Saracatinib (AZD0530) 化学構造
分子量: 542.03

高品質保証

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カスタマーフィードバック(8)

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 M2rvNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmP2TWM2OD1yLkC2NVQ{KM7:TR?= NXjUdml6W0GQR1XS
LAMA-84 NVr4dWtzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkD5TWM2OD1yLkG1PVkh|ryP M{DhdXNCVkeHUh?=
MEG-01 NHLxfVZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmfZTWM2OD1yLkKzOlg5KM7:TR?= M1v3RXNCVkeHUh?=
EM-2 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVrJU45VUUN3ME2wMlI3PSEQvF2= M{OzTHNCVkeHUh?=
TE-15 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3H5RmlEPTB;MD6yO|QyOiEQvF2= MlnwV2FPT0WU
NCI-H1648 NG\SO4NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVnJR|UxRTBwMkixNVYh|ryP M13LOHNCVkeHUh?=
TE-12 NH;Tb2xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3PlTWlEPTB;MD6zNlY5KM7:TR?= NIH5R|RUSU6JRWK=
LB996-RCC M1vrXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGLqR3lKSzVyPUCuOFQyQTZizszN NI\jTWRUSU6JRWK=
K-562 M2jzbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWi3R284UUN3ME2wMlQ1QTZ5IN88US=> MlfBV2FPT0WU
D-336MG NIDBbXJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M33TdmlEPTB;MD61NFMxPCEQvF2= NYfDR2hOW0GQR1XS
NOS-1 NYDP[ZdxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFjGR|dKSzVyPUCuOlA2OjlizszN NYT0[40xW0GQR1XS
EW-24 NEjqV3NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEPUeFNKSzVyPUCuOlI3QTNizszN Mo\NV2FPT0WU
BV-173 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M33SR2lEPTB;MD62OVI1QSEQvF2= MmjKV2FPT0WU
NCCIT NV3xeWxqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2TtVmlEPTB;MD63N|IyQCEQvF2= NEPMR29USU6JRWK=
NCI-H1436 NXrLPFdHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3rWbmlEPTB;MD63PVA1QSEQvF2= NF:3RolUSU6JRWK=
BB30-HNC NYPOdodtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mo\yTWM2OD1yLki2NlA{KM7:TR?= NH;CcHRUSU6JRWK=
TE-8 NFy4WHRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml[5TWM2OD1yLki3Nlc2KM7:TR?= NF76V3RUSU6JRWK=
A704 M{O1V2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWHa[nJHUUN3ME2wMlg6OjFizszN NGCyWnFUSU6JRWK=
TK10 NX7Nb5U{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoG4TWM2OD1yLkmwOlY6KM7:TR?= NH7MdY9USU6JRWK=
KS-1 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmrhTWM2OD1zLkG5O|c6KM7:TR?= MVvTRW5ITVJ?
C2BBe1 NYXZXWlJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWnJR|UxRTFwMkC1NFch|ryP NYe0Zmh7W0GQR1XS
RXF393 MknBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NITycZFKSzVyPUGuNlQ{PiEQvF2= M4fwcHNCVkeHUh?=
KGN NYXGbHZ{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmXaTWM2OD1zLkK3Olg4KM7:TR?= NHHwSZZUSU6JRWK=
NB69 NVPaWHU3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWfJR|UxRTFwM{e0PVch|ryP M1vadXNCVkeHUh?=
TE-11 NEj5TGpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NW\Oe5M2UUN3ME2xMlQ{PDF6IN88US=> NX[2ToEyW0GQR1XS
TE-1 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml:0TWM2OD1zLkS0NVA2KM7:TR?= M1vI[HNCVkeHUh?=
ST486 NFfBSZhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{O4UmlEPTB;MT60OVg2OiEQvF2= Mn\SV2FPT0WU
HOP-62 NH\ZNnVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NW\pWoo1UUN3ME2xMlUxOjR4IN88US=> MW\TRW5ITVJ?
EW-16 NGLCN3pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYXIT5lvUUN3ME2xMlU2ODh|IN88US=> NUPhNFVpW0GQR1XS
LB1047-RCC NY\lOohVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{KyZ2lEPTB;MT61OVQ2OyEQvF2= MorxV2FPT0WU
TE-10 NV;RXZNoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXT3TIl4UUN3ME2xMlY3OjV{IN88US=> M2C4dnNCVkeHUh?=
RL95-2 M3\xfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXvT[4s1UUN3ME2xMlY3QTB{IN88US=> NHyzUItUSU6JRWK=
DOHH-2 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoDmTWM2OD1zLkexO|gzKM7:TR?= MYPTRW5ITVJ?
MFH-ino MnGwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NI\XVZBKSzVyPUGuO|c5PyEQvF2= NYr4OpE3W0GQR1XS
GB-1 NXK5PXVWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXPsNpd7UUN3ME2xMlc6QDN|IN88US=> NVi4SHRbW0GQR1XS
SK-N-DZ M4rNUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHLiVZZKSzVyPUGuPFQ3QDhizszN NXvjV5BDW0GQR1XS
OS-RC-2 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUjvVo9MUUN3ME2xMlg5PTd2IN88US=> NUnpfXF5W0GQR1XS
SW982 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX;JR|UxRTFwOUKwPVMh|ryP NWjxc4p[W0GQR1XS
KALS-1 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGrYXIZKSzVyPUGuPVg4OjJizszN NH3rbnRUSU6JRWK=
TGBC24TKB NH3SRZVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHnFT5dKSzVyPUKuNFU6PThizszN NUD0V2lyW0GQR1XS
GI-1 M3exXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVP5blA4UUN3ME2yMlE3ODh2IN88US=> NEjHWodUSU6JRWK=
SW962 MlezS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFf2VplKSzVyPUKuNVcyPzhizszN NG\PelRUSU6JRWK=
SW872 NIDZPIhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkLHTWM2OD1{LkG4OVA4KM7:TR?= NUTzUZAzW0GQR1XS
NCI-H747 NX\XWJV4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHXZepNKSzVyPUKuNlU4OTRizszN MUXTRW5ITVJ?
MZ1-PC MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWjJR|UxRTJwMkmzOVYh|ryP M{f0[XNCVkeHUh?=
MSTO-211H MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYXJR|UxRTJwM{W3NlMh|ryP MWrTRW5ITVJ?
BL-70 M3vPSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYXxTGtrUUN3ME2yMlQ4PDJ{IN88US=> M1fB[nNCVkeHUh?=
SW954 Mn3IS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVrJR|UxRTJwNUe0NFgh|ryP MlfuV2FPT0WU
SNB75 NHXMUGVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M37BbWlEPTB;Mj62PFU6PCEQvF2= MnPUV2FPT0WU
IST-SL2 M3[x[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3P5RWlEPTB;Mj63NlM4QSEQvF2= NVn4boJTW0GQR1XS
GCIY NHq0fYdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFfjcYtKSzVyPUKuPFcxODVizszN NITNenJUSU6JRWK=
KU812 NWTpTGVYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV;5U|BMUUN3ME2zMlA2Ojl7IN88US=> MkjkV2FPT0WU
LXF-289 MlTrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF7LcmdKSzVyPUOuNVIyODlizszN MnrTV2FPT0WU
ETK-1 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3vGNGlEPTB;Mz6yNFc3PyEQvF2= MXzTRW5ITVJ?
SF126 M3THc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX7JR|UxRTNwM{GxO|Qh|ryP NEn2bXRUSU6JRWK=
LC-2-ad NWTm[nV1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NY[xU3B4UUN3ME2zMlU2PyEQvF2= MYPTRW5ITVJ?
KNS-42 NWPkPXZqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnjnTWM2OD1|Lk[1JO69VQ>? MW\TRW5ITVJ?
OVCAR-4 NUPJdlQ5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1HCfWlEPTB;Mz63N|Q{OyEQvF2= NH;OWW9USU6JRWK=
PF-382 NVL3RXA{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mk\mTWM2OD1|LkizOlk5KM7:TR?= Mom1V2FPT0WU
SH-4 M1PqU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYnJR|UxRTRwMkWyOVkh|ryP M2L1SXNCVkeHUh?=
KM12 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH3HWItKSzVyPUSuN|I1OTZizszN NGfHUINUSU6JRWK=
NB5 MoDGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1PWVGlEPTB;ND60NVg3PCEQvF2= NVS0N5RMW0GQR1XS
KURAMOCHI MnzlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1fodWlEPTB;ND62OVI2PiEQvF2= MVfTRW5ITVJ?
Becker MkfoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXjJR|UxRTRwNk[0NVYh|ryP M13UfnNCVkeHUh?=
MV-4-11 MoDvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVXWenJ1UUN3ME20MlgyOzR2IN88US=> MUfTRW5ITVJ?
KINGS-1 MlPQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGHGRVZKSzVyPUSuPFI{PzNizszN NWXDSGRnW0GQR1XS
LS-123 M1n3[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2q4Z2lEPTB;NT60PVY5PCEQvF2= MmfiV2FPT0WU
SF268 NX:0WJJJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2\6d2lEPTB;NT62NVI3OiEQvF2= M372cXNCVkeHUh?=
A388 NX;GN4JiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4Dvd2lEPTB;NT62N|Y3PyEQvF2= NX\sVG1zW0GQR1XS
NMC-G1 NYn1cXloT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWPYXHJPUUN3ME22MlAyQDFzIN88US=> M{HkVXNCVkeHUh?=
CGTH-W-1 NHPrT2NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn7HTWM2OD14LkCyNFc2KM7:TR?= M1nIeXNCVkeHUh?=
ES4 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYDXclZQUUN3ME22MlU{ODd2IN88US=> M4KzSXNCVkeHUh?=
SR M32zfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX61foFyUUN3ME22MlU5QDB5IN88US=> M3\ab3NCVkeHUh?=
BB49-HNC NInzV2NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHHJeZRKSzVyPU[uO|MzODZizszN MnG0V2FPT0WU
KLE MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{foSWlEPTB;Nj63PFM4PyEQvF2= MkXjV2FPT0WU
HUTU-80 MmfGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXzWXm9mUUN3ME22Mlk5PDZ4IN88US=> NYL0bGRyW0GQR1XS
SNU-C2B NXzZUIp7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWjJR|UxRTdwOEK3N|ch|ryP NFPVb3lUSU6JRWK=
BB65-RCC NVfw[3d6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGPZTpBKSzVyPUeuPVQ6ODRizszN MUDTRW5ITVJ?
QIMR-WIL M{Plbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3izfGlEPTB;OD60NlgxQCEQvF2= NHHHfolUSU6JRWK=
GDM-1 NHXhPHpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUnKTol{UUN3ME24Mlk4Ojl{IN88US=> MlXkV2FPT0WU
LC4-1 NIT3U|hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX3rTmxHUUN3ME25MlAxQTFzIN88US=> NUP5SZg3W0GQR1XS
MLMA MoPNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUfJR|UxRTlwMUWwNFYh|ryP NH;oXldUSU6JRWK=
EoL-1-cell MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3fRfWlEPTB;OT6zNFE6OiEQvF2= MYXTRW5ITVJ?
BOKU M3LFR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1zCWWlEPTB;OT65OlQ3PiEQvF2= Mn7MV2FPT0WU
EVSA-T M1P3PGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUfJR|UxRTFyLk[1Olgh|ryP M3PjeHNCVkeHUh?=
D-283MED NY\uSmIzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3fRWGlEPTB;MUCuPVE4PiEQvF2= NGDGVmtUSU6JRWK=
NB1 MlfhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXq3c|NCUUN3ME2xNU4xOjR{IN88US=> NHnqZ25USU6JRWK=
RPMI-8402 NFjqcmdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NG\qXHBKSzVyPUGxMlE4QCEQvF2= M2\RenNCVkeHUh?=
NCI-H1355 NF3HUWhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{n5dWlEPTB;MUGuNVgxPiEQvF2= MkDzV2FPT0WU
NB7 M3vmNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYrJR|UxRTFzLkOyPVch|ryP NYWyZZJ1W0GQR1XS
RPMI-6666 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NELrZphKSzVyPUGyMlk2PjdizszN NVvVd2hzW0GQR1XS
697 Mkf3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHfLOllKSzVyPUGzMlI4ODFizszN MWPTRW5ITVJ?
CTB-1 NX3BSo9GT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIf1bFdKSzVyPUGzMlU6PDhizszN M3\TTHNCVkeHUh?=
VA-ES-BJ MnL4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVjJR|UxRTF|LkmyN|Qh|ryP MmL0V2FPT0WU
BE-13 NWn1NFdyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NULsW3NPUUN3ME2xOE4{QTF3IN88US=> M4D2NXNCVkeHUh?=
SKM-1 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF7qO2lKSzVyPUG0MlQ1QTlizszN NUfy[XVIW0GQR1XS
TE-6 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYfJR|UxRTF2Lke1PVEh|ryP Mom4V2FPT0WU
LB771-HNC NILlR5pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVz5SZpPUUN3ME2xOE44QDl6IN88US=> NXywVZY3W0GQR1XS
ECC4 MoPQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkLCTWM2OD1zNz6wNlc4KM7:TR?= MkXTV2FPT0WU
ES3 NYDrUVhtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mle4TWM2OD1zNz60OlU2KM7:TR?= NGDpcGVUSU6JRWK=
LB647-SCLC NF3FVIJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGfWdZBKSzVyPUG3MlQ6PDlizszN M37LfnNCVkeHUh?=
NB10 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml71TWM2OD1zOD61NlU3KM7:TR?= MoH6V2FPT0WU
L-540 M2\QSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX[xPYxZUUN3ME2xPE45OTB7IN88US=> MXXTRW5ITVJ?
NCI-H2126 MkX4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYHJR|UxRTF7LkWxJO69VQ>? NVHEc|VZW0GQR1XS
HH MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnvvTWM2OD1{MD6wNFk6KM7:TR?= M3TLcXNCVkeHUh?=
MPP-89 MmnMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkL4TWM2OD1{Mz6yNlg6KM7:TR?= M{fOV3NCVkeHUh?=
IST-MEL1 M2\udmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGLaSpZKSzVyPUKzMlg3PThizszN NV;3dXdbW0GQR1XS
KP-N-YS MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXjJUYNxUUN3ME2yN{46OjV3IN88US=> M3TlfHNCVkeHUh?=
EC-GI-10 MnvTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1XWb2lEPTB;MkSuOVk5QSEQvF2= MnrBV2FPT0WU
EKVX NInaTodIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlW5TWM2OD1{Nj6wNlA{KM7:TR?= NXfWXoJsW0GQR1XS
TGBC1TKB MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF62b4pKSzVyPUK2MlQ{PCEQvF2= MVXTRW5ITVJ?
Daudi MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NI\XUYZKSzVyPUK3MlA4PzNizszN NYTZPFh6W0GQR1XS
ALL-PO NWXEd2JOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3;Nc2lEPTB;MkeuNFgyKM7:TR?= NXLzXJNGW0GQR1XS
NB6 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUTJR|UxRTJ5LkS4PEDPxE1? MVnTRW5ITVJ?
ES6 NVq2TXVsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M33vOmlEPTB;MkeuPVEzOyEQvF2= MVjTRW5ITVJ?
COLO-320-HSR M4O0XWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGrENlRKSzVyPUK4MlA{PzNizszN Ml7GV2FPT0WU
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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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