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 67 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 NYjyWW4{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIHER3RKSzVyPUCuNFYyPDNizszN MV;TRW5ITVJ?
LAMA-84 NIfQR2xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1;FfGlEPTB;MD6xOVk6KM7:TR?= M{f2cnNCVkeHUh?=
MEG-01 M1zweWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmLwTWM2OD1yLkKzOlg5KM7:TR?= NEDoOZpUSU6JRWK=
EM-2 M{O4Vmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1PsOmlEPTB;MD6yOlUh|ryP MVnTRW5ITVJ?
TE-15 MlP1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mnr4TWM2OD1yLkK3OFEzKM7:TR?= MUXTRW5ITVJ?
NCI-H1648 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2fQeGlEPTB;MD6yPFEyPiEQvF2= NWGyV|FiW0GQR1XS
TE-12 MkfnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXW3UlBJUUN3ME2wMlMzPjhizszN Mo\QV2FPT0WU
LB996-RCC NEL1UmVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnPDTWM2OD1yLkS0NVk3KM7:TR?= NInBdmFUSU6JRWK=
K-562 NGm3ZlNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlvZTWM2OD1yLkS0PVY4KM7:TR?= MYnTRW5ITVJ?
D-336MG M4fSNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmLLTWM2OD1yLkWwN|A1KM7:TR?= MULTRW5ITVJ?
NOS-1 NW\TfW9LT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWr6dmFzUUN3ME2wMlYxPTJ7IN88US=> NF7ye|dUSU6JRWK=
EW-24 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlO1TWM2OD1yLk[yOlk{KM7:TR?= M3jYZXNCVkeHUh?=
BV-173 M1v0fWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1LSVGlEPTB;MD62OVI1QSEQvF2= NHW2S4NUSU6JRWK=
NCCIT MnHQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{f6VGlEPTB;MD63N|IyQCEQvF2= MoXWV2FPT0WU
NCI-H1436 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWjJR|UxRTBwN{mwOFkh|ryP M4X5U3NCVkeHUh?=
BB30-HNC M4C0Umdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXvoZodyUUN3ME2wMlg3OjB|IN88US=> NFTwRYtUSU6JRWK=
TE-8 NHXVTVNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MW\JR|UxRTBwOEeyO|Uh|ryP Mk[1V2FPT0WU
A704 NVXjVHlvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGjOdFBKSzVyPUCuPFkzOSEQvF2= M4jueHNCVkeHUh?=
TK10 MoOzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVzJR|UxRTBwOUC2Olkh|ryP MU\TRW5ITVJ?
KS-1 M2n6Zmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1TqdGlEPTB;MT6xPVc4QSEQvF2= NVTreollW0GQR1XS
C2BBe1 MojwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYHGRZVmUUN3ME2xMlIxPTB5IN88US=> NEPsWWxUSU6JRWK=
RXF393 M3v5Smdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3G2O2lEPTB;MT6yOFM3KM7:TR?= NIGwT29USU6JRWK=
KGN NVPsZZN6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M324VGlEPTB;MT6yO|Y5PyEQvF2= NFmwR|BUSU6JRWK=
NB69 MnK4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXnJR|UxRTFwM{e0PVch|ryP NXL0WXJUW0GQR1XS
TE-11 NXrrW5VmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mm\HTWM2OD1zLkSzOFE5KM7:TR?= MoXNV2FPT0WU
TE-1 NH\QS4xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mor2TWM2OD1zLkS0NVA2KM7:TR?= NYX3SlVWW0GQR1XS
ST486 NX3BSpROT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXnJR|UxRTFwNEW4OVIh|ryP NHHmW4pUSU6JRWK=
HOP-62 M4jZWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MU\JR|UxRTFwNUCyOFYh|ryP NGXIcnVUSU6JRWK=
EW-16 NFTtWFBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVjJR|UxRTFwNUWwPFMh|ryP MXHTRW5ITVJ?
LB1047-RCC M4HOUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1\FWmlEPTB;MT61OVQ2OyEQvF2= NFLSfmhUSU6JRWK=
TE-10 NFjVVFhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MU\JR|UxRTFwNk[yOVIh|ryP MnLVV2FPT0WU
RL95-2 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnrPTWM2OD1zLk[2PVAzKM7:TR?= NUDUd4FIW0GQR1XS
DOHH-2 MlPHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUjIXGRDUUN3ME2xMlcyPzh{IN88US=> M3nIbXNCVkeHUh?=
MFH-ino M{e4Vmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVHJR|UxRTFwN{e4O{DPxE1? NFT0eWdUSU6JRWK=
GB-1 NHKyfnlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NU\JdoN6UUN3ME2xMlc6QDN|IN88US=> NUi4bmRmW0GQR1XS
SK-N-DZ MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NY\XfVV2UUN3ME2xMlg1Pjh6IN88US=> MnTFV2FPT0WU
OS-RC-2 NFyxU5JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkT1TWM2OD1zLki4OVc1KM7:TR?= M3PzZnNCVkeHUh?=
SW982 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFPhPG9KSzVyPUGuPVIxQTNizszN NWDVZoRKW0GQR1XS
KALS-1 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3\5XGlEPTB;MT65PFczOiEQvF2= MX3TRW5ITVJ?
TGBC24TKB NH7Re|NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnGwTWM2OD1{LkC1PVU5KM7:TR?= M2fTZXNCVkeHUh?=
GI-1 MnrVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3rvOWlEPTB;Mj6xOlA5PCEQvF2= NV\CeIdMW0GQR1XS
SW962 NXnmcpJ7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1TPOmlEPTB;Mj6xO|E4QCEQvF2= NVjRNnp7W0GQR1XS
SW872 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NE\qW5pKSzVyPUKuNVg2ODdizszN NEOwcWRUSU6JRWK=
NCI-H747 MkG1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIn6NHZKSzVyPUKuNlU4OTRizszN MVjTRW5ITVJ?
MZ1-PC NUe4bpJPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVO1VFl3UUN3ME2yMlI6OzV4IN88US=> M4nQUXNCVkeHUh?=
MSTO-211H MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M37v[mlEPTB;Mj6zOVczOyEQvF2= M4qwcHNCVkeHUh?=
BL-70 MmTHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIntS5FKSzVyPUKuOFc1OjJizszN M1vT[HNCVkeHUh?=
SW954 NVrIfZB4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4r0d2lEPTB;Mj61O|QxQCEQvF2= M1jBT3NCVkeHUh?=
SNB75 NXe4[IpJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGrVT5FKSzVyPUKuOlg2QTRizszN Mn7mV2FPT0WU
IST-SL2 NELq[JFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoPmTWM2OD1{LkeyN|c6KM7:TR?= MVzTRW5ITVJ?
GCIY MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NILmTFRKSzVyPUKuPFcxODVizszN NFi2VlVUSU6JRWK=
KU812 NES1OWtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mmn1TWM2OD1|LkC1Nlk6KM7:TR?= NXX3TotCW0GQR1XS
LXF-289 M164OWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFjidnVKSzVyPUOuNVIyODlizszN M2jTRXNCVkeHUh?=
ETK-1 NVyyVYFQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{LwOGlEPTB;Mz6yNFc3PyEQvF2= NI\nd2ZUSU6JRWK=
SF126 NYS4PYtCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXTsXFNzUUN3ME2zMlMyOTd2IN88US=> MmDmV2FPT0WU
LC-2-ad MoXTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV3JR|UxRTNwNUW3JO69VQ>? M{TJdHNCVkeHUh?=
KNS-42 NHXUS|NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX;JR|UxRTNwNkWg{txO M4XUNnNCVkeHUh?=
OVCAR-4 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIrGUY9KSzVyPUOuO|M1OzNizszN NVOwOpZnW0GQR1XS
PF-382 NHHzPZNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4PiNmlEPTB;Mz64N|Y6QCEQvF2= MXHTRW5ITVJ?
SH-4 NIKwU3FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYfJR|UxRTRwMkWyOVkh|ryP Mnr2V2FPT0WU
KM12 NE\MXpRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXrJR|UxRTRwM{K0NVYh|ryP M4HuO3NCVkeHUh?=
NB5 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIn6SodKSzVyPUSuOFE5PjRizszN MVnTRW5ITVJ?
KURAMOCHI M{K4U2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnT1TWM2OD12Lk[1NlU3KM7:TR?= NF61RpFUSU6JRWK=
Becker MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH;yb3JKSzVyPUSuOlY1OTZizszN NEXPTWxUSU6JRWK=
MV-4-11 NFu1T3dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3jK[2lEPTB;ND64NVM1PCEQvF2= M4XtSnNCVkeHUh?=
KINGS-1 NWDvcWRpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYPnZpp[UUN3ME20MlgzOzd|IN88US=> MV7TRW5ITVJ?
LS-123 NIToSWRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWLJR|UxRTVwNEm2PFQh|ryP NIHCUodUSU6JRWK=
SF268 MkO0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4\XS2lEPTB;NT62NVI3OiEQvF2= M1vnRXNCVkeHUh?=
A388 NXnDUmpoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmrRTWM2OD13Lk[zOlY4KM7:TR?= NEDEcIlUSU6JRWK=
NMC-G1 NGXSSYNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX3JR|UxRTZwMEG4NVEh|ryP MUHTRW5ITVJ?
CGTH-W-1 Mo\PS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGW1VopKSzVyPU[uNFIxPzVizszN NV63SWFxW0GQR1XS
ES4 NIfqNYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWHPc2ZJUUN3ME22MlU{ODd2IN88US=> MUTTRW5ITVJ?
SR Mo\tS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3zDeGlEPTB;Nj61PFgxPyEQvF2= MknGV2FPT0WU
BB49-HNC NFX0N|NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml7NTWM2OD14LkezNlA3KM7:TR?= NWDHNox4W0GQR1XS
KLE MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFrNO|dKSzVyPU[uO|g{PzdizszN NHruPVlUSU6JRWK=
HUTU-80 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkfKTWM2OD14Lkm4OFY3KM7:TR?= NFnJUWFUSU6JRWK=
SNU-C2B M2LSWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NY\rbWE3UUN3ME23MlgzPzN5IN88US=> NFLqd|ZUSU6JRWK=
BB65-RCC NUTnV4d6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1PhXmlEPTB;Nz65OFkxPCEQvF2= NInTU|BUSU6JRWK=
QIMR-WIL NGrKOoxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkD6TWM2OD16LkSyPFA5KM7:TR?= MXHTRW5ITVJ?
GDM-1 M1zGe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFXDW3pKSzVyPUiuPVczQTJizszN NUjlTYxOW0GQR1XS
LC4-1 NEjiTFFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYK0WJVvUUN3ME25MlAxQTFzIN88US=> MXLTRW5ITVJ?
MLMA MkXQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH3aRZVKSzVyPUmuNVUxODZizszN NUC2TnZ7W0GQR1XS
EoL-1-cell MnTqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmfBTWM2OD17LkOwNVkzKM7:TR?= M2\xZnNCVkeHUh?=
BOKU MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlfGTWM2OD17Lkm2OFY3KM7:TR?= M2O1ZnNCVkeHUh?=
EVSA-T MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MljuTWM2OD1zMD62OVY5KM7:TR?= MnH0V2FPT0WU
D-283MED M{Cwfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYjJR|UxRTFyLkmxO|Yh|ryP MUfTRW5ITVJ?
NB1 NV3XTII{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWKy[|BvUUN3ME2xNU4xOjR{IN88US=> MWLTRW5ITVJ?
RPMI-8402 NYiwcJpiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1vFdWlEPTB;MUGuNVc5KM7:TR?= Moe1V2FPT0WU
NCI-H1355 NYXXOotlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{jYdmlEPTB;MUGuNVgxPiEQvF2= NHW5RWRUSU6JRWK=
NB7 NVu0NXl2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1vhS2lEPTB;MUGuN|I6PyEQvF2= NF3WU2tUSU6JRWK=
RPMI-6666 MnTXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn33TWM2OD1zMj65OVY4KM7:TR?= MlzMV2FPT0WU
697 M1vIZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4jzNGlEPTB;MUOuNlcxOSEQvF2= MV3TRW5ITVJ?
CTB-1 MmLxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYXJR|UxRTF|LkW5OFgh|ryP M321dXNCVkeHUh?=
VA-ES-BJ Mn2xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEnxfJZKSzVyPUGzMlkzOzRizszN NUfaeG56W0GQR1XS
BE-13 MoW2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2f0TmlEPTB;MUSuN|kyPSEQvF2= MljGV2FPT0WU
SKM-1 M3nMPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmXlTWM2OD1zND60OFk6KM7:TR?= MlzCV2FPT0WU
TE-6 Ml7PS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGfpO3ZKSzVyPUG0Mlc2QTFizszN NXjyeWVLW0GQR1XS
LB771-HNC M1XMfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{fheGlEPTB;MUSuO|g6QCEQvF2= M125b3NCVkeHUh?=
ECC4 M{\iR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVS2XZZqUUN3ME2xO{4xOjd5IN88US=> NEm1RYJUSU6JRWK=
ES3 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{fMR2lEPTB;MUeuOFY2PSEQvF2= NIDDVlRUSU6JRWK=
LB647-SCLC M2LjZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYLJR|UxRTF5LkS5OFkh|ryP MkW0V2FPT0WU
NB10 MmDES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2H3[mlEPTB;MUiuOVI2PiEQvF2= MnTJV2FPT0WU
L-540 NWe2[ZpqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWnoOmFIUUN3ME2xPE45OTB7IN88US=> NHyxTHBUSU6JRWK=
NCI-H2126 NIPYcIlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFK0eW1KSzVyPUG5MlUyKM7:TR?= M4C3ZnNCVkeHUh?=
HH NX36c41NT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mm\uTWM2OD1{MD6wNFk6KM7:TR?= MVnTRW5ITVJ?
MPP-89 NH\z[FVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYTENGl3UUN3ME2yN{4zOjh7IN88US=> NYLDSIJVW0GQR1XS
IST-MEL1 NXLsTHk{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV3JR|UxRTJ|Lki2OVgh|ryP M2nzdXNCVkeHUh?=
KP-N-YS M373W2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mlj0TWM2OD1{Mz65NlU2KM7:TR?= M4PEdnNCVkeHUh?=
EC-GI-10 MmHNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3jDeWlEPTB;MkSuOVk5QSEQvF2= M{jwWXNCVkeHUh?=
EKVX NWjEcYVFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUjJR|UxRTJ4LkCyNFMh|ryP MX3TRW5ITVJ?
TGBC1TKB NEToXnNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MonyTWM2OD1{Nj60N|Qh|ryP M2\iTHNCVkeHUh?=
Daudi M2XaZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlrjTWM2OD1{Nz6wO|c{KM7:TR?= MVTTRW5ITVJ?
ALL-PO M3fLdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWrJR|UxRTJ5LkC4NUDPxE1? Mn7NV2FPT0WU
NB6 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXPSbFNwUUN3ME2yO{41QDhizszN M1\adnNCVkeHUh?=
ES6 NXrmd3JOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVXpeZREUUN3ME2yO{46OTJ|IN88US=> Mk\lV2FPT0WU
COLO-320-HSR NWPVT5hPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHrST5FKSzVyPUK4MlA{PzNizszN MkfMV2FPT0WU
K5 M2GxPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEHMR|NKSzVyPUK4MlEzQDdizszN MUXTRW5ITVJ?
ES1 M33E[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV3JR|UxRTJ6Lke3O|Mh|ryP MYrTRW5ITVJ?
LC-1F NFLQZllIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnvzTWM2OD1{OT63N|Q3KM7:TR?= M3jqd3NCVkeHUh?=
SCLC-21H MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWTGZ3NVUUN3ME2zNE44OzF5IN88US=> Mnf2V2FPT0WU
SK-PN-DW MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV3JR|UxRTN{LkW1PVgh|ryP NEXV[JlUSU6JRWK=
D-247MG NIDQbmlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkToTWM2OD1|Mj65O|c{KM7:TR?= MYPTRW5ITVJ?
TE-5 Mnj0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mlj0TWM2OD1|Mz6wN|YzKM7:TR?= MUjTRW5ITVJ?
MONO-MAC-6 MnX4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{LTc2lEPTB;M{OuOVA1QCEQvF2= MUXTRW5ITVJ?
LB2518-MEL NETGc4FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MojqTWM2OD1|Mz63OlY3KM7:TR?= NFPtNpdUSU6JRWK=
LOXIMVI MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M33LXGlEPTB;M{OuO|kzQCEQvF2= M3q3b3NCVkeHUh?=
NCI-H209 MkLnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2\4XmlEPTB;M{WuNVQ1KM7:TR?= NYfIemJYW0GQR1XS
A253 MoeyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWfJR|UxRTN3Lke0Nlkh|ryP NFvucZdUSU6JRWK=
HCC1599 NHzzO5JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmrTTWM2OD1|Nj63NFU{KM7:TR?= NXG0bno2W0GQR1XS
EB-3 M2ThbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mm\zTWM2OD1|Nj65OVE5KM7:TR?= MkDDV2FPT0WU
GOTO NVfVfXNrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1nNS2lEPTB;M{euN|IzPCEQvF2= M3:zdHNCVkeHUh?=
SW684 NFnIcpVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVPJR|UxRTRzLki0PVUh|ryP NUWzZ3pRW0GQR1XS
DEL NYTpd3d5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{jwWGlEPTB;NEKuNFUzOiEQvF2= MXzTRW5ITVJ?
HT-144 Mn;NS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2DI[WlEPTB;NEKuNVY4PiEQvF2= NYfQc49mW0GQR1XS
TE-9 NUL1[ZhvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYHJR|UxRTR|LkS1PVYh|ryP MVrTRW5ITVJ?
KARPAS-45 MkjKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkHYTWM2OD12ND6zPVI2KM7:TR?= NHPLe5RUSU6JRWK=
HAL-01 NIPpRpdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV:weXpQUUN3ME20OE42ODN2IN88US=> Ml;ZV2FPT0WU
RCC10RGB M2r5UWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVrJR|UxRTR2LkezPVIh|ryP MkDKV2FPT0WU
CP67-MEL NUnNfGdrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{f5ZWlEPTB;NEWuOlI1OSEQvF2= NHP5[mVUSU6JRWK=
NB17 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MY\JR|UxRTR3Lk[2OFMh|ryP MlX1V2FPT0WU
SK-UT-1 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGXzdnNKSzVyPUS1Mlk1PjRizszN MUHTRW5ITVJ?
JiyoyeP-2003 NUW3eZUzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWXJR|UxRTR4LkCxNVkh|ryP NVPEUYdXW0GQR1XS
HCE-4 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV\JR|UxRTR4LkW5Olgh|ryP NUDV[mVvW0GQR1XS
NCI-H720 NXfwepZIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2r6V2lEPTB;NE[uO|Y5OiEQvF2= M1PtV3NCVkeHUh?=
KARPAS-422 MlOzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlTYTWM2OD12Nz6wPFk2KM7:TR?= M3rhT3NCVkeHUh?=
Ramos-2G6-4C10 M3rZfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXTJR|UxRTR5LkG2NlIh|ryP NHziNJBUSU6JRWK=
HCE-T MnThS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWjFcm1OUUN3ME20O{43QDJ6IN88US=> NFX6T4pUSU6JRWK=
PSN1 M3;sWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXuyd3hyUUN3ME20O{44QDF|IN88US=> MUfTRW5ITVJ?

... 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]
+ Expand

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]
+ Expand
  • 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]
+ Expand
  • 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

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Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

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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)

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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:

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Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

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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

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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

selleck catalog

Src Signaling Pathway Map

Src Inhibitors with Unique Features

  • Most Potent Src Inhibitor

    Dasatinib : Src, IC50=0.8 nM.

  • FDA-approved Src Inhibitor

    Bosutinib (SKI-606) : Approved by FDA for Ph+ chronic myelogenous leukemia (CML).

  • Newest Src Inhibitor

    PP1 : Potent and selective Src inhibitor for Lck/Fyn with IC50 of 5 nM/ 6 nM.

  • Classic Src Inhibitor

    KX2-391 : The first clinical Src inhibitor (peptidomimetic class) that targets the peptide substrate site of Src, with GI50 of 9-60 nM in cancer cell lines.

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  • PX-478 2HCl New

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  • Bosutinib (SKI-606)

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  • Dasatinib

    Dasatinib is a novel, potent and multi-targeted inhibitor that targets Abl, Src and c-Kit, with IC50 of <1 nM, 0.8 nM and 79 nM in cell-free assays, respectively.

  • KX2-391

    KX2-391, the first clinical Src inhibitor (peptidomimetic class) that targets the peptide substrate site of Src, with GI50 of 9-60 nM in cancer cell lines. Phase 2.

  • PP1

    PP1 is a potent and selective Src inhibitor for Lck/Fyn with IC50 of 5 nM/ 6 nM.

  • PP2

    PP2, a Src family kinase inhibitor, potently inhibits Lck/Fyn with IC50 of 4 nM/5 nM in cell-free assays, ~100-fold less potent to EGFR, inactive for ZAP-70, JAK2 and PKA.

  • WH-4-023

    WH-4-023 is a potent and orally active Lck/Src inhibitor with IC50s of 2 nM and 6 nM in cell-free assays, respectively. Exhibits >300-fold selectivity against p38α and KDR. Also potently inhibits SIK (IC50 values are 10, 22 and 60 nM for SIK 1, 2 and 3 respectively) and displays selectivity over a range of closely related kinases.

  • Ibrutinib (PCI-32765)

    Ibrutinib (PCI-32765) is a potent and highly selective Brutons tyrosine kinase (Btk) inhibitor with IC50 of 0.5 nM in cell-free assays, modestly potent to Bmx, CSK, FGR, BRK, HCK, less potent to EGFR, Yes, ErbB2, JAK3, etc.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID