Saracatinib (AZD0530)

For research use only.

Catalog No.S1006

200 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 200 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 NYTqVWtGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXPJR|UxRTBwME[xOFMh|ryP MVrTRW5ITVJ?
LAMA-84 MoX0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVe5UVdVUUN3ME2wMlE2QTlizszN M2TRZ3NCVkeHUh?=
MEG-01 MknxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV\6OW8zUUN3ME2wMlI{Pjh6IN88US=> NEnRUFBUSU6JRWK=
EM-2 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3O0VWlEPTB;MD6yOlUh|ryP NFf1c49USU6JRWK=
TE-15 Ml\6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1zOcmlEPTB;MD6yO|QyOiEQvF2= NYXo[phNW0GQR1XS
NCI-H1648 NXnPUnlHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2HmXmlEPTB;MD6yPFEyPiEQvF2= MYPTRW5ITVJ?
TE-12 NXrp[XBFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYLJR|UxRTBwM{K2PEDPxE1? NYLL[ppQW0GQR1XS
LB996-RCC MkPoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVjJR|UxRTBwNESxPVYh|ryP Mne4V2FPT0WU
K-562 M3\6Rmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYTJR|UxRTBwNES5Olch|ryP M3TVWXNCVkeHUh?=
D-336MG M{DGPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{L5dWlEPTB;MD61NFMxPCEQvF2= NUHndoZwW0GQR1XS
NOS-1 NFLQPHBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWPyNFJmUUN3ME2wMlYxPTJ7IN88US=> MYnTRW5ITVJ?
EW-24 NXXUdIJtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NITwemtKSzVyPUCuOlI3QTNizszN Moi3V2FPT0WU
BV-173 MnPkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NE\lWINKSzVyPUCuOlUzPDlizszN MV3TRW5ITVJ?
NCCIT NXezVGM4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NE[yXopKSzVyPUCuO|MzOThizszN MlfVV2FPT0WU
NCI-H1436 NUH6fW1YT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3\XRmlEPTB;MD63PVA1QSEQvF2= M2DwSHNCVkeHUh?=
BB30-HNC Mn3pS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1nwdWlEPTB;MD64OlIxOyEQvF2= M2Tod3NCVkeHUh?=
TE-8 NIXs[pBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXLJR|UxRTBwOEeyO|Uh|ryP M{fUV3NCVkeHUh?=
A704 M3LxT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkHxTWM2OD1yLki5NlEh|ryP MkTZV2FPT0WU
TK10 NHT4ZXZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml;sTWM2OD1yLkmwOlY6KM7:TR?= MYfTRW5ITVJ?
KS-1 MmjmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVXJR|UxRTFwMUm3O|kh|ryP M{e1Z3NCVkeHUh?=
C2BBe1 Ml;rS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXzJR|UxRTFwMkC1NFch|ryP MXTTRW5ITVJ?
RXF393 NGXuXVBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHG4TIZKSzVyPUGuNlQ{PiEQvF2= MWXTRW5ITVJ?
KGN MoLNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2roXmlEPTB;MT6yO|Y5PyEQvF2= MW\TRW5ITVJ?
NB69 NGThe|FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUXMfIw3UUN3ME2xMlM4PDl5IN88US=> MmfzV2FPT0WU
TE-11 NH;XWohIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVPLTm4yUUN3ME2xMlQ{PDF6IN88US=> Moi0V2FPT0WU
TE-1 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2j0ZWlEPTB;MT60OFExPSEQvF2= MoniV2FPT0WU
ST486 M4jjVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVjJR|UxRTFwNEW4OVIh|ryP M33wenNCVkeHUh?=
HOP-62 M2n3Wmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF[xWXVKSzVyPUGuOVAzPDZizszN MYXTRW5ITVJ?
EW-16 NF;UeJBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXT0O49lUUN3ME2xMlU2ODh|IN88US=> MVHTRW5ITVJ?
LB1047-RCC Mk\6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NG\yOZhKSzVyPUGuOVU1PTNizszN MWLTRW5ITVJ?
TE-10 M2G2dGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYDJR|UxRTFwNk[yOVIh|ryP M1zNS3NCVkeHUh?=
RL95-2 NYLmcIJjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXrJR|UxRTFwNk[5NFIh|ryP MYTTRW5ITVJ?
DOHH-2 NF3WfmhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVy3VWRvUUN3ME2xMlcyPzh{IN88US=> NV7DU|VOW0GQR1XS
MFH-ino NFXKc2xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVnJR|UxRTFwN{e4O{DPxE1? M{jDSXNCVkeHUh?=
GB-1 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHfteXhKSzVyPUGuO|k5OzNizszN NHTiSpdUSU6JRWK=
SK-N-DZ M2PJWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3HafGlEPTB;MT64OFY5QCEQvF2= MV\TRW5ITVJ?
OS-RC-2 NFLlNopIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFnTco1KSzVyPUGuPFg2PzRizszN MYXTRW5ITVJ?
SW982 NWDuTpBrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVr4[lNZUUN3ME2xMlkzODl|IN88US=> MWHTRW5ITVJ?
KALS-1 MnfES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHPT[oZKSzVyPUGuPVg4OjJizszN NEHITpJUSU6JRWK=
TGBC24TKB Mn35S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYq4N5RHUUN3ME2yMlA2QTV6IN88US=> Ml\YV2FPT0WU
GI-1 NFTucWxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGnsT5hKSzVyPUKuNVYxQDRizszN NYfyV5d5W0GQR1XS
SW962 M2L0OWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXviOYRjUUN3ME2yMlE4OTd6IN88US=> NWLydIk1W0GQR1XS
SW872 MmjtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXLJR|UxRTJwMUi1NFch|ryP NGqxbmVUSU6JRWK=
NCI-H747 MnjJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXPFSGFQUUN3ME2yMlI2PzF2IN88US=> NV;5OWJrW0GQR1XS
MZ1-PC M1Sy[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHm0WGVKSzVyPUKuNlk{PTZizszN MYTTRW5ITVJ?
MSTO-211H NHLOVmFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn;QTWM2OD1{LkO1O|I{KM7:TR?= MXjTRW5ITVJ?
BL-70 NF\LfJNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV3vSFJjUUN3ME2yMlQ4PDJ{IN88US=> NHvTRXhUSU6JRWK=
SW954 NH64W4NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVLNcod2UUN3ME2yMlU4PDB6IN88US=> M1u3NHNCVkeHUh?=
SNB75 M3\jS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVXJR|UxRTJwNki1PVQh|ryP NG\tPXJUSU6JRWK=
IST-SL2 M4DIUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX7JR|UxRTJwN{KzO|kh|ryP MkSxV2FPT0WU
GCIY NIfxTYhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEPsc4dKSzVyPUKuPFcxODVizszN NUHVVZZTW0GQR1XS
KU812 NFjKcmJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVm1VHZYUUN3ME2zMlA2Ojl7IN88US=> NVfiXYlVW0GQR1XS
LXF-289 MlvHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3Htd2lEPTB;Mz6xNlExQSEQvF2= Mm\ZV2FPT0WU
ETK-1 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MW\JR|UxRTNwMkC3Olch|ryP MXHTRW5ITVJ?
SF126 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnXETWM2OD1|LkOxNVc1KM7:TR?= MlPwV2FPT0WU
LC-2-ad M{LtNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXPKRYc4UUN3ME2zMlU2PyEQvF2= MoPTV2FPT0WU
KNS-42 MoG2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX3JR|UxRTNwNkWg{txO MmDnV2FPT0WU
OVCAR-4 NHH3N4tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NI\zOWZKSzVyPUOuO|M1OzNizszN M17aOXNCVkeHUh?=
PF-382 NX\NV2szT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mkf0TWM2OD1|LkizOlk5KM7:TR?= NWe2N4ZIW0GQR1XS
SH-4 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M17hVWlEPTB;ND6yOVI2QSEQvF2= NV;u[ZFpW0GQR1XS
KM12 M{XIZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFTvb2hKSzVyPUSuN|I1OTZizszN M{TlbXNCVkeHUh?=
NB5 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3jtcmlEPTB;ND60NVg3PCEQvF2= Mm\1V2FPT0WU
KURAMOCHI NEG5TFlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXrJR|UxRTRwNkWyOVYh|ryP MW\TRW5ITVJ?
Becker M{j1N2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVTJR|UxRTRwNk[0NVYh|ryP NVTHcW9bW0GQR1XS
MV-4-11 MnjOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUDHNldqUUN3ME20MlgyOzR2IN88US=> Ml\CV2FPT0WU
KINGS-1 NFHOWW9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEnNRXZKSzVyPUSuPFI{PzNizszN NV\JWo5EW0GQR1XS
LS-123 NVvYbnUyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1fDVGlEPTB;NT60PVY5PCEQvF2= NWHWV3hzW0GQR1XS
SF268 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3TsU2lEPTB;NT62NVI3OiEQvF2= NXHxbW5wW0GQR1XS
A388 Mof3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2PKcGlEPTB;NT62N|Y3PyEQvF2= M{PTeXNCVkeHUh?=
NMC-G1 M1TodWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUfJR|UxRTZwMEG4NVEh|ryP NEfHXWdUSU6JRWK=
CGTH-W-1 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnTzTWM2OD14LkCyNFc2KM7:TR?= MYTTRW5ITVJ?
ES4 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX\oN4JlUUN3ME22MlU{ODd2IN88US=> NGDwW4RUSU6JRWK=
SR NW\5OIZET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MU\JR|UxRTZwNUi4NFch|ryP NFG3XndUSU6JRWK=
BB49-HNC NWP5WW9IT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGjYeldKSzVyPU[uO|MzODZizszN MnnnV2FPT0WU
KLE MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIjBXZlKSzVyPU[uO|g{PzdizszN M4W3[3NCVkeHUh?=
HUTU-80 NXzMTpdDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmnhTWM2OD14Lkm4OFY3KM7:TR?= M{\zSHNCVkeHUh?=
SNU-C2B MlHES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXrTZ45kUUN3ME23MlgzPzN5IN88US=> Ml\2V2FPT0WU
BB65-RCC NITXb21Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXzJR|UxRTdwOUS5NFQh|ryP NEjBNVRUSU6JRWK=
QIMR-WIL MkDWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1O1b2lEPTB;OD60NlgxQCEQvF2= MnnRV2FPT0WU
GDM-1 NFTa[ZJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NELkOW9KSzVyPUiuPVczQTJizszN NYjidYJpW0GQR1XS
LC4-1 M4XCWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXrJR|UxRTlwMEC5NVEh|ryP MmfWV2FPT0WU
MLMA NWLGbm9wT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF3YUo1KSzVyPUmuNVUxODZizszN NVS3W5BKW0GQR1XS
EoL-1-cell NFLjcW9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX\EU3NsUUN3ME25MlMxOTl{IN88US=> MkXqV2FPT0WU
BOKU NVjFbnlIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2nvSmlEPTB;OT65OlQ3PiEQvF2= MWTTRW5ITVJ?
EVSA-T MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoW3TWM2OD1zMD62OVY5KM7:TR?= M4DyWXNCVkeHUh?=
D-283MED NFPqNGNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXnJR|UxRTFyLkmxO|Yh|ryP NXXZbGdsW0GQR1XS
NB1 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3zX[mlEPTB;MUGuNFI1OiEQvF2= NWrvSGdPW0GQR1XS
RPMI-8402 MnHES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{DWTmlEPTB;MUGuNVc5KM7:TR?= MWLTRW5ITVJ?
NCI-H1355 NI[3WXBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHHBT4hKSzVyPUGxMlE5ODZizszN NGi3[GJUSU6JRWK=
NB7 MmTHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYPJR|UxRTFzLkOyPVch|ryP NXjK[WlTW0GQR1XS
RPMI-6666 NY\IfZRxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkXSTWM2OD1zMj65OVY4KM7:TR?= MlTJV2FPT0WU
697 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnHvTWM2OD1zMz6yO|AyKM7:TR?= NE\tPWRUSU6JRWK=
CTB-1 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWLxfJZDUUN3ME2xN{42QTR6IN88US=> MVPTRW5ITVJ?
VA-ES-BJ M3LPTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1LvbWlEPTB;MUOuPVI{PCEQvF2= MnTvV2FPT0WU
BE-13 NHLw[nRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXnJR|UxRTF2LkO5NVUh|ryP M2PQSXNCVkeHUh?=
SKM-1 NInFSFdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M17RUGlEPTB;MUSuOFQ6QSEQvF2= MXHTRW5ITVJ?
TE-6 M2\vSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmHLTWM2OD1zND63OVkyKM7:TR?= MX;TRW5ITVJ?
LB771-HNC M4j5UWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3XQPWlEPTB;MUSuO|g6QCEQvF2= NHP6eZRUSU6JRWK=
ECC4 M4HPfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXHJR|UxRTF5LkCyO|ch|ryP NVG4NIRsW0GQR1XS
ES3 M3jjS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYrqNJZPUUN3ME2xO{41PjV3IN88US=> MUHTRW5ITVJ?
LB647-SCLC NFXrZ4VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3LK[2lEPTB;MUeuOFk1QSEQvF2= M3LlZnNCVkeHUh?=
NB10 NX7sWG42T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVPJR|UxRTF6LkWyOVYh|ryP MVPTRW5ITVJ?
L-540 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1X3Z2lEPTB;MUiuPFExQSEQvF2= NHTCR3dUSU6JRWK=
NCI-H2126 MkXGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlPXTWM2OD1zOT61NUDPxE1? NWjKeW9KW0GQR1XS
HH NGrKTVlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoTjTWM2OD1{MD6wNFk6KM7:TR?= NGHONlVUSU6JRWK=
MPP-89 NWDpcWR5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV[yZXhkUUN3ME2yN{4zOjh7IN88US=> Mm\RV2FPT0WU
IST-MEL1 M160WGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUPJR|UxRTJ|Lki2OVgh|ryP MXTTRW5ITVJ?
KP-N-YS NGnUS2JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoXNTWM2OD1{Mz65NlU2KM7:TR?= NEH2WGtUSU6JRWK=
EC-GI-10 NXz3ZpQzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXfJR|UxRTJ2LkW5PFkh|ryP NVjwOYN4W0GQR1XS
EKVX NHLoWZdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYDJR|UxRTJ4LkCyNFMh|ryP M{jlTHNCVkeHUh?=
TGBC1TKB NIizeFdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUnySY1KUUN3ME2yOk41OzRizszN NFG2N2VUSU6JRWK=
Daudi NE\0UohIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MY\JR|UxRTJ5LkC3O|Mh|ryP NW\JOIVTW0GQR1XS
ALL-PO M{iyS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGH3S2dKSzVyPUK3MlA5OSEQvF2= M17WPHNCVkeHUh?=
NB6 NIeybplIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnXTTWM2OD1{Nz60PFgh|ryP MlyxV2FPT0WU
ES6 M4TnNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3nGcmlEPTB;MkeuPVEzOyEQvF2= MV7TRW5ITVJ?
COLO-320-HSR M4D0fWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NILsSVRKSzVyPUK4MlA{PzNizszN NH;aPIVUSU6JRWK=
K5 M2nyemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXzEflV[UUN3ME2yPE4yOjh5IN88US=> MVrTRW5ITVJ?
ES1 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH;FXYdKSzVyPUK4Mlc4PzNizszN M2XrO3NCVkeHUh?=
LC-1F NInJOm1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXTJR|UxRTJ7LkezOFYh|ryP NHTNc4JUSU6JRWK=
SCLC-21H MojyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NW[5XIQ4UUN3ME2zNE44OzF5IN88US=> NGrJS3RUSU6JRWK=
SK-PN-DW NVTGWYNoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MljJTWM2OD1|Mj61OVk5KM7:TR?= M{XJcnNCVkeHUh?=
D-247MG NX;VWWo1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn36TWM2OD1|Mj65O|c{KM7:TR?= NEX4RZBUSU6JRWK=
TE-5 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYf3W5hjUUN3ME2zN{4xOzZ{IN88US=> M1XzSnNCVkeHUh?=
MONO-MAC-6 NX\EdFFtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1n0NWlEPTB;M{OuOVA1QCEQvF2= MYfTRW5ITVJ?
LB2518-MEL MmrrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1LKVmlEPTB;M{OuO|Y3PiEQvF2= Mn\UV2FPT0WU
LOXIMVI M1nWSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MljLTWM2OD1|Mz63PVI5KM7:TR?= MVPTRW5ITVJ?
NCI-H209 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{\iZmlEPTB;M{WuNVQ1KM7:TR?= M{XaUXNCVkeHUh?=
A253 M{G1cmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3XlVmlEPTB;M{WuO|QzQSEQvF2= NGfuepNUSU6JRWK=
HCC1599 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYPkfIJnUUN3ME2zOk44ODV|IN88US=> MXjTRW5ITVJ?
EB-3 NH;nSXFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYHJR|UxRTN4Lkm1NVgh|ryP M{TGN3NCVkeHUh?=
GOTO MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn7NTWM2OD1|Nz6zNlI1KM7:TR?= MWDTRW5ITVJ?
SW684 NYO3cnBOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIn2SIVKSzVyPUSxMlg1QTVizszN M{LaUHNCVkeHUh?=
DEL M{HpPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIK5VJBKSzVyPUSyMlA2OjJizszN M3W4UXNCVkeHUh?=
HT-144 NIP3S|RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M13pfmlEPTB;NEKuNVY4PiEQvF2= MUTTRW5ITVJ?
TE-9 NXLWcotsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFjT[GlKSzVyPUSzMlQ2QTZizszN NVTWcmxmW0GQR1XS
KARPAS-45 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlnZTWM2OD12ND6zPVI2KM7:TR?= M4D1enNCVkeHUh?=
HAL-01 NVrFb2J5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{fuS2lEPTB;NESuOVA{PCEQvF2= M4HaN3NCVkeHUh?=
RCC10RGB MlPXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mlm2TWM2OD12ND63N|kzKM7:TR?= NXS2[lZ4W0GQR1XS
CP67-MEL M{e2d2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1LMU2lEPTB;NEWuOlI1OSEQvF2= M2DzSXNCVkeHUh?=
NB17 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4XURmlEPTB;NEWuOlY1OyEQvF2= NFH3OIZUSU6JRWK=
SK-UT-1 NEfLfmZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVHGdHdVUUN3ME20OU46PDZ2IN88US=> MofRV2FPT0WU
JiyoyeP-2003 M3TROGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkLyTWM2OD12Nj6wNVE6KM7:TR?= MVvTRW5ITVJ?
HCE-4 NVLo[G1[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF\2WmxKSzVyPUS2MlU6PjhizszN MUXTRW5ITVJ?
NCI-H720 MkLES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYTUdGhkUUN3ME20Ok44Pjh{IN88US=> NWmwWWtWW0GQR1XS
KARPAS-422 Mo\jS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXzJR|UxRTR5LkC4PVUh|ryP MljRV2FPT0WU
Ramos-2G6-4C10 MoPNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1zRVGlEPTB;NEeuNVYzOiEQvF2= MYjTRW5ITVJ?
HCE-T M2fkfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1\6RmlEPTB;NEeuOlgzQCEQvF2= MXjTRW5ITVJ?
PSN1 M33Gdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUfJR|UxRTR5Lke4NVMh|ryP MmnzV2FPT0WU

... 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)
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

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 (Different batches have different solubility ratios, please contact Selleck to provide you with the correct ratio)
% 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):
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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
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