Saracatinib (AZD0530)

Catalog No.S1006

Saracatinib (AZD0530) Chemical Structure

Molecular Weight(MW): 542.03

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). Phase 2/3.

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Cited by 49 Publications

Purity & Quality Control

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). 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 Mk[1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX7JR|UxRTBwME[xOFMh|ryP NIX4XoFUSU6JRWK=
LAMA-84 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWHpUpdXUUN3ME2wMlE2QTlizszN MnjpV2FPT0WU
MEG-01 M3vQXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3zwR2lEPTB;MD6yN|Y5QCEQvF2= M1ziNXNCVkeHUh?=
EM-2 NYDsSYUzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYL1PIE3UUN3ME2wMlI3PSEQvF2= NH\1U5ZUSU6JRWK=
TE-15 NVrhN5d5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2TkZ2lEPTB;MD6yO|QyOiEQvF2= MVfTRW5ITVJ?
NCI-H1648 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWnJR|UxRTBwMkixNVYh|ryP MkC5V2FPT0WU
TE-12 M4fhU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX\JR|UxRTBwM{K2PEDPxE1? M2q3dnNCVkeHUh?=
LB996-RCC M{mxVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3\0W2lEPTB;MD60OFE6PiEQvF2= MWHTRW5ITVJ?
K-562 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{PodmlEPTB;MD60OFk3PyEQvF2= NYr0VGd7W0GQR1XS
D-336MG MlnyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHTYVFZKSzVyPUCuOVA{ODRizszN MnX4V2FPT0WU
NOS-1 NU\6XpJST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MY\JR|UxRTBwNkC1Nlkh|ryP NWXKUZdmW0GQR1XS
EW-24 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYXJR|UxRTBwNkK2PVMh|ryP NYfofXM2W0GQR1XS
BV-173 M1jXeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVfJR|UxRTBwNkWyOFkh|ryP M3flWHNCVkeHUh?=
NCCIT M1;hZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkPlTWM2OD1yLkezNlE5KM7:TR?= Mnf3V2FPT0WU
NCI-H1436 NEXPe4tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3\TVmlEPTB;MD63PVA1QSEQvF2= MUPTRW5ITVJ?
BB30-HNC NXT1Zmh7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mlq5TWM2OD1yLki2NlA{KM7:TR?= NFvvcVhUSU6JRWK=
TE-8 Ml\CS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn\OTWM2OD1yLki3Nlc2KM7:TR?= NIe5UXhUSU6JRWK=
A704 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn;tTWM2OD1yLki5NlEh|ryP NFjPTGtUSU6JRWK=
TK10 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2rMWWlEPTB;MD65NFY3QSEQvF2= NVO4NmhyW0GQR1XS
KS-1 NFTYXnRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWDxT21uUUN3ME2xMlE6Pzd7IN88US=> Mm\LV2FPT0WU
C2BBe1 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{PpXWlEPTB;MT6yNFUxPyEQvF2= NVTVcGlpW0GQR1XS
RXF393 MkjKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEfGXZNKSzVyPUGuNlQ{PiEQvF2= NWraSW5uW0GQR1XS
KGN M2m3RWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVT1VXpxUUN3ME2xMlI4Pjh5IN88US=> MYXTRW5ITVJ?
NB69 MmXGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoXqTWM2OD1zLkO3OFk4KM7:TR?= M3nXfHNCVkeHUh?=
TE-11 M4jHd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlfUTWM2OD1zLkSzOFE5KM7:TR?= MXzTRW5ITVJ?
TE-1 Mn3HS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX6zNIhvUUN3ME2xMlQ1OTB3IN88US=> M2XpW3NCVkeHUh?=
ST486 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUTBWY4{UUN3ME2xMlQ2QDV{IN88US=> NIDldG5USU6JRWK=
HOP-62 M3nQZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4GzPGlEPTB;MT61NFI1PiEQvF2= NV\4bIRLW0GQR1XS
EW-16 MnvCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVvhempyUUN3ME2xMlU2ODh|IN88US=> NYe4TlU6W0GQR1XS
LB1047-RCC MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVnJR|UxRTFwNUW0OVMh|ryP MUnTRW5ITVJ?
TE-10 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NILufIFKSzVyPUGuOlYzPTJizszN NX7M[2hpW0GQR1XS
RL95-2 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXTkOJp5UUN3ME2xMlY3QTB{IN88US=> MWLTRW5ITVJ?
DOHH-2 NWmxZ44xT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1LTfmlEPTB;MT63NVc5OiEQvF2= MXvTRW5ITVJ?
MFH-ino MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYTJR|UxRTFwN{e4O{DPxE1? MV\TRW5ITVJ?
GB-1 Mli2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkfMTWM2OD1zLke5PFM{KM7:TR?= M4izc3NCVkeHUh?=
SK-N-DZ NGLXUGpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHPUTHVKSzVyPUGuPFQ3QDhizszN MVXTRW5ITVJ?
OS-RC-2 M1HNdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MofuTWM2OD1zLki4OVc1KM7:TR?= M4PGeXNCVkeHUh?=
SW982 NI[2OnNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHrWSpFKSzVyPUGuPVIxQTNizszN MlXNV2FPT0WU
KALS-1 M4HhVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYTsUI1LUUN3ME2xMlk5PzJ{IN88US=> NWjqbYE3W0GQR1XS
TGBC24TKB MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn;4TWM2OD1{LkC1PVU5KM7:TR?= NUXzW2QzW0GQR1XS
GI-1 M2L6c2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYnJR|UxRTJwMU[wPFQh|ryP MYjTRW5ITVJ?
SW962 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWjJR|UxRTJwMUexO|gh|ryP MY\TRW5ITVJ?
SW872 NWXwRnNOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmrYTWM2OD1{LkG4OVA4KM7:TR?= NHLrUFhUSU6JRWK=
NCI-H747 Ml3TS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnHpTWM2OD1{LkK1O|E1KM7:TR?= NEP4UXFUSU6JRWK=
MZ1-PC NFvadWtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn:wTWM2OD1{LkK5N|U3KM7:TR?= NFzjRpJUSU6JRWK=
MSTO-211H MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWLJR|UxRTJwM{W3NlMh|ryP M4\HNnNCVkeHUh?=
BL-70 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHSxN4pKSzVyPUKuOFc1OjJizszN NIOwc5VUSU6JRWK=
SW954 NVOyRpI4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFzWZ5JKSzVyPUKuOVc1ODhizszN MYrTRW5ITVJ?
SNB75 NFHCOpNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{[wc2lEPTB;Mj62PFU6PCEQvF2= Mny3V2FPT0WU
IST-SL2 NF:1TGlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWXJR|UxRTJwN{KzO|kh|ryP NVrDXlRmW0GQR1XS
GCIY Ml34S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4Ds[WlEPTB;Mj64O|AxPSEQvF2= M1uwc3NCVkeHUh?=
KU812 M33tUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV:1RVdkUUN3ME2zMlA2Ojl7IN88US=> M4rB[3NCVkeHUh?=
LXF-289 M3rJTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MofITWM2OD1|LkGyNVA6KM7:TR?= MUnTRW5ITVJ?
ETK-1 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXLaXo5{UUN3ME2zMlIxPzZ5IN88US=> M37wNXNCVkeHUh?=
SF126 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NE\6WHNKSzVyPUOuN|EyPzRizszN MUDTRW5ITVJ?
LC-2-ad MoTSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MknGTWM2OD1|LkW1O{DPxE1? MVTTRW5ITVJ?
KNS-42 MmT1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUDVNodXUUN3ME2zMlY2KM7:TR?= NWXS[ot{W0GQR1XS
OVCAR-4 MmLMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4WyWmlEPTB;Mz63N|Q{OyEQvF2= NUfIV4VDW0GQR1XS
PF-382 Mmn5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWLJR|UxRTNwOEO2PVgh|ryP Mn\vV2FPT0WU
SH-4 M1HLfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYDacJoyUUN3ME20MlI2OjV7IN88US=> Mn:1V2FPT0WU
KM12 M{\wdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1jlOmlEPTB;ND6zNlQyPiEQvF2= NIjyemdUSU6JRWK=
NB5 MmLiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXPoXGsxUUN3ME20MlQyQDZ2IN88US=> NI\VepZUSU6JRWK=
KURAMOCHI NVSwbGw5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYjJR|UxRTRwNkWyOVYh|ryP NX;wVJhTW0GQR1XS
Becker NIPqbGJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlfHTWM2OD12Lk[2OFE3KM7:TR?= M{iyfnNCVkeHUh?=
MV-4-11 NVvDXnQ3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWnJR|UxRTRwOEGzOFQh|ryP NEmyV5BUSU6JRWK=
KINGS-1 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVrNSYR{UUN3ME20MlgzOzd|IN88US=> M3vrfnNCVkeHUh?=
LS-123 MnyzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnHwTWM2OD13LkS5Olg1KM7:TR?= M1rtRnNCVkeHUh?=
SF268 MnnPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV3JR|UxRTVwNkGyOlIh|ryP Mn24V2FPT0WU
A388 NUnLZYx7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NG[0XFRKSzVyPUWuOlM3PjdizszN NGfwU45USU6JRWK=
NMC-G1 M1;aOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUPJR|UxRTZwMEG4NVEh|ryP MWPTRW5ITVJ?
CGTH-W-1 M3u1fGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnXITWM2OD14LkCyNFc2KM7:TR?= M2q5[HNCVkeHUh?=
ES4 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFLjUHVKSzVyPU[uOVMxPzRizszN NF;OZWJUSU6JRWK=
SR MlSzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml\0TWM2OD14LkW4PFA4KM7:TR?= MmPPV2FPT0WU
BB49-HNC MmLpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYfJR|UxRTZwN{OyNFYh|ryP M4rZOHNCVkeHUh?=
KLE M4PBeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVL3XWRyUUN3ME22Mlc5Ozd5IN88US=> NWrpT5FtW0GQR1XS
HUTU-80 Mm\mS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M37oXWlEPTB;Nj65PFQ3PiEQvF2= MVrTRW5ITVJ?
SNU-C2B NUjVZZlWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmLyTWM2OD15LkiyO|M4KM7:TR?= NUG3fpJqW0GQR1XS
BB65-RCC MojwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2L0SWlEPTB;Nz65OFkxPCEQvF2= M{j4bXNCVkeHUh?=
QIMR-WIL M1zVOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{m1fmlEPTB;OD60NlgxQCEQvF2= NXrEVox[W0GQR1XS
GDM-1 M4XFTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXvJR|UxRThwOUeyPVIh|ryP NVviRY5bW0GQR1XS
LC4-1 NYHoWnYyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkfxTWM2OD17LkCwPVEyKM7:TR?= MYXTRW5ITVJ?
MLMA MlLXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWrmVodxUUN3ME25MlE2ODB4IN88US=> Ml3YV2FPT0WU
EoL-1-cell M3rxXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIjH[oZKSzVyPUmuN|AyQTJizszN NUjhNJVOW0GQR1XS
BOKU Mnz5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M176RWlEPTB;OT65OlQ3PiEQvF2= MVrTRW5ITVJ?
EVSA-T M4O3SGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYDJR|UxRTFyLk[1Olgh|ryP NUDZOIdiW0GQR1XS
D-283MED NIfsdGxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX\2O4pFUUN3ME2xNE46OTd4IN88US=> M1;jbnNCVkeHUh?=
NB1 M3HZN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml7UTWM2OD1zMT6wNlQzKM7:TR?= NIPXelRUSU6JRWK=
RPMI-8402 NVvYb2JzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NULaNIxxUUN3ME2xNU4yPzhizszN MljZV2FPT0WU
NCI-H1355 NHTUbnNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MljlTWM2OD1zMT6xPFA3KM7:TR?= NWny[VZOW0GQR1XS
NB7 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1mwT2lEPTB;MUGuN|I6PyEQvF2= NFPyTpBUSU6JRWK=
RPMI-6666 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEXwUW5KSzVyPUGyMlk2PjdizszN Mk\HV2FPT0WU
697 Mk\YS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{\hVGlEPTB;MUOuNlcxOSEQvF2= NGi5SoVUSU6JRWK=
CTB-1 MmjyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmSwTWM2OD1zMz61PVQ5KM7:TR?= MWjTRW5ITVJ?
VA-ES-BJ NF3kZVFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4PIXGlEPTB;MUOuPVI{PCEQvF2= MnH6V2FPT0WU
BE-13 NHexWmNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2riW2lEPTB;MUSuN|kyPSEQvF2= MmDZV2FPT0WU
SKM-1 NUS1VnB5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFLQTnBKSzVyPUG0MlQ1QTlizszN NFjWOFZUSU6JRWK=
TE-6 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX\JR|UxRTF2Lke1PVEh|ryP M3PlcHNCVkeHUh?=
LB771-HNC M3nUOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkXSTWM2OD1zND63PFk5KM7:TR?= MVrTRW5ITVJ?
ECC4 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEPhS5hKSzVyPUG3MlAzPzdizszN NH3iV4lUSU6JRWK=
ES3 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2fhe2lEPTB;MUeuOFY2PSEQvF2= MkHFV2FPT0WU
LB647-SCLC NVHaVm14T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUTJR|UxRTF5LkS5OFkh|ryP MYrTRW5ITVJ?
NB10 MknuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWLJR|UxRTF6LkWyOVYh|ryP MXfTRW5ITVJ?
L-540 M4q3PGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVm5VphUUUN3ME2xPE45OTB7IN88US=> NGi4O|ZUSU6JRWK=
NCI-H2126 NWLENHhqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1:1WmlEPTB;MUmuOVEh|ryP NYe2T4ZFW0GQR1XS
HH MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3nHVWlEPTB;MkCuNFA6QSEQvF2= NHnCWWRUSU6JRWK=
MPP-89 MnfFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXj2NIRxUUN3ME2yN{4zOjh7IN88US=> NIDiTHFUSU6JRWK=
IST-MEL1 NEO4VWNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M16yO2lEPTB;MkOuPFY2QCEQvF2= MnqwV2FPT0WU
KP-N-YS M1\XPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4nuXmlEPTB;MkOuPVI2PSEQvF2= MX\TRW5ITVJ?
EC-GI-10 NIDDN4VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXTJR|UxRTJ2LkW5PFkh|ryP M{PoWnNCVkeHUh?=
EKVX MnTaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mle4TWM2OD1{Nj6wNlA{KM7:TR?= M1jRSHNCVkeHUh?=
TGBC1TKB MoXoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NID3VXJKSzVyPUK2MlQ{PCEQvF2= NYL3SoRMW0GQR1XS
Daudi NF;PcYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYLufVhFUUN3ME2yO{4xPzd|IN88US=> NWXXZXJTW0GQR1XS
ALL-PO NYXyVJN1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2LYXGlEPTB;MkeuNFgyKM7:TR?= M1X4UXNCVkeHUh?=
NB6 NIj1XXNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWPsVpF4UUN3ME2yO{41QDhizszN MYXTRW5ITVJ?
ES6 NITHT|JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVHJR|UxRTJ5LkmxNlMh|ryP M3PTdnNCVkeHUh?=
COLO-320-HSR M1jYXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWHJR|UxRTJ6LkCzO|Mh|ryP M12y[nNCVkeHUh?=
K5 M2GzR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV\JR|UxRTJ6LkGyPFch|ryP NFHFUldUSU6JRWK=
ES1 NYXVR5VLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlT5TWM2OD1{OD63O|c{KM7:TR?= M2n0eXNCVkeHUh?=
LC-1F MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4TYNWlEPTB;MkmuO|M1PiEQvF2= NXTzO2VqW0GQR1XS
SCLC-21H NXfYUWtDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVXJR|UxRTNyLkezNVch|ryP M3jXOnNCVkeHUh?=
SK-PN-DW NF;UTFFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoXMTWM2OD1|Mj61OVk5KM7:TR?= Mk\qV2FPT0WU
D-247MG M{PEeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NILV[HRKSzVyPUOyMlk4PzNizszN NHzadGhUSU6JRWK=
TE-5 Ml;PS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXvJR|UxRTN|LkCzOlIh|ryP NYPZVmVVW0GQR1XS
MONO-MAC-6 MljSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1v4XmlEPTB;M{OuOVA1QCEQvF2= M1jNVnNCVkeHUh?=
LB2518-MEL NWLudmdGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGfafIJKSzVyPUOzMlc3PjZizszN MUXTRW5ITVJ?
LOXIMVI MnXmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYXFW|Z4UUN3ME2zN{44QTJ6IN88US=> NH7ZcmhUSU6JRWK=
NCI-H209 M1PpOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NG\weFJKSzVyPUO1MlE1PCEQvF2= MkXoV2FPT0WU
A253 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWjSTHFJUUN3ME2zOU44PDJ7IN88US=> MnjvV2FPT0WU
HCC1599 MljNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWLJR|UxRTN4LkewOVMh|ryP NGrPNpJUSU6JRWK=
EB-3 NF3IdnZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2ixdGlEPTB;M{[uPVUyQCEQvF2= Ml\oV2FPT0WU
GOTO Ml3VS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoHMTWM2OD1|Nz6zNlI1KM7:TR?= NELVcZlUSU6JRWK=
SW684 NVvvZ3k2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYSzSZFrUUN3ME20NU45PDl3IN88US=> NI\jb5JUSU6JRWK=
DEL NHrYWJpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1n1NGlEPTB;NEKuNFUzOiEQvF2= MU\TRW5ITVJ?
HT-144 MmDXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEf5cHVKSzVyPUSyMlE3PzZizszN NXK0Rm5WW0GQR1XS
TE-9 Mm\6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoDLTWM2OD12Mz60OVk3KM7:TR?= NHrwU45USU6JRWK=
KARPAS-45 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEDhOoRKSzVyPUS0MlM6OjVizszN MmnuV2FPT0WU
HAL-01 NWX1RoVxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmDxTWM2OD12ND61NFM1KM7:TR?= Mn;jV2FPT0WU
RCC10RGB M173Zmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2\aWGlEPTB;NESuO|M6OiEQvF2= M1XySXNCVkeHUh?=
CP67-MEL NFPLcHBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml3JTWM2OD12NT62NlQyKM7:TR?= MVjTRW5ITVJ?
NB17 M3;E[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{nIXmlEPTB;NEWuOlY1OyEQvF2= MmHCV2FPT0WU
SK-UT-1 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mnz1TWM2OD12NT65OFY1KM7:TR?= M3nQcnNCVkeHUh?=
JiyoyeP-2003 MorJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFT5d2NKSzVyPUS2MlAyOTlizszN Mn7UV2FPT0WU
HCE-4 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MknUTWM2OD12Nj61PVY5KM7:TR?= MWDTRW5ITVJ?
NCI-H720 NX:2bWE5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVn5eWRJUUN3ME20Ok44Pjh{IN88US=> MXLTRW5ITVJ?
KARPAS-422 NXXhNVNLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIq5TWVKSzVyPUS3MlA5QTVizszN NHe1[3ZUSU6JRWK=
Ramos-2G6-4C10 NGC2PZVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2K2eGlEPTB;NEeuNVYzOiEQvF2= NXrjZo5[W0GQR1XS
HCE-T MoHkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVXaXJpZUUN3ME20O{43QDJ6IN88US=> M3f2PHNCVkeHUh?=
PSN1 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn7oTWM2OD12Nz63PFE{KM7:TR?= NHnaenZUSU6JRWK=

... 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]
+ Expand

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]
+ Expand
  • 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]
+ Expand
  • Animal Models: CB17 mice are implanted with DU145 cells.
  • Formulation: Dissolved in 0.5% hydroxypropyl methylcellulose, 0.1% Tween 80
  • 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 powder
in solvent
Synonyms N/A

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 (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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*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 )

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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

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

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Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03661125 Not yet recruiting Parkinson Disease Psychosis King''s College London|AstraZeneca|King''s College Hospital NHS Trust April 11 2019 Early Phase 1
NCT03661125 Not yet recruiting Parkinson Disease Psychosis King''s College London|AstraZeneca|King''s College Hospital NHS Trust April 11 2019 Early Phase 1
NCT02955186 Recruiting Alcohol Drinking Yale University May 9 2017 Phase 2
NCT02955186 Recruiting Alcohol Drinking Yale University May 9 2017 Phase 2
NCT02737202 Recruiting Pulmonary Lymphangioleiomyomatosis Baylor College of Medicine|University of Cincinnati|Brigham and Women''s Hospital|Stanford University|Loyola University|University of South Florida|National Institutes of Health (NIH) April 2016 Phase 2
NCT02737202 Recruiting Pulmonary Lymphangioleiomyomatosis Baylor College of Medicine|University of Cincinnati|Brigham and Women''s Hospital|Stanford University|Loyola University|University of South Florida|National Institutes of Health (NIH) April 2016 Phase 2

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.

  • * Indicates a Required Field

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

selleck catalog

Src Signaling Pathway Map

Src Inhibitors with Unique Features

  • Most Potent Src Inhibitor

    Dasatinib : Src, IC50=0.8 nM.

  • FDA-approved Src Inhibitor

    Bosutinib (SKI-606) : Approved by FDA for Ph+ chronic myelogenous leukemia (CML).

  • Newest Src Inhibitor

    PP1 : Potent and selective Src inhibitor for Lck/Fyn with IC50 of 5 nM/ 6 nM.

  • Classic Src Inhibitor

    KX2-391 : The first clinical Src inhibitor (peptidomimetic class) that targets the peptide substrate site of Src, with GI50 of 9-60 nM in cancer cell lines.

Related Src Products4

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  • SU6656 New

    SU 6656 is a selective Src family kinase inhibitor with IC50 of 280 nM, 20 nM, 130 nM, and 170 nM for Src, Yes, Lyn, and Fyn, respectively.

  • PX-478 2HCl New

    PX-478 2HCl is an orally active, and selective hypoxia-inducible factor-1α (HIF-1α) inhibitor. Phase 1.

  • Bosutinib (SKI-606)

    Bosutinib (SKI-606) is a novel, dual Src/Abl inhibitor with IC50 of 1.2 nM and 1 nM in cell-free assays, respectively.

  • Dasatinib

    Dasatinib is a novel, potent and multi-targeted inhibitor that targets Abl, Src and c-Kit, with IC50 of <1 nM, 0.8 nM and 79 nM in cell-free assays, respectively.

  • KX2-391

    KX2-391, the first clinical Src inhibitor (peptidomimetic class) that targets the peptide substrate site of Src, with GI50 of 9-60 nM in cancer cell lines. Phase 2.

  • PP1

    PP1 is a potent and selective Src inhibitor for Lck/Fyn with IC50 of 5 nM/ 6 nM.

  • PP2

    PP2, a Src family kinase inhibitor, potently inhibits Lck/Fyn with IC50 of 4 nM/5 nM in cell-free assays, ~100-fold less potent to EGFR, inactive for ZAP-70, JAK2 and PKA.

  • WH-4-023

    WH-4-023 is a potent and orally active Lck/Src inhibitor with IC50s of 2 nM and 6 nM in cell-free assays, respectively. Exhibits >300-fold selectivity against p38α and KDR. Also potently inhibits SIK (IC50 values are 10, 22 and 60 nM for SIK 1, 2 and 3 respectively) and displays selectivity over a range of closely related kinases.

  • Ibrutinib (PCI-32765)

    Ibrutinib (PCI-32765) is a potent and highly selective Brutons tyrosine kinase (Btk) inhibitor with IC50 of 0.5 nM in cell-free assays, modestly potent to Bmx, CSK, FGR, BRK, HCK, less potent to EGFR, Yes, ErbB2, JAK3, etc.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID