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 NWPZc4tkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUHJR|UxRTBwME[xOFMh|ryP NI\ENVlUSU6JRWK=
LAMA-84 NYrRRnBGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX7JR|UxRTBwMUW5PUDPxE1? Mke0V2FPT0WU
MEG-01 NWfMepp1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXHL[4cxUUN3ME2wMlI{Pjh6IN88US=> NGPo[5BUSU6JRWK=
EM-2 M2DHNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX;JR|UxRTBwMk[1JO69VQ>? M2q5OXNCVkeHUh?=
TE-15 M{TLSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mlv2TWM2OD1yLkK3OFEzKM7:TR?= M1vEUnNCVkeHUh?=
NCI-H1648 Ml3tS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4PEdGlEPTB;MD6yPFEyPiEQvF2= MkPuV2FPT0WU
TE-12 M{D2R2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M17DXWlEPTB;MD6zNlY5KM7:TR?= M{PyWnNCVkeHUh?=
LB996-RCC NWH0bFVLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV3JR|UxRTBwNESxPVYh|ryP NHXoUZVUSU6JRWK=
K-562 M1y4eGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWDJR|UxRTBwNES5Olch|ryP Mnf1V2FPT0WU
D-336MG MofkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX\vb5FVUUN3ME2wMlUxOzB2IN88US=> NGrRUWpUSU6JRWK=
NOS-1 M17oNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVLJR|UxRTBwNkC1Nlkh|ryP Mme3V2FPT0WU
EW-24 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2\zUWlEPTB;MD62NlY6OyEQvF2= NH3lOVlUSU6JRWK=
BV-173 M3HMS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3\aSGlEPTB;MD62OVI1QSEQvF2= MWnTRW5ITVJ?
NCCIT MoHuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlnMTWM2OD1yLkezNlE5KM7:TR?= NX\ETWhOW0GQR1XS
NCI-H1436 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF;ITIhKSzVyPUCuO|kxPDlizszN NVfs[GJpW0GQR1XS
BB30-HNC MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX;JR|UxRTBwOE[yNFMh|ryP MkPRV2FPT0WU
TE-8 Mnq0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NY\t[VJWUUN3ME2wMlg4Ojd3IN88US=> NF:4cW5USU6JRWK=
A704 NUjUV5NbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIjmbWhKSzVyPUCuPFkzOSEQvF2= M3jLSnNCVkeHUh?=
TK10 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV\L[WdTUUN3ME2wMlkxPjZ7IN88US=> NVzHSG9IW0GQR1XS
KS-1 NYLsXYxIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYXH[WVxUUN3ME2xMlE6Pzd7IN88US=> MoDtV2FPT0WU
C2BBe1 MlTDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1O4U2lEPTB;MT6yNFUxPyEQvF2= NIixXoNUSU6JRWK=
RXF393 NUXUd4tWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4jyfWlEPTB;MT6yOFM3KM7:TR?= MVfTRW5ITVJ?
KGN M2\Kfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV7hTXJzUUN3ME2xMlI4Pjh5IN88US=> MnvpV2FPT0WU
NB69 NXvTb4lIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1TnRmlEPTB;MT6zO|Q6PyEQvF2= M372O3NCVkeHUh?=
TE-11 M1\5O2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoHpTWM2OD1zLkSzOFE5KM7:TR?= MXHTRW5ITVJ?
TE-1 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{K3fWlEPTB;MT60OFExPSEQvF2= M16ySnNCVkeHUh?=
ST486 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXLJR|UxRTFwNEW4OVIh|ryP NIfGbnNUSU6JRWK=
HOP-62 NX3TSHRQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mm\pTWM2OD1zLkWwNlQ3KM7:TR?= MVHTRW5ITVJ?
EW-16 M2Hzbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NELqVolKSzVyPUGuOVUxQDNizszN MoTNV2FPT0WU
LB1047-RCC MmjUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWrJR|UxRTFwNUW0OVMh|ryP NVvmfZh6W0GQR1XS
TE-10 NUP1dG44T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2PYc2lEPTB;MT62OlI2OiEQvF2= M1;ZPXNCVkeHUh?=
RL95-2 M1ryOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2nkSWlEPTB;MT62OlkxOiEQvF2= MWjTRW5ITVJ?
DOHH-2 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmXSTWM2OD1zLkexO|gzKM7:TR?= Mlv6V2FPT0WU
MFH-ino MkXPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NI\mTJFKSzVyPUGuO|c5PyEQvF2= M4T1bnNCVkeHUh?=
GB-1 NELZ[INIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYHj[5NjUUN3ME2xMlc6QDN|IN88US=> M2TnbHNCVkeHUh?=
SK-N-DZ NUPOSI1GT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3XmOmlEPTB;MT64OFY5QCEQvF2= M2CwZnNCVkeHUh?=
OS-RC-2 Mk\WS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mnj4TWM2OD1zLki4OVc1KM7:TR?= NHj2bIpUSU6JRWK=
SW982 NXf1bVd6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWDH[WFuUUN3ME2xMlkzODl|IN88US=> MnLjV2FPT0WU
KALS-1 NF;uUXpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoHZTWM2OD1zLkm4O|IzKM7:TR?= MWrTRW5ITVJ?
TGBC24TKB NFT1dZpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Moe0TWM2OD1{LkC1PVU5KM7:TR?= MUfTRW5ITVJ?
GI-1 M1jQS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXPJR|UxRTJwMU[wPFQh|ryP MkCzV2FPT0WU
SW962 M33GWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlG4TWM2OD1{LkG3NVc5KM7:TR?= MWDTRW5ITVJ?
SW872 NGDE[4NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnruTWM2OD1{LkG4OVA4KM7:TR?= NGDTNFFUSU6JRWK=
NCI-H747 Ml;uS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkT4TWM2OD1{LkK1O|E1KM7:TR?= M1PWNXNCVkeHUh?=
MZ1-PC MlvBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmXTTWM2OD1{LkK5N|U3KM7:TR?= MUnTRW5ITVJ?
MSTO-211H Ml64S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIWxNWRKSzVyPUKuN|U4OjNizszN MlizV2FPT0WU
BL-70 MmH4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYLFc5VoUUN3ME2yMlQ4PDJ{IN88US=> NH20UVVUSU6JRWK=
SW954 NIjtb2dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3vLR2lEPTB;Mj61O|QxQCEQvF2= NYS0SVA4W0GQR1XS
SNB75 NGPScohIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVnJR|UxRTJwNki1PVQh|ryP MYjTRW5ITVJ?
IST-SL2 NHq4OWVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnHZTWM2OD1{LkeyN|c6KM7:TR?= M3[wOHNCVkeHUh?=
GCIY NFKxNFRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkTGTWM2OD1{Lki3NFA2KM7:TR?= NXu4TGFQW0GQR1XS
KU812 NYfXUFNuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV\JR|UxRTNwMEWyPVkh|ryP NGDLXVVUSU6JRWK=
LXF-289 NV3tfXV3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVWyXVhrUUN3ME2zMlEzOTB7IN88US=> NIPNSHJUSU6JRWK=
ETK-1 M3HlTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{HDSGlEPTB;Mz6yNFc3PyEQvF2= NIKwWIhUSU6JRWK=
SF126 NF\2d49Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVTGNG95UUN3ME2zMlMyOTd2IN88US=> M2Kxd3NCVkeHUh?=
LC-2-ad NVvFWGJzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVXJR|UxRTNwNUW3JO69VQ>? NF3zc3FUSU6JRWK=
KNS-42 NHTyVIlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mlq0TWM2OD1|Lk[1JO69VQ>? MoC3V2FPT0WU
OVCAR-4 NH3vbVRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFL5OGdKSzVyPUOuO|M1OzNizszN M3[yZnNCVkeHUh?=
PF-382 NVfLRlhJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoLaTWM2OD1|LkizOlk5KM7:TR?= M3fpfHNCVkeHUh?=
SH-4 NWmweXhDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYrJR|UxRTRwMkWyOVkh|ryP NVvtN45RW0GQR1XS
KM12 NHjjeWFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXu5c3kxUUN3ME20MlMzPDF4IN88US=> M3vQWXNCVkeHUh?=
NB5 MnLvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHuyWmVKSzVyPUSuOFE5PjRizszN NF7lfo1USU6JRWK=
KURAMOCHI NHrIOJVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVrJR|UxRTRwNkWyOVYh|ryP NHmwO|FUSU6JRWK=
Becker NYS5N3RFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVjJR|UxRTRwNk[0NVYh|ryP M4TufnNCVkeHUh?=
MV-4-11 MmHOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIn1[2lKSzVyPUSuPFE{PDRizszN NEDVWmFUSU6JRWK=
KINGS-1 MonpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1rIWWlEPTB;ND64NlM4OyEQvF2= MWXTRW5ITVJ?
LS-123 MlPhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFv4fo5KSzVyPUWuOFk3QDRizszN NWDycZN4W0GQR1XS
SF268 NIDoZ29Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn\MTWM2OD13Lk[xNlYzKM7:TR?= MVTTRW5ITVJ?
A388 NVTINZBsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEXLeI1KSzVyPUWuOlM3PjdizszN M4\RTXNCVkeHUh?=
NMC-G1 M{HaV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWLjfG81UUN3ME22MlAyQDFzIN88US=> NFHHfWpUSU6JRWK=
CGTH-W-1 NUXaU2lRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWHJR|UxRTZwMEKwO|Uh|ryP M{\TbXNCVkeHUh?=
ES4 MnLHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUX6cVZLUUN3ME22MlU{ODd2IN88US=> NYTmbWRCW0GQR1XS
SR M1LzXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml;2TWM2OD14LkW4PFA4KM7:TR?= MUTTRW5ITVJ?
BB49-HNC NEDpeWVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MULJR|UxRTZwN{OyNFYh|ryP M2D2W3NCVkeHUh?=
KLE NV2wdnpLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2O1UWlEPTB;Nj63PFM4PyEQvF2= M3TWXHNCVkeHUh?=
HUTU-80 NUfWSVBbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmKyTWM2OD14Lkm4OFY3KM7:TR?= M4D6ZnNCVkeHUh?=
SNU-C2B MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2rncGlEPTB;Nz64Nlc{PyEQvF2= NXLCW3JVW0GQR1XS
BB65-RCC MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVPvN5I6UUN3ME23Mlk1QTB2IN88US=> MVHTRW5ITVJ?
QIMR-WIL MkPXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{DiNmlEPTB;OD60NlgxQCEQvF2= NVfmbYVsW0GQR1XS
GDM-1 M1LWcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3LMNGlEPTB;OD65O|I6OiEQvF2= NX[1PWZFW0GQR1XS
LC4-1 M3\zN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mkm2TWM2OD17LkCwPVEyKM7:TR?= NX7LfWhRW0GQR1XS
MLMA NFziRlhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnPGTWM2OD17LkG1NFA3KM7:TR?= NIG1WVJUSU6JRWK=
EoL-1-cell NYO1VVBOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF3pSmFKSzVyPUmuN|AyQTJizszN NHjUe5RUSU6JRWK=
BOKU MoezS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGDBZXdKSzVyPUmuPVY1PjZizszN M2e4bnNCVkeHUh?=
EVSA-T MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWrJR|UxRTFyLk[1Olgh|ryP MYjTRW5ITVJ?
D-283MED NUjIe5p[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoDITWM2OD1zMD65NVc3KM7:TR?= MnXGV2FPT0WU
NB1 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml\NTWM2OD1zMT6wNlQzKM7:TR?= NVv4WmFiW0GQR1XS
RPMI-8402 M{nTXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M174fmlEPTB;MUGuNVc5KM7:TR?= MWXTRW5ITVJ?
NCI-H1355 MlK3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYrJR|UxRTFzLkG4NFYh|ryP M2fQU3NCVkeHUh?=
NB7 M{XiVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXPJR|UxRTFzLkOyPVch|ryP NUPVW3UxW0GQR1XS
RPMI-6666 NHnpTYtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkSzTWM2OD1zMj65OVY4KM7:TR?= MXHTRW5ITVJ?
697 NXPGVXQxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWTXXIlNUUN3ME2xN{4zPzBzIN88US=> Ml;aV2FPT0WU
CTB-1 NGTFUFRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWLJR|UxRTF|LkW5OFgh|ryP NWfNPVFrW0GQR1XS
VA-ES-BJ NYPvWGxtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXSyRW8{UUN3ME2xN{46OjN2IN88US=> MkLoV2FPT0WU
BE-13 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWLJR|UxRTF2LkO5NVUh|ryP MWPTRW5ITVJ?
SKM-1 MkG5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4XDZ2lEPTB;MUSuOFQ6QSEQvF2= MoDMV2FPT0WU
TE-6 NGHxd4RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlfnTWM2OD1zND63OVkyKM7:TR?= MmS5V2FPT0WU
LB771-HNC NYTLS486T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2GzZWlEPTB;MUSuO|g6QCEQvF2= M3TFU3NCVkeHUh?=
ECC4 MkWzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4nLZ2lEPTB;MUeuNFI4PyEQvF2= NH74fZVUSU6JRWK=
ES3 M{Pxe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmezTWM2OD1zNz60OlU2KM7:TR?= M3flUHNCVkeHUh?=
LB647-SCLC NFzWZlhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmXvTWM2OD1zNz60PVQ6KM7:TR?= M4XMbHNCVkeHUh?=
NB10 NVfLWZU1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV7JR|UxRTF6LkWyOVYh|ryP MWTTRW5ITVJ?
L-540 NVPFT3BFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUjudnBzUUN3ME2xPE45OTB7IN88US=> NFjYOGFUSU6JRWK=
NCI-H2126 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlXnTWM2OD1zOT61NUDPxE1? NYH0dmtvW0GQR1XS
HH M3S0ZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkDsTWM2OD1{MD6wNFk6KM7:TR?= M1TsOHNCVkeHUh?=
MPP-89 NG[1WYdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1yyfGlEPTB;MkOuNlI5QSEQvF2= MnW5V2FPT0WU
IST-MEL1 NX23VpNIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3[4XmlEPTB;MkOuPFY2QCEQvF2= MYfTRW5ITVJ?
KP-N-YS NILwTIlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1v3VmlEPTB;MkOuPVI2PSEQvF2= M4n3bnNCVkeHUh?=
EC-GI-10 NGfaOJpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{n0eGlEPTB;MkSuOVk5QSEQvF2= MlPCV2FPT0WU
EKVX M1O3eWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkLLTWM2OD1{Nj6wNlA{KM7:TR?= M{\2SHNCVkeHUh?=
TGBC1TKB MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXrJR|UxRTJ4LkSzOEDPxE1? MlzsV2FPT0WU
Daudi M2X3Umdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmC4TWM2OD1{Nz6wO|c{KM7:TR?= NG\lb5RUSU6JRWK=
ALL-PO NUXKcIZHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4PVSmlEPTB;MkeuNFgyKM7:TR?= MnnHV2FPT0WU
NB6 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIfaXJhKSzVyPUK3MlQ5QCEQvF2= M4fRWXNCVkeHUh?=
ES6 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{PhcWlEPTB;MkeuPVEzOyEQvF2= M4L3XHNCVkeHUh?=
COLO-320-HSR NWjwRVFST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYjJR|UxRTJ6LkCzO|Mh|ryP MUnTRW5ITVJ?
K5 NVLRdYhST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkWwTWM2OD1{OD6xNlg4KM7:TR?= MYPTRW5ITVJ?
ES1 NGTFU2ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlHBTWM2OD1{OD63O|c{KM7:TR?= Moq4V2FPT0WU
LC-1F NGrKXphIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFe5WJdKSzVyPUK5Mlc{PDZizszN MXvTRW5ITVJ?
SCLC-21H Mke1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1Ph[GlEPTB;M{CuO|MyPyEQvF2= NV3UdVhVW0GQR1XS
SK-PN-DW M3jJdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoHZTWM2OD1|Mj61OVk5KM7:TR?= MUjTRW5ITVJ?
D-247MG NVXZWWp4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnPVTWM2OD1|Mj65O|c{KM7:TR?= NXPMV4JnW0GQR1XS
TE-5 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUe3UpRKUUN3ME2zN{4xOzZ{IN88US=> NXK4T5JVW0GQR1XS
MONO-MAC-6 NG\tbGxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWnJR|UxRTN|LkWwOFgh|ryP MnTSV2FPT0WU
LB2518-MEL M{LuNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmPpTWM2OD1|Mz63OlY3KM7:TR?= M13Z[nNCVkeHUh?=
LOXIMVI NXfMWIRmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnvXTWM2OD1|Mz63PVI5KM7:TR?= M3rG[nNCVkeHUh?=
NCI-H209 MoL4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVjJR|UxRTN3LkG0OEDPxE1? NIroSZRUSU6JRWK=
A253 MkHrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWLJR|UxRTN3Lke0Nlkh|ryP M2D6eHNCVkeHUh?=
HCC1599 Mm\zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3zxXmlEPTB;M{[uO|A2OyEQvF2= NG\3dGFUSU6JRWK=
EB-3 M37VZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkO4TWM2OD1|Nj65OVE5KM7:TR?= MULTRW5ITVJ?
GOTO NXKzc4o4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFLsc5pKSzVyPUO3MlMzOjRizszN M4HHcHNCVkeHUh?=
SW684 M4izfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnrXTWM2OD12MT64OFk2KM7:TR?= MkXhV2FPT0WU
DEL MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2e0R2lEPTB;NEKuNFUzOiEQvF2= MXLTRW5ITVJ?
HT-144 MlTrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV3JR|UxRTR{LkG2O|Yh|ryP MojSV2FPT0WU
TE-9 M2fJemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mmm3TWM2OD12Mz60OVk3KM7:TR?= NHjZZpFUSU6JRWK=
KARPAS-45 NHjjcoFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnT5TWM2OD12ND6zPVI2KM7:TR?= NGXMOnFUSU6JRWK=
HAL-01 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIeyN3dKSzVyPUS0MlUxOzRizszN M4TiNnNCVkeHUh?=
RCC10RGB MoS0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYHpbVZSUUN3ME20OE44Ozl{IN88US=> M1\pUHNCVkeHUh?=
CP67-MEL NH\sPFhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVW4fnRkUUN3ME20OU43OjRzIN88US=> MX7TRW5ITVJ?
NB17 MnnVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYjJR|UxRTR3Lk[2OFMh|ryP NV[4dGtGW0GQR1XS
SK-UT-1 NWn2SHRTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHPzRWZKSzVyPUS1Mlk1PjRizszN M4XmNXNCVkeHUh?=
JiyoyeP-2003 M2TaZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIPpfo9KSzVyPUS2MlAyOTlizszN MWPTRW5ITVJ?
HCE-4 NEXhS4VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUi4T|JMUUN3ME20Ok42QTZ6IN88US=> NU\sN|lRW0GQR1XS
NCI-H720 M3;mVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmPFTWM2OD12Nj63OlgzKM7:TR?= MlK3V2FPT0WU
KARPAS-422 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3v4ZWlEPTB;NEeuNFg6PSEQvF2= NFX0cIVUSU6JRWK=
Ramos-2G6-4C10 NUX3cpV{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYPJR|UxRTR5LkG2NlIh|ryP MoLhV2FPT0WU
HCE-T NGGxfJdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnLITWM2OD12Nz62PFI5KM7:TR?= MnznV2FPT0WU
PSN1 M3PFNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWrieW1LUUN3ME20O{44QDF|IN88US=> NVPxUJdVW0GQR1XS

... 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 warmed (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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Rating
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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Rating
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 (33)

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