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 170 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 NH3GdGdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{TzdGlEPTB;MD6wOlE1OyEQvF2= MkDuV2FPT0WU
LAMA-84 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX;JR|UxRTBwMUW5PUDPxE1? NGjKcFJUSU6JRWK=
MEG-01 MmPRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2PVPGlEPTB;MD6yN|Y5QCEQvF2= MX;TRW5ITVJ?
EM-2 NWXROZV4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NE\EbnJKSzVyPUCuNlY2KM7:TR?= NHr5UHBUSU6JRWK=
TE-15 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHvGTmtKSzVyPUCuNlc1OTJizszN NEHUV2JUSU6JRWK=
NCI-H1648 MlvXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M33lNGlEPTB;MD6yPFEyPiEQvF2= MXzTRW5ITVJ?
TE-12 NVzQSWFkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoHVTWM2OD1yLkOyOlgh|ryP M3TCe3NCVkeHUh?=
LB996-RCC NFrVVmpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGjvUoxKSzVyPUCuOFQyQTZizszN NVToU5JMW0GQR1XS
K-562 MnG3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYXJR|UxRTBwNES5Olch|ryP M336cXNCVkeHUh?=
D-336MG NYHkOolnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFzzS5hKSzVyPUCuOVA{ODRizszN NI\HVnNUSU6JRWK=
NOS-1 M{nYW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NInYTW1KSzVyPUCuOlA2OjlizszN NITWfXlUSU6JRWK=
EW-24 M4jmSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MU\JR|UxRTBwNkK2PVMh|ryP NVXCb44yW0GQR1XS
BV-173 NYPGbo96T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1;mdmlEPTB;MD62OVI1QSEQvF2= M{nXV3NCVkeHUh?=
NCCIT MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWTuUnFOUUN3ME2wMlc{OjF6IN88US=> MVfTRW5ITVJ?
NCI-H1436 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUPBcIozUUN3ME2wMlc6ODR7IN88US=> MnPpV2FPT0WU
BB30-HNC NGXsUXlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmfZTWM2OD1yLki2NlA{KM7:TR?= NIH5eHhUSU6JRWK=
TE-8 M3zyTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnLGTWM2OD1yLki3Nlc2KM7:TR?= NUTiWFFDW0GQR1XS
A704 NEfrdnJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFu5NGNKSzVyPUCuPFkzOSEQvF2= M130[XNCVkeHUh?=
TK10 NH;LfZRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXPlPVFGUUN3ME2wMlkxPjZ7IN88US=> NIPKbnJUSU6JRWK=
KS-1 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFrEbGNKSzVyPUGuNVk4PzlizszN NFPNSotUSU6JRWK=
C2BBe1 NUPVcIU1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFXGXJZKSzVyPUGuNlA2ODdizszN MoXUV2FPT0WU
RXF393 NGP0c5NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUHJR|UxRTFwMkSzOkDPxE1? M{iyW3NCVkeHUh?=
KGN MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVO1dnczUUN3ME2xMlI4Pjh5IN88US=> Ml6yV2FPT0WU
NB69 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH60d2RKSzVyPUGuN|c1QTdizszN M4DZR3NCVkeHUh?=
TE-11 NXfHVYJKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGflRlBKSzVyPUGuOFM1OThizszN NFL6e29USU6JRWK=
TE-1 NFy1UndIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlmzTWM2OD1zLkS0NVA2KM7:TR?= Mkj5V2FPT0WU
ST486 M1H5cWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXPJR|UxRTFwNEW4OVIh|ryP MWDTRW5ITVJ?
HOP-62 NWjGdZVMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVv6PXY2UUN3ME2xMlUxOjR4IN88US=> M4fudnNCVkeHUh?=
EW-16 NHvHdHBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYfJR|UxRTFwNUWwPFMh|ryP MXLTRW5ITVJ?
LB1047-RCC MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoL0TWM2OD1zLkW1OFU{KM7:TR?= M3KwbnNCVkeHUh?=
TE-10 NEjscIZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnS1TWM2OD1zLk[2NlUzKM7:TR?= MmPqV2FPT0WU
RL95-2 M1PNO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkH4TWM2OD1zLk[2PVAzKM7:TR?= M3yyVHNCVkeHUh?=
DOHH-2 NWmyTXVwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEPiNpBKSzVyPUGuO|E4QDJizszN NGi5SJNUSU6JRWK=
MFH-ino NWi5Voo1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHG0dFRKSzVyPUGuO|c5PyEQvF2= NXfxfWd3W0GQR1XS
GB-1 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWrJR|UxRTFwN{m4N|Mh|ryP NHq4SHBUSU6JRWK=
SK-N-DZ NV7BNYxzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEDzUIhKSzVyPUGuPFQ3QDhizszN MWnTRW5ITVJ?
OS-RC-2 MnnyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXLNXVZQUUN3ME2xMlg5PTd2IN88US=> NUi5VplmW0GQR1XS
SW982 NXfWbmNWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2X2cWlEPTB;MT65NlA6OyEQvF2= MoHXV2FPT0WU
KALS-1 Mk\aS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnqxTWM2OD1zLkm4O|IzKM7:TR?= MUXTRW5ITVJ?
TGBC24TKB NH;sfXZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFjTZo1KSzVyPUKuNFU6PThizszN NITxb|JUSU6JRWK=
GI-1 M2G1eWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2\2PWlEPTB;Mj6xOlA5PCEQvF2= MUXTRW5ITVJ?
SW962 Mkn3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmjQTWM2OD1{LkG3NVc5KM7:TR?= NVrteYNxW0GQR1XS
SW872 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1\sc2lEPTB;Mj6xPFUxPyEQvF2= NH\MVZBUSU6JRWK=
NCI-H747 Mo\WS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUfJR|UxRTJwMkW3NVQh|ryP NUHk[pBWW0GQR1XS
MZ1-PC Ml:3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MU\JR|UxRTJwMkmzOVYh|ryP NVr2SGN4W0GQR1XS
MSTO-211H MlraS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoXOTWM2OD1{LkO1O|I{KM7:TR?= MUHTRW5ITVJ?
BL-70 Mon1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYHJR|UxRTJwNEe0NlIh|ryP MVPTRW5ITVJ?
SW954 NYLBPYt4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIPxS4VKSzVyPUKuOVc1ODhizszN MXfTRW5ITVJ?
SNB75 M4j4WGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVPLelczUUN3ME2yMlY5PTl2IN88US=> MWDTRW5ITVJ?
IST-SL2 NHrScI9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MofLTWM2OD1{LkeyN|c6KM7:TR?= M2X5b3NCVkeHUh?=
GCIY MknKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmPLTWM2OD1{Lki3NFA2KM7:TR?= Mm\zV2FPT0WU
KU812 MkG3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3jGcmlEPTB;Mz6wOVI6QSEQvF2= M3nPeXNCVkeHUh?=
LXF-289 NFjw[3JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYnJR|UxRTNwMUKxNFkh|ryP MnvJV2FPT0WU
ETK-1 MkjWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX7JR|UxRTNwMkC3Olch|ryP NXzicJh4W0GQR1XS
SF126 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml7ETWM2OD1|LkOxNVc1KM7:TR?= M{D4dHNCVkeHUh?=
LC-2-ad M1K1e2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3LHNGlEPTB;Mz61OVch|ryP M1jRU3NCVkeHUh?=
KNS-42 NV:2RVk6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2rMXmlEPTB;Mz62OUDPxE1? NXnqO4U3W0GQR1XS
OVCAR-4 NVLjVohET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoTFTWM2OD1|LkezOFM{KM7:TR?= MVnTRW5ITVJ?
PF-382 Mm[2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV[5eWZ[UUN3ME2zMlg{Pjl6IN88US=> NXvv[IFrW0GQR1XS
SH-4 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEDqZmlKSzVyPUSuNlUzPTlizszN MXrTRW5ITVJ?
KM12 NVu4W5J1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NInJSm9KSzVyPUSuN|I1OTZizszN MWLTRW5ITVJ?
NB5 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWfJR|UxRTRwNEG4OlQh|ryP NWixRnFbW0GQR1XS
KURAMOCHI NIfQc3dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml[4TWM2OD12Lk[1NlU3KM7:TR?= MlSxV2FPT0WU
Becker M3z6[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWXJR|UxRTRwNk[0NVYh|ryP NFLPZpNUSU6JRWK=
MV-4-11 NHnGTIJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoHOTWM2OD12LkixN|Q1KM7:TR?= NV7w[Y5SW0GQR1XS
KINGS-1 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHnjdpBKSzVyPUSuPFI{PzNizszN NF\ZbYtUSU6JRWK=
LS-123 NFrJXmpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MU\JR|UxRTVwNEm2PFQh|ryP NXvnS45jW0GQR1XS
SF268 M{\SbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGDPcpJKSzVyPUWuOlEzPjJizszN Mk[yV2FPT0WU
A388 NHvrb5BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mo\5TWM2OD13Lk[zOlY4KM7:TR?= MWjTRW5ITVJ?
NMC-G1 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF3mb2JKSzVyPU[uNFE5OTFizszN NXn1eGZWW0GQR1XS
CGTH-W-1 Mnj5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFO5XXJKSzVyPU[uNFIxPzVizszN MXHTRW5ITVJ?
ES4 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2POZ2lEPTB;Nj61N|A4PCEQvF2= NVrvRmQ5W0GQR1XS
SR M2DsTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4K0XmlEPTB;Nj61PFgxPyEQvF2= NGHtbG1USU6JRWK=
BB49-HNC MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1fPcmlEPTB;Nj63N|IxPiEQvF2= Mn\FV2FPT0WU
KLE NIOyWIpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV\MUolSUUN3ME22Mlc5Ozd5IN88US=> MnSyV2FPT0WU
HUTU-80 NEjFRpdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoDzTWM2OD14Lkm4OFY3KM7:TR?= NUnCRmJiW0GQR1XS
SNU-C2B M1HOW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEDDWXlKSzVyPUeuPFI4OzdizszN NH7SWpdUSU6JRWK=
BB65-RCC NH3YOVRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmPlTWM2OD15Lkm0PVA1KM7:TR?= NWjPdpRqW0GQR1XS
QIMR-WIL NXnaRYUzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4HIbGlEPTB;OD60NlgxQCEQvF2= NX\aTXNmW0GQR1XS
GDM-1 M{HaS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoTPTWM2OD16Lkm3NlkzKM7:TR?= MWrTRW5ITVJ?
LC4-1 NUXNd4RkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYniVYVvUUN3ME25MlAxQTFzIN88US=> MnfMV2FPT0WU
MLMA Mn\uS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWjlfHdYUUN3ME25MlE2ODB4IN88US=> NVXvTZFxW0GQR1XS
EoL-1-cell MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M33zV2lEPTB;OT6zNFE6OiEQvF2= MnLOV2FPT0WU
BOKU M{HyTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{XDOWlEPTB;OT65OlQ3PiEQvF2= MXHTRW5ITVJ?
EVSA-T NYnKeYd[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHHQSHpKSzVyPUGwMlY2PjhizszN NIn6R4lUSU6JRWK=
D-283MED M1K1R2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWXXXnlwUUN3ME2xNE46OTd4IN88US=> Mm[3V2FPT0WU
NB1 MorTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{HkSGlEPTB;MUGuNFI1OiEQvF2= M2OwZ3NCVkeHUh?=
RPMI-8402 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHrJZ|hKSzVyPUGxMlE4QCEQvF2= NWnBfpBsW0GQR1XS
NCI-H1355 M2Kwfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHX3TpFKSzVyPUGxMlE5ODZizszN M1LkUXNCVkeHUh?=
NB7 NYDmUZI6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV;5fmVoUUN3ME2xNU4{Ojl5IN88US=> NWfZTWxYW0GQR1XS
RPMI-6666 M2W4fGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlrxTWM2OD1zMj65OVY4KM7:TR?= M2\TV3NCVkeHUh?=
697 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkDaTWM2OD1zMz6yO|AyKM7:TR?= M4iwenNCVkeHUh?=
CTB-1 MknkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mmq4TWM2OD1zMz61PVQ5KM7:TR?= MU\TRW5ITVJ?
VA-ES-BJ NVjmdXNuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGjLV3RKSzVyPUGzMlkzOzRizszN NGTme5RUSU6JRWK=
BE-13 M1;TV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHPqZlNKSzVyPUG0MlM6OTVizszN MlzqV2FPT0WU
SKM-1 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH;Db|NKSzVyPUG0MlQ1QTlizszN M{nR[3NCVkeHUh?=
TE-6 NGjmS3RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXHJR|UxRTF2Lke1PVEh|ryP NFfQepFUSU6JRWK=
LB771-HNC MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUPSUFRkUUN3ME2xOE44QDl6IN88US=> NHj0S|BUSU6JRWK=
ECC4 NED5[2FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYDjZnFwUUN3ME2xO{4xOjd5IN88US=> MoraV2FPT0WU
ES3 NFuyS5ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXLJR|UxRTF5LkS2OVUh|ryP NXn0c4RjW0GQR1XS
LB647-SCLC MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWDJR|UxRTF5LkS5OFkh|ryP NEXiTFZUSU6JRWK=
NB10 M{PxWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGK1SJdKSzVyPUG4MlUzPTZizszN Mn\zV2FPT0WU
L-540 NFLYZWpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUfJR|UxRTF6LkixNFkh|ryP MkHjV2FPT0WU
NCI-H2126 NFiyOnNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIHXZY5KSzVyPUG5MlUyKM7:TR?= MXnTRW5ITVJ?
HH M4rmdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUnJR|UxRTJyLkCwPVkh|ryP NV\0cndzW0GQR1XS
MPP-89 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXvMPFdGUUN3ME2yN{4zOjh7IN88US=> NWHFTlM4W0GQR1XS
IST-MEL1 NHLITVlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIXQVI1KSzVyPUKzMlg3PThizszN NVTLPGJiW0GQR1XS
KP-N-YS NXfSbG5vT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NETpPZVKSzVyPUKzMlkzPTVizszN MWTTRW5ITVJ?
EC-GI-10 NYm4cZh6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnnUTWM2OD1{ND61PVg6KM7:TR?= M3\ZNXNCVkeHUh?=
EKVX MkTxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoDoTWM2OD1{Nj6wNlA{KM7:TR?= NEfQOFBUSU6JRWK=
TGBC1TKB M3TqbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWXiZZJLUUN3ME2yOk41OzRizszN MYfTRW5ITVJ?
Daudi M3fT[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVzpWHBXUUN3ME2yO{4xPzd|IN88US=> Mk\zV2FPT0WU
ALL-PO NU\ScVJCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3XJNmlEPTB;MkeuNFgyKM7:TR?= Ml;QV2FPT0WU
NB6 MlLRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4rIPWlEPTB;MkeuOFg5KM7:TR?= MYLTRW5ITVJ?
ES6 NYK0R5NWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn;tTWM2OD1{Nz65NVI{KM7:TR?= MX;TRW5ITVJ?
COLO-320-HSR MlPmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWnJR|UxRTJ6LkCzO|Mh|ryP NFz1S5lUSU6JRWK=
K5 MoLDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXXxem1yUUN3ME2yPE4yOjh5IN88US=> NFnOU4ZUSU6JRWK=
ES1 M2DteGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoniTWM2OD1{OD63O|c{KM7:TR?= MWTTRW5ITVJ?
LC-1F MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3LyNWlEPTB;MkmuO|M1PiEQvF2= MnKxV2FPT0WU
SCLC-21H NYPLN2pFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4nKfWlEPTB;M{CuO|MyPyEQvF2= NEjzNFFUSU6JRWK=
SK-PN-DW MkfhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmPoTWM2OD1|Mj61OVk5KM7:TR?= NUHCe2V{W0GQR1XS
D-247MG MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIL3Wm5KSzVyPUOyMlk4PzNizszN M1n6WnNCVkeHUh?=
TE-5 MkfQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVmz[lF7UUN3ME2zN{4xOzZ{IN88US=> MWPTRW5ITVJ?
MONO-MAC-6 MknNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml3UTWM2OD1|Mz61NFQ5KM7:TR?= NH;WOo1USU6JRWK=
LB2518-MEL MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXrJR|UxRTN|Lke2OlYh|ryP NHruWYFUSU6JRWK=
LOXIMVI M3jBUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Moj6TWM2OD1|Mz63PVI5KM7:TR?= MVzTRW5ITVJ?
NCI-H209 NUnIVHR7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV3JR|UxRTN3LkG0OEDPxE1? NIDreIJUSU6JRWK=
A253 NIfyc|VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4DuVGlEPTB;M{WuO|QzQSEQvF2= MmXjV2FPT0WU
HCC1599 NYLoTppZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1fqTWlEPTB;M{[uO|A2OyEQvF2= NEjsS29USU6JRWK=
EB-3 M3jOe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MluzTWM2OD1|Nj65OVE5KM7:TR?= NWTIdZo2W0GQR1XS
GOTO MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnjkTWM2OD1|Nz6zNlI1KM7:TR?= NXzRNlZEW0GQR1XS
SW684 M4fSNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEjFTGRKSzVyPUSxMlg1QTVizszN MV;TRW5ITVJ?
DEL NWnGS|NFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUnJR|UxRTR{LkC1NlIh|ryP M{\BbnNCVkeHUh?=
HT-144 M3Pybmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFLEZYVKSzVyPUSyMlE3PzZizszN MWDTRW5ITVJ?
TE-9 NWjrZXBoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXfPcmkxUUN3ME20N{41PTl4IN88US=> MUHTRW5ITVJ?
KARPAS-45 M2j3Umdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUXUR4o5UUN3ME20OE4{QTJ3IN88US=> Mmn3V2FPT0WU
HAL-01 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHT4fJdKSzVyPUS0MlUxOzRizszN MWjTRW5ITVJ?
RCC10RGB MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4DKd2lEPTB;NESuO|M6OiEQvF2= MmSzV2FPT0WU
CP67-MEL MkKyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWDJZ403UUN3ME20OU43OjRzIN88US=> M4HZUXNCVkeHUh?=
NB17 M3jj[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYPJR|UxRTR3Lk[2OFMh|ryP NX7yNnFFW0GQR1XS
SK-UT-1 MoPaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M17RUmlEPTB;NEWuPVQ3PCEQvF2= NH\xcXNUSU6JRWK=
JiyoyeP-2003 M4TlNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEnWNVhKSzVyPUS2MlAyOTlizszN NXm5OFR1W0GQR1XS
HCE-4 M17Ce2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1Th[GlEPTB;NE[uOVk3QCEQvF2= NHX0c3FUSU6JRWK=
NCI-H720 NUDyZWRVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEiyVYdKSzVyPUS2Mlc3QDJizszN MUTTRW5ITVJ?
KARPAS-422 NU\aeWVjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHvPR5lKSzVyPUS3MlA5QTVizszN MkTmV2FPT0WU
Ramos-2G6-4C10 M3:zUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHfWVINKSzVyPUS3MlE3OjJizszN NYHDbFJVW0GQR1XS
HCE-T MoLpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVzJR|UxRTR5Lk[4Nlgh|ryP NH3POVBUSU6JRWK=
PSN1 MnvhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWCyVYJNUUN3ME20O{44QDF|IN88US=> M2XXd3NCVkeHUh?=

... 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)

  • 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 )

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

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
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    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

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

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

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

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02085603 Completed Drug: Saracatinib|Drug: Placebo Cancer Sheffield Teaching Hospitals NHS Foundation Trust|AstraZeneca March 2014 Phase 2
NCT01864655 Completed Drug: saracatinib|Drug: Placebo Alzheimer''s Disease Stephen M. Strittmatter|Yale University July 2013 Phase 1
NCT01000896 Withdrawn Drug: AZD0530|Drug: Carboplatin|Drug: paclitaxel Cancer|Non Small Cell Lung Cancer|Epithelial Ovarian Cancer AstraZeneca January 2010 Phase 1
NCT00853983 Completed Drug: [14C] AZD0530 Healthy AstraZeneca March 2009 Phase 1
NCT00752206 Completed Drug: Saracatinib|Drug: Placebo Osteosarcoma Sarcoma Alliance for Research through Collaboration|AstraZeneca March 2009 Phase 2
NCT00771979 Completed Drug: AZD0530 Healthy AstraZeneca November 2008 Phase 1

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

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Frequently Asked Questions

  • Question 1:

    What is the half-life of Saracatinib?

  • Answer:

    Based on the following paper, the half-life of Saracatinib in vivo is around 40hours and it reaches its peak lever around 2-4 hours after dosing: http://clincancerres.aacrjournals.org/content/16/19/4876.long

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID