Saracatinib (AZD0530) 化学構造
分子量: 542.03

高品質保証

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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 NXGzR5d[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFnGcphKSzVyPUCuNFYyPDNizszN M1SyS3NCVkeHUh?=
LAMA-84 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MW\JR|UxRTBwMUW5PUDPxE1? M2HRTXNCVkeHUh?=
MEG-01 NFXucWhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlG3TWM2OD1yLkKzOlg5KM7:TR?= NFy0eXlUSU6JRWK=
EM-2 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml\HTWM2OD1yLkK2OUDPxE1? M4nNV3NCVkeHUh?=
TE-15 NE\UVnFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVzJR|UxRTBwMke0NVIh|ryP MXXTRW5ITVJ?
NCI-H1648 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIjJbGdKSzVyPUCuNlgyOTZizszN MX;TRW5ITVJ?
TE-12 MnOyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkH5TWM2OD1yLkOyOlgh|ryP NFXyTHFUSU6JRWK=
LB996-RCC NH;oRVZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1\uTmlEPTB;MD60OFE6PiEQvF2= MUPTRW5ITVJ?
K-562 NYLnUFRST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2H5NGlEPTB;MD60OFk3PyEQvF2= NXrue4lxW0GQR1XS
D-336MG Mn;HS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnK0TWM2OD1yLkWwN|A1KM7:TR?= M1[1RXNCVkeHUh?=
NOS-1 MnvSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXfhepd{UUN3ME2wMlYxPTJ7IN88US=> M4HBcXNCVkeHUh?=
EW-24 M1HXVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4izb2lEPTB;MD62NlY6OyEQvF2= NIT5SI5USU6JRWK=
BV-173 NVPqd|F7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWnJR|UxRTBwNkWyOFkh|ryP Mm[xV2FPT0WU
NCCIT Mn3FS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4jZeWlEPTB;MD63N|IyQCEQvF2= MorRV2FPT0WU
NCI-H1436 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkjqTWM2OD1yLke5NFQ6KM7:TR?= MlviV2FPT0WU
BB30-HNC NXnr[YhtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVLSdlRoUUN3ME2wMlg3OjB|IN88US=> M{K0UnNCVkeHUh?=
TE-8 NFPMSIdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2nFbWlEPTB;MD64O|I4PSEQvF2= MlSxV2FPT0WU
A704 MnfiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXLJR|UxRTBwOEmyNUDPxE1? NHzmUpJUSU6JRWK=
TK10 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYHJR|UxRTBwOUC2Olkh|ryP MVrTRW5ITVJ?
KS-1 MnjYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1jVSGlEPTB;MT6xPVc4QSEQvF2= NY\QW2hbW0GQR1XS
C2BBe1 NILFU4pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2D0[mlEPTB;MT6yNFUxPyEQvF2= NH3jTI9USU6JRWK=
RXF393 M2TXcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHXMdIFKSzVyPUGuNlQ{PiEQvF2= NYrOfmJ4W0GQR1XS
KGN MoHES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2m5SWlEPTB;MT6yO|Y5PyEQvF2= NVPJclkxW0GQR1XS
NB69 NXjSNI02T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFXMXoVKSzVyPUGuN|c1QTdizszN NFLtcYdUSU6JRWK=
TE-11 NUHqS2NYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MorvTWM2OD1zLkSzOFE5KM7:TR?= MkHlV2FPT0WU
TE-1 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXLpcVVZUUN3ME2xMlQ1OTB3IN88US=> NUXERmMzW0GQR1XS
ST486 M2TQO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVy1SWVbUUN3ME2xMlQ2QDV{IN88US=> NF:0VVhUSU6JRWK=
HOP-62 NUOxUGVCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIDSWpBKSzVyPUGuOVAzPDZizszN NGjQVotUSU6JRWK=
EW-16 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{XXeWlEPTB;MT61OVA5OyEQvF2= Mn\tV2FPT0WU
LB1047-RCC NF3wdGxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV7JR|UxRTFwNUW0OVMh|ryP MkLXV2FPT0WU
TE-10 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEKyW2pKSzVyPUGuOlYzPTJizszN NXz3Nm1CW0GQR1XS
RL95-2 NFPHXWxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXPBd5pEUUN3ME2xMlY3QTB{IN88US=> M1HsT3NCVkeHUh?=
DOHH-2 NELKOIpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{To[2lEPTB;MT63NVc5OiEQvF2= NWrCU4xnW0GQR1XS
MFH-ino MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFK3XWFKSzVyPUGuO|c5PyEQvF2= MWjTRW5ITVJ?
GB-1 NIDUeYtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4j5ZWlEPTB;MT63PVg{OyEQvF2= NILjS4ZUSU6JRWK=
SK-N-DZ MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml7RTWM2OD1zLki0Olg5KM7:TR?= MkjPV2FPT0WU
OS-RC-2 M3jWXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3XifmlEPTB;MT64PFU4PCEQvF2= M2rYVXNCVkeHUh?=
SW982 Mn21S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mlv0TWM2OD1zLkmyNFk{KM7:TR?= NWjCcmJbW0GQR1XS
KALS-1 NXj3[WF7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3nENGlEPTB;MT65PFczOiEQvF2= MlHPV2FPT0WU
TGBC24TKB NHvZbFRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn;oTWM2OD1{LkC1PVU5KM7:TR?= M1LXXXNCVkeHUh?=
GI-1 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXLEc|E1UUN3ME2yMlE3ODh2IN88US=> MUnTRW5ITVJ?
SW962 NIHwXFNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NU\VRW1VUUN3ME2yMlE4OTd6IN88US=> MVfTRW5ITVJ?
SW872 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3LnNWlEPTB;Mj6xPFUxPyEQvF2= NHO4UFBUSU6JRWK=
NCI-H747 MljES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3;1SGlEPTB;Mj6yOVcyPCEQvF2= NH[zOXJUSU6JRWK=
MZ1-PC MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXzJR|UxRTJwMkmzOVYh|ryP MVTTRW5ITVJ?
MSTO-211H M1\QUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NInxcWhKSzVyPUKuN|U4OjNizszN NVrnTFRKW0GQR1XS
BL-70 M2nNZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWPJR|UxRTJwNEe0NlIh|ryP NGXZbFJUSU6JRWK=
SW954 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MorDTWM2OD1{LkW3OFA5KM7:TR?= MoW5V2FPT0WU
SNB75 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUfDcpV4UUN3ME2yMlY5PTl2IN88US=> M3fUcnNCVkeHUh?=
IST-SL2 NFnJTIVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnzKTWM2OD1{LkeyN|c6KM7:TR?= M4LFdnNCVkeHUh?=
GCIY MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmraTWM2OD1{Lki3NFA2KM7:TR?= NWTRR5NrW0GQR1XS
KU812 NXfjPYVvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NILT[3JKSzVyPUOuNFUzQTlizszN NXjw[XNWW0GQR1XS
LXF-289 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGjiW4FKSzVyPUOuNVIyODlizszN M1H2N3NCVkeHUh?=
ETK-1 NILaOGNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2SzXGlEPTB;Mz6yNFc3PyEQvF2= MXXTRW5ITVJ?
SF126 M{ewemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF;i[lRKSzVyPUOuN|EyPzRizszN MXHTRW5ITVJ?
LC-2-ad MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoTQTWM2OD1|LkW1O{DPxE1? M2e5NnNCVkeHUh?=
KNS-42 Mn\qS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmnDTWM2OD1|Lk[1JO69VQ>? M1TjSHNCVkeHUh?=
OVCAR-4 M1TuTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmeyTWM2OD1|LkezOFM{KM7:TR?= MXnTRW5ITVJ?
PF-382 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MULJR|UxRTNwOEO2PVgh|ryP MYrTRW5ITVJ?
SH-4 M3fKd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlqyTWM2OD12LkK1NlU6KM7:TR?= M4TEPHNCVkeHUh?=
KM12 NXTBc|JsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUjJR|UxRTRwM{K0NVYh|ryP MVLTRW5ITVJ?
NB5 MnfHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1rBXWlEPTB;ND60NVg3PCEQvF2= M2OzXHNCVkeHUh?=
KURAMOCHI MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoXaTWM2OD12Lk[1NlU3KM7:TR?= NX\BdZptW0GQR1XS
Becker NY\wVFVzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV3lWnkzUUN3ME20MlY3PDF4IN88US=> NGj6TGhUSU6JRWK=
MV-4-11 NWDHS5hvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVLsZms{UUN3ME20MlgyOzR2IN88US=> NWq0TZFmW0GQR1XS
KINGS-1 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnyzTWM2OD12LkiyN|c{KM7:TR?= NF7SSYJUSU6JRWK=
LS-123 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnXPTWM2OD13LkS5Olg1KM7:TR?= NYPubWg6W0GQR1XS
SF268 NH21[mFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUjJR|UxRTVwNkGyOlIh|ryP MnTuV2FPT0WU
A388 M3;ub2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUDJR|UxRTVwNkO2Olch|ryP NVe5eFhDW0GQR1XS
NMC-G1 Mke0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkjuTWM2OD14LkCxPFEyKM7:TR?= MYLTRW5ITVJ?
CGTH-W-1 M1\n[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVrJR|UxRTZwMEKwO|Uh|ryP NW\De5VTW0GQR1XS
ES4 M1\CNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkPSTWM2OD14LkWzNFc1KM7:TR?= NUO2WJN7W0GQR1XS
SR MlLSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX3aTGpMUUN3ME22MlU5QDB5IN88US=> Mn\TV2FPT0WU
BB49-HNC MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUnJR|UxRTZwN{OyNFYh|ryP M{fMbnNCVkeHUh?=
KLE MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEC0WWFKSzVyPU[uO|g{PzdizszN MmLhV2FPT0WU
HUTU-80 NYG5dlljT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2HU[WlEPTB;Nj65PFQ3PiEQvF2= NXjOXJB3W0GQR1XS
SNU-C2B NIe1eXZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVnnc|Q5UUN3ME23MlgzPzN5IN88US=> M1\rTXNCVkeHUh?=
BB65-RCC NHvacVVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHPGe5JKSzVyPUeuPVQ6ODRizszN MmnVV2FPT0WU
QIMR-WIL MnvOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGPGR4hKSzVyPUiuOFI5ODhizszN M{S1c3NCVkeHUh?=
GDM-1 NWq3dmhST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVTJR|UxRThwOUeyPVIh|ryP NHnMVZBUSU6JRWK=
LC4-1 MoPWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVr3ZYNHUUN3ME25MlAxQTFzIN88US=> M2e4cHNCVkeHUh?=
MLMA MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlXQTWM2OD17LkG1NFA3KM7:TR?= MnPCV2FPT0WU
EoL-1-cell NYHXTmVLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NELtO21KSzVyPUmuN|AyQTJizszN NEXDfVNUSU6JRWK=
BOKU MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXXJR|UxRTlwOU[0OlYh|ryP MonZV2FPT0WU
EVSA-T MnrmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4TWNGlEPTB;MUCuOlU3QCEQvF2= MXTTRW5ITVJ?
D-283MED NHqxVHRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYT0PYNjUUN3ME2xNE46OTd4IN88US=> MlrDV2FPT0WU
NB1 M3GxR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M13nWGlEPTB;MUGuNFI1OiEQvF2= NHvoOJlUSU6JRWK=
RPMI-8402 NX\SbYc4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1Xob2lEPTB;MUGuNVc5KM7:TR?= MlKxV2FPT0WU
NCI-H1355 M2P6XWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkHmTWM2OD1zMT6xPFA3KM7:TR?= MlTuV2FPT0WU
NB7 MkPXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVT1WWJFUUN3ME2xNU4{Ojl5IN88US=> NH;hboNUSU6JRWK=
RPMI-6666 NHfjXI5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmnUTWM2OD1zMj65OVY4KM7:TR?= NYDDR4FOW0GQR1XS
697 NXLFTIp3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUXCVIFGUUN3ME2xN{4zPzBzIN88US=> MnHqV2FPT0WU
CTB-1 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYfJR|UxRTF|LkW5OFgh|ryP NUezNlE{W0GQR1XS
VA-ES-BJ MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH;ZcY9KSzVyPUGzMlkzOzRizszN MW\TRW5ITVJ?
BE-13 NWPNNIhuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUfQNnU{UUN3ME2xOE4{QTF3IN88US=> M33HOXNCVkeHUh?=
SKM-1 MkfES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2TpXmlEPTB;MUSuOFQ6QSEQvF2= MX7TRW5ITVJ?
TE-6 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M170dGlEPTB;MUSuO|U6OSEQvF2= Ml24V2FPT0WU
LB771-HNC MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWXJR|UxRTF2Lke4PVgh|ryP NWTHcYVpW0GQR1XS
ECC4 M3vJXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3PhOmlEPTB;MUeuNFI4PyEQvF2= NITsZ3VUSU6JRWK=
ES3 NYm5SHEzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV:2RWVWUUN3ME2xO{41PjV3IN88US=> NVLOSnBmW0GQR1XS
LB647-SCLC MlmwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mk[xTWM2OD1zNz60PVQ6KM7:TR?= NWH1SJluW0GQR1XS
NB10 M{X0d2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M121bGlEPTB;MUiuOVI2PiEQvF2= MknKV2FPT0WU
L-540 Mmn2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mof6TWM2OD1zOD64NVA6KM7:TR?= MXrTRW5ITVJ?
NCI-H2126 NG\hSFdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NICyRWNKSzVyPUG5MlUyKM7:TR?= NWmyc256W0GQR1XS
HH MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NULTUHU{UUN3ME2yNE4xODl7IN88US=> NH\kR29USU6JRWK=
MPP-89 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVfJR|UxRTJ|LkKyPFkh|ryP M{C4RnNCVkeHUh?=
IST-MEL1 NIG1RZBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4G4NWlEPTB;MkOuPFY2QCEQvF2= MmjMV2FPT0WU
KP-N-YS NFnVO2JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGXSZXlKSzVyPUKzMlkzPTVizszN NXTQcVVkW0GQR1XS
EC-GI-10 M3Lsbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NG[3WXJKSzVyPUK0MlU6QDlizszN NY\l[YxlW0GQR1XS
EKVX MkPMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mk\3TWM2OD1{Nj6wNlA{KM7:TR?= MXnTRW5ITVJ?
TGBC1TKB Mnm1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEHzXpZKSzVyPUK2MlQ{PCEQvF2= NWm1[296W0GQR1XS
Daudi M{TlUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NITreVNKSzVyPUK3MlA4PzNizszN M1rpWXNCVkeHUh?=
ALL-PO NHjzTm5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYXJR|UxRTJ5LkC4NUDPxE1? MV;TRW5ITVJ?
NB6 NHHaZ|ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1riS2lEPTB;MkeuOFg5KM7:TR?= M2TsS3NCVkeHUh?=
ES6 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3:3e2lEPTB;MkeuPVEzOyEQvF2= M3;ZbXNCVkeHUh?=
COLO-320-HSR NEi2PIRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MY\JR|UxRTJ6LkCzO|Mh|ryP NULEXpZMW0GQR1XS
K5 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV7JR|UxRTJ6LkGyPFch|ryP MoXXV2FPT0WU
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... 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 3年-20℃
2年-80℃in solvent
別名 N/A
溶解度 (25°C) * In vitro DMSO 35 mg/mL warming (64.57 mM)
Ethanol 31 mg/mL (57.19 mM)
Water <1 mg/mL
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)

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