Saracatinib (AZD0530)

For research use only. Not for use in humans.

製品コードS1006

Saracatinib (AZD0530)化学構造

分子量(MW):542.03

Saracatinib (AZD0530) is a potent Src inhibitor with IC50 of 2.7 nM in cell-free assays, and potent to c-Yes, Fyn, Lyn, Blk, Fgr and Lck; less active for Abl and EGFR (L858R and L861Q). Saracatinib induces autophagy. Phase 2/3.

サイズ 価格(税別) 在庫  
10mM (1mL in DMSO) JPY 17100 あり
JPY 13600 あり
JPY 30200 あり
JPY 113200 あり
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バルク問合せ

文献中Selleckの製品使用例(189)

製品安全説明書

Src阻害剤の選択性比較

生物活性

製品説明 Saracatinib (AZD0530) is a potent Src inhibitor with IC50 of 2.7 nM in cell-free assays, and potent to c-Yes, Fyn, Lyn, Blk, Fgr and Lck; less active for Abl and EGFR (L858R and L861Q). Saracatinib induces autophagy. Phase 2/3.
特性 The 1st Src inhibitor to show inhibition of the Src pathway in human tumor tissue.
ターゲット
c-Src [2]
(Cell-free assay)
LCK [2]
(Cell-free assay)
c-YES [2]
(Cell-free assay)
EGFR (L861Q) [2]
(Cell-free assay)
Lyn [2]
(Cell-free assay)
2.7 nM <4 nM 4 nM 4 nM 5 nM
体外試験

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]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
CTV-1 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWHG[5JbUUN3ME2wMlA3OTR|IN88US=> MWTTRW5ITVJ?
LAMA-84 NFLkR5JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MW\JR|UxRTBwMUW5PUDPxE1? NWLIZo52W0GQR1XS
MEG-01 MnfCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUnJR|UxRTBwMkO2PFgh|ryP NX:x[ZRNW0GQR1XS
EM-2 Mnf6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{TiTWlEPTB;MD6yOlUh|ryP M1TZNXNCVkeHUh?=
TE-15 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXTJR|UxRTBwMke0NVIh|ryP MUTTRW5ITVJ?
NCI-H1648 MkTSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4LpOGlEPTB;MD6yPFEyPiEQvF2= M{DXVnNCVkeHUh?=
TE-12 NEXRZW9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVHJR|UxRTBwM{K2PEDPxE1? M3\XXHNCVkeHUh?=
LB996-RCC M4[ySGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmXvTWM2OD1yLkS0NVk3KM7:TR?= Ml:2V2FPT0WU
K-562 MlzVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEP6PW9KSzVyPUCuOFQ6PjdizszN NEjpT3FUSU6JRWK=
D-336MG MorKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUO0SItLUUN3ME2wMlUxOzB2IN88US=> M3;hZ3NCVkeHUh?=
NOS-1 M3XadWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEPuS49KSzVyPUCuOlA2OjlizszN MYnTRW5ITVJ?
EW-24 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGf0U5BKSzVyPUCuOlI3QTNizszN NIS3e4lUSU6JRWK=
BV-173 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4XoT2lEPTB;MD62OVI1QSEQvF2= NFfBUHpUSU6JRWK=
NCCIT NEfJbo5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX;6NJZnUUN3ME2wMlc{OjF6IN88US=> M2LRO3NCVkeHUh?=
NCI-H1436 NIHsOW9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYrNUZV4UUN3ME2wMlc6ODR7IN88US=> MkPZV2FPT0WU
BB30-HNC NXO2VYpWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGjFOY1KSzVyPUCuPFYzODNizszN NVnJfZNMW0GQR1XS
TE-8 M3HkWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M17NPGlEPTB;MD64O|I4PSEQvF2= M{HPbnNCVkeHUh?=
A704 Mn\ES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUD0VWtbUUN3ME2wMlg6OjFizszN NU\uenNLW0GQR1XS
TK10 NFrFe2hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn3ETWM2OD1yLkmwOlY6KM7:TR?= NFTHTVRUSU6JRWK=
KS-1 M3fGTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUL3WYU{UUN3ME2xMlE6Pzd7IN88US=> MmLIV2FPT0WU
C2BBe1 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFX1bnhKSzVyPUGuNlA2ODdizszN Ml64V2FPT0WU
RXF393 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXfKWlBqUUN3ME2xMlI1OzZizszN Mkm1V2FPT0WU
KGN MoCzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWrJR|UxRTFwMke2PFch|ryP MVvTRW5ITVJ?
NB69 NGrpRnlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV;JR|UxRTFwM{e0PVch|ryP NYXpTWsyW0GQR1XS
TE-11 Mkm0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml;BTWM2OD1zLkSzOFE5KM7:TR?= NX\vV|U5W0GQR1XS
TE-1 MmfuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX\ZTmh[UUN3ME2xMlQ1OTB3IN88US=> MXfTRW5ITVJ?
ST486 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXHJR|UxRTFwNEW4OVIh|ryP NWL3UJM5W0GQR1XS
HOP-62 M{T3N2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVW5V5pyUUN3ME2xMlUxOjR4IN88US=> MVfTRW5ITVJ?
EW-16 MnjpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmPQTWM2OD1zLkW1NFg{KM7:TR?= NFjOOHJUSU6JRWK=
LB1047-RCC MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{nxSWlEPTB;MT61OVQ2OyEQvF2= MlfoV2FPT0WU
TE-10 M{jEOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUftS5JmUUN3ME2xMlY3OjV{IN88US=> M1;abnNCVkeHUh?=
RL95-2 NF[wWFZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWj3W2s{UUN3ME2xMlY3QTB{IN88US=> NXSxc5RiW0GQR1XS
DOHH-2 NIjxeHhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVvJR|UxRTFwN{G3PFIh|ryP MlXwV2FPT0WU
MFH-ino NFTlRlVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4L0WGlEPTB;MT63O|g4KM7:TR?= Mn;wV2FPT0WU
GB-1 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGHEZVdKSzVyPUGuO|k5OzNizszN NIHaeZpUSU6JRWK=
SK-N-DZ MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVfFNHVZUUN3ME2xMlg1Pjh6IN88US=> MXvTRW5ITVJ?
OS-RC-2 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoTPTWM2OD1zLki4OVc1KM7:TR?= MYHTRW5ITVJ?
SW982 MmTRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlHwTWM2OD1zLkmyNFk{KM7:TR?= NYqz[nhjW0GQR1XS
KALS-1 NYfjNVl1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mly2TWM2OD1zLkm4O|IzKM7:TR?= M{LqWHNCVkeHUh?=
TGBC24TKB NHnsOFlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3HwVmlEPTB;Mj6wOVk2QCEQvF2= NGO5UVdUSU6JRWK=
GI-1 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYfEPFhsUUN3ME2yMlE3ODh2IN88US=> M{noSHNCVkeHUh?=
SW962 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mkf5TWM2OD1{LkG3NVc5KM7:TR?= NUji[XZtW0GQR1XS
SW872 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWTh[ZkyUUN3ME2yMlE5PTB5IN88US=> NUTjcnJ{W0GQR1XS
NCI-H747 NYDlTW1{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2ni[2lEPTB;Mj6yOVcyPCEQvF2= MlzHV2FPT0WU
MZ1-PC NVvDbHR1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFH2[|ZKSzVyPUKuNlk{PTZizszN M2PL[XNCVkeHUh?=
MSTO-211H NIfKS4pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmGxTWM2OD1{LkO1O|I{KM7:TR?= MonPV2FPT0WU
BL-70 NHPBNmFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEDIVZZKSzVyPUKuOFc1OjJizszN NXTTXWJlW0GQR1XS
SW954 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVj1U25ZUUN3ME2yMlU4PDB6IN88US=> NWLwU5dOW0GQR1XS
SNB75 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mki0TWM2OD1{Lk[4OVk1KM7:TR?= MmrLV2FPT0WU
IST-SL2 M{TTcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2fH[WlEPTB;Mj63NlM4QSEQvF2= MYHTRW5ITVJ?
GCIY MkPsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF;ZNmNKSzVyPUKuPFcxODVizszN NITIb45USU6JRWK=
KU812 NIT3eWdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlfNTWM2OD1|LkC1Nlk6KM7:TR?= M2HheHNCVkeHUh?=
LXF-289 NI\LfnRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NELLZXBKSzVyPUOuNVIyODlizszN MX7TRW5ITVJ?
ETK-1 M2O3SWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWfJR|UxRTNwMkC3Olch|ryP M4L1N3NCVkeHUh?=
SF126 M1jIPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVPD[WM3UUN3ME2zMlMyOTd2IN88US=> M13We3NCVkeHUh?=
LC-2-ad MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX3JR|UxRTNwNUW3JO69VQ>? M1OxSHNCVkeHUh?=
KNS-42 M13VTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHzqOXBKSzVyPUOuOlUh|ryP M17uS3NCVkeHUh?=
OVCAR-4 NHLBe3NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXjJR|UxRTNwN{O0N|Mh|ryP NFrzNm5USU6JRWK=
PF-382 NHP4cZJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoTkTWM2OD1|LkizOlk5KM7:TR?= MmTwV2FPT0WU
SH-4 NHTGbIVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NITjfoNKSzVyPUSuNlUzPTlizszN MmTqV2FPT0WU
KM12 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVjQUZJIUUN3ME20MlMzPDF4IN88US=> NVG0UIl{W0GQR1XS
NB5 M3f6dmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHjEV41KSzVyPUSuOFE5PjRizszN M{fzSHNCVkeHUh?=
KURAMOCHI M1rHZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlvQTWM2OD12Lk[1NlU3KM7:TR?= MWnTRW5ITVJ?
Becker NUfVZo43T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUDJR|UxRTRwNk[0NVYh|ryP MVnTRW5ITVJ?
MV-4-11 Mk\xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{HaOmlEPTB;ND64NVM1PCEQvF2= NIfLO3RUSU6JRWK=
KINGS-1 MkTLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2D5dWlEPTB;ND64NlM4OyEQvF2= NEHTXWlUSU6JRWK=
LS-123 NYjBWlZ1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWnJR|UxRTVwNEm2PFQh|ryP MnHCV2FPT0WU
SF268 NGrPVoZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV\IZnlXUUN3ME21MlYyOjZ{IN88US=> NYjB[ZZ7W0GQR1XS
A388 NGHjSIZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYTJR|UxRTVwNkO2Olch|ryP NVHaWlBtW0GQR1XS
NMC-G1 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4X3ZmlEPTB;Nj6wNVgyOSEQvF2= NG\H[mxUSU6JRWK=
CGTH-W-1 MoXKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4SyZWlEPTB;Nj6wNlA4PSEQvF2= MYjTRW5ITVJ?
ES4 NGf5d5BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlHaTWM2OD14LkWzNFc1KM7:TR?= NW\ycmZPW0GQR1XS
SR NILId45Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXXsOWd3UUN3ME22MlU5QDB5IN88US=> M4\rS3NCVkeHUh?=
BB49-HNC MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NG[wVHpKSzVyPU[uO|MzODZizszN NV7nbYZZW0GQR1XS
KLE MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIO4dXZKSzVyPU[uO|g{PzdizszN Mm\yV2FPT0WU
HUTU-80 M2nRc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn\TTWM2OD14Lkm4OFY3KM7:TR?= M3;nO3NCVkeHUh?=
SNU-C2B M1\yemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF;lcoZKSzVyPUeuPFI4OzdizszN M333d3NCVkeHUh?=
BB65-RCC NFWySm5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NImyT2lKSzVyPUeuPVQ6ODRizszN M{TDV3NCVkeHUh?=
QIMR-WIL MnzSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnTvTWM2OD16LkSyPFA5KM7:TR?= MUXTRW5ITVJ?
GDM-1 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MW\JR|UxRThwOUeyPVIh|ryP M1X0ZXNCVkeHUh?=
LC4-1 MmPNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVjJR|UxRTlwMEC5NVEh|ryP MnmwV2FPT0WU
MLMA MljaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVzJR|UxRTlwMUWwNFYh|ryP NEXLb2VUSU6JRWK=
EoL-1-cell Mlu2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXnJR|UxRTlwM{CxPVIh|ryP MWLTRW5ITVJ?
BOKU NGDW[FVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYLJR|UxRTlwOU[0OlYh|ryP Mkj3V2FPT0WU
EVSA-T MnjTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUXJR|UxRTFyLk[1Olgh|ryP NH3jWWpUSU6JRWK=
D-283MED NE\wNVBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2jKUWlEPTB;MUCuPVE4PiEQvF2= M3zsVXNCVkeHUh?=
NB1 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXzJR|UxRTFzLkCyOFIh|ryP MkT4V2FPT0WU
RPMI-8402 NWDWdmF{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1TyWWlEPTB;MUGuNVc5KM7:TR?= Mo\DV2FPT0WU
NCI-H1355 NVnPe5VFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3TuRmlEPTB;MUGuNVgxPiEQvF2= MYPTRW5ITVJ?
NB7 NVHnW4prT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWTvSZhEUUN3ME2xNU4{Ojl5IN88US=> MV7TRW5ITVJ?
RPMI-6666 Mk[3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2f4bWlEPTB;MUKuPVU3PyEQvF2= NVnrSYRzW0GQR1XS
697 NFfuXmtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4\yU2lEPTB;MUOuNlcxOSEQvF2= MXnTRW5ITVJ?
CTB-1 M1HPZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUfJR|UxRTF|LkW5OFgh|ryP M1m2NXNCVkeHUh?=
VA-ES-BJ MlS2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXzJR|UxRTF|LkmyN|Qh|ryP MorRV2FPT0WU
BE-13 NYfOVpdwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF;FS4tKSzVyPUG0MlM6OTVizszN M13UbXNCVkeHUh?=
SKM-1 NIPDXZZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3fvVGlEPTB;MUSuOFQ6QSEQvF2= MXPTRW5ITVJ?
TE-6 NVq3SWp4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYWyU45oUUN3ME2xOE44PTlzIN88US=> NIflTINUSU6JRWK=
LB771-HNC NVXXc5UyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEiyemJKSzVyPUG0Mlc5QThizszN MmnUV2FPT0WU
ECC4 NYnoSGZ2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4\KeWlEPTB;MUeuNFI4PyEQvF2= MlfqV2FPT0WU
ES3 MnnTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHPGTWlKSzVyPUG3MlQ3PTVizszN NGjJT3FUSU6JRWK=
LB647-SCLC M4f3OWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2HaSmlEPTB;MUeuOFk1QSEQvF2= NVTrXJFMW0GQR1XS
NB10 M1rOfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXXJR|UxRTF6LkWyOVYh|ryP NUn2XmZrW0GQR1XS
L-540 MmLyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVLjS3NmUUN3ME2xPE45OTB7IN88US=> NH\rR2FUSU6JRWK=
NCI-H2126 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYPJR|UxRTF7LkWxJO69VQ>? MkHaV2FPT0WU
HH NYXpV3NjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHPLSZdKSzVyPUKwMlAxQTlizszN MWnTRW5ITVJ?
MPP-89 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mmi4TWM2OD1{Mz6yNlg6KM7:TR?= NWLNbVRwW0GQR1XS
IST-MEL1 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnvGTWM2OD1{Mz64OlU5KM7:TR?= MmD3V2FPT0WU
KP-N-YS MlLxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV\JR|UxRTJ|LkmyOVUh|ryP NH3HdphUSU6JRWK=
EC-GI-10 M4Lxe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYDwfHFJUUN3ME2yOE42QTh7IN88US=> MYfTRW5ITVJ?
EKVX MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH:w[XRKSzVyPUK2MlAzODNizszN NGLVbYtUSU6JRWK=
TGBC1TKB MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlHWTWM2OD1{Nj60N|Qh|ryP MU\TRW5ITVJ?
Daudi NX;RVlRDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2HuRmlEPTB;MkeuNFc4OyEQvF2= MY\TRW5ITVJ?
ALL-PO M{TKc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1TH[GlEPTB;MkeuNFgyKM7:TR?= NFjXblhUSU6JRWK=
NB6 NX35SY5[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn3jTWM2OD1{Nz60PFgh|ryP NVXmWW86W0GQR1XS
ES6 Mnz2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXTySYRMUUN3ME2yO{46OTJ|IN88US=> NF;kS|FUSU6JRWK=
COLO-320-HSR MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkHvTWM2OD1{OD6wN|c{KM7:TR?= MV\TRW5ITVJ?
K5 MmroS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH;WSW1KSzVyPUK4MlEzQDdizszN MmfRV2FPT0WU
ES1 NUjDcZhHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUjpN2J4UUN3ME2yPE44Pzd|IN88US=> NFe0OJhUSU6JRWK=
LC-1F NVf1cldCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXrJR|UxRTJ7LkezOFYh|ryP M2G1UHNCVkeHUh?=
SCLC-21H MofZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVLB[nJTUUN3ME2zNE44OzF5IN88US=> MWrTRW5ITVJ?
SK-PN-DW MoS5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVHJR|UxRTN{LkW1PVgh|ryP MVnTRW5ITVJ?
D-247MG M{XZT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3rDOWlEPTB;M{KuPVc4OyEQvF2= MUDTRW5ITVJ?
TE-5 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3[0RmlEPTB;M{OuNFM3OiEQvF2= Mlr3V2FPT0WU
MONO-MAC-6 NFP2V2RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYPJR|UxRTN|LkWwOFgh|ryP M{H1VXNCVkeHUh?=
LB2518-MEL NULm[pNGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXnJR|UxRTN|Lke2OlYh|ryP NHHIOYRUSU6JRWK=
LOXIMVI NGPVVY9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVrJR|UxRTN|Lke5Nlgh|ryP M3zFU3NCVkeHUh?=
NCI-H209 NYeyXmxQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUHJR|UxRTN3LkG0OEDPxE1? NFzqfoFUSU6JRWK=
A253 Mkn1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUG4dZUyUUN3ME2zOU44PDJ7IN88US=> NWPIT4tpW0GQR1XS
HCC1599 Mk[2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVHJR|UxRTN4LkewOVMh|ryP NXfDTItJW0GQR1XS
EB-3 Mm\uS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWLJR|UxRTN4Lkm1NVgh|ryP M{DkXXNCVkeHUh?=
GOTO M1y5XGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3\rTmlEPTB;M{euN|IzPCEQvF2= NGTBTlFUSU6JRWK=
SW684 M3PsZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGTMSlJKSzVyPUSxMlg1QTVizszN NVHGdY1DW0GQR1XS
DEL NHW4NnBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mo[5TWM2OD12Mj6wOVIzKM7:TR?= MYPTRW5ITVJ?
HT-144 NUHXWJlNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2fsVGlEPTB;NEKuNVY4PiEQvF2= M{\VeHNCVkeHUh?=
TE-9 M4DhPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVf2UXV2UUN3ME20N{41PTl4IN88US=> MUTTRW5ITVJ?
KARPAS-45 M2XyVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkTiTWM2OD12ND6zPVI2KM7:TR?= NGrx[G1USU6JRWK=
HAL-01 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYf0Om1UUUN3ME20OE42ODN2IN88US=> NYPRPYtpW0GQR1XS
RCC10RGB MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWDT[pM2UUN3ME20OE44Ozl{IN88US=> NFTOZ4pUSU6JRWK=
CP67-MEL MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NW\xfWh1UUN3ME20OU43OjRzIN88US=> MVjTRW5ITVJ?
NB17 Mn;zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX;6TYZSUUN3ME20OU43PjR|IN88US=> NH7v[lZUSU6JRWK=
SK-UT-1 NUjB[5FxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1radGlEPTB;NEWuPVQ3PCEQvF2= NGC1clBUSU6JRWK=
JiyoyeP-2003 NWi5XVVqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoTzTWM2OD12Nj6wNVE6KM7:TR?= NULYTXk1W0GQR1XS
HCE-4 NH;0Z41Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYLoT3ZRUUN3ME20Ok42QTZ6IN88US=> Mor0V2FPT0WU
NCI-H720 NXX4[5pzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYryfmUxUUN3ME20Ok44Pjh{IN88US=> NVzK[2d3W0GQR1XS
KARPAS-422 NUfofY83T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4CzVmlEPTB;NEeuNFg6PSEQvF2= NXXzOHJTW0GQR1XS
Ramos-2G6-4C10 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3fN[GlEPTB;NEeuNVYzOiEQvF2= MUfTRW5ITVJ?
HCE-T NX7RcoxlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmLLTWM2OD12Nz62PFI5KM7:TR?= M4nzTHNCVkeHUh?=
PSN1 NFz3U5lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIqxV2NKSzVyPUS3Mlc5OTNizszN NFyxUGlUSU6JRWK=

他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい

アッセイ
Methods Test Index PMID
Western blot
pY576-FAK / pY861-FAK / FAK; 

PubMed: 20551056     


(A) HCT116 (left) and WiDr (right) cells were exposed to the indicated concentrations of saracatinib for 24 hours and the effect on total FAK or FAK phosphorylation on tyrosine 576 or 861 was assessed by western blotting. Result is representative of three independent experiments.

pY418 Src / Src / pY410 CAS / CAS / Py421 Cortactin / Cortactin; 

PubMed: 20505783     


Saracatinib inhibits Src activity and downstream Src substrate phosphorylation in HNSCC cell lines. HN31, UMSCC1 and 1483 cells were treated with DMSO vehicle or saracatinib (0.01–1 μM) for 24 h. Cells were lysed and total protein amounts were analyzed by Western blotting with total or phosphorylation site-specific antibodies for Src and the indicated substrates. Blots shown are representative of at least four independent experiments, with band intensities for each substrate quantified relative to the untreated (0 μM) condition for each cell line.

p-Akt / p-mTOR / Akt / mTOR / p-S6 / S6 / p-AMPKα / AMPKα; 

PubMed: 20811583     


PC3 cells were treated with 10 μM PP2 (left panel)/1 μM saracatinib (right panel) for 0.5, 1, 2, 4, 8, and 24 h. Cell lysates were analyzed by immunoblotting with antibodies as indicated. Controls were treated with vehicle alone. β-actin was detected as loading control.

20551056 20505783 20811583
Growth inhibition assay
Cell number; 

PubMed: 24349321     


LNCaP 104-S, 104-R1, 104-R2, PC-3, and DU-145 cells were treated with increasing concentrations of  Saracatinib for 72 hrs. Relative cell number of LNCaP cells was determined by Hoechst dye 33258-based 96-well proliferation assay. Cell numbers were normalized to control (dimethylsulfoxide) of each cell line. Triple asterisks (***) represent statistically significant difference p <0.001 between the treated group and the control group.

24349321
体内試験

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]

お薦めの試験操作(参考用のみ)

キナーゼ試験:

[1]

- 合併

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.
細胞試験:

[1]

- 合併
  • 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


    (参考用のみ)
動物試験:

[1]

- 合併
  • 動物モデル: CB17 mice are implanted with DU145 cells.
  • 投薬量: 25 mg/kg
  • 投与方法: Orally administered daily
    (参考用のみ)

溶解度 (25°C)

体外 DMSO 35 mg/mL (64.57 mM) warming
Water Insoluble
Ethanol '31 mg/mL '31
体内 左から(NMPから)右の順に溶剤を製品に加えます(文献ではなく、Selleckの実験によるデータ):
2% DMSO+30% PEG 300+ddH2O
混合させたのち直ちに使用することを推奨します。
5mg/mL

* 溶解度測定はSelleck技術部門によって行われており、その他文献に示されている溶解度と差異がある可能性がありますが、同一ロットの生産工程で起きる正常な現象ですからご安心ください。

化学情報

分子量 542.03
化学式

C27H32ClN5O5

CAS No. 379231-04-6
Storage powder
in solvent
別名 N/A
Smiles CN1CCN(CCOC2=CC(=C3C(=NC=NC3=C2)NC4=C(Cl)C=CC5=C4OCO5)OC6CCOCC6)CC1

投与溶媒組成計算器(クリア溶液)

ステップ1:実験データを入力してください。(実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します)
投与量 mg/kg 動物平均体重 g 投与体積(動物毎) ul 動物数
ステップ2:投与溶媒の組成を入力してください。(ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください)
% DMSO % % Tween 80 % ddH2O
計算リセット

便利ツール

モル濃度計算器

モル濃度計算器

求めたい質量、体積または濃度を計算してください。

質量 (mg) = 濃度 (mM) x 体積 (mL) x 分子量 (g/mol)

モル濃度計算器方程式

  • 質量
    濃度
    体積
    分子量

*貯蔵液を準備するとき、常に、オンであるとわかる製品のバッチに特有の分子量を使って、を通してラベルとMSDS/COA(製品ページで利用可能な)。

希釈計算器

希釈計算器

貯蔵液を準備するために必要な希釈率を計算してください。Selleck希釈計算器は、以下の方程式に基づきます:

開始濃度 x 開始体積 = 最終濃度 x 最終体積

希釈の計算式

この方程式は、一般に略語を使われます:C1V1 = C2V2 ( 入力 出力 )

  • C1
    V1
    C2
    V2

常に貯蔵液を準備するとき、小びんラベルとMSDS/COA(オンラインで利用できる)で見つかる製品のバッチに特有の分子量を使ってください。

連続希釈計算器方程式

  • 連続希釈剤

  • 計算結果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量計算器

分子量计算器

そのモル質量と元素組成を計算するために、合成物の化学式を入力してください:

総分子量:g/mol

チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2

モル濃度計算器

質量 濃度 体積 分子量

臨床試験

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04307953 Recruiting Drug: AZD0530 Difumarate|Drug: Matching placebo Fibrodysplasia Ossificans Progressiva VU University Medical Center|Royal National Orthopaedic Hospital NHS Trust|Klinikum Garmisch-Patenkirchen|University of Oxford|Brigham and Women''s Hospital|AstraZeneca|Innovative Medicines Initiative March 13 2020 Phase 2
NCT02085603 Completed Drug: Saracatinib|Drug: Placebo Cancer Sheffield Teaching Hospitals NHS Foundation Trust|AstraZeneca March 2014 Phase 2
NCT01864655 Completed Drug: saracatinib|Drug: Placebo Alzheimer''s Disease Stephen M. Strittmatter|Yale University July 2013 Phase 1
NCT01000896 Withdrawn Drug: AZD0530|Drug: Carboplatin|Drug: paclitaxel Cancer|Non Small Cell Lung Cancer|Epithelial Ovarian Cancer AstraZeneca January 2010 Phase 1
NCT00853983 Completed Drug: [14C] AZD0530 Healthy AstraZeneca March 2009 Phase 1

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

  • * 必須

よくある質問(FAQ)

  • 質問1:

    What is the half-life of Saracatinib?

  • 回答:

    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

Srcシグナル伝達経路

Src Inhibitors with Unique Features

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Tags: Saracatinib (AZD0530)を買う | Saracatinib (AZD0530) ic50 | Saracatinib (AZD0530)供給者 | Saracatinib (AZD0530)を購入する | Saracatinib (AZD0530)費用 | Saracatinib (AZD0530)生産者 | オーダーSaracatinib (AZD0530) | Saracatinib (AZD0530)化学構造 | Saracatinib (AZD0530)分子量 | Saracatinib (AZD0530)代理店
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細胞株 試験類型 濃度 培養時間 溶剤類型 活性叙述 PMID