GQR1XS
SW684 M1ewSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MofHTWM2OD12MT64OFk2KM7:TR?= MXvTRW5ITVJ?
DEL MonjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUfJR|UxRTR{LkC1NlIh|ryP NGrtdoRUSU6JRWK=
HT-144 NXGzW|RMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHz4ZYRKSzVyPUSyMlE3PzZizszN NW\6NGNSW0GQR1XS
TE-9 Mn\DS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUHJR|UxRTR|LkS1PVYh|ryP M1f5OHNCVkeHUh?=
KARPAS-45 MoLRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnvPTWM2OD12ND6zPVI2KM7:TR?= M164VHNCVkeHUh?=
HAL-01 NEfDeoNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX;JR|UxRTR2LkWwN|Qh|ryP NI\6SVZUSU6JRWK=
RCC10RGB MoLKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{TYWGlEPTB;NESuO|M6OiEQvF2= M12ycnNCVkeHUh?=
CP67-MEL MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmLITWM2OD12NT62NlQyKM7:TR?= NHGwfHJUSU6JRWK=
NB17 M3fmemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmHKTWM2OD12NT62OlQ{KM7:TR?= NYTtSHVtW0GQR1XS
SK-UT-1 NEj4VGJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIXuTZZKSzVyPUS1Mlk1PjRizszN Ml\wV2FPT0WU
JiyoyeP-2003 NEfC[49Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFj0RWFKSzVyPUS2MlAyOTlizszN NWC4bmJ2W0GQR1XS
HCE-4 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGDnR5ZKSzVyPUS2MlU6PjhizszN M{DoTHNCVkeHUh?=
NCI-H720 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYG3VY1uUUN3ME20Ok44Pjh{IN88US=> NFr3[5VUSU6JRWK=
KARPAS-422 NVnjcoYzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mk\FTWM2OD12Nz6wPFk2KM7:TR?= M3HWPHNCVkeHUh?=
Ramos-2G6-4C10 NXLqV5V4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEXpNWFKSzVyPUS3MlE3OjJizszN MWDTRW5ITVJ?
HCE-T MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1HY[GlEPTB;NEeuOlgzQCEQvF2= MXrTRW5ITVJ?
PSN1 MlHaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVP0[|ZnUUN3ME20O{44QDF|IN88US=> MX;TRW5ITVJ?

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
pY576-FAK / pY861-FAK / FAK; 

PubMed: 20551056     


(A) HCT116 (left) and WiDr (right) cells were exposed to the indicated concentrations of saracatinib for 24 hours and the effect on total FAK or FAK phosphorylation on tyrosine 576 or 861 was assessed by western blotting. Result is representative of three independent experiments.

pY418 Src / Src / pY410 CAS / CAS / Py421 Cortactin / Cortactin; 

PubMed: 20505783     


Saracatinib inhibits Src activity and downstream Src substrate phosphorylation in HNSCC cell lines. HN31, UMSCC1 and 1483 cells were treated with DMSO vehicle or saracatinib (0.01–1 μM) for 24 h. Cells were lysed and total protein amounts were analyzed by Western blotting with total or phosphorylation site-specific antibodies for Src and the indicated substrates. Blots shown are representative of at least four independent experiments, with band intensities for each substrate quantified relative to the untreated (0 μM) condition for each cell line.

p-Akt / p-mTOR / Akt / mTOR / p-S6 / S6 / p-AMPKα / AMPKα; 

PubMed: 20811583     


PC3 cells were treated with 10 μM PP2 (left panel)/1 μM saracatinib (right panel) for 0.5, 1, 2, 4, 8, and 24 h. Cell lysates were analyzed by immunoblotting with antibodies as indicated. Controls were treated with vehicle alone. β-actin was detected as loading control.

20551056 20505783 20811583
Growth inhibition assay
Cell number; 

PubMed: 24349321     


LNCaP 104-S, 104-R1, 104-R2, PC-3, and DU-145 cells were treated with increasing concentrations of  Saracatinib for 72 hrs. Relative cell number of LNCaP cells was determined by Hoechst dye 33258-based 96-well proliferation assay. Cell numbers were normalized to control (dimethylsulfoxide) of each cell line. Triple asterisks (***) represent statistically significant difference p <0.001 between the treated group and the control group.

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

Kinase Assay:

[1]

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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]

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  • 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]

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  • 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)
Water Insoluble
Ethanol '31 mg/mL
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 powder
in solvent
Synonyms N/A
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)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O
CalculateReset

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • 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):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
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 June 1 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|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
NCT00853983 Completed Drug: [14C] AZD0530 Healthy AstraZeneca March 2009 Phase 1

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

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

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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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID