Saracatinib (AZD0530)

Catalog No.S1006

Saracatinib (AZD0530) Chemical Structure

Molecular Weight(MW): 542.03

Saracatinib (AZD0530) is a potent Src inhibitor with IC50 of 2.7 nM in cell-free assays, and potent to c-Yes, Fyn, Lyn, Blk, Fgr and Lck; less active for Abl and EGFR (L858R and L861Q). Phase 2/3.

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Cited by 177 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 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYmzSWRnUUN3ME2wMlA3OTR|IN88US=> MYrTRW5ITVJ?
LAMA-84 M1TmVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV\tTm9ZUUN3ME2wMlE2QTlizszN NIX6TXBUSU6JRWK=
MEG-01 NGDlcG9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHPQbGhKSzVyPUCuNlM3QDhizszN NULPPFdTW0GQR1XS
EM-2 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn\CTWM2OD1yLkK2OUDPxE1? NWDyeHZCW0GQR1XS
TE-15 NWfPTZVyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXfHSnlXUUN3ME2wMlI4PDF{IN88US=> MUHTRW5ITVJ?
NCI-H1648 NXLZNoV7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NImwWmhKSzVyPUCuNlgyOTZizszN NUHUe5dGW0GQR1XS
TE-12 M{\qc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4DTeGlEPTB;MD6zNlY5KM7:TR?= MnTSV2FPT0WU
LB996-RCC MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MU\JR|UxRTBwNESxPVYh|ryP NHLDXWNUSU6JRWK=
K-562 M{\F[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVvJR|UxRTBwNES5Olch|ryP MVHTRW5ITVJ?
D-336MG M{TMNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlG1TWM2OD1yLkWwN|A1KM7:TR?= NX3VfWU6W0GQR1XS
NOS-1 Mof4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIjK[IhKSzVyPUCuOlA2OjlizszN MVXTRW5ITVJ?
EW-24 NEjWNY5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVXiepA3UUN3ME2wMlYzPjl|IN88US=> M2Lm[nNCVkeHUh?=
BV-173 M1zWTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn3NTWM2OD1yLk[1NlQ6KM7:TR?= MWTTRW5ITVJ?
NCCIT M1;zcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIfadIFKSzVyPUCuO|MzOThizszN MmPoV2FPT0WU
NCI-H1436 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2fmRmlEPTB;MD63PVA1QSEQvF2= NGrNbWtUSU6JRWK=
BB30-HNC MnnUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlXZTWM2OD1yLki2NlA{KM7:TR?= NGj2R|BUSU6JRWK=
TE-8 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M17EWWlEPTB;MD64O|I4PSEQvF2= NHnmWHlUSU6JRWK=
A704 MmjMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1WySGlEPTB;MD64PVIyKM7:TR?= MV;TRW5ITVJ?
TK10 NGXvfWJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnTGTWM2OD1yLkmwOlY6KM7:TR?= M4fsW3NCVkeHUh?=
KS-1 NIK4eHNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3zKVWlEPTB;MT6xPVc4QSEQvF2= M4DTOnNCVkeHUh?=
C2BBe1 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml;iTWM2OD1zLkKwOVA4KM7:TR?= NYHlVmxqW0GQR1XS
RXF393 NX;lNY1rT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVG4dJh6UUN3ME2xMlI1OzZizszN M1X6THNCVkeHUh?=
KGN MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYTVNmZkUUN3ME2xMlI4Pjh5IN88US=> MYTTRW5ITVJ?
NB69 NXrMWJV5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2LSbWlEPTB;MT6zO|Q6PyEQvF2= MYnTRW5ITVJ?
TE-11 NXHie2hpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlG0TWM2OD1zLkSzOFE5KM7:TR?= NG\jO2xUSU6JRWK=
TE-1 NEHDN4dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlzDTWM2OD1zLkS0NVA2KM7:TR?= NX3v[mZrW0GQR1XS
ST486 NFTidVNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{jONGlEPTB;MT60OVg2OiEQvF2= NV7WZWs3W0GQR1XS
HOP-62 M1vjc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlHQTWM2OD1zLkWwNlQ3KM7:TR?= MnHvV2FPT0WU
EW-16 MmnUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoXpTWM2OD1zLkW1NFg{KM7:TR?= MmLKV2FPT0WU
LB1047-RCC NWnRSXZnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXrBWJRGUUN3ME2xMlU2PDV|IN88US=> Mn3GV2FPT0WU
TE-10 NEPxV2xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYnJ[HBqUUN3ME2xMlY3OjV{IN88US=> MXvTRW5ITVJ?
RL95-2 MnnlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVLQTmg2UUN3ME2xMlY3QTB{IN88US=> MUjTRW5ITVJ?
DOHH-2 NHjhOIpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1jsZmlEPTB;MT63NVc5OiEQvF2= M3nIZnNCVkeHUh?=
MFH-ino NWHBRXdIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWrJR|UxRTFwN{e4O{DPxE1? M2G3b3NCVkeHUh?=
GB-1 M1rRR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUHJbGljUUN3ME2xMlc6QDN|IN88US=> M4O1bHNCVkeHUh?=
SK-N-DZ MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2fuTmlEPTB;MT64OFY5QCEQvF2= NIrpXohUSU6JRWK=
OS-RC-2 NEnDeXpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{XLPGlEPTB;MT64PFU4PCEQvF2= NFy1TFBUSU6JRWK=
SW982 NWfrO5c{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWLoVotNUUN3ME2xMlkzODl|IN88US=> MUTTRW5ITVJ?
KALS-1 NHm3cWdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4P1S2lEPTB;MT65PFczOiEQvF2= M4\HO3NCVkeHUh?=
TGBC24TKB MmD1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2fvemlEPTB;Mj6wOVk2QCEQvF2= NYW5fGE4W0GQR1XS
GI-1 NH3yVmtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWDpXnVxUUN3ME2yMlE3ODh2IN88US=> NWLkNHdzW0GQR1XS
SW962 NUDMcFc4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mk\PTWM2OD1{LkG3NVc5KM7:TR?= MXfTRW5ITVJ?
SW872 NUjtWFAyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGHPXYtKSzVyPUKuNVg2ODdizszN NEHsc5NUSU6JRWK=
NCI-H747 M1[wbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYPr[IdCUUN3ME2yMlI2PzF2IN88US=> NHH3NmdUSU6JRWK=
MZ1-PC NV3lO2dWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NETPNJZKSzVyPUKuNlk{PTZizszN NWLJbIJTW0GQR1XS
MSTO-211H MonhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnHHTWM2OD1{LkO1O|I{KM7:TR?= NILRdZVUSU6JRWK=
BL-70 MmiwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYDPO2d[UUN3ME2yMlQ4PDJ{IN88US=> MVrTRW5ITVJ?
SW954 NH3pZohIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MonPTWM2OD1{LkW3OFA5KM7:TR?= MlSwV2FPT0WU
SNB75 M3X2dmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHv4WHVKSzVyPUKuOlg2QTRizszN MlPRV2FPT0WU
IST-SL2 MlLoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mm\sTWM2OD1{LkeyN|c6KM7:TR?= M33h[HNCVkeHUh?=
GCIY MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEm4V2VKSzVyPUKuPFcxODVizszN MoLYV2FPT0WU
KU812 MmTLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkS4TWM2OD1|LkC1Nlk6KM7:TR?= NG[4cXZUSU6JRWK=
LXF-289 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFriPYRKSzVyPUOuNVIyODlizszN M1X0S3NCVkeHUh?=
ETK-1 MlXqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M37OUWlEPTB;Mz6yNFc3PyEQvF2= MlLGV2FPT0WU
SF126 NFXXSlVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnHLTWM2OD1|LkOxNVc1KM7:TR?= MXrTRW5ITVJ?
LC-2-ad MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFTlTHVKSzVyPUOuOVU4KM7:TR?= M4jUT3NCVkeHUh?=
KNS-42 MoHTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXPJR|UxRTNwNkWg{txO Mn\4V2FPT0WU
OVCAR-4 MorHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1zRUmlEPTB;Mz63N|Q{OyEQvF2= MVnTRW5ITVJ?
PF-382 NITrVppIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYrJR|UxRTNwOEO2PVgh|ryP MXHTRW5ITVJ?
SH-4 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIP1cYRKSzVyPUSuNlUzPTlizszN NV70e2o1W0GQR1XS
KM12 NHjiSpNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEPKc2NKSzVyPUSuN|I1OTZizszN NVTpUZJ[W0GQR1XS
NB5 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkjGTWM2OD12LkSxPFY1KM7:TR?= MUnTRW5ITVJ?
KURAMOCHI Mm\3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWnJR|UxRTRwNkWyOVYh|ryP NFm0ToRUSU6JRWK=
Becker MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF3TW5hKSzVyPUSuOlY1OTZizszN M3n4RXNCVkeHUh?=
MV-4-11 NHPTfFBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHjIZ21KSzVyPUSuPFE{PDRizszN M3nQeHNCVkeHUh?=
KINGS-1 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1q1Z2lEPTB;ND64NlM4OyEQvF2= MnrjV2FPT0WU
LS-123 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3rNfWlEPTB;NT60PVY5PCEQvF2= NULyNWlnW0GQR1XS
SF268 M1vpSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlHlTWM2OD13Lk[xNlYzKM7:TR?= NUXqO|J5W0GQR1XS
A388 NH3Ydo1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnOwTWM2OD13Lk[zOlY4KM7:TR?= NHHQUnFUSU6JRWK=
NMC-G1 NY\N[WJTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXfDN|djUUN3ME22MlAyQDFzIN88US=> MnG4V2FPT0WU
CGTH-W-1 NEPFS2ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4OxZWlEPTB;Nj6wNlA4PSEQvF2= MoPHV2FPT0WU
ES4 MmLuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1jHNmlEPTB;Nj61N|A4PCEQvF2= NVfRUZZwW0GQR1XS
SR M4LGXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{nZNWlEPTB;Nj61PFgxPyEQvF2= NVzETYZMW0GQR1XS
BB49-HNC NW[2eVhyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHHJRlNKSzVyPU[uO|MzODZizszN MWjTRW5ITVJ?
KLE NXXMc|JpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXPpZXkzUUN3ME22Mlc5Ozd5IN88US=> NHvKTpRUSU6JRWK=
HUTU-80 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoTaTWM2OD14Lkm4OFY3KM7:TR?= MVzTRW5ITVJ?
SNU-C2B NUT3e5p2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVLzVXNXUUN3ME23MlgzPzN5IN88US=> MluwV2FPT0WU
BB65-RCC M1:z[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXPJR|UxRTdwOUS5NFQh|ryP NVTrPJhVW0GQR1XS
QIMR-WIL NULz[nVwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYDJR|UxRThwNEK4NFgh|ryP M{\YTHNCVkeHUh?=
GDM-1 MonlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWTUWVBPUUN3ME24Mlk4Ojl{IN88US=> MUDTRW5ITVJ?
LC4-1 NGnpW4NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoHYTWM2OD17LkCwPVEyKM7:TR?= NXzGdlg2W0GQR1XS
MLMA M1rheWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYLuN3ZXUUN3ME25MlE2ODB4IN88US=> MWnTRW5ITVJ?
EoL-1-cell Mn;VS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1f2VWlEPTB;OT6zNFE6OiEQvF2= NHzIbHlUSU6JRWK=
BOKU NFzseHRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUC0eY13UUN3ME25Mlk3PDZ4IN88US=> NH\EVXBUSU6JRWK=
EVSA-T MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVjJR|UxRTFyLk[1Olgh|ryP NELuZ2xUSU6JRWK=
D-283MED M1roUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3nxcmlEPTB;MUCuPVE4PiEQvF2= NYnpN2RGW0GQR1XS
NB1 NXP6ZW43T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF3sWlBKSzVyPUGxMlAzPDJizszN Mn\nV2FPT0WU
RPMI-8402 M4KzTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVHJR|UxRTFzLkG3PEDPxE1? NFz0[npUSU6JRWK=
NCI-H1355 M{j4Tmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH;ONmpKSzVyPUGxMlE5ODZizszN MkTRV2FPT0WU
NB7 Mny1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mnq2TWM2OD1zMT6zNlk4KM7:TR?= NGP4Om1USU6JRWK=
RPMI-6666 NWfmfnB4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWflUIFkUUN3ME2xNk46PTZ5IN88US=> NVrnO4xQW0GQR1XS
697 MoLLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXHDOGpyUUN3ME2xN{4zPzBzIN88US=> NXfKPG8yW0GQR1XS
CTB-1 NF\MTlJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M322[GlEPTB;MUOuOVk1QCEQvF2= MnH1V2FPT0WU
VA-ES-BJ M2DPPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWjCNmgzUUN3ME2xN{46OjN2IN88US=> NFH1TFZUSU6JRWK=
BE-13 NI\hNohIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHXhZohKSzVyPUG0MlM6OTVizszN NFjkbJdUSU6JRWK=
SKM-1 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVix[4FtUUN3ME2xOE41PDl7IN88US=> M2DMNXNCVkeHUh?=
TE-6 M1GwfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnP1TWM2OD1zND63OVkyKM7:TR?= MoLWV2FPT0WU
LB771-HNC MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2\yPWlEPTB;MUSuO|g6QCEQvF2= MVTTRW5ITVJ?
ECC4 NFHu[2lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIHSSYlKSzVyPUG3MlAzPzdizszN NE\3TphUSU6JRWK=
ES3 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX7JR|UxRTF5LkS2OVUh|ryP M1;aXHNCVkeHUh?=
LB647-SCLC NXrj[5FpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mm[3TWM2OD1zNz60PVQ6KM7:TR?= NV3Zb|BmW0GQR1XS
NB10 M1LnbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUTMelU4UUN3ME2xPE42OjV4IN88US=> M{W0W3NCVkeHUh?=
L-540 NHzPXmtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmL6TWM2OD1zOD64NVA6KM7:TR?= NFvtdGdUSU6JRWK=
NCI-H2126 NGHJXYJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3HyZWlEPTB;MUmuOVEh|ryP MojMV2FPT0WU
HH NUm5OVFpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV\GVGZiUUN3ME2yNE4xODl7IN88US=> NFnt[mZUSU6JRWK=
MPP-89 MknZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFrKNGRKSzVyPUKzMlIzQDlizszN MlK3V2FPT0WU
IST-MEL1 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV;VWHJYUUN3ME2yN{45PjV6IN88US=> MkLJV2FPT0WU
KP-N-YS MoLBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1;VO2lEPTB;MkOuPVI2PSEQvF2= MVPTRW5ITVJ?
EC-GI-10 M4\O[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFPJdlRKSzVyPUK0MlU6QDlizszN MVvTRW5ITVJ?
EKVX NX7XdZJnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWPJR|UxRTJ4LkCyNFMh|ryP M{XScXNCVkeHUh?=
TGBC1TKB NFHhXXBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYXmO5AxUUN3ME2yOk41OzRizszN NEnRVllUSU6JRWK=
Daudi NID1ZW5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmfmTWM2OD1{Nz6wO|c{KM7:TR?= NFW2NFNUSU6JRWK=
ALL-PO NWLOUJpJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHHYeGlKSzVyPUK3MlA5OSEQvF2= NE\NTFlUSU6JRWK=
NB6 Ml7RS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3\s[mlEPTB;MkeuOFg5KM7:TR?= MX;TRW5ITVJ?
ES6 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX\4ZlRVUUN3ME2yO{46OTJ|IN88US=> M3v6cXNCVkeHUh?=
COLO-320-HSR NWjMPFZuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYTidVByUUN3ME2yPE4xOzd|IN88US=> Mn;5V2FPT0WU
K5 M121Zmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{m0d2lEPTB;MkiuNVI5PyEQvF2= NE\LSnJUSU6JRWK=
ES1 M33s[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXvXU2FOUUN3ME2yPE44Pzd|IN88US=> Ml;tV2FPT0WU
LC-1F NWLHZ5dTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUjJR|UxRTJ7LkezOFYh|ryP NIDKTmhUSU6JRWK=
SCLC-21H MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml3CTWM2OD1|MD63N|E4KM7:TR?= M1HoTnNCVkeHUh?=
SK-PN-DW NXLKN4dDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4jacGlEPTB;M{KuOVU6QCEQvF2= M{XLeHNCVkeHUh?=
D-247MG MlPoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYrJR|UxRTN{Lkm3O|Mh|ryP MULTRW5ITVJ?
TE-5 NIHB[llIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M33xfWlEPTB;M{OuNFM3OiEQvF2= NG\OfYRUSU6JRWK=
MONO-MAC-6 MonJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4C5TGlEPTB;M{OuOVA1QCEQvF2= MV7TRW5ITVJ?
LB2518-MEL NH;VdphIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUe3dXk1UUN3ME2zN{44PjZ4IN88US=> NXTST5RHW0GQR1XS
LOXIMVI MlX6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{fKZ2lEPTB;M{OuO|kzQCEQvF2= NYnERm9SW0GQR1XS
NCI-H209 NWLGfpI3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{KwUmlEPTB;M{WuNVQ1KM7:TR?= NYTIXXhRW0GQR1XS
A253 MkXoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1zmPWlEPTB;M{WuO|QzQSEQvF2= MkPvV2FPT0WU
HCC1599 M3HGfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV;VOnJDUUN3ME2zOk44ODV|IN88US=> M1nyeHNCVkeHUh?=
EB-3 NUHNO4ZjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEXESXdKSzVyPUO2Mlk2OThizszN MX3TRW5ITVJ?
GOTO NGTtW3RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGDLRXJKSzVyPUO3MlMzOjRizszN M4fk[3NCVkeHUh?=
SW684 MlXNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2XjRWlEPTB;NEGuPFQ6PSEQvF2= MYrTRW5ITVJ?
DEL Mn;YS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmDITWM2OD12Mj6wOVIzKM7:TR?= NX\qNXJjW0GQR1XS
HT-144 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHXpbplKSzVyPUSyMlE3PzZizszN NIfzV25USU6JRWK=
TE-9 NV7LSZhbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIfJXWxKSzVyPUSzMlQ2QTZizszN NVXlWHp6W0GQR1XS
KARPAS-45 NFPjfpRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn;STWM2OD12ND6zPVI2KM7:TR?= MXrTRW5ITVJ?
HAL-01 MluxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYHTS5JHUUN3ME20OE42ODN2IN88US=> MlLPV2FPT0WU
RCC10RGB NUnicmp7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmjXTWM2OD12ND63N|kzKM7:TR?= MYLTRW5ITVJ?
CP67-MEL M2LNS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGPHSG1KSzVyPUS1MlYzPDFizszN MXzTRW5ITVJ?
NB17 NYHCWHhpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkjJTWM2OD12NT62OlQ{KM7:TR?= NH7aZYZUSU6JRWK=
SK-UT-1 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGHKWnJKSzVyPUS1Mlk1PjRizszN M1vEdnNCVkeHUh?=
JiyoyeP-2003 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXHJR|UxRTR4LkCxNVkh|ryP NWi2dXF6W0GQR1XS
HCE-4 MmrGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVO2Wog4UUN3ME20Ok42QTZ6IN88US=> MYTTRW5ITVJ?
NCI-H720 Ml\FS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWTBSodzUUN3ME20Ok44Pjh{IN88US=> NVfjO4dRW0GQR1XS
KARPAS-422 MoiwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXv0Ro9SUUN3ME20O{4xQDl3IN88US=> NV7Lb5F7W0GQR1XS
Ramos-2G6-4C10 MlTqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MonrTWM2OD12Nz6xOlIzKM7:TR?= Mlq4V2FPT0WU
HCE-T NUjzcotpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF7yXYVKSzVyPUS3MlY5OjhizszN NYrtPXVSW0GQR1XS
PSN1 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX;5W5FPUUN3ME20O{44QDF|IN88US=> NYPreo5qW0GQR1XS

... 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

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)

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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

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The Serial Dilution Calculator Equation

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Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

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

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)
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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