Saracatinib (AZD0530)

For research use only. Not for use in humans.

Catalog No.S1006

183 publications

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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Selleck's Saracatinib (AZD0530) has been cited by 183 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 NULCeJFnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkHQTWM2OD1yLkC2NVQ{KM7:TR?= M13vcXNCVkeHUh?=
LAMA-84 M2DDfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlzFTWM2OD1yLkG1PVkh|ryP MlPNV2FPT0WU
MEG-01 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnX2TWM2OD1yLkKzOlg5KM7:TR?= Ml3EV2FPT0WU
EM-2 MnLWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkDaTWM2OD1yLkK2OUDPxE1? MlvnV2FPT0WU
TE-15 M2m1emdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXm0fY53UUN3ME2wMlI4PDF{IN88US=> NESydXZUSU6JRWK=
NCI-H1648 M4XHRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXTJR|UxRTBwMkixNVYh|ryP NF;xcppUSU6JRWK=
TE-12 MlvrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIjjWllKSzVyPUCuN|I3QCEQvF2= M3y0bnNCVkeHUh?=
LB996-RCC M4T0dWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{PRb2lEPTB;MD60OFE6PiEQvF2= M2DRXnNCVkeHUh?=
K-562 NGLwS5VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX\IVI81UUN3ME2wMlQ1QTZ5IN88US=> MU\TRW5ITVJ?
D-336MG NFHJSoFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX;JR|UxRTBwNUCzNFQh|ryP NUf4fY42W0GQR1XS
NOS-1 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUPJR|UxRTBwNkC1Nlkh|ryP M1G1cHNCVkeHUh?=
EW-24 M3jkd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUPk[lFNUUN3ME2wMlYzPjl|IN88US=> NFn6PYFUSU6JRWK=
BV-173 MmDSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1j1ZWlEPTB;MD62OVI1QSEQvF2= NHjrVYRUSU6JRWK=
NCCIT MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIXYbppKSzVyPUCuO|MzOThizszN M{\XcnNCVkeHUh?=
NCI-H1436 NYnXWphVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3;LcWlEPTB;MD63PVA1QSEQvF2= Mln1V2FPT0WU
BB30-HNC NVXINHJvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX3VPHkzUUN3ME2wMlg3OjB|IN88US=> M4jXVXNCVkeHUh?=
TE-8 MmHWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{\0emlEPTB;MD64O|I4PSEQvF2= MUTTRW5ITVJ?
A704 NGH2RoJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnjQTWM2OD1yLki5NlEh|ryP NV;LUXZCW0GQR1XS
TK10 NXrmfWo6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXfJcINRUUN3ME2wMlkxPjZ7IN88US=> M3K1O3NCVkeHUh?=
KS-1 NWXubJBwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2LEdGlEPTB;MT6xPVc4QSEQvF2= MWjTRW5ITVJ?
C2BBe1 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml3jTWM2OD1zLkKwOVA4KM7:TR?= MWLTRW5ITVJ?
RXF393 MmSxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml3xTWM2OD1zLkK0N|Yh|ryP MU\TRW5ITVJ?
KGN MmnuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUXWeoNPUUN3ME2xMlI4Pjh5IN88US=> MUDTRW5ITVJ?
NB69 NXz2N3N[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1jSRmlEPTB;MT6zO|Q6PyEQvF2= MlvUV2FPT0WU
TE-11 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEnacpJKSzVyPUGuOFM1OThizszN NV\DfGE2W0GQR1XS
TE-1 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml[zTWM2OD1zLkS0NVA2KM7:TR?= M4PyfHNCVkeHUh?=
ST486 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYrJR|UxRTFwNEW4OVIh|ryP NFqzdodUSU6JRWK=
HOP-62 NXjzRWhLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2T5SGlEPTB;MT61NFI1PiEQvF2= MWLTRW5ITVJ?
EW-16 M3fxVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVnJR|UxRTFwNUWwPFMh|ryP MUDTRW5ITVJ?
LB1047-RCC MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEflU4NKSzVyPUGuOVU1PTNizszN NFq0UXpUSU6JRWK=
TE-10 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXOx[3M5UUN3ME2xMlY3OjV{IN88US=> MknnV2FPT0WU
RL95-2 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmLpTWM2OD1zLk[2PVAzKM7:TR?= MU\TRW5ITVJ?
DOHH-2 NWO2cWdDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV72UXh4UUN3ME2xMlcyPzh{IN88US=> MXLTRW5ITVJ?
MFH-ino NWjYd41tT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYfk[JAyUUN3ME2xMlc4QDdizszN NGHYNJNUSU6JRWK=
GB-1 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWTJR|UxRTFwN{m4N|Mh|ryP M{Pa[HNCVkeHUh?=
SK-N-DZ MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHjyT5lKSzVyPUGuPFQ3QDhizszN NVXvenBrW0GQR1XS
OS-RC-2 Ml7LS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1GyWWlEPTB;MT64PFU4PCEQvF2= MWDTRW5ITVJ?
SW982 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXfJR|UxRTFwOUKwPVMh|ryP NH;0NIpUSU6JRWK=
KALS-1 MlXGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFmyXINKSzVyPUGuPVg4OjJizszN NILueWFUSU6JRWK=
TGBC24TKB MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmLUTWM2OD1{LkC1PVU5KM7:TR?= MmrKV2FPT0WU
GI-1 NYfvWFhqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWq0e4lKUUN3ME2yMlE3ODh2IN88US=> NVfSTnlzW0GQR1XS
SW962 NHLyV2JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVHJR|UxRTJwMUexO|gh|ryP NH3SOGVUSU6JRWK=
SW872 NF3lcohIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2DtOmlEPTB;Mj6xPFUxPyEQvF2= NV62N3V4W0GQR1XS
NCI-H747 NFnTZ41Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml7rTWM2OD1{LkK1O|E1KM7:TR?= MonOV2FPT0WU
MZ1-PC NHXCXXJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVPJR|UxRTJwMkmzOVYh|ryP M3XVc3NCVkeHUh?=
MSTO-211H NVXu[ldQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGrVU3JKSzVyPUKuN|U4OjNizszN NVjVbGN5W0GQR1XS
BL-70 NF;N[JBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGnwSWNKSzVyPUKuOFc1OjJizszN NVXWe2o6W0GQR1XS
SW954 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHflfnhKSzVyPUKuOVc1ODhizszN M{W0ZXNCVkeHUh?=
SNB75 M1PmT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{DBfGlEPTB;Mj62PFU6PCEQvF2= MmraV2FPT0WU
IST-SL2 MkTlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXrJR|UxRTJwN{KzO|kh|ryP M1rOfXNCVkeHUh?=
GCIY MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVLjU2s6UUN3ME2yMlg4ODB3IN88US=> NYC2NVVRW0GQR1XS
KU812 NHj6R2hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEPsTJZKSzVyPUOuNFUzQTlizszN NIXHc2hUSU6JRWK=
LXF-289 M1fOOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX;PeG05UUN3ME2zMlEzOTB7IN88US=> NHPQSI9USU6JRWK=
ETK-1 M{n2Zmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4H0VmlEPTB;Mz6yNFc3PyEQvF2= NUOy[GxMW0GQR1XS
SF126 NILacIJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlrRTWM2OD1|LkOxNVc1KM7:TR?= NVfB[IszW0GQR1XS
LC-2-ad NX3Xc29IT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1vZbGlEPTB;Mz61OVch|ryP M2fQdHNCVkeHUh?=
KNS-42 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF35TmlKSzVyPUOuOlUh|ryP M2jLTXNCVkeHUh?=
OVCAR-4 Mlf3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEPae|dKSzVyPUOuO|M1OzNizszN M1OzOXNCVkeHUh?=
PF-382 M2raV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVTJR|UxRTNwOEO2PVgh|ryP M1XUS3NCVkeHUh?=
SH-4 NHj0[YlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlzRTWM2OD12LkK1NlU6KM7:TR?= NUTLZmxwW0GQR1XS
KM12 NUG5VVdIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVjJR|UxRTRwM{K0NVYh|ryP MYnTRW5ITVJ?
NB5 NH;RU2dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV;JR|UxRTRwNEG4OlQh|ryP M{LFeXNCVkeHUh?=
KURAMOCHI M4TWXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXfDSm5OUUN3ME20MlY2OjV4IN88US=> NVvnUFRbW0GQR1XS
Becker NEnUUmtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlzBTWM2OD12Lk[2OFE3KM7:TR?= NH32PXBUSU6JRWK=
MV-4-11 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUXJR|UxRTRwOEGzOFQh|ryP M1r2N3NCVkeHUh?=
KINGS-1 NVrTeox7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEPCdW1KSzVyPUSuPFI{PzNizszN MlzTV2FPT0WU
LS-123 NXz6ephNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkPuTWM2OD13LkS5Olg1KM7:TR?= MlzGV2FPT0WU
SF268 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUG1cIRSUUN3ME21MlYyOjZ{IN88US=> NXTuWGd6W0GQR1XS
A388 NF[5clhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1;NVmlEPTB;NT62N|Y3PyEQvF2= MlWzV2FPT0WU
NMC-G1 M{n1dGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF\aWW1KSzVyPU[uNFE5OTFizszN NEL3SHlUSU6JRWK=
CGTH-W-1 NGLjPIZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIPmXZhKSzVyPU[uNFIxPzVizszN MkKxV2FPT0WU
ES4 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF3N[|ZKSzVyPU[uOVMxPzRizszN M2fsXnNCVkeHUh?=
SR M3vGSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYTZV2J[UUN3ME22MlU5QDB5IN88US=> NELEOoFUSU6JRWK=
BB49-HNC M1u2Tmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2HMNmlEPTB;Nj63N|IxPiEQvF2= MkTaV2FPT0WU
KLE M1fGU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1z2[GlEPTB;Nj63PFM4PyEQvF2= M3qzTnNCVkeHUh?=
HUTU-80 NVj4cYxCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVjUXoJ4UUN3ME22Mlk5PDZ4IN88US=> NGLheIRUSU6JRWK=
SNU-C2B NWnLdYVrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFL0ZolKSzVyPUeuPFI4OzdizszN MnKxV2FPT0WU
BB65-RCC NV7VSnk{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NETFO3NKSzVyPUeuPVQ6ODRizszN NXrXSnBHW0GQR1XS
QIMR-WIL MnL5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXLJR|UxRThwNEK4NFgh|ryP M2Pqe3NCVkeHUh?=
GDM-1 NUW0Z4hNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4jxbGlEPTB;OD65O|I6OiEQvF2= M2HBdXNCVkeHUh?=
LC4-1 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmTKTWM2OD17LkCwPVEyKM7:TR?= MlPKV2FPT0WU
MLMA NW\XeGR6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWnFT|BzUUN3ME25MlE2ODB4IN88US=> MXfTRW5ITVJ?
EoL-1-cell MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGrKSYpKSzVyPUmuN|AyQTJizszN MXvTRW5ITVJ?
BOKU MnyzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHvoV3RKSzVyPUmuPVY1PjZizszN NHTpOHNUSU6JRWK=
EVSA-T M{[1dWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2G5RWlEPTB;MUCuOlU3QCEQvF2= NIPtUVRUSU6JRWK=
D-283MED M1rG[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NW\tXXRTUUN3ME2xNE46OTd4IN88US=> NH;5fYZUSU6JRWK=
NB1 M1zF[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWPJR|UxRTFzLkCyOFIh|ryP NILKU2pUSU6JRWK=
RPMI-8402 M{DoeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MknWTWM2OD1zMT6xO|gh|ryP MXnTRW5ITVJ?
NCI-H1355 M3XON2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUD6VXA5UUN3ME2xNU4yQDB4IN88US=> NED6WG1USU6JRWK=
NB7 NYfHXHl7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGPKSIhKSzVyPUGxMlMzQTdizszN MlPIV2FPT0WU
RPMI-6666 NVXSXXZlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWTsNoNnUUN3ME2xNk46PTZ5IN88US=> NX24PHpHW0GQR1XS
697 Mm\4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVjJR|UxRTF|LkK3NFEh|ryP M3OxVnNCVkeHUh?=
CTB-1 M{ficGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGrD[GFKSzVyPUGzMlU6PDhizszN NG\hR2pUSU6JRWK=
VA-ES-BJ MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWnJR|UxRTF|LkmyN|Qh|ryP MWDTRW5ITVJ?
BE-13 M4P3Omdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnHQTWM2OD1zND6zPVE2KM7:TR?= NVfZRopOW0GQR1XS
SKM-1 NXXFbGxOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGrobVJKSzVyPUG0MlQ1QTlizszN MmXxV2FPT0WU
TE-6 M{jpfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFLSR5VKSzVyPUG0Mlc2QTFizszN MX\TRW5ITVJ?
LB771-HNC MkXOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkjlTWM2OD1zND63PFk5KM7:TR?= MVPTRW5ITVJ?
ECC4 NHe5T3hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXjtZ2tJUUN3ME2xO{4xOjd5IN88US=> NFrmSVNUSU6JRWK=
ES3 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWfmfFNXUUN3ME2xO{41PjV3IN88US=> M{C0UnNCVkeHUh?=
LB647-SCLC MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmXtTWM2OD1zNz60PVQ6KM7:TR?= M4Die3NCVkeHUh?=
NB10 Mki3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGPKS3pKSzVyPUG4MlUzPTZizszN MVzTRW5ITVJ?
L-540 NVvvbYE6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmDiTWM2OD1zOD64NVA6KM7:TR?= NIniT4VUSU6JRWK=
NCI-H2126 MmnxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHHkfnRKSzVyPUG5MlUyKM7:TR?= NWru[2FsW0GQR1XS
HH M2T3eGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXHJR|UxRTJyLkCwPVkh|ryP Mn7lV2FPT0WU
MPP-89 NVz0TVBtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NW\GfGE3UUN3ME2yN{4zOjh7IN88US=> NX30PJFKW0GQR1XS
IST-MEL1 Ml\QS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mnr4TWM2OD1{Mz64OlU5KM7:TR?= MY\TRW5ITVJ?
KP-N-YS M4LF[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFTD[Y1KSzVyPUKzMlkzPTVizszN MVjTRW5ITVJ?
EC-GI-10 M2PiWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4O5OGlEPTB;MkSuOVk5QSEQvF2= NYTxUWJGW0GQR1XS
EKVX NUS3fIdbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGjtVHJKSzVyPUK2MlAzODNizszN NVniXIhxW0GQR1XS
TGBC1TKB MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF\ITGFKSzVyPUK2MlQ{PCEQvF2= MXnTRW5ITVJ?
Daudi NUD5V2JOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NY\OZZA3UUN3ME2yO{4xPzd|IN88US=> NHLLbFFUSU6JRWK=
ALL-PO NF;3U2hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mnq0TWM2OD1{Nz6wPFEh|ryP MW\TRW5ITVJ?
NB6 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2mycmlEPTB;MkeuOFg5KM7:TR?= MWLTRW5ITVJ?
ES6 NVqwdYtCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYXJR|UxRTJ5LkmxNlMh|ryP Mn;iV2FPT0WU
COLO-320-HSR NXH2N5B5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoPpTWM2OD1{OD6wN|c{KM7:TR?= NXri[VM1W0GQR1XS
K5 M2XMOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVfJR|UxRTJ6LkGyPFch|ryP MorWV2FPT0WU
ES1 MoH1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MofqTWM2OD1{OD63O|c{KM7:TR?= M4O2enNCVkeHUh?=
LC-1F NWHLT3JNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mnr0TWM2OD1{OT63N|Q3KM7:TR?= MX;TRW5ITVJ?
SCLC-21H NVy3R283T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV\0ZY9JUUN3ME2zNE44OzF5IN88US=> M1\HcnNCVkeHUh?=
SK-PN-DW NYniVYJFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M37rXWlEPTB;M{KuOVU6QCEQvF2= MmDkV2FPT0WU
D-247MG M3r5Umdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mo\BTWM2OD1|Mj65O|c{KM7:TR?= NVvJTWY3W0GQR1XS
TE-5 MkXaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MljqTWM2OD1|Mz6wN|YzKM7:TR?= NXGyNod6W0GQR1XS
MONO-MAC-6 MnHFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXrJ[W9JUUN3ME2zN{42ODR6IN88US=> NILXTmtUSU6JRWK=
LB2518-MEL M2rw[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFywUXhKSzVyPUOzMlc3PjZizszN M173NXNCVkeHUh?=
LOXIMVI NUe0V2hDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mlj0TWM2OD1|Mz63PVI5KM7:TR?= NGTqSXlUSU6JRWK=
NCI-H209 NYTuZlJjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkjlTWM2OD1|NT6xOFQh|ryP NGHreIFUSU6JRWK=
A253 NUC3TGo3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUTJR|UxRTN3Lke0Nlkh|ryP M1jSTHNCVkeHUh?=
HCC1599 M3jjOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVnJR|UxRTN4LkewOVMh|ryP MWXTRW5ITVJ?
EB-3 NIXUeZJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlXsTWM2OD1|Nj65OVE5KM7:TR?= NFXBRolUSU6JRWK=
GOTO MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{LoOmlEPTB;M{euN|IzPCEQvF2= M1PvPXNCVkeHUh?=
SW684 NUfRc4VyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYTDXoxxUUN3ME20NU45PDl3IN88US=> NWjKOo93W0GQR1XS
DEL M3HPNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnnyTWM2OD12Mj6wOVIzKM7:TR?= MYrTRW5ITVJ?
HT-144 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUTZUVlNUUN3ME20Nk4yPjd4IN88US=> M2PJZXNCVkeHUh?=
TE-9 M{jJWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnzmTWM2OD12Mz60OVk3KM7:TR?= NFXoRYpUSU6JRWK=
KARPAS-45 NUTab|FzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHzEcHRKSzVyPUS0MlM6OjVizszN M4\1dXNCVkeHUh?=
HAL-01 M1jMVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4jP[mlEPTB;NESuOVA{PCEQvF2= NH;uT2VUSU6JRWK=
RCC10RGB NITmZlNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlzsTWM2OD12ND63N|kzKM7:TR?= NVXP[ZNUW0GQR1XS
CP67-MEL NHfJSmpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX3JR|UxRTR3Lk[yOFEh|ryP M{LmR3NCVkeHUh?=
NB17 MmPtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHjacFhKSzVyPUS1MlY3PDNizszN MlX1V2FPT0WU
SK-UT-1 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2fn[GlEPTB;NEWuPVQ3PCEQvF2= Ml\mV2FPT0WU
JiyoyeP-2003 M3O5R2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF73VYtKSzVyPUS2MlAyOTlizszN NIridIRUSU6JRWK=
HCE-4 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX;JR|UxRTR4LkW5Olgh|ryP Mk\lV2FPT0WU
NCI-H720 M{X3TWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIXDb3hKSzVyPUS2Mlc3QDJizszN MYDTRW5ITVJ?
KARPAS-422 MmjzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmXvTWM2OD12Nz6wPFk2KM7:TR?= M3HsRnNCVkeHUh?=
Ramos-2G6-4C10 NH;mV2JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlLVTWM2OD12Nz6xOlIzKM7:TR?= NHTM[I1USU6JRWK=
HCE-T MnznS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{DVWWlEPTB;NEeuOlgzQCEQvF2= NVHnUZNmW0GQR1XS
PSN1 NVXhVZNVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3P5NGlEPTB;NEeuO|gyOyEQvF2= NUDjTJV[W0GQR1XS

... 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.
  • 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
Smiles CN1CCN(CCOC2=CC(=C3C(=NC=NC3=C2)NC4=C(Cl)C=CC5=C4OCO5)OC6CCOCC6)CC1

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
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    Volume
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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 )

  • C1
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    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):
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    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
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
NCT00752206 Completed Drug: Saracatinib|Drug: Placebo Osteosarcoma Sarcoma Alliance for Research through Collaboration|AstraZeneca March 2009 Phase 2
NCT00771979 Completed Drug: AZD0530 Healthy AstraZeneca November 2008 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