Saracatinib (AZD0530)

For research use only.

Catalog No.S1006

209 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.

Size Price Stock Quantity  
10mM (1mL in DMSO) USD 91 In stock
USD 70 In stock
USD 170 In stock
USD 670 In stock
Bulk Discount

Free Overnight Delivery on orders over $ 500
Next day delivery by 10:00 a.m. Order now.

Selleck's Saracatinib (AZD0530) has been cited by 209 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). 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 NXfmZ|dMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MojKTWM2OD1yLkC2NVQ{KM7:TR?= NVnMd|FEW0GQR1XS
LAMA-84 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1nicmlEPTB;MD6xOVk6KM7:TR?= M2O3e3NCVkeHUh?=
MEG-01 M{jMV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{nadmlEPTB;MD6yN|Y5QCEQvF2= NX7iS|UyW0GQR1XS
EM-2 M2\j[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4m3NGlEPTB;MD6yOlUh|ryP MU\TRW5ITVJ?
TE-15 NHTOTXhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYS5eYR[UUN3ME2wMlI4PDF{IN88US=> MWTTRW5ITVJ?
NCI-H1648 NFq4UGxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUjJR|UxRTBwMkixNVYh|ryP NXTBSIZtW0GQR1XS
TE-12 MoflS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF;qfHRKSzVyPUCuN|I3QCEQvF2= MU\TRW5ITVJ?
LB996-RCC Mm\RS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXzJR|UxRTBwNESxPVYh|ryP M{nIO3NCVkeHUh?=
K-562 M2[zR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHXJUlVKSzVyPUCuOFQ6PjdizszN NHz0cJpUSU6JRWK=
D-336MG NG\XUpVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX;JR|UxRTBwNUCzNFQh|ryP MVPTRW5ITVJ?
NOS-1 NYDwTI4yT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFXYeXlKSzVyPUCuOlA2OjlizszN M2XHR3NCVkeHUh?=
EW-24 MkHFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWrJR|UxRTBwNkK2PVMh|ryP M1eyRXNCVkeHUh?=
BV-173 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{X6[GlEPTB;MD62OVI1QSEQvF2= NXHNZ2NJW0GQR1XS
NCCIT NHLmdG1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH3lRWRKSzVyPUCuO|MzOThizszN M4nqbHNCVkeHUh?=
NCI-H1436 M1LmTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXTJR|UxRTBwN{mwOFkh|ryP M3vESnNCVkeHUh?=
BB30-HNC NFHZRmtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFzZRoJKSzVyPUCuPFYzODNizszN MVjTRW5ITVJ?
TE-8 MlS1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVTJR|UxRTBwOEeyO|Uh|ryP Ml7WV2FPT0WU
A704 NIPjVYhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGLUT2tKSzVyPUCuPFkzOSEQvF2= MkS0V2FPT0WU
TK10 MkWwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF;ofXRKSzVyPUCuPVA3PjlizszN NHK0NotUSU6JRWK=
KS-1 NXq0S5ROT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYXJR|UxRTFwMUm3O|kh|ryP NGLrXJpUSU6JRWK=
C2BBe1 NF7kb2hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXX3fGp4UUN3ME2xMlIxPTB5IN88US=> MmC4V2FPT0WU
RXF393 M1zheWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4e0NGlEPTB;MT6yOFM3KM7:TR?= MoDtV2FPT0WU
KGN MojBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGjkWnJKSzVyPUGuNlc3QDdizszN NUXOfZN4W0GQR1XS
NB69 NGK3bmtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWDJZoxJUUN3ME2xMlM4PDl5IN88US=> NUO2THp[W0GQR1XS
TE-11 NGfrc2RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3HhWGlEPTB;MT60N|QyQCEQvF2= MUPTRW5ITVJ?
TE-1 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHXodYJKSzVyPUGuOFQyODVizszN MnrsV2FPT0WU
ST486 NHHtZnhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYjLUFNqUUN3ME2xMlQ2QDV{IN88US=> M4\6NXNCVkeHUh?=
HOP-62 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkHGTWM2OD1zLkWwNlQ3KM7:TR?= MYTTRW5ITVJ?
EW-16 Mn;rS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlzjTWM2OD1zLkW1NFg{KM7:TR?= M{XUcHNCVkeHUh?=
LB1047-RCC NH:1SHVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlrPTWM2OD1zLkW1OFU{KM7:TR?= NGnYbYxUSU6JRWK=
TE-10 MmS0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXLXWmd[UUN3ME2xMlY3OjV{IN88US=> MojiV2FPT0WU
RL95-2 NWPicnI6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWnJR|UxRTFwNk[5NFIh|ryP M{e0UXNCVkeHUh?=
DOHH-2 NIfjWXhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVfJR|UxRTFwN{G3PFIh|ryP NWfMd3JnW0GQR1XS
MFH-ino MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1zXdWlEPTB;MT63O|g4KM7:TR?= NH\WSVBUSU6JRWK=
GB-1 MoHvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUf1XnNxUUN3ME2xMlc6QDN|IN88US=> NIPmZVZUSU6JRWK=
SK-N-DZ NF7DW3lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlHUTWM2OD1zLki0Olg5KM7:TR?= M4fGS3NCVkeHUh?=
OS-RC-2 M3zYUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlrSTWM2OD1zLki4OVc1KM7:TR?= MkjoV2FPT0WU
SW982 NE[1WGlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVi3b4FRUUN3ME2xMlkzODl|IN88US=> MXrTRW5ITVJ?
KALS-1 NF7TRXpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXzEdHhDUUN3ME2xMlk5PzJ{IN88US=> NUXMW4NJW0GQR1XS
TGBC24TKB MnT6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{TDTmlEPTB;Mj6wOVk2QCEQvF2= M4TzNHNCVkeHUh?=
GI-1 M4nTfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH[2T5BKSzVyPUKuNVYxQDRizszN NFjrR2xUSU6JRWK=
SW962 NVvjVXJQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXLJR|UxRTJwMUexO|gh|ryP NX[2NXFHW0GQR1XS
SW872 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml\yTWM2OD1{LkG4OVA4KM7:TR?= NG\wU2NUSU6JRWK=
NCI-H747 NXjReYtxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlH2TWM2OD1{LkK1O|E1KM7:TR?= MVXTRW5ITVJ?
MZ1-PC M17ye2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGLiNHVKSzVyPUKuNlk{PTZizszN MnfNV2FPT0WU
MSTO-211H MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUH5RoV[UUN3ME2yMlM2PzJ|IN88US=> NGjUdZpUSU6JRWK=
BL-70 MljoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFHXcmJKSzVyPUKuOFc1OjJizszN NV\iPYIxW0GQR1XS
SW954 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXrJR|UxRTJwNUe0NFgh|ryP M3:3NXNCVkeHUh?=
SNB75 NEfmN21Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4rUZWlEPTB;Mj62PFU6PCEQvF2= MXfTRW5ITVJ?
IST-SL2 NYrGTY9wT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIXqWIRKSzVyPUKuO|I{PzlizszN NHL2S3hUSU6JRWK=
GCIY MmrRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUDjdVlHUUN3ME2yMlg4ODB3IN88US=> MmnOV2FPT0WU
KU812 NYqzTnRRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2jIZmlEPTB;Mz6wOVI6QSEQvF2= NEC4VGtUSU6JRWK=
LXF-289 Mmq0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MY\JR|UxRTNwMUKxNFkh|ryP NVH0eIZIW0GQR1XS
ETK-1 M{SxV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX7JR|UxRTNwMkC3Olch|ryP MV3TRW5ITVJ?
SF126 NUf0[Yt[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF\reI5KSzVyPUOuN|EyPzRizszN M4S3b3NCVkeHUh?=
LC-2-ad NU\TR29mT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1e5TGlEPTB;Mz61OVch|ryP MlK3V2FPT0WU
KNS-42 NUHuWlRQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWDJR|UxRTNwNkWg{txO MXHTRW5ITVJ?
OVCAR-4 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn[xTWM2OD1|LkezOFM{KM7:TR?= MX3TRW5ITVJ?
PF-382 NXHuS5pZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWfJR|UxRTNwOEO2PVgh|ryP Mlr1V2FPT0WU
SH-4 NUXU[|R6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXXReoF2UUN3ME20MlI2OjV7IN88US=> NVnmV5dPW0GQR1XS
KM12 NHzxN5dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkjTTWM2OD12LkOyOFE3KM7:TR?= M2fPe3NCVkeHUh?=
NB5 NGPtXm5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH7jWGdKSzVyPUSuOFE5PjRizszN NF\FSGNUSU6JRWK=
KURAMOCHI NGC4VYNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUmySJNuUUN3ME20MlY2OjV4IN88US=> MXnTRW5ITVJ?
Becker M2naVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEPacWZKSzVyPUSuOlY1OTZizszN NYjNfJRoW0GQR1XS
MV-4-11 MmfoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH\qcZNKSzVyPUSuPFE{PDRizszN NHHJeolUSU6JRWK=
KINGS-1 NHzwR3hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2fYemlEPTB;ND64NlM4OyEQvF2= NHfiV4ZUSU6JRWK=
LS-123 NHXYZYlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{fVeWlEPTB;NT60PVY5PCEQvF2= NYHJOHJoW0GQR1XS
SF268 M3fabmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnLITWM2OD13Lk[xNlYzKM7:TR?= NIrzeFhUSU6JRWK=
A388 M3G5Wmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3;Hc2lEPTB;NT62N|Y3PyEQvF2= Ml3oV2FPT0WU
NMC-G1 M4e3R2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIf0fm5KSzVyPU[uNFE5OTFizszN MlfMV2FPT0WU
CGTH-W-1 MlLGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmPZTWM2OD14LkCyNFc2KM7:TR?= M3LvRXNCVkeHUh?=
ES4 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnH2TWM2OD14LkWzNFc1KM7:TR?= MWjTRW5ITVJ?
SR M1PDNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXvV[JltUUN3ME22MlU5QDB5IN88US=> NWLL[GU3W0GQR1XS
BB49-HNC NYj2bpg2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXrJR|UxRTZwN{OyNFYh|ryP Ml\BV2FPT0WU
KLE NWXjeJdKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4nMSmlEPTB;Nj63PFM4PyEQvF2= MVzTRW5ITVJ?
HUTU-80 MoTCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYfJR|UxRTZwOUi0OlYh|ryP MlnQV2FPT0WU
SNU-C2B M{jqfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWK5cnNWUUN3ME23MlgzPzN5IN88US=> NUjYRlRqW0GQR1XS
BB65-RCC M4fTSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkXxTWM2OD15Lkm0PVA1KM7:TR?= NID2bmhUSU6JRWK=
QIMR-WIL NW\MUGlJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGe3TohKSzVyPUiuOFI5ODhizszN NULlRnBNW0GQR1XS
GDM-1 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUDC[JhKUUN3ME24Mlk4Ojl{IN88US=> MVrTRW5ITVJ?
LC4-1 NEnEbW5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGniU3hKSzVyPUmuNFA6OTFizszN MmXHV2FPT0WU
MLMA NUHiPYp4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnPqTWM2OD17LkG1NFA3KM7:TR?= Mlr1V2FPT0WU
EoL-1-cell MoPUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUXJR|UxRTlwM{CxPVIh|ryP NV\tZ25jW0GQR1XS
BOKU NW[wU4I2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEnKTW9KSzVyPUmuPVY1PjZizszN NFvXdlRUSU6JRWK=
EVSA-T M2\wOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn3HTWM2OD1zMD62OVY5KM7:TR?= NV;mR3E5W0GQR1XS
D-283MED NXWyOFVnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEHMT|lKSzVyPUGwMlkyPzZizszN MUnTRW5ITVJ?
NB1 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGXVTVRKSzVyPUGxMlAzPDJizszN Mn;CV2FPT0WU
RPMI-8402 MlPxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX\RS4VOUUN3ME2xNU4yPzhizszN MoLEV2FPT0WU
NCI-H1355 MnvTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4e2e2lEPTB;MUGuNVgxPiEQvF2= NYnxcI1lW0GQR1XS
NB7 M2DQO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHTj[29KSzVyPUGxMlMzQTdizszN MkDwV2FPT0WU
RPMI-6666 NITNd2xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGDiRVVKSzVyPUGyMlk2PjdizszN MmHXV2FPT0WU
697 M3HwOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmPXTWM2OD1zMz6yO|AyKM7:TR?= MWnTRW5ITVJ?
CTB-1 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUOxfYV3UUN3ME2xN{42QTR6IN88US=> MYrTRW5ITVJ?
VA-ES-BJ MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUHJR|UxRTF|LkmyN|Qh|ryP MkO0V2FPT0WU
BE-13 MmTuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2TFeWlEPTB;MUSuN|kyPSEQvF2= M3vYd3NCVkeHUh?=
SKM-1 NWnFPWRiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MW\JR|UxRTF2LkS0PVkh|ryP M2fRdnNCVkeHUh?=
TE-6 Mm\BS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVrIPId7UUN3ME2xOE44PTlzIN88US=> MW\TRW5ITVJ?
LB771-HNC MlXOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV7Fe2hEUUN3ME2xOE44QDl6IN88US=> M2KxV3NCVkeHUh?=
ECC4 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{\keWlEPTB;MUeuNFI4PyEQvF2= MWXTRW5ITVJ?
ES3 M1;2Nmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnnaTWM2OD1zNz60OlU2KM7:TR?= NUmxSngzW0GQR1XS
LB647-SCLC NEToXWRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXXBToRMUUN3ME2xO{41QTR7IN88US=> MUHTRW5ITVJ?
NB10 M{fTZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX3JR|UxRTF6LkWyOVYh|ryP NFrPNnFUSU6JRWK=
L-540 M3Txd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3TXSWlEPTB;MUiuPFExQSEQvF2= NYj5T2d[W0GQR1XS
NCI-H2126 M{DQR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWrJR|UxRTF7LkWxJO69VQ>? MYTTRW5ITVJ?
HH MoDKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWnJR|UxRTJyLkCwPVkh|ryP NGO3ZolUSU6JRWK=
MPP-89 NUjZU3F4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF;GSpFKSzVyPUKzMlIzQDlizszN M3rMfHNCVkeHUh?=
IST-MEL1 Mm\2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkXZTWM2OD1{Mz64OlU5KM7:TR?= MWHTRW5ITVJ?
KP-N-YS MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX7JR|UxRTJ|LkmyOVUh|ryP M4XLZ3NCVkeHUh?=
EC-GI-10 M{DXdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVPJR|UxRTJ2LkW5PFkh|ryP M4DG[HNCVkeHUh?=
EKVX MmTLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEnYR2VKSzVyPUK2MlAzODNizszN M4G5fHNCVkeHUh?=
TGBC1TKB NFjie3pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MU\JR|UxRTJ4LkSzOEDPxE1? NXW0Z2V{W0GQR1XS
Daudi NWXqXHZ6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHywSmhKSzVyPUK3MlA4PzNizszN MVvTRW5ITVJ?
ALL-PO MluwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUXJR|UxRTJ5LkC4NUDPxE1? M2TZb3NCVkeHUh?=
NB6 NV7lT2J4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYDJR|UxRTJ5LkS4PEDPxE1? MWPTRW5ITVJ?
ES6 NXXoWG1sT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIDpdGVKSzVyPUK3MlkyOjNizszN M{XTbHNCVkeHUh?=
COLO-320-HSR NWS2SlFET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHvZcoVKSzVyPUK4MlA{PzNizszN MmLkV2FPT0WU
K5 NHG4V4NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGW1SJJKSzVyPUK4MlEzQDdizszN NHLO[41USU6JRWK=
ES1 NUDtV5pwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFjiOpFKSzVyPUK4Mlc4PzNizszN M2DmSHNCVkeHUh?=
LC-1F NGTBfVdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYPJR|UxRTJ7LkezOFYh|ryP NGDXOohUSU6JRWK=
SCLC-21H NUC1OJlmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUH3N3piUUN3ME2zNE44OzF5IN88US=> M3;oN3NCVkeHUh?=
SK-PN-DW MnuwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVXJR|UxRTN{LkW1PVgh|ryP MWTTRW5ITVJ?
D-247MG NVPmcGxiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXnJR|UxRTN{Lkm3O|Mh|ryP MUHTRW5ITVJ?
TE-5 NVzYNmtZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoTtTWM2OD1|Mz6wN|YzKM7:TR?= NEHPdmpUSU6JRWK=
MONO-MAC-6 MnexS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{jhfmlEPTB;M{OuOVA1QCEQvF2= MmmxV2FPT0WU
LB2518-MEL NGHaUHBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVfJR|UxRTN|Lke2OlYh|ryP M1PFUHNCVkeHUh?=
LOXIMVI MmrvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWDJR|UxRTN|Lke5Nlgh|ryP MUfTRW5ITVJ?
NCI-H209 NEjPSVFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1\tSWlEPTB;M{WuNVQ1KM7:TR?= NVzXV3ZEW0GQR1XS
A253 M{\vT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2XDfmlEPTB;M{WuO|QzQSEQvF2= M4q4SHNCVkeHUh?=
HCC1599 M3\YO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYnJR|UxRTN4LkewOVMh|ryP M1vtSXNCVkeHUh?=
EB-3 NXO3OFQ4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVjJR|UxRTN4Lkm1NVgh|ryP M4TQOXNCVkeHUh?=
GOTO MlTqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NI\4VlVKSzVyPUO3MlMzOjRizszN NXH1T44yW0GQR1XS
SW684 NFzkbHhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVLJR|UxRTRzLki0PVUh|ryP MXnTRW5ITVJ?
DEL MlXIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVzJR|UxRTR{LkC1NlIh|ryP MojZV2FPT0WU
HT-144 M1yyU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVzJR|UxRTR{LkG2O|Yh|ryP MXnTRW5ITVJ?
TE-9 NH7GdXhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3;acmlEPTB;NEOuOFU6PiEQvF2= NH\xUXdUSU6JRWK=
KARPAS-45 MmTNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWDJR|UxRTR2LkO5NlUh|ryP NVjlPIk6W0GQR1XS
HAL-01 NYniepdIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlnuTWM2OD12ND61NFM1KM7:TR?= MnHOV2FPT0WU
RCC10RGB NX\kdlRxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHLoVnNKSzVyPUS0Mlc{QTJizszN NH7DRWdUSU6JRWK=
CP67-MEL NHTzV3NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX7Wd4pvUUN3ME20OU43OjRzIN88US=> M{XRfXNCVkeHUh?=
NB17 M4LmfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEnXN2JKSzVyPUS1MlY3PDNizszN NWLmfoxoW0GQR1XS
SK-UT-1 NUXzd2FDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWfEeGRXUUN3ME20OU46PDZ2IN88US=> MlznV2FPT0WU
JiyoyeP-2003 NWTHfFdJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NETpcG5KSzVyPUS2MlAyOTlizszN MkDBV2FPT0WU
HCE-4 MlnFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1L6N2lEPTB;NE[uOVk3QCEQvF2= NHf1WYJUSU6JRWK=
NCI-H720 MlzGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXnyd4h4UUN3ME20Ok44Pjh{IN88US=> MXfTRW5ITVJ?
KARPAS-422 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYWzOYdXUUN3ME20O{4xQDl3IN88US=> MoCxV2FPT0WU
Ramos-2G6-4C10 NX7JOVZmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2HybWlEPTB;NEeuNVYzOiEQvF2= M4P2TnNCVkeHUh?=
HCE-T MnuwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF\pdW1KSzVyPUS3MlY5OjhizszN M4TpTnNCVkeHUh?=
PSN1 MnvwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn36TWM2OD12Nz63PFE{KM7:TR?= NWXUeGZVW0GQR1XS

... 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]

- Collapse

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]

- Collapse
  • 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]

- Collapse
  • 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 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
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|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

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

Src Signaling Pathway Map

Src Inhibitors with Unique Features

Related Src Products

Tags: buy Saracatinib (AZD0530) | Saracatinib (AZD0530) supplier | purchase Saracatinib (AZD0530) | Saracatinib (AZD0530) cost | Saracatinib (AZD0530) manufacturer | order Saracatinib (AZD0530) | Saracatinib (AZD0530) distributor
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID