Saracatinib (AZD0530) 化学構造
分子量: 542.03

高品質保証

文献中の引用(35)

カスタマーフィードバック(8)

Quality Control & MSDS

製品説明

  • Compare Src Inhibitors
    Src製品生物活性の比較
  • 研究分野
  • Combination Therapy
    併用療法
  • Saracatinib (AZD0530)のメカニズム

製品の説明

生物活性

製品説明 Saracatinib(AZD0530)は、c-SrcのためのSrc阻害剤で、IC50 が2.7 nMです。
ターゲット c-Src v-Abl
IC50 2.7 nM 30 nM [1]
In vitro試験 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 LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
CTV-1 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MU\JR|UxRTBwME[xOFMh|ryP MmrMV2FPT0WU
LAMA-84 M4DkRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn\MTWM2OD1yLkG1PVkh|ryP NVLGV5JQW0GQR1XS
MEG-01 NFq4TZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX7JR|UxRTBwMkO2PFgh|ryP M1LxZnNCVkeHUh?=
EM-2 MnHNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX\JR|UxRTBwMk[1JO69VQ>? MoPPV2FPT0WU
TE-15 MlvTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYHJR|UxRTBwMke0NVIh|ryP NUXPN2FYW0GQR1XS
NCI-H1648 NInTZnZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXHCWnhvUUN3ME2wMlI5OTF4IN88US=> Mnf5V2FPT0WU
TE-12 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXXqRXJoUUN3ME2wMlMzPjhizszN MWHTRW5ITVJ?
LB996-RCC NFHPNGhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVnJR|UxRTBwNESxPVYh|ryP MXTTRW5ITVJ?
K-562 MnHsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVPLNZdlUUN3ME2wMlQ1QTZ5IN88US=> MoW3V2FPT0WU
D-336MG MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn3CTWM2OD1yLkWwN|A1KM7:TR?= MmjGV2FPT0WU
NOS-1 NHnzR3RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFXvOYFKSzVyPUCuOlA2OjlizszN NXTmWIdoW0GQR1XS
EW-24 MoLsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVjJR|UxRTBwNkK2PVMh|ryP NGrz[GdUSU6JRWK=
BV-173 NGXZW25Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkC1TWM2OD1yLk[1NlQ6KM7:TR?= MYTTRW5ITVJ?
NCCIT MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2nxdWlEPTB;MD63N|IyQCEQvF2= MnO2V2FPT0WU
NCI-H1436 NUXhcVhtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGP2d3FKSzVyPUCuO|kxPDlizszN MVjTRW5ITVJ?
BB30-HNC MmjES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2rYV2lEPTB;MD64OlIxOyEQvF2= MWXTRW5ITVJ?
TE-8 MoXLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NITCZ5pKSzVyPUCuPFczPzVizszN M3vUVHNCVkeHUh?=
A704 NXTUdHJyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYSzS3lxUUN3ME2wMlg6OjFizszN M2i0OXNCVkeHUh?=
TK10 M33lT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYPOeYh5UUN3ME2wMlkxPjZ7IN88US=> MmHmV2FPT0WU
KS-1 MnfGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVTiblhwUUN3ME2xMlE6Pzd7IN88US=> M2DaXXNCVkeHUh?=
C2BBe1 NWK1TGZwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGrNWlNKSzVyPUGuNlA2ODdizszN MnPEV2FPT0WU
RXF393 NWrCXlNCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2ThRmlEPTB;MT6yOFM3KM7:TR?= NV;kTJVsW0GQR1XS
KGN NVPORpNGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1\pZmlEPTB;MT6yO|Y5PyEQvF2= M1nSSXNCVkeHUh?=
NB69 NHjJXoNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHLN[FRKSzVyPUGuN|c1QTdizszN NH7pfY9USU6JRWK=
TE-11 NWW4VWNKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NELTcXJKSzVyPUGuOFM1OThizszN NWHSNlZ2W0GQR1XS
TE-1 NFTjVmhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVjjXFQzUUN3ME2xMlQ1OTB3IN88US=> MkDjV2FPT0WU
ST486 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmnhTWM2OD1zLkS1PFUzKM7:TR?= M1[xc3NCVkeHUh?=
HOP-62 NVPsc|FnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYjJR|UxRTFwNUCyOFYh|ryP MVLTRW5ITVJ?
EW-16 NUj4dppLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnTvTWM2OD1zLkW1NFg{KM7:TR?= Mm\BV2FPT0WU
LB1047-RCC M2XoUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{\qRWlEPTB;MT61OVQ2OyEQvF2= Mk\QV2FPT0WU
TE-10 NGO5c25Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1rZWmlEPTB;MT62OlI2OiEQvF2= NHflbWxUSU6JRWK=
RL95-2 M{LuWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mk\TTWM2OD1zLk[2PVAzKM7:TR?= MkTiV2FPT0WU
DOHH-2 MmPsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3T6e2lEPTB;MT63NVc5OiEQvF2= NXHDN5hJW0GQR1XS
MFH-ino NFzE[mRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFPsWpNKSzVyPUGuO|c5PyEQvF2= M2XEVnNCVkeHUh?=
GB-1 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1r3ZmlEPTB;MT63PVg{OyEQvF2= MnXVV2FPT0WU
SK-N-DZ M3vKd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M372U2lEPTB;MT64OFY5QCEQvF2= MlPtV2FPT0WU
OS-RC-2 NV\hWI5sT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnXOTWM2OD1zLki4OVc1KM7:TR?= NVvRfWJkW0GQR1XS
SW982 NGPJTm9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYDkO4JzUUN3ME2xMlkzODl|IN88US=> MYrTRW5ITVJ?
KALS-1 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1zUb2lEPTB;MT65PFczOiEQvF2= M1HaNHNCVkeHUh?=
TGBC24TKB NFXKNZhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFPF[2JKSzVyPUKuNFU6PThizszN MWHTRW5ITVJ?
GI-1 NWjLdIV6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXzJR|UxRTJwMU[wPFQh|ryP MWrTRW5ITVJ?
SW962 MnruS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXyyendpUUN3ME2yMlE4OTd6IN88US=> M{HMd3NCVkeHUh?=
SW872 NHf4UlhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVLJR|UxRTJwMUi1NFch|ryP NHi3VFJUSU6JRWK=
NCI-H747 MkPqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3HzXGlEPTB;Mj6yOVcyPCEQvF2= NX3RNHR6W0GQR1XS
MZ1-PC M37JV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2m4cmlEPTB;Mj6yPVM2PiEQvF2= NH:yOXlUSU6JRWK=
MSTO-211H MmewS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHnXbYRKSzVyPUKuN|U4OjNizszN Mln6V2FPT0WU
BL-70 M2O4eGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGmwempKSzVyPUKuOFc1OjJizszN NEPLR4ZUSU6JRWK=
SW954 NHzPU49Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWnOOYkzUUN3ME2yMlU4PDB6IN88US=> M3no[nNCVkeHUh?=
SNB75 M1LKRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFXJb3FKSzVyPUKuOlg2QTRizszN NXfndZE1W0GQR1XS
IST-SL2 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NE[0cJhKSzVyPUKuO|I{PzlizszN MVLTRW5ITVJ?
GCIY MmC3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUL3c|lxUUN3ME2yMlg4ODB3IN88US=> Mmq4V2FPT0WU
KU812 Ml;aS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVHJR|UxRTNwMEWyPVkh|ryP MmHjV2FPT0WU
LXF-289 M1zNN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYPJR|UxRTNwMUKxNFkh|ryP Mn7yV2FPT0WU
ETK-1 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGXqdHBKSzVyPUOuNlA4PjdizszN M4HTUnNCVkeHUh?=
SF126 MmL2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYDwSmdUUUN3ME2zMlMyOTd2IN88US=> M4\MeXNCVkeHUh?=
LC-2-ad NXSyN3o3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NE\tNFVKSzVyPUOuOVU4KM7:TR?= M1PN[XNCVkeHUh?=
KNS-42 NFnnSI5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVLDfJBwUUN3ME2zMlY2KM7:TR?= MVvTRW5ITVJ?
OVCAR-4 MmG0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIrNVYlKSzVyPUOuO|M1OzNizszN M3X1b3NCVkeHUh?=
PF-382 MonhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoPnTWM2OD1|LkizOlk5KM7:TR?= NVThVmMxW0GQR1XS
SH-4 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYXJR|UxRTRwMkWyOVkh|ryP M4L0eXNCVkeHUh?=
KM12 M1\CWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVvJR|UxRTRwM{K0NVYh|ryP NV\6Z5l{W0GQR1XS
NB5 NVvJd|VIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXjMN5Z3UUN3ME20MlQyQDZ2IN88US=> MlfhV2FPT0WU
KURAMOCHI NXzNNWdiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3\1T2lEPTB;ND62OVI2PiEQvF2= MnHwV2FPT0WU
Becker MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1PqRWlEPTB;ND62OlQyPiEQvF2= MmnLV2FPT0WU
MV-4-11 NImxXHVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MljVTWM2OD12LkixN|Q1KM7:TR?= NX[zeHE3W0GQR1XS
KINGS-1 MmHLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWTJR|UxRTRwOEKzO|Mh|ryP MmrMV2FPT0WU
LS-123 M1X0Zmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MY\JR|UxRTVwNEm2PFQh|ryP MkLNV2FPT0WU
SF268 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2fsOGlEPTB;NT62NVI3OiEQvF2= M1Hqe3NCVkeHUh?=
A388 M{fwdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3TDVGlEPTB;NT62N|Y3PyEQvF2= NXzwR4x7W0GQR1XS
NMC-G1 NHXaTlZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIfabY5KSzVyPU[uNFE5OTFizszN MkK4V2FPT0WU
CGTH-W-1 NHOxSFNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHrTd4JKSzVyPU[uNFIxPzVizszN NYTDbVZIW0GQR1XS
ES4 M3HpbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4PHNGlEPTB;Nj61N|A4PCEQvF2= M{OzOHNCVkeHUh?=
SR MlXtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn34TWM2OD14LkW4PFA4KM7:TR?= NGnQ[2JUSU6JRWK=
BB49-HNC Mmi0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1L3NGlEPTB;Nj63N|IxPiEQvF2= NWW5VW9yW0GQR1XS
KLE Mom2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NY\qOYQ1UUN3ME22Mlc5Ozd5IN88US=> NEf5W|NUSU6JRWK=
HUTU-80 Mn;NS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXXJR|UxRTZwOUi0OlYh|ryP MWrTRW5ITVJ?
SNU-C2B MonYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnLzTWM2OD15LkiyO|M4KM7:TR?= NFXmO5RUSU6JRWK=
BB65-RCC NHjJd5BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH3ieGxKSzVyPUeuPVQ6ODRizszN MmfrV2FPT0WU
QIMR-WIL MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVPVRldpUUN3ME24MlQzQDB6IN88US=> NF7CTXlUSU6JRWK=
GDM-1 M2Xp[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIK5UmhKSzVyPUiuPVczQTJizszN NGjBZmpUSU6JRWK=
LC4-1 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3jGV2lEPTB;OT6wNFkyOSEQvF2= NH:0XmxUSU6JRWK=
MLMA M17TUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX3kOnVzUUN3ME25MlE2ODB4IN88US=> M3v5XXNCVkeHUh?=
EoL-1-cell MmfhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUPJR|UxRTlwM{CxPVIh|ryP MW\TRW5ITVJ?
BOKU M4XCXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2mwWWlEPTB;OT65OlQ3PiEQvF2= NV;VeGt4W0GQR1XS
EVSA-T NILjXopIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWjQc|A1UUN3ME2xNE43PTZ6IN88US=> M3vkVHNCVkeHUh?=
D-283MED Mk\sS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2LSeGlEPTB;MUCuPVE4PiEQvF2= M3LBXHNCVkeHUh?=
NB1 NFnWW5BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkHCTWM2OD1zMT6wNlQzKM7:TR?= MofYV2FPT0WU
RPMI-8402 MlnDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWrJR|UxRTFzLkG3PEDPxE1? NU[yfllmW0GQR1XS
NCI-H1355 M3rQfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUjJR|UxRTFzLkG4NFYh|ryP NGjkW4tUSU6JRWK=
NB7 NFTUNFFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFvsPYlKSzVyPUGxMlMzQTdizszN MVTTRW5ITVJ?
RPMI-6666 NWOzd4ZZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2DzPWlEPTB;MUKuPVU3PyEQvF2= M4SwdnNCVkeHUh?=
697 MoPmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{HaPGlEPTB;MUOuNlcxOSEQvF2= MoLFV2FPT0WU
CTB-1 NIO1eJVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkLWTWM2OD1zMz61PVQ5KM7:TR?= M{HGRXNCVkeHUh?=
VA-ES-BJ NUXwOHRrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3nYWWlEPTB;MUOuPVI{PCEQvF2= MXTTRW5ITVJ?
BE-13 MoTZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmTsTWM2OD1zND6zPVE2KM7:TR?= MkHNV2FPT0WU
SKM-1 NG\FOllIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUfJR|UxRTF2LkS0PVkh|ryP NYq5bGpFW0GQR1XS
TE-6 MkX6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUf3O3Q5UUN3ME2xOE44PTlzIN88US=> Mm[xV2FPT0WU
LB771-HNC NXLSOYlKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUjGXVgzUUN3ME2xOE44QDl6IN88US=> NGnmVZlUSU6JRWK=
ECC4 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmTtTWM2OD1zNz6wNlc4KM7:TR?= MVLTRW5ITVJ?
ES3 MlrpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXPJR|UxRTF5LkS2OVUh|ryP MnTDV2FPT0WU
LB647-SCLC MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXTBU|VjUUN3ME2xO{41QTR7IN88US=> NVqyW5FYW0GQR1XS
NB10 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1qyT2lEPTB;MUiuOVI2PiEQvF2= NWCxbmN5W0GQR1XS
L-540 M2rKZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1npOmlEPTB;MUiuPFExQSEQvF2= M3iwOnNCVkeHUh?=
NCI-H2126 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWnJR|UxRTF7LkWxJO69VQ>? MVLTRW5ITVJ?
HH MkHRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MljTTWM2OD1{MD6wNFk6KM7:TR?= NXrEW5pNW0GQR1XS
MPP-89 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mm\sTWM2OD1{Mz6yNlg6KM7:TR?= Mn\vV2FPT0WU
IST-MEL1 NXGxXoZ7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3\HXGlEPTB;MkOuPFY2QCEQvF2= MkHvV2FPT0WU
KP-N-YS NUXrPHc6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3Hk[WlEPTB;MkOuPVI2PSEQvF2= NHLCSmFUSU6JRWK=
EC-GI-10 NVPxZ4trT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVLjWlJiUUN3ME2yOE42QTh7IN88US=> MVXTRW5ITVJ?
EKVX MmLmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIDvfI1KSzVyPUK2MlAzODNizszN MYPTRW5ITVJ?
TGBC1TKB NIDxUmpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3vGbmlEPTB;Mk[uOFM1KM7:TR?= MVPTRW5ITVJ?
Daudi NYrVWW97T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{H4O2lEPTB;MkeuNFc4OyEQvF2= NHvyeGFUSU6JRWK=
ALL-PO M{GzSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHzWR3NKSzVyPUK3MlA5OSEQvF2= MlOzV2FPT0WU
NB6 MkfRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M174eGlEPTB;MkeuOFg5KM7:TR?= M2fHe3NCVkeHUh?=
ES6 M37zOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVmzTGlCUUN3ME2yO{46OTJ|IN88US=> MVvTRW5ITVJ?
COLO-320-HSR Ml\YS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYXJR|UxRTJ6LkCzO|Mh|ryP MknqV2FPT0WU
K5 NXvBXWJRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVPJR|UxRTJ6LkGyPFch|ryP MX;TRW5ITVJ?
ES1 Mn\5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV7qXpVxUUN3ME2yPE44Pzd|IN88US=> MmjQV2FPT0WU
LC-1F NFriXWZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX7iPIlJUUN3ME2yPU44OzR4IN88US=> M4f2PHNCVkeHUh?=
SCLC-21H MoC1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4f6VGlEPTB;M{CuO|MyPyEQvF2= NHu1N3pUSU6JRWK=
SK-PN-DW NV;Hd45mT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1\sRWlEPTB;M{KuOVU6QCEQvF2= MUjTRW5ITVJ?
D-247MG MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1\xVGlEPTB;M{KuPVc4OyEQvF2= NXLxTJFKW0GQR1XS
TE-5 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MULJR|UxRTN|LkCzOlIh|ryP M4HxfXNCVkeHUh?=
MONO-MAC-6 NYjNNo5wT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVjHXlEyUUN3ME2zN{42ODR6IN88US=> MU\TRW5ITVJ?
LB2518-MEL M{PUSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUXJR|UxRTN|Lke2OlYh|ryP NGS2cHNUSU6JRWK=
LOXIMVI NILQW2dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUPJR|UxRTN|Lke5Nlgh|ryP MUfTRW5ITVJ?
NCI-H209 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYLCeplnUUN3ME2zOU4yPDRizszN NIDBV29USU6JRWK=
A253 NFPVXJBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUDnTlJ{UUN3ME2zOU44PDJ7IN88US=> M1GzUHNCVkeHUh?=
HCC1599 NFvrWFNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NITofmdKSzVyPUO2MlcxPTNizszN NF31bnZUSU6JRWK=
EB-3 M4m3eGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVGyUHJbUUN3ME2zOk46PTF6IN88US=> Mk\UV2FPT0WU
GOTO MnfVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4LDV2lEPTB;M{euN|IzPCEQvF2= M{S4WXNCVkeHUh?=
SW684 MnfyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn7ITWM2OD12MT64OFk2KM7:TR?= M{jtcHNCVkeHUh?=
DEL MkHES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlTsTWM2OD12Mj6wOVIzKM7:TR?= MUPTRW5ITVJ?
HT-144 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHjoTFRKSzVyPUSyMlE3PzZizszN NGjSWlZUSU6JRWK=
TE-9 NFTMfWVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUPJR|UxRTR|LkS1PVYh|ryP M{DIWHNCVkeHUh?=
KARPAS-45 MlTTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4L2fmlEPTB;NESuN|kzPSEQvF2= MnTHV2FPT0WU
HAL-01 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXjJR|UxRTR2LkWwN|Qh|ryP MXzTRW5ITVJ?
RCC10RGB MonKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M130eWlEPTB;NESuO|M6OiEQvF2= Ml[2V2FPT0WU
CP67-MEL MojyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFHQVJRKSzVyPUS1MlYzPDFizszN M4jBO3NCVkeHUh?=
NB17 NG\zeFZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVL6dmkxUUN3ME20OU43PjR|IN88US=> NIXCTIRUSU6JRWK=
SK-UT-1 NWX1dIpJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnnsTWM2OD12NT65OFY1KM7:TR?= NEH0R2dUSU6JRWK=
JiyoyeP-2003 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mk\mTWM2OD12Nj6wNVE6KM7:TR?= M2jHN3NCVkeHUh?=
HCE-4 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1eyb2lEPTB;NE[uOVk3QCEQvF2= Ml7GV2FPT0WU
NCI-H720 NH2wR4pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYPJR|UxRTR4Lke2PFIh|ryP NXvIZlR{W0GQR1XS
KARPAS-422 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXGzOoNCUUN3ME20O{4xQDl3IN88US=> M3TEWXNCVkeHUh?=
Ramos-2G6-4C10 NHXuRm1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHTYRZFKSzVyPUS3MlE3OjJizszN NHj0dmRUSU6JRWK=
HCE-T M1nJUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2D1emlEPTB;NEeuOlgzQCEQvF2= MkjPV2FPT0WU
PSN1 NXPaXIpST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{nNPGlEPTB;NEeuO|gyOyEQvF2= MV\TRW5ITVJ?

... Click to View More Cell Line Experimental Data

In vivo試験 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]
臨床試験 Saracatinib is currently in Phase II clinical trial in recurrent osteosarcoma localized to the lung.
特集 The 1st Src inhibitor to show inhibition of the Src pathway in human tumor tissue.

プロトコル (参考用のみ)

キナーゼアッセイ: [1]

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.

細胞アッセイ: [1]

細胞株 PC3, DU145, CWR22Rv1, LNCaP, LAPC-4, PZ-HPV7 and RWPE-1 cells
濃度 62.5 nM - 16 mM
反応時間 1, 3 and 5 days
実験の流れ 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

動物実験: [1]

動物モデル CB17 mice are implanted with DU145 cells.
製剤 Dissolved in 0.5% hydroxypropyl methylcellulose, 0.1% Tween 80
投薬量 25 mg/kg
投与方法 Orally administered daily

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDogMonkeyBaboon
Weight (kg)0.020.151.80.40.0810312
Body Surface Area (m2)0.0070.0250.150.050.020.50.240.6
Km factor361285201220
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

参考

化学情報

Download Saracatinib (AZD0530) SDF
分子量 542.03
化学式

C27H32ClN5O5

CAS No. 379231-04-6
保管 2年-20℃
6月-80℃in solvent
別名 N/A
溶解度 (25°C) * In vitro DMSO 35 mg/mL warming (64.57 mM)
エタノール 31 mg/mL (57.19 mM)
<1 mg/mL (<1 mM)
In vivo 2% DMSO+30% PEG 300+ddH2O 5mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* 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.
化学名 N-(5-chlorobenzo[d][1,3]dioxol-4-yl)-7-(2-(4-methylpiperazin-1-yl)ethoxy)-5-(tetrahydro-2H-pyran-4-yloxy)quinazolin-4-amine

文献中の引用 (35)

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

技術サポート&よくある質問(FAQ)

ストックの作り方、阻害剤の保管する方法、細胞実験や動物実験に注意すべきな点を全部含めており、製品を取扱う時よくあった質問に対して取扱説明書でお答えいたします。

電話番号: +1-832-582-8158 Ext:3月曜日〜金曜日 9:00 AM–5:00 PM (米国中部標準時)

他の質問がある場合は、お気軽くお問合せください。

* 必須

Related Src 阻害剤

  • Dasatinib Monohydrate

    Dasatinib Monohydrate 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, respectively.

  • SU6656

    SU 6656 is a selective Src family kinase inhibitor with IC50 of 280 nM, 20 nM, 130 nM, and 170 nM for Src, Yes, Lyn, and Fyn, respectively.

  • PX-478 2HCl

    PX-478 2HCl is an orally active, and selective hypoxia-inducible factor-1α (HIF-1α) inhibitor. Phase 1.

  • Defactinib (VS-6063, PF-04554878)

    Defactinib (VS-6063, PF-04554878) is a selective, and orally active FAK inhibitor. Phase 2.

  • Bosutinib (SKI-606)

    Bosutinib(SKI-606)はそれぞれ1.2nMと1nMのIC50値による新しい二重Sarcoma/アベルソン(Src/Abl)チロシン・キナーゼ阻害剤です。

  • Dasatinib

    Dasatinib は、野生型ablとSrcのためのSrc/abl阻害剤で、IC50 がそれぞれ 0.6 nM と 0.8 nMです。

  • KX2-391

    KX2-391は、Srcのサブストレート結合部位を目標とする非常に選択的な非ATP Srcキナーゼ阻害剤で、Srcの高水準を表すガン細胞線で、非常に強い反増殖的な活性を示します。

  • PP1

    PP1は、Lck/Fynのための強力で選択的なSrc阻害剤で、IC50 が 5 nM/ 6 nMです。

  • PP2

    PP2は、Src キナーゼ阻害剤で、GST-Src活動を強力に禁止します。

最近チェックしたアイテム

Tags: Saracatinib (AZD0530)を買う | Saracatinib (AZD0530)供給者 | Saracatinib (AZD0530)を購入する | Saracatinib (AZD0530)費用 | Saracatinib (AZD0530)生産者 | オーダーSaracatinib (AZD0530) | Saracatinib (AZD0530)代理店
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
お問い合わせ