Saracatinib (AZD0530) 化学構造
分子量: 542.03

高品質保証

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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 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWLkb2w4UUN3ME2wMlA3OTR|IN88US=> NFX4[lVUSU6JRWK=
LAMA-84 MkDwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWnJR|UxRTBwMUW5PUDPxE1? MnWyV2FPT0WU
MEG-01 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2LrWmlEPTB;MD6yN|Y5QCEQvF2= NH22fHNUSU6JRWK=
EM-2 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX3JR|UxRTBwMk[1JO69VQ>? NHXhRlhUSU6JRWK=
TE-15 NY\ofY5NT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV7JR|UxRTBwMke0NVIh|ryP MX\TRW5ITVJ?
NCI-H1648 NH[zfnRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{\HemlEPTB;MD6yPFEyPiEQvF2= MofrV2FPT0WU
TE-12 MlPuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEXVfIhKSzVyPUCuN|I3QCEQvF2= MmjmV2FPT0WU
LB996-RCC MlX2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3Py[WlEPTB;MD60OFE6PiEQvF2= NFjNVodUSU6JRWK=
K-562 M{S1SGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUnJR|UxRTBwNES5Olch|ryP MYLTRW5ITVJ?
D-336MG M4XPSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2rlemlEPTB;MD61NFMxPCEQvF2= MkTTV2FPT0WU
NOS-1 MmXmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mo\5TWM2OD1yLk[wOVI6KM7:TR?= M4DKfXNCVkeHUh?=
EW-24 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV;JR|UxRTBwNkK2PVMh|ryP NEDPSnpUSU6JRWK=
BV-173 M3zEdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVvJR|UxRTBwNkWyOFkh|ryP MVjTRW5ITVJ?
NCCIT NEHVRVRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH[3VFZKSzVyPUCuO|MzOThizszN MkWzV2FPT0WU
NCI-H1436 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYnJR|UxRTBwN{mwOFkh|ryP MXPTRW5ITVJ?
BB30-HNC Ml7IS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWXJR|UxRTBwOE[yNFMh|ryP MmLnV2FPT0WU
TE-8 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{LLemlEPTB;MD64O|I4PSEQvF2= MWTTRW5ITVJ?
A704 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3zq[mlEPTB;MD64PVIyKM7:TR?= MlXMV2FPT0WU
TK10 NYfGdos{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoLXTWM2OD1yLkmwOlY6KM7:TR?= M3;WN3NCVkeHUh?=
KS-1 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIj2eoNKSzVyPUGuNVk4PzlizszN NWPPSlJLW0GQR1XS
C2BBe1 NFTPe25Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3ey[WlEPTB;MT6yNFUxPyEQvF2= NY\HSYZ4W0GQR1XS
RXF393 Mn;OS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M33hbWlEPTB;MT6yOFM3KM7:TR?= NF;PfFJUSU6JRWK=
KGN M3rDOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1XURmlEPTB;MT6yO|Y5PyEQvF2= MkLrV2FPT0WU
NB69 MlvUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYXJR|UxRTFwM{e0PVch|ryP NXXnTFN4W0GQR1XS
TE-11 NF6zZlVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYfJR|UxRTFwNEO0NVgh|ryP MknqV2FPT0WU
TE-1 NELzNllIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYfJR|UxRTFwNESxNFUh|ryP M4rR[HNCVkeHUh?=
ST486 NILPTHVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M33RRWlEPTB;MT60OVg2OiEQvF2= NH7SdFdUSU6JRWK=
HOP-62 M4fxT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXm0TZhJUUN3ME2xMlUxOjR4IN88US=> NITOUFdUSU6JRWK=
EW-16 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4izb2lEPTB;MT61OVA5OyEQvF2= MUjTRW5ITVJ?
LB1047-RCC MlPvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIjsOohKSzVyPUGuOVU1PTNizszN M2nKSnNCVkeHUh?=
TE-10 NYXrb|dnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVvJR|UxRTFwNk[yOVIh|ryP NFfQ[|RUSU6JRWK=
RL95-2 MmTZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3rjS2lEPTB;MT62OlkxOiEQvF2= MlzEV2FPT0WU
DOHH-2 NGPlZoFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1i2fGlEPTB;MT63NVc5OiEQvF2= MUjTRW5ITVJ?
MFH-ino M1m0Wmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWLJR|UxRTFwN{e4O{DPxE1? NX\T[WRZW0GQR1XS
GB-1 NGfHWI9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYH3TJB[UUN3ME2xMlc6QDN|IN88US=> NIfkPWNUSU6JRWK=
SK-N-DZ MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlPBTWM2OD1zLki0Olg5KM7:TR?= MVvTRW5ITVJ?
OS-RC-2 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M36wb2lEPTB;MT64PFU4PCEQvF2= MnX4V2FPT0WU
SW982 Mo\ES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHPE[4dKSzVyPUGuPVIxQTNizszN NVrGVphVW0GQR1XS
KALS-1 M2fBVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYm3WW5QUUN3ME2xMlk5PzJ{IN88US=> NF\rPJFUSU6JRWK=
TGBC24TKB MnXsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH7xO3JKSzVyPUKuNFU6PThizszN NWTP[5JZW0GQR1XS
GI-1 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3jQWGlEPTB;Mj6xOlA5PCEQvF2= MoPzV2FPT0WU
SW962 MmHMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYnJR|UxRTJwMUexO|gh|ryP Mkm4V2FPT0WU
SW872 NVnYNGZGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4XNWGlEPTB;Mj6xPFUxPyEQvF2= NIS4[mNUSU6JRWK=
NCI-H747 M4fqbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGDnbVhKSzVyPUKuNlU4OTRizszN NWjOelV7W0GQR1XS
MZ1-PC NVS0dIpvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1ToZ2lEPTB;Mj6yPVM2PiEQvF2= M1fHTHNCVkeHUh?=
MSTO-211H NYjqeIxPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MojhTWM2OD1{LkO1O|I{KM7:TR?= MoD0V2FPT0WU
BL-70 NHPmcGpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVXjdYxQUUN3ME2yMlQ4PDJ{IN88US=> NE[zcYRUSU6JRWK=
SW954 NWPI[HI2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUjJR|UxRTJwNUe0NFgh|ryP NWfQRXlEW0GQR1XS
SNB75 M{T2e2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn\VTWM2OD1{Lk[4OVk1KM7:TR?= M2LncXNCVkeHUh?=
IST-SL2 Ml\BS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH20bWVKSzVyPUKuO|I{PzlizszN M2XYfHNCVkeHUh?=
GCIY NYmwVFg{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYPJR|UxRTJwOEewNFUh|ryP M1jBc3NCVkeHUh?=
KU812 MlLaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHjFcFVKSzVyPUOuNFUzQTlizszN Mmn2V2FPT0WU
LXF-289 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3fqSmlEPTB;Mz6xNlExQSEQvF2= NH7zc4pUSU6JRWK=
ETK-1 MlvxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGftPXJKSzVyPUOuNlA4PjdizszN Ml\iV2FPT0WU
SF126 M{DseWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3q3c2lEPTB;Mz6zNVE4PCEQvF2= NIHvbVNUSU6JRWK=
LC-2-ad MlzrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX:3b5VyUUN3ME2zMlU2PyEQvF2= NELyOWxUSU6JRWK=
KNS-42 MljiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkToTWM2OD1|Lk[1JO69VQ>? MmnBV2FPT0WU
OVCAR-4 M{XEWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoDBTWM2OD1|LkezOFM{KM7:TR?= MVjTRW5ITVJ?
PF-382 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{nQNGlEPTB;Mz64N|Y6QCEQvF2= NHnQVWVUSU6JRWK=
SH-4 MlvmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUDlSpNFUUN3ME20MlI2OjV7IN88US=> NWfMWlhSW0GQR1XS
KM12 NUnle3dlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{DRcmlEPTB;ND6zNlQyPiEQvF2= MXrTRW5ITVJ?
NB5 NUH0OmY6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYXJR|UxRTRwNEG4OlQh|ryP NXjteZVPW0GQR1XS
KURAMOCHI M1rSN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF\6VGhKSzVyPUSuOlUzPTZizszN NUXZenhTW0GQR1XS
Becker M3H1PWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWXQXmhXUUN3ME20MlY3PDF4IN88US=> NIXZcWRUSU6JRWK=
MV-4-11 MnWyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUjnU2xnUUN3ME20MlgyOzR2IN88US=> M124ZXNCVkeHUh?=
KINGS-1 MlS3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mo\DTWM2OD12LkiyN|c{KM7:TR?= NEK1XXNUSU6JRWK=
LS-123 M4XDemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUnZ[XlGUUN3ME21MlQ6Pjh2IN88US=> MnH6V2FPT0WU
SF268 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYmycmJwUUN3ME21MlYyOjZ{IN88US=> MUPTRW5ITVJ?
A388 NXLNO5Z4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYjJR|UxRTVwNkO2Olch|ryP MXTTRW5ITVJ?
NMC-G1 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGq4bWZKSzVyPU[uNFE5OTFizszN MVzTRW5ITVJ?
CGTH-W-1 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYrJR|UxRTZwMEKwO|Uh|ryP MonFV2FPT0WU
ES4 M4O5Umdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXzEb25bUUN3ME22MlU{ODd2IN88US=> MULTRW5ITVJ?
SR NEnMSFZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEGyeFFKSzVyPU[uOVg5ODdizszN NILkPJRUSU6JRWK=
BB49-HNC NGfJRpVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHHIbI9KSzVyPU[uO|MzODZizszN NUW1dZV7W0GQR1XS
KLE MmXtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHXLNXVKSzVyPU[uO|g{PzdizszN MnzSV2FPT0WU
HUTU-80 MnfPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkPyTWM2OD14Lkm4OFY3KM7:TR?= M4jU[3NCVkeHUh?=
SNU-C2B NIq0UpBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFWzNo5KSzVyPUeuPFI4OzdizszN NHradJVUSU6JRWK=
BB65-RCC MmXjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml3rTWM2OD15Lkm0PVA1KM7:TR?= M4LDXXNCVkeHUh?=
QIMR-WIL NILrOVhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX7JR|UxRThwNEK4NFgh|ryP MWHTRW5ITVJ?
GDM-1 NFLWTVlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1XFOWlEPTB;OD65O|I6OiEQvF2= M1fwTHNCVkeHUh?=
LC4-1 M3m4fWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3PW[2lEPTB;OT6wNFkyOSEQvF2= NHLuc5hUSU6JRWK=
MLMA NV;qOlhlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYDZ[GFkUUN3ME25MlE2ODB4IN88US=> MVjTRW5ITVJ?
EoL-1-cell M4mwOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUHJR|UxRTlwM{CxPVIh|ryP MXjTRW5ITVJ?
BOKU MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX3JR|UxRTlwOU[0OlYh|ryP NImzcGlUSU6JRWK=
EVSA-T NIHCUYFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWLJR|UxRTFyLk[1Olgh|ryP NIr4fYJUSU6JRWK=
D-283MED NG\aR|hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NW\QNYpZUUN3ME2xNE46OTd4IN88US=> MkDHV2FPT0WU
NB1 M2Dpbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGHJdm1KSzVyPUGxMlAzPDJizszN MUDTRW5ITVJ?
RPMI-8402 NYHieHRiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnyyTWM2OD1zMT6xO|gh|ryP NUnxfndLW0GQR1XS
NCI-H1355 NXvreFdwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUfnOFZOUUN3ME2xNU4yQDB4IN88US=> M2\2bnNCVkeHUh?=
NB7 NFjDN2FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1m1UGlEPTB;MUGuN|I6PyEQvF2= M1S2N3NCVkeHUh?=
RPMI-6666 M2rafWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3zZWWlEPTB;MUKuPVU3PyEQvF2= NXTUOohLW0GQR1XS
697 NYnpSVk4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIHMVpNKSzVyPUGzMlI4ODFizszN NHXDTm9USU6JRWK=
CTB-1 NUXjS3VnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXjJR|UxRTF|LkW5OFgh|ryP NVywWHBSW0GQR1XS
VA-ES-BJ MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH\YblRKSzVyPUGzMlkzOzRizszN NV3GWVhxW0GQR1XS
BE-13 MlruS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXPkOZVmUUN3ME2xOE4{QTF3IN88US=> NIDF[FBUSU6JRWK=
SKM-1 NUHFb|dYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGfub5lKSzVyPUG0MlQ1QTlizszN NX3zSnNJW0GQR1XS
TE-6 MoLKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2fRS2lEPTB;MUSuO|U6OSEQvF2= NYDUO3FKW0GQR1XS
LB771-HNC MmrVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MW\JR|UxRTF2Lke4PVgh|ryP M2T5R3NCVkeHUh?=
ECC4 MnzSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoLlTWM2OD1zNz6wNlc4KM7:TR?= NXnRW3pyW0GQR1XS
ES3 NFXUO3dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml[4TWM2OD1zNz60OlU2KM7:TR?= NXnhb5E3W0GQR1XS
LB647-SCLC NET3OJNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXTGTIhFUUN3ME2xO{41QTR7IN88US=> NGjU[HZUSU6JRWK=
NB10 NF24PGhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1XwRmlEPTB;MUiuOVI2PiEQvF2= MmjPV2FPT0WU
L-540 NVLHfWtOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVzLWHhRUUN3ME2xPE45OTB7IN88US=> NVLPTY8xW0GQR1XS
NCI-H2126 M4DSV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M173N2lEPTB;MUmuOVEh|ryP NUi2OYpQW0GQR1XS
HH M{LOemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVrQbod6UUN3ME2yNE4xODl7IN88US=> MkfaV2FPT0WU
MPP-89 M{TGXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2LzRmlEPTB;MkOuNlI5QSEQvF2= MlfkV2FPT0WU
IST-MEL1 NWDSeos5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MU\JR|UxRTJ|Lki2OVgh|ryP MlG4V2FPT0WU
KP-N-YS NWfVVXdHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIewRWVKSzVyPUKzMlkzPTVizszN MX;TRW5ITVJ?
EC-GI-10 M1rrTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1nidGlEPTB;MkSuOVk5QSEQvF2= NV;aV5VNW0GQR1XS
EKVX MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{D4XWlEPTB;Mk[uNFIxOyEQvF2= MofMV2FPT0WU
TGBC1TKB NGrv[YNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml\zTWM2OD1{Nj60N|Qh|ryP MlzMV2FPT0WU
Daudi NVL1eGRGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXjJR|UxRTJ5LkC3O|Mh|ryP MVzTRW5ITVJ?
ALL-PO MlfvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGX4Um1KSzVyPUK3MlA5OSEQvF2= NEnjWZpUSU6JRWK=
NB6 NXS0R2d6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX\3dmpyUUN3ME2yO{41QDhizszN NEnjZY5USU6JRWK=
ES6 M1;sXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHL0cVZKSzVyPUK3MlkyOjNizszN MUTTRW5ITVJ?
COLO-320-HSR NXHtWVE6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVzJR|UxRTJ6LkCzO|Mh|ryP NEHLWWtUSU6JRWK=
K5 M{DQVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXzJepJXUUN3ME2yPE4yOjh5IN88US=> NXH4NJVkW0GQR1XS
ES1 NEjvSY1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MluwTWM2OD1{OD63O|c{KM7:TR?= Ml3lV2FPT0WU
LC-1F MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVvJR|UxRTJ7LkezOFYh|ryP NUPTfVB4W0GQR1XS
SCLC-21H MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWfJR|UxRTNyLkezNVch|ryP MkjJV2FPT0WU
SK-PN-DW MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXL2eYJTUUN3ME2zNk42PTl6IN88US=> M{DRRXNCVkeHUh?=
D-247MG MmLNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MojLTWM2OD1|Mj65O|c{KM7:TR?= MV7TRW5ITVJ?
TE-5 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGHLUVZKSzVyPUOzMlA{PjJizszN NVzue5BWW0GQR1XS
MONO-MAC-6 Ml;kS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWfJR|UxRTN|LkWwOFgh|ryP M1LvSHNCVkeHUh?=
LB2518-MEL M1nqWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoDUTWM2OD1|Mz63OlY3KM7:TR?= NXm3eI1pW0GQR1XS
LOXIMVI MoGzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEHQV|dKSzVyPUOzMlc6OjhizszN NX;1[|M4W0GQR1XS
NCI-H209 M{T6[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mmi1TWM2OD1|NT6xOFQh|ryP MmqyV2FPT0WU
A253 NELyfFhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M17kSGlEPTB;M{WuO|QzQSEQvF2= M2PUOnNCVkeHUh?=
HCC1599 NFrrfoRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXXL[W5QUUN3ME2zOk44ODV|IN88US=> NXLjXlR{W0GQR1XS
EB-3 M3nkeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUPYR5VTUUN3ME2zOk46PTF6IN88US=> MVLTRW5ITVJ?
GOTO NUntS5BlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M33KcmlEPTB;M{euN|IzPCEQvF2= NVvST4RTW0GQR1XS
SW684 M3fVUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkTCTWM2OD12MT64OFk2KM7:TR?= MnXIV2FPT0WU
DEL M{PZT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NI[5XIRKSzVyPUSyMlA2OjJizszN MX;TRW5ITVJ?
HT-144 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWDJR|UxRTR{LkG2O|Yh|ryP MnPvV2FPT0WU
TE-9 NHHweFFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFfpXo9KSzVyPUSzMlQ2QTZizszN MVHTRW5ITVJ?
KARPAS-45 M4DuXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mmi4TWM2OD12ND6zPVI2KM7:TR?= MXvTRW5ITVJ?
HAL-01 M4j1dGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH;mdItKSzVyPUS0MlUxOzRizszN MYXTRW5ITVJ?
RCC10RGB MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M17hNmlEPTB;NESuO|M6OiEQvF2= MYfTRW5ITVJ?
CP67-MEL MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MW\JR|UxRTR3Lk[yOFEh|ryP MnzsV2FPT0WU
NB17 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYLDU5M6UUN3ME20OU43PjR|IN88US=> NHjXd5JUSU6JRWK=
SK-UT-1 Mn7NS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUjOTXYzUUN3ME20OU46PDZ2IN88US=> M2jYWHNCVkeHUh?=
JiyoyeP-2003 M1jCNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVXJR|UxRTR4LkCxNVkh|ryP NULRdWJRW0GQR1XS
HCE-4 M1fRSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUf2Onp7UUN3ME20Ok42QTZ6IN88US=> M1Ppb3NCVkeHUh?=
NCI-H720 NXu2bI1oT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXfJR|UxRTR4Lke2PFIh|ryP MkH1V2FPT0WU
KARPAS-422 M3fkbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlHBTWM2OD12Nz6wPFk2KM7:TR?= NIDjfGNUSU6JRWK=
Ramos-2G6-4C10 M1XkSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWf3XZBkUUN3ME20O{4yPjJ{IN88US=> NX3zb5NRW0GQR1XS
HCE-T NGPvOHZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2HISmlEPTB;NEeuOlgzQCEQvF2= NFu4UmtUSU6JRWK=
PSN1 NI\2SWxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV7JR|UxRTR5Lke4NVMh|ryP MkDXV2FPT0WU

... 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 0.5% methylcellulose+0.2% Tween 80 30 mg/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

カスタマーフィードバック (8)


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Source Cancer Res, 2012, 71, 7547-57. Saracatinib (AZD0530) purchased from Selleck
Method Cell proliferation assay
Cell Lines Huh7 cells/SK-Hep1 cells
Concentrations 1 μmol/L
Incubation Time
Results Results of cell proliferation assay showed that saracatinib treatment could significantly atten-uate promotive hepatoma cellular proliferation conferred by stable LHBs expression in Huh7 and SK-Hep1 cells (Fig. A and B).

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Source Cancer Res, 2013, 71, 7547-57. Saracatinib (AZD0530) purchased from Selleck
Method Tumor xenograft experiments
Cell Lines tumor xenografted nude mice
Concentrations 25 mg/kg
Incubation Time 4 weeks
Results tumor xenograft experiments in nude mice showed that orally saracatinib administration could also alleviate instigative tumor formation induced by stable LHBs expression in Huh7 and SK-Hep1 cells .

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Rating
Source Mol Cancer Res, 2011, 9, 249-258. Saracatinib (AZD0530) purchased from Selleck
Method Cell Viability Assay
Cell Lines MDA-MB-231/1205Lu cells
Concentrations 50 uM
Incubation Time 1 h
Results To verify this observation, we used a second Src inhibitor, AZD0530, which also caused cell rounding (data not shown) and TRAIL sensitization.

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Rating
Source Cancer Biol Ther, 2011, 12(3), 215-28. Saracatinib (AZD0530) purchased from Selleck
Method Cell viability assays
Cell Lines embryonic fibroblasts
Concentrations 125 nM
Incubation Time 48 h
Results In transformed embryonic fibroblasts genetically deleted for toxic BH3 domain proteins BAX and BAK, but not deleted for BID, the combination of a SRC inhibitor (AZD0530; PP2; dasatinib) with a CHK1 inhibitor (UCN-01, AZD7762) was unable to cause cell killing.

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Rating
Source Transl Oncol, 2011, 4, 92-100. Saracatinib (AZD0530) purchased from Selleck
Method Western Blot
Cell Lines Hs683 cells
Concentrations 10 μM
Incubation Time 4 d
Results Figure 4 shows that AZD0530 prevented TMZ-induced soluble caveolin-1 expression but did not change basal levels of soluble caveolin-1 in Hs683 GBM cells. In contrast, erlotinib increased soluble caveolin-1 expression to a similar degree as TMZ in these Hs683 GBM cells.

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Rating
Source J Biomol Screen, 2013, 18, 54-66. Saracatinib (AZD0530) purchased from Selleck
Method 3D Tumor Growth Assay
Cell Lines PC-3M cells
Concentrations 0-10 uM
Incubation Time 7 d
Results Reduction of colony size was observed for a number of established anticancer drugs, and IC 50 values for those reference compounds were determined based on the average area size of the cluster. IC 50 values were determined in two independent experiments and were quite reproducible.

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Rating
Source J Biomol Screen, 2013, 18, 54-66. Saracatinib (AZD0530) purchased from Selleck
Method 3D Tumor Growth Assay
Cell Lines PC-3M cells
Concentrations 0-10uM
Incubation Time 7 day
Results Reduction of colony size was observed for a number of established anticancer drugs, and IC 50 values for those reference compounds were determined based on the average area size of the cluster. IC 50 values were determined in two independent experiments and were quite reproducible.

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Rating
Source 2010, Dr. Shuxin Han of Kent State University. Saracatinib (AZD0530) purchased from Selleck
Method IP assay, Q-PCR assay
Cell Lines Primary human hepatocytes
Concentrations 5 μM
Incubation Time 6 h
Results

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

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