Saracatinib (AZD0530)

For research use only.

Catalog No.S1006

189 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). Saracatinib induces autophagy. Phase 2/3.

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Selleck's Saracatinib (AZD0530) has been cited by 189 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 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlS4TWM2OD1yLkC2NVQ{KM7:TR?= NFf2cINUSU6JRWK=
LAMA-84 M1n4Tmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1;nU2lEPTB;MD6xOVk6KM7:TR?= MV7TRW5ITVJ?
MEG-01 M{TKWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{f3T2lEPTB;MD6yN|Y5QCEQvF2= M1PMV3NCVkeHUh?=
EM-2 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV7TTHFiUUN3ME2wMlI3PSEQvF2= MkP3V2FPT0WU
TE-15 NWLWO5NuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnnhTWM2OD1yLkK3OFEzKM7:TR?= NV\EcWpQW0GQR1XS
NCI-H1648 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1va[GlEPTB;MD6yPFEyPiEQvF2= NXjXe29WW0GQR1XS
TE-12 NUO3Z4pnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEXM[I5KSzVyPUCuN|I3QCEQvF2= MXXTRW5ITVJ?
LB996-RCC MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3zUVWlEPTB;MD60OFE6PiEQvF2= MVzTRW5ITVJ?
K-562 NE\NXnBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn60TWM2OD1yLkS0PVY4KM7:TR?= NFzr[|ZUSU6JRWK=
D-336MG MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlruTWM2OD1yLkWwN|A1KM7:TR?= MVnTRW5ITVJ?
NOS-1 NGP4doRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH\wS5BKSzVyPUCuOlA2OjlizszN M2ruNXNCVkeHUh?=
EW-24 NILsfYNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlznTWM2OD1yLk[yOlk{KM7:TR?= M4ntSHNCVkeHUh?=
BV-173 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnH5TWM2OD1yLk[1NlQ6KM7:TR?= MUDTRW5ITVJ?
NCCIT M{LoZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUHJR|UxRTBwN{OyNVgh|ryP M1n4W3NCVkeHUh?=
NCI-H1436 NV3xR4pDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWDJR|UxRTBwN{mwOFkh|ryP NFzZbWVUSU6JRWK=
BB30-HNC M1PlVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnjkTWM2OD1yLki2NlA{KM7:TR?= NUP1PIM1W0GQR1XS
TE-8 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV73VG9JUUN3ME2wMlg4Ojd3IN88US=> MYnTRW5ITVJ?
A704 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2fzXWlEPTB;MD64PVIyKM7:TR?= MYPTRW5ITVJ?
TK10 MnjhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXT6XIZUUUN3ME2wMlkxPjZ7IN88US=> MkK1V2FPT0WU
KS-1 NVS4ZoJvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYPJR|UxRTFwMUm3O|kh|ryP NXjrOmxXW0GQR1XS
C2BBe1 NV7LW3I{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWHJR|UxRTFwMkC1NFch|ryP NUDLbYlvW0GQR1XS
RXF393 M1zvXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFrRe5JKSzVyPUGuNlQ{PiEQvF2= NFjlXlJUSU6JRWK=
KGN MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVr3cmlTUUN3ME2xMlI4Pjh5IN88US=> M4nrcnNCVkeHUh?=
NB69 NI[xTpBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIm2cZBKSzVyPUGuN|c1QTdizszN MVHTRW5ITVJ?
TE-11 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUDJR|UxRTFwNEO0NVgh|ryP NEnaUJZUSU6JRWK=
TE-1 NXPNSGQ3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4K4eGlEPTB;MT60OFExPSEQvF2= NU\WfIFFW0GQR1XS
ST486 Mn7zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIKxVpdKSzVyPUGuOFU5PTJizszN M4HIdHNCVkeHUh?=
HOP-62 NIHib3FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml:5TWM2OD1zLkWwNlQ3KM7:TR?= MnLIV2FPT0WU
EW-16 M37mZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4HHe2lEPTB;MT61OVA5OyEQvF2= MlLSV2FPT0WU
LB1047-RCC MlLKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{SwW2lEPTB;MT61OVQ2OyEQvF2= M2LWc3NCVkeHUh?=
TE-10 MnLtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NULpdWhFUUN3ME2xMlY3OjV{IN88US=> M1P4VnNCVkeHUh?=
RL95-2 M3;GT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHvvT41KSzVyPUGuOlY6ODJizszN MX;TRW5ITVJ?
DOHH-2 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVzJR|UxRTFwN{G3PFIh|ryP NFXn[WJUSU6JRWK=
MFH-ino M3;3bGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWfCcZFlUUN3ME2xMlc4QDdizszN NIixV3RUSU6JRWK=
GB-1 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVztW4htUUN3ME2xMlc6QDN|IN88US=> NXnjNpVMW0GQR1XS
SK-N-DZ MoPiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkHVTWM2OD1zLki0Olg5KM7:TR?= M4S2Z3NCVkeHUh?=
OS-RC-2 NYGwfpI3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXPJR|UxRTFwOEi1O|Qh|ryP NF73SWpUSU6JRWK=
SW982 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn;ITWM2OD1zLkmyNFk{KM7:TR?= NFyybm9USU6JRWK=
KALS-1 NXjvbGp1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYnJR|UxRTFwOUi3NlIh|ryP NUHKcYZMW0GQR1XS
TGBC24TKB MkjsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXPJR|UxRTJwMEW5OVgh|ryP NIe1VlBUSU6JRWK=
GI-1 NVT0NmFWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUfJR|UxRTJwMU[wPFQh|ryP MmXCV2FPT0WU
SW962 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1LGNWlEPTB;Mj6xO|E4QCEQvF2= M{Lie3NCVkeHUh?=
SW872 NGXHNYtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3fvRmlEPTB;Mj6xPFUxPyEQvF2= Mn3pV2FPT0WU
NCI-H747 MkftS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWjPTJJYUUN3ME2yMlI2PzF2IN88US=> M4HRbHNCVkeHUh?=
MZ1-PC MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFn6U3hKSzVyPUKuNlk{PTZizszN NICyUoRUSU6JRWK=
MSTO-211H M2nJZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGLl[ZlKSzVyPUKuN|U4OjNizszN M2fuSXNCVkeHUh?=
BL-70 M1vaS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX3JR|UxRTJwNEe0NlIh|ryP MmHaV2FPT0WU
SW954 NFTK[2JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2G2emlEPTB;Mj61O|QxQCEQvF2= NFjpTZJUSU6JRWK=
SNB75 MoDTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{n5VWlEPTB;Mj62PFU6PCEQvF2= Mo\5V2FPT0WU
IST-SL2 MlXKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHjBR|BKSzVyPUKuO|I{PzlizszN MlKzV2FPT0WU
GCIY M{XtSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUfJR|UxRTJwOEewNFUh|ryP MlnWV2FPT0WU
KU812 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M37wemlEPTB;Mz6wOVI6QSEQvF2= NYTheJlbW0GQR1XS
LXF-289 M3nNOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXrJR|UxRTNwMUKxNFkh|ryP MV7TRW5ITVJ?
ETK-1 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3jXVWlEPTB;Mz6yNFc3PyEQvF2= Mo\KV2FPT0WU
SF126 MnXzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{GwOGlEPTB;Mz6zNVE4PCEQvF2= NUnvRoZzW0GQR1XS
LC-2-ad MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYq2T3c5UUN3ME2zMlU2PyEQvF2= NWDYc5dqW0GQR1XS
KNS-42 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXvpNGJVUUN3ME2zMlY2KM7:TR?= M1jYVXNCVkeHUh?=
OVCAR-4 NWLNUJpmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnnFTWM2OD1|LkezOFM{KM7:TR?= NXXuR4loW0GQR1XS
PF-382 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVLUSHl[UUN3ME2zMlg{Pjl6IN88US=> MXfTRW5ITVJ?
SH-4 M2XrfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYPJR|UxRTRwMkWyOVkh|ryP MnXpV2FPT0WU
KM12 MoixS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkPNTWM2OD12LkOyOFE3KM7:TR?= MnHCV2FPT0WU
NB5 NGTxS2hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXzJR|UxRTRwNEG4OlQh|ryP NWf6W4hoW0GQR1XS
KURAMOCHI M3TlTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEDvVIVKSzVyPUSuOlUzPTZizszN MmTVV2FPT0WU
Becker M4rCcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3vTc2lEPTB;ND62OlQyPiEQvF2= NWfabW1rW0GQR1XS
MV-4-11 NWPq[mR5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmDDTWM2OD12LkixN|Q1KM7:TR?= M4fjRnNCVkeHUh?=
KINGS-1 NYHy[o5RT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mk\6TWM2OD12LkiyN|c{KM7:TR?= MlfRV2FPT0WU
LS-123 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NImx[WNKSzVyPUWuOFk3QDRizszN NU\DfIUzW0GQR1XS
SF268 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlLYTWM2OD13Lk[xNlYzKM7:TR?= NH3IdZJUSU6JRWK=
A388 NY\sbIl6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYjJR|UxRTVwNkO2Olch|ryP MWXTRW5ITVJ?
NMC-G1 NUfabHlYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3HZSmlEPTB;Nj6wNVgyOSEQvF2= M1TBN3NCVkeHUh?=
CGTH-W-1 M3TEWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYTJR|UxRTZwMEKwO|Uh|ryP NV3yWId6W0GQR1XS
ES4 MoDES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoLoTWM2OD14LkWzNFc1KM7:TR?= M2K1VHNCVkeHUh?=
SR NWnBPJFET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml\qTWM2OD14LkW4PFA4KM7:TR?= MoXHV2FPT0WU
BB49-HNC NIDXOmNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIe5XpRKSzVyPU[uO|MzODZizszN M1nxenNCVkeHUh?=
KLE NGfiWnVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUnqcpUxUUN3ME22Mlc5Ozd5IN88US=> M3XRe3NCVkeHUh?=
HUTU-80 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2K3ZWlEPTB;Nj65PFQ3PiEQvF2= NYjlRnl6W0GQR1XS
SNU-C2B NG[wS2lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NILTTmpKSzVyPUeuPFI4OzdizszN MlvKV2FPT0WU
BB65-RCC M1HzfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkS1TWM2OD15Lkm0PVA1KM7:TR?= MWPTRW5ITVJ?
QIMR-WIL NFrY[phIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIHURoxKSzVyPUiuOFI5ODhizszN NFz0W2pUSU6JRWK=
GDM-1 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGnVRWpKSzVyPUiuPVczQTJizszN MWfTRW5ITVJ?
LC4-1 NUKydpQ{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGHzfYRKSzVyPUmuNFA6OTFizszN MoHzV2FPT0WU
MLMA NVrL[HdvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWPJR|UxRTlwMUWwNFYh|ryP MWfTRW5ITVJ?
EoL-1-cell MlPHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH\CSppKSzVyPUmuN|AyQTJizszN MXfTRW5ITVJ?
BOKU MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVy3e|RmUUN3ME25Mlk3PDZ4IN88US=> NVfZV41iW0GQR1XS
EVSA-T Moi4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4ra[mlEPTB;MUCuOlU3QCEQvF2= MmjGV2FPT0WU
D-283MED MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYDJR|UxRTFyLkmxO|Yh|ryP NYHkW5l1W0GQR1XS
NB1 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWHZXnNCUUN3ME2xNU4xOjR{IN88US=> NXW2ZpEyW0GQR1XS
RPMI-8402 M13PbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVXadYpLUUN3ME2xNU4yPzhizszN MYDTRW5ITVJ?
NCI-H1355 NGHabmJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUfJR|UxRTFzLkG4NFYh|ryP M3S4eHNCVkeHUh?=
NB7 NFTQNZFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M13EUWlEPTB;MUGuN|I6PyEQvF2= NX;Je|ZtW0GQR1XS
RPMI-6666 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4XLe2lEPTB;MUKuPVU3PyEQvF2= MVfTRW5ITVJ?
697 MmjUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnruTWM2OD1zMz6yO|AyKM7:TR?= NULQfIVIW0GQR1XS
CTB-1 M2TNRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVzGXHN1UUN3ME2xN{42QTR6IN88US=> MWXTRW5ITVJ?
VA-ES-BJ MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmH1TWM2OD1zMz65NlM1KM7:TR?= MmTQV2FPT0WU
BE-13 M3mye2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHG0UJJKSzVyPUG0MlM6OTVizszN MnTVV2FPT0WU
SKM-1 M2\ueGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUjJR|UxRTF2LkS0PVkh|ryP NIOyT2NUSU6JRWK=
TE-6 NWjDWJQyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{PDeWlEPTB;MUSuO|U6OSEQvF2= M{f5U3NCVkeHUh?=
LB771-HNC Mlr1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIjWXWtKSzVyPUG0Mlc5QThizszN M33Pd3NCVkeHUh?=
ECC4 NHvGd4lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoLWTWM2OD1zNz6wNlc4KM7:TR?= MVLTRW5ITVJ?
ES3 NHnIZmpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmPiTWM2OD1zNz60OlU2KM7:TR?= M{nwWXNCVkeHUh?=
LB647-SCLC MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXLJR|UxRTF5LkS5OFkh|ryP NYjRfIdKW0GQR1XS
NB10 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXrJR|UxRTF6LkWyOVYh|ryP MUXTRW5ITVJ?
L-540 MmnnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHXmOnNKSzVyPUG4MlgyODlizszN MlHGV2FPT0WU
NCI-H2126 MlS5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4PueGlEPTB;MUmuOVEh|ryP NFXwdGJUSU6JRWK=
HH NIL3RlFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVK1Tm55UUN3ME2yNE4xODl7IN88US=> NILqXlNUSU6JRWK=
MPP-89 NFLxbZBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4fRUWlEPTB;MkOuNlI5QSEQvF2= NUW2W|VTW0GQR1XS
IST-MEL1 NWjMTnVkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYrJR|UxRTJ|Lki2OVgh|ryP NVfLfGx3W0GQR1XS
KP-N-YS NULaWYlnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlWyTWM2OD1{Mz65NlU2KM7:TR?= MXPTRW5ITVJ?
EC-GI-10 NHXydYVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmnTTWM2OD1{ND61PVg6KM7:TR?= NHrFcnhUSU6JRWK=
EKVX MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEL4dFhKSzVyPUK2MlAzODNizszN NVvm[I5oW0GQR1XS
TGBC1TKB MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYXodJVOUUN3ME2yOk41OzRizszN MUHTRW5ITVJ?
Daudi Ml61S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnjyTWM2OD1{Nz6wO|c{KM7:TR?= NIPmXZNUSU6JRWK=
ALL-PO MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NI[0dXBKSzVyPUK3MlA5OSEQvF2= MonuV2FPT0WU
NB6 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHWzeW5KSzVyPUK3MlQ5QCEQvF2= MoXuV2FPT0WU
ES6 NEL3XVZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1W5TmlEPTB;MkeuPVEzOyEQvF2= MYLTRW5ITVJ?
COLO-320-HSR NYDmVo5iT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnrrTWM2OD1{OD6wN|c{KM7:TR?= MnH3V2FPT0WU
K5 M1;Lemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmrsTWM2OD1{OD6xNlg4KM7:TR?= MVjTRW5ITVJ?
ES1 M3XrW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWfJR|UxRTJ6Lke3O|Mh|ryP M4PlTHNCVkeHUh?=
LC-1F NHGzZ3NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWK0[pY5UUN3ME2yPU44OzR4IN88US=> MXTTRW5ITVJ?
SCLC-21H NXfNZmJFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3\xV2lEPTB;M{CuO|MyPyEQvF2= MV3TRW5ITVJ?
SK-PN-DW MkTGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHHnSo1KSzVyPUOyMlU2QThizszN NIDQSVhUSU6JRWK=
D-247MG MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYfJR|UxRTN{Lkm3O|Mh|ryP M1rxOnNCVkeHUh?=
TE-5 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnPmTWM2OD1|Mz6wN|YzKM7:TR?= MVzTRW5ITVJ?
MONO-MAC-6 MlHRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXPJR|UxRTN|LkWwOFgh|ryP NHXsd49USU6JRWK=
LB2518-MEL NUjEZ4VqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVnJR|UxRTN|Lke2OlYh|ryP MWTTRW5ITVJ?
LOXIMVI MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoTGTWM2OD1|Mz63PVI5KM7:TR?= M3Wy[HNCVkeHUh?=
NCI-H209 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX;JR|UxRTN3LkG0OEDPxE1? NFPVSGFUSU6JRWK=
A253 M132WGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2\Rc2lEPTB;M{WuO|QzQSEQvF2= MXfTRW5ITVJ?
HCC1599 NGTQSlRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXrJR|UxRTN4LkewOVMh|ryP MmiwV2FPT0WU
EB-3 NH2xXJZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHfDfJhKSzVyPUO2Mlk2OThizszN M{nWWXNCVkeHUh?=
GOTO NX7hTFZPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUjJR|UxRTN5LkOyNlQh|ryP MknFV2FPT0WU
SW684 NY[wSXplT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYTCNZlkUUN3ME20NU45PDl3IN88US=> MlvVV2FPT0WU
DEL M3LiZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVjJR|UxRTR{LkC1NlIh|ryP NGTP[4tUSU6JRWK=
HT-144 NEToPFFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYfJR|UxRTR{LkG2O|Yh|ryP MoHJV2FPT0WU
TE-9 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlPITWM2OD12Mz60OVk3KM7:TR?= MnLaV2FPT0WU
KARPAS-45 Mn3kS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUHtcHRzUUN3ME20OE4{QTJ3IN88US=> MnnJV2FPT0WU
HAL-01 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1zubGlEPTB;NESuOVA{PCEQvF2= MnjSV2FPT0WU
RCC10RGB NXi5enRWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGC4botKSzVyPUS0Mlc{QTJizszN NWXzNGhQW0GQR1XS
CP67-MEL MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUfJWZpTUUN3ME20OU43OjRzIN88US=> MmKyV2FPT0WU
NB17 NXLDbmJ2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkHNTWM2OD12NT62OlQ{KM7:TR?= MmmyV2FPT0WU
SK-UT-1 MoHaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVG4cpFQUUN3ME20OU46PDZ2IN88US=> NVHTdJRZW0GQR1XS
JiyoyeP-2003 Mn65S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXjJR|UxRTR4LkCxNVkh|ryP Mk\4V2FPT0WU
HCE-4 NHz5U2RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NG\pXmlKSzVyPUS2MlU6PjhizszN NInl[41USU6JRWK=
NCI-H720 MlPIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2PI[GlEPTB;NE[uO|Y5OiEQvF2= MUnTRW5ITVJ?
KARPAS-422 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVnJR|UxRTR5LkC4PVUh|ryP MULTRW5ITVJ?
Ramos-2G6-4C10 Moj5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYW1W5F3UUN3ME20O{4yPjJ{IN88US=> NVr0bVNTW0GQR1XS
HCE-T MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkXaTWM2OD12Nz62PFI5KM7:TR?= MWnTRW5ITVJ?
PSN1 MmToS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEXxbWpKSzVyPUS3Mlc5OTNizszN Ml3DV2FPT0WU

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

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
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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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*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 March 13 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