Saracatinib (AZD0530)

Saracatinib (AZD0530)は一種の有効なSrc阻害剤で、無細胞試験でIC50値が2.7 nMです。Saracatinib (AZD0530)はc-Yes、Fyn、Lyn、Blk、FgrとLckにも活性をしていますが、AblとEGFR (L858RとL861Q)に作用する活性が低いです。臨床2/3期。

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Saracatinib (AZD0530) 化学構造
分子量: 542.03

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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)は一種の有効なSrc阻害剤で、無細胞試験でIC50値が2.7 nMです。Saracatinib (AZD0530)はc-Yes、Fyn、Lyn、Blk、FgrとLckにも活性をしていますが、AblとEGFR (L858RとL861Q)に作用する活性が低いです。臨床2/3期。
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 MmW0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3Xqe2lEPTB;MD6wOlE1OyEQvF2= MVPTRW5ITVJ?
LAMA-84 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXHJR|UxRTBwMUW5PUDPxE1? Mn\nV2FPT0WU
MEG-01 NVTKdFFZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnK5TWM2OD1yLkKzOlg5KM7:TR?= NFnXZ3FUSU6JRWK=
EM-2 NVnw[201T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYrJR|UxRTBwMk[1JO69VQ>? NF\yUlFUSU6JRWK=
TE-15 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoTUTWM2OD1yLkK3OFEzKM7:TR?= NHv3WotUSU6JRWK=
NCI-H1648 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NU\PbVQyUUN3ME2wMlI5OTF4IN88US=> MWDTRW5ITVJ?
TE-12 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUXVXXg6UUN3ME2wMlMzPjhizszN MUfTRW5ITVJ?
LB996-RCC MnnwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml7iTWM2OD1yLkS0NVk3KM7:TR?= NEOyZ41USU6JRWK=
K-562 NF7IUZpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXHrcIdRUUN3ME2wMlQ1QTZ5IN88US=> NIPKU3FUSU6JRWK=
D-336MG NI\JSldIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHTKUnRKSzVyPUCuOVA{ODRizszN MnL4V2FPT0WU
NOS-1 Ml;KS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGrydpdKSzVyPUCuOlA2OjlizszN MWDTRW5ITVJ?
EW-24 M3zkN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoPmTWM2OD1yLk[yOlk{KM7:TR?= M1z4enNCVkeHUh?=
BV-173 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXjJR|UxRTBwNkWyOFkh|ryP NEfKT5VUSU6JRWK=
NCCIT NHzqS2VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH\Lb4ZKSzVyPUCuO|MzOThizszN NH;pRphUSU6JRWK=
NCI-H1436 NF;wNJhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1\4ZmlEPTB;MD63PVA1QSEQvF2= MWTTRW5ITVJ?
BB30-HNC M3GzNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVvvSZJIUUN3ME2wMlg3OjB|IN88US=> NF\vfHNUSU6JRWK=
TE-8 NFPXXJVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIrTSppKSzVyPUCuPFczPzVizszN MkPTV2FPT0WU
A704 MmHjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoG0TWM2OD1yLki5NlEh|ryP Mn;PV2FPT0WU
TK10 NHfjS4dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2PuRWlEPTB;MD65NFY3QSEQvF2= MYXTRW5ITVJ?
KS-1 NIW4boVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn\DTWM2OD1zLkG5O|c6KM7:TR?= NFn1XIxUSU6JRWK=
C2BBe1 NH\UdGNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1PhVmlEPTB;MT6yNFUxPyEQvF2= NXG0eWxtW0GQR1XS
RXF393 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFHYfGpKSzVyPUGuNlQ{PiEQvF2= MWTTRW5ITVJ?
KGN MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NW[xT2hqUUN3ME2xMlI4Pjh5IN88US=> NGfDTG5USU6JRWK=
NB69 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUfJR|UxRTFwM{e0PVch|ryP NHTTR3BUSU6JRWK=
TE-11 M13Kd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXfJR|UxRTFwNEO0NVgh|ryP NHfDRo9USU6JRWK=
TE-1 NH;lWIRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYLJR|UxRTFwNESxNFUh|ryP MnzPV2FPT0WU
ST486 NV;NUJVbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGPsV2xKSzVyPUGuOFU5PTJizszN MXrTRW5ITVJ?
HOP-62 MnvmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoDpTWM2OD1zLkWwNlQ3KM7:TR?= NFrvcphUSU6JRWK=
EW-16 NUjN[m1JT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYTPRppbUUN3ME2xMlU2ODh|IN88US=> M1nvOnNCVkeHUh?=
LB1047-RCC M2S0Xmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3fxc2lEPTB;MT61OVQ2OyEQvF2= M3nPNXNCVkeHUh?=
TE-10 M3HMZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{nRO2lEPTB;MT62OlI2OiEQvF2= NUD4W2lHW0GQR1XS
RL95-2 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlrhTWM2OD1zLk[2PVAzKM7:TR?= MnTnV2FPT0WU
DOHH-2 Ml;US5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWXJR|UxRTFwN{G3PFIh|ryP M{nV[nNCVkeHUh?=
MFH-ino M3;BbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Moi3TWM2OD1zLke3PFch|ryP NGP5SYJUSU6JRWK=
GB-1 M3LpO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml3MTWM2OD1zLke5PFM{KM7:TR?= M1:3c3NCVkeHUh?=
SK-N-DZ NFPVTodIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2rYdGlEPTB;MT64OFY5QCEQvF2= NVXQWIxmW0GQR1XS
OS-RC-2 NILx[ldIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHnNO2RKSzVyPUGuPFg2PzRizszN M4GyfXNCVkeHUh?=
SW982 M2riTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnrnTWM2OD1zLkmyNFk{KM7:TR?= MY\TRW5ITVJ?
KALS-1 MmjqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWrJR|UxRTFwOUi3NlIh|ryP NUfEXFFEW0GQR1XS
TGBC24TKB M2fF[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1\ZVmlEPTB;Mj6wOVk2QCEQvF2= M3j2fnNCVkeHUh?=
GI-1 M3\tfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXXJR|UxRTJwMU[wPFQh|ryP NVLVXYh6W0GQR1XS
SW962 NXridlhlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mmn4TWM2OD1{LkG3NVc5KM7:TR?= Mn;3V2FPT0WU
SW872 MkfOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUfWfGQ1UUN3ME2yMlE5PTB5IN88US=> MnXYV2FPT0WU
NCI-H747 NH3QVYFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWDNUFNFUUN3ME2yMlI2PzF2IN88US=> MYPTRW5ITVJ?
MZ1-PC MlHPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIKxc3FKSzVyPUKuNlk{PTZizszN M2DObXNCVkeHUh?=
MSTO-211H MoHSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH3V[4JKSzVyPUKuN|U4OjNizszN MmjxV2FPT0WU
BL-70 NV3kSGkzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2LOO2lEPTB;Mj60O|QzOiEQvF2= MmjZV2FPT0WU
SW954 MlTrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEXifYpKSzVyPUKuOVc1ODhizszN NEX3RlhUSU6JRWK=
SNB75 NXjaNnpyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M37xT2lEPTB;Mj62PFU6PCEQvF2= NEDhOIxUSU6JRWK=
IST-SL2 MmHVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWDJR|UxRTJwN{KzO|kh|ryP NHzxTWZUSU6JRWK=
GCIY MkCxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3TWZ2lEPTB;Mj64O|AxPSEQvF2= M1LYR3NCVkeHUh?=
KU812 M4DIUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlXMTWM2OD1|LkC1Nlk6KM7:TR?= MlfVV2FPT0WU
LXF-289 M3;COmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3LJTWlEPTB;Mz6xNlExQSEQvF2= NH;ibmtUSU6JRWK=
ETK-1 M{jCdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWDJR|UxRTNwMkC3Olch|ryP M3O4NHNCVkeHUh?=
SF126 MlPrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mk[1TWM2OD1|LkOxNVc1KM7:TR?= MUjTRW5ITVJ?
LC-2-ad NFTLUZJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF;qeXJKSzVyPUOuOVU4KM7:TR?= MX3TRW5ITVJ?
KNS-42 NUm1bXhyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWPJR|UxRTNwNkWg{txO NEXEVINUSU6JRWK=
OVCAR-4 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX3JR|UxRTNwN{O0N|Mh|ryP MVnTRW5ITVJ?
PF-382 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlTiTWM2OD1|LkizOlk5KM7:TR?= NI\sVFVUSU6JRWK=
SH-4 NYnuVFZzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWC2ZVhTUUN3ME20MlI2OjV7IN88US=> NU\6RndxW0GQR1XS
KM12 NYP0bFA5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml;zTWM2OD12LkOyOFE3KM7:TR?= MWTTRW5ITVJ?
NB5 NV30eHB1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHvtbnRKSzVyPUSuOFE5PjRizszN NHX4SldUSU6JRWK=
KURAMOCHI NW[wXnB6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVfJR|UxRTRwNkWyOVYh|ryP NYrVXZFCW0GQR1XS
Becker NF\Hbo5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVrqepRjUUN3ME20MlY3PDF4IN88US=> MUXTRW5ITVJ?
MV-4-11 Ml3MS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH7Je|lKSzVyPUSuPFE{PDRizszN NWHHeYdpW0GQR1XS
KINGS-1 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUD5[oUyUUN3ME20MlgzOzd|IN88US=> M{\L[XNCVkeHUh?=
LS-123 MkTES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVjJR|UxRTVwNEm2PFQh|ryP MoTnV2FPT0WU
SF268 MlHYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYrJR|UxRTVwNkGyOlIh|ryP NVG4eJhxW0GQR1XS
A388 NXfTO5VET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MW\JR|UxRTVwNkO2Olch|ryP NX74c4JiW0GQR1XS
NMC-G1 NW\iVHZ{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2nIRmlEPTB;Nj6wNVgyOSEQvF2= NILFS|hUSU6JRWK=
CGTH-W-1 NH7aVW5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVHJR|UxRTZwMEKwO|Uh|ryP NXXkdJZ4W0GQR1XS
ES4 NIn0OnJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH3xc|ZKSzVyPU[uOVMxPzRizszN MV\TRW5ITVJ?
SR NHn3ZohIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXL4[o5XUUN3ME22MlU5QDB5IN88US=> M{m3RnNCVkeHUh?=
BB49-HNC NYrzN5VUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVT5bIptUUN3ME22Mlc{OjB4IN88US=> NV[5OGcyW0GQR1XS
KLE MmjmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmjlTWM2OD14Lke4N|c4KM7:TR?= NUT5d5BUW0GQR1XS
HUTU-80 Ml\KS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV7ZU49XUUN3ME22Mlk5PDZ4IN88US=> NF;nfZJUSU6JRWK=
SNU-C2B MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIn6S5FKSzVyPUeuPFI4OzdizszN MlPEV2FPT0WU
BB65-RCC NXPxcHV7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml\JTWM2OD15Lkm0PVA1KM7:TR?= NUDMc4NtW0GQR1XS
QIMR-WIL MojUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWnJR|UxRThwNEK4NFgh|ryP M1zmT3NCVkeHUh?=
GDM-1 NFW2b4RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWXJR|UxRThwOUeyPVIh|ryP NV:wSFZIW0GQR1XS
LC4-1 MoTBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX;JR|UxRTlwMEC5NVEh|ryP MX;TRW5ITVJ?
MLMA NYO4[pZKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NG\VdZRKSzVyPUmuNVUxODZizszN MWrTRW5ITVJ?
EoL-1-cell Mn\tS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUDJR|UxRTlwM{CxPVIh|ryP NWfBbndzW0GQR1XS
BOKU MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVjIOG9kUUN3ME25Mlk3PDZ4IN88US=> M4nQT3NCVkeHUh?=
EVSA-T NIraTYhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHP2RppKSzVyPUGwMlY2PjhizszN NESwUJZUSU6JRWK=
D-283MED MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2XDZWlEPTB;MUCuPVE4PiEQvF2= NETUVGxUSU6JRWK=
NB1 M4DPTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlTSTWM2OD1zMT6wNlQzKM7:TR?= NIjWZlVUSU6JRWK=
RPMI-8402 MmjKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWXJR|UxRTFzLkG3PEDPxE1? NXznPXd5W0GQR1XS
NCI-H1355 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFr4TnJKSzVyPUGxMlE5ODZizszN MnTtV2FPT0WU
NB7 NWjXcWpHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVHBOlU6UUN3ME2xNU4{Ojl5IN88US=> M4PiTnNCVkeHUh?=
RPMI-6666 NYDCemp2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYPJR|UxRTF{Lkm1Olch|ryP MXTTRW5ITVJ?
697 Mm\0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHH2VmNKSzVyPUGzMlI4ODFizszN NXnCUZhlW0GQR1XS
CTB-1 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MljMTWM2OD1zMz61PVQ5KM7:TR?= NXfSRlc6W0GQR1XS
VA-ES-BJ NF\Je4tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3nUNWlEPTB;MUOuPVI{PCEQvF2= NVzHdVk1W0GQR1XS
BE-13 M{TRV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXjJR|UxRTF2LkO5NVUh|ryP NH3oRodUSU6JRWK=
SKM-1 M{PFdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4HGRmlEPTB;MUSuOFQ6QSEQvF2= M{nPN3NCVkeHUh?=
TE-6 NUXjS2hWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFXhc|JKSzVyPUG0Mlc2QTFizszN MXHTRW5ITVJ?
LB771-HNC M2LqUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYDJR|UxRTF2Lke4PVgh|ryP MkS0V2FPT0WU
ECC4 NH\HO|FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2npcmlEPTB;MUeuNFI4PyEQvF2= MXHTRW5ITVJ?
ES3 M1yxcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWnJR|UxRTF5LkS2OVUh|ryP MkG1V2FPT0WU
LB647-SCLC M4X2cGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXfYWWNJUUN3ME2xO{41QTR7IN88US=> M{fnXXNCVkeHUh?=
NB10 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2ewdGlEPTB;MUiuOVI2PiEQvF2= NHH2WolUSU6JRWK=
L-540 Mnm4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX74Npp5UUN3ME2xPE45OTB7IN88US=> MY\TRW5ITVJ?
NCI-H2126 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NID1N3JKSzVyPUG5MlUyKM7:TR?= NVzDO4ZKW0GQR1XS
HH Ml;tS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFLlVmtKSzVyPUKwMlAxQTlizszN Mny3V2FPT0WU
MPP-89 MoDmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWf1XFRsUUN3ME2yN{4zOjh7IN88US=> NXPwT2x4W0GQR1XS
IST-MEL1 NUHQ[FFET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUWxOlV{UUN3ME2yN{45PjV6IN88US=> MY\TRW5ITVJ?
KP-N-YS M1TBSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWHJR|UxRTJ|LkmyOVUh|ryP MmD2V2FPT0WU
EC-GI-10 M4fiSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWC1dmJCUUN3ME2yOE42QTh7IN88US=> M4HWfHNCVkeHUh?=
EKVX MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVvJR|UxRTJ4LkCyNFMh|ryP M2rQNHNCVkeHUh?=
TGBC1TKB NWDZbm5bT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NI\selhKSzVyPUK2MlQ{PCEQvF2= NH34fJpUSU6JRWK=
Daudi MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF72SWdKSzVyPUK3MlA4PzNizszN MU\TRW5ITVJ?
ALL-PO MoD1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3\NRWlEPTB;MkeuNFgyKM7:TR?= Mn\4V2FPT0WU
NB6 NHTPS4hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHL1W|dKSzVyPUK3MlQ5QCEQvF2= MWjTRW5ITVJ?
ES6 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M13JVmlEPTB;MkeuPVEzOyEQvF2= M4jqSHNCVkeHUh?=
COLO-320-HSR M3XHUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoS2TWM2OD1{OD6wN|c{KM7:TR?= M3X3OHNCVkeHUh?=
K5 Mln4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH:wNItKSzVyPUK4MlEzQDdizszN MofBV2FPT0WU
ES1 M1\hPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4TRXGlEPTB;MkiuO|c4OyEQvF2= MnTQV2FPT0WU
LC-1F MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXf3eJNoUUN3ME2yPU44OzR4IN88US=> M3HicXNCVkeHUh?=
SCLC-21H M3;rOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2P6XmlEPTB;M{CuO|MyPyEQvF2= MYPTRW5ITVJ?
SK-PN-DW MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWTVb4YxUUN3ME2zNk42PTl6IN88US=> MYPTRW5ITVJ?
D-247MG NYTCO45WT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVrJR|UxRTN{Lkm3O|Mh|ryP M1zyTnNCVkeHUh?=
TE-5 M3PWNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmfCTWM2OD1|Mz6wN|YzKM7:TR?= NH23RmtUSU6JRWK=
MONO-MAC-6 NXS3UW4yT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHnMRnhKSzVyPUOzMlUxPDhizszN NIj0XnNUSU6JRWK=
LB2518-MEL MkDWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnTVTWM2OD1|Mz63OlY3KM7:TR?= NE\HelZUSU6JRWK=
LOXIMVI M{GyfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUjC[o83UUN3ME2zN{44QTJ6IN88US=> NVjMSlZoW0GQR1XS
NCI-H209 MmPJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2XwfGlEPTB;M{WuNVQ1KM7:TR?= MmTyV2FPT0WU
A253 NFnue3hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{DlSGlEPTB;M{WuO|QzQSEQvF2= MXnTRW5ITVJ?
HCC1599 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUjvVGNLUUN3ME2zOk44ODV|IN88US=> Mor6V2FPT0WU
EB-3 MlvJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3HYSGlEPTB;M{[uPVUyQCEQvF2= NWfSdJFlW0GQR1XS
GOTO MmP0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUTJR|UxRTN5LkOyNlQh|ryP M3vYfnNCVkeHUh?=
SW684 MnGxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2D2eGlEPTB;NEGuPFQ6PSEQvF2= MkP6V2FPT0WU
DEL NIL1W4hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUDCXGlDUUN3ME20Nk4xPTJ{IN88US=> NGPhSXpUSU6JRWK=
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TE-9 MmTZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWLJR|UxRTR|LkS1PVYh|ryP NV\EVZdCW0GQR1XS
KARPAS-45 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlnuTWM2OD12ND6zPVI2KM7:TR?= M2Tl[3NCVkeHUh?=
HAL-01 NEXDUmdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4mxUmlEPTB;NESuOVA{PCEQvF2= MoDrV2FPT0WU
RCC10RGB NWriN|NQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHHibXFKSzVyPUS0Mlc{QTJizszN NFm0Z5BUSU6JRWK=
CP67-MEL M2rLTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUf0eJJVUUN3ME20OU43OjRzIN88US=> MmLRV2FPT0WU
NB17 NEL1W2NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV3JR|UxRTR3Lk[2OFMh|ryP NVzUfZluW0GQR1XS
SK-UT-1 NGLUOYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUjJR|UxRTR3Lkm0OlQh|ryP NUfMbXFYW0GQR1XS
JiyoyeP-2003 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mm\3TWM2OD12Nj6wNVE6KM7:TR?= NVXt[HVnW0GQR1XS
HCE-4 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWL5eoF5UUN3ME20Ok42QTZ6IN88US=> MkPhV2FPT0WU
NCI-H720 NIGzd|dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M37DTWlEPTB;NE[uO|Y5OiEQvF2= MVHTRW5ITVJ?
KARPAS-422 Mn7rS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX6xU3VMUUN3ME20O{4xQDl3IN88US=> MX;TRW5ITVJ?
Ramos-2G6-4C10 MkD2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnT1TWM2OD12Nz6xOlIzKM7:TR?= MkX0V2FPT0WU
HCE-T MnjsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXjJR|UxRTR5Lk[4Nlgh|ryP NUC3ZYNvW0GQR1XS
PSN1 NH\ofYlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUPJR|UxRTR5Lke4NVMh|ryP M2\nPXNCVkeHUh?=

... 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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