Saracatinib (AZD0530)

目录号:S1006

Saracatinib (AZD0530) Chemical Structure

Molecular Weight(MW): 542.03

Saracatinib (AZD0530)是一种有效的Src抑制剂,无细胞试验中IC50为2.7 nM,对c-Yes, Fyn, Lyn, Blk, Fgr和Lck也具有活性;但对Abl和EGFR (L858R和L861Q)活性较低。Phase 2/3。

规格 价格 库存 购买数量  
In DMSO RMB 746.35 现货
RMB 569.55 现货
RMB 1395.95 现货
RMB 5472.84 现货
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产品安全说明书

Src抑制剂选择性比较

生物活性

产品描述 Saracatinib (AZD0530)是一种有效的Src抑制剂,无细胞试验中IC50为2.7 nM,对c-Yes, Fyn, Lyn, Blk, Fgr和Lck也具有活性;但对Abl和EGFR (L858R和L861Q)活性较低。Phase 2/3。
特性 Saracatinib是第一个作用于人类肿瘤组织Src通路的抑制剂。
靶点
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
体外研究

Saracatinib也有效抑制其他Src酪氨酸激酶家族成员,包括c-Yes, Fyn, Lyn, Blk, Fgr, 和Lck,IC50为4到10 nM。Saracatinib有效抑制SrcY530F突变的NIH 3T3细胞,IC50为80 nM。在NBT-II膀胱癌细胞中,Saracatinib显著阻断HT1080细胞通过立体骨胶原基质的入侵,且完全抑制EGF诱导的细胞分散。[1]Saracatinib作用于DU145和PC3细胞,通过抑制Y419磷酸化而有效抑制Src激活。Saracatinib抑制前列腺癌包括PC3, DU145, CWR22Rv1和 LNCaP的生长,而Saracatinib作用于 LAPC-4, PZ-HPV7和RWPE-1细胞时却显示低活性。Saracatinib使细胞周期停止在G1/S期,但是不使caspase 3断裂。Saracatinib 也明显抑制Boyden 小室的DU145和PC3 移动。[2]Saracatinib有效且持久抑制Akt,且增强A549和Calu-6细胞对放射处理的敏感性。[3]Saracatinib在活性,再吸收,及组成上抑制蚀骨细胞。Saracatinib也可逆阻断蚀骨细胞前体的移动。[4]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
CTV-1 Mn\FS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUXJR|UxRTBwME[xOFMh|ryP M2S4SnNCVkeHUh?=
LAMA-84 NFrvSFFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX[wPGh7UUN3ME2wMlE2QTlizszN M{LlUnNCVkeHUh?=
MEG-01 MlP4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2fMb2lEPTB;MD6yN|Y5QCEQvF2= MYrTRW5ITVJ?
EM-2 NGPaUIxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXfJR|UxRTBwMk[1JO69VQ>? NFS0eXZUSU6JRWK=
TE-15 M37J[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3;seWlEPTB;MD6yO|QyOiEQvF2= M4e3R3NCVkeHUh?=
NCI-H1648 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXzJR|UxRTBwMkixNVYh|ryP NGC4WYJUSU6JRWK=
TE-12 NF7kN|hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MULJR|UxRTBwM{K2PEDPxE1? M1npVXNCVkeHUh?=
LB996-RCC M3G5dWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF70R2dKSzVyPUCuOFQyQTZizszN NIPZd5NUSU6JRWK=
K-562 NUPRTXFZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV[4SWh3UUN3ME2wMlQ1QTZ5IN88US=> Ml3BV2FPT0WU
D-336MG M4PPSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX3JR|UxRTBwNUCzNFQh|ryP M4i3ZXNCVkeHUh?=
NOS-1 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFzaVVdKSzVyPUCuOlA2OjlizszN MnSyV2FPT0WU
EW-24 Mke4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlraTWM2OD1yLk[yOlk{KM7:TR?= MnHnV2FPT0WU
BV-173 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEHrXm5KSzVyPUCuOlUzPDlizszN M3rrbXNCVkeHUh?=
NCCIT MmX6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MU\JR|UxRTBwN{OyNVgh|ryP NV:zUJBkW0GQR1XS
NCI-H1436 NX7OO|hLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXjJR|UxRTBwN{mwOFkh|ryP NEXiUYJUSU6JRWK=
BB30-HNC NWnheJdPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEPKUXBKSzVyPUCuPFYzODNizszN M1jzPHNCVkeHUh?=
TE-8 NV[wNZNET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF7YZ3dKSzVyPUCuPFczPzVizszN MXLTRW5ITVJ?
A704 NHfxXJRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmLNTWM2OD1yLki5NlEh|ryP MXvTRW5ITVJ?
TK10 M1TtVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWLuT2F6UUN3ME2wMlkxPjZ7IN88US=> MWjTRW5ITVJ?
KS-1 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFv4TVlKSzVyPUGuNVk4PzlizszN MnPmV2FPT0WU
C2BBe1 Mkf0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlXRTWM2OD1zLkKwOVA4KM7:TR?= NF\tVlZUSU6JRWK=
RXF393 NU[wNokxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEH4NWpKSzVyPUGuNlQ{PiEQvF2= M3HrcHNCVkeHUh?=
KGN M3fPOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnXLTWM2OD1zLkK3Olg4KM7:TR?= MYjTRW5ITVJ?
NB69 NYrrNXdMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV\JR|UxRTFwM{e0PVch|ryP MV;TRW5ITVJ?
TE-11 M4m4bmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVTWTZRZUUN3ME2xMlQ{PDF6IN88US=> Mlv5V2FPT0WU
TE-1 NGHnR5dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M13WR2lEPTB;MT60OFExPSEQvF2= M2q3TnNCVkeHUh?=
ST486 NH;GfYFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUKyXo9xUUN3ME2xMlQ2QDV{IN88US=> MmLZV2FPT0WU
HOP-62 NFrRWolIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXjJR|UxRTFwNUCyOFYh|ryP NWnwVYI{W0GQR1XS
EW-16 M{Lr[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2D0TGlEPTB;MT61OVA5OyEQvF2= NEfZfodUSU6JRWK=
LB1047-RCC NGLCT41Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVnJR|UxRTFwNUW0OVMh|ryP M1fySXNCVkeHUh?=
TE-10 MkjPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFywVoFKSzVyPUGuOlYzPTJizszN MWnTRW5ITVJ?
RL95-2 M3vnWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MonHTWM2OD1zLk[2PVAzKM7:TR?= MX7TRW5ITVJ?
DOHH-2 M3[y[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnHyTWM2OD1zLkexO|gzKM7:TR?= NHPNbodUSU6JRWK=
MFH-ino NIL1NW9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXnJR|UxRTFwN{e4O{DPxE1? M1X6OHNCVkeHUh?=
GB-1 NH7Db5BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkD5TWM2OD1zLke5PFM{KM7:TR?= NITWdFZUSU6JRWK=
SK-N-DZ MnPzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MojDTWM2OD1zLki0Olg5KM7:TR?= NGjuUHVUSU6JRWK=
OS-RC-2 MlnkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYnJR|UxRTFwOEi1O|Qh|ryP MkW2V2FPT0WU
SW982 M2\heWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIPTTWhKSzVyPUGuPVIxQTNizszN MkXQV2FPT0WU
KALS-1 NX;KWmZOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnjETWM2OD1zLkm4O|IzKM7:TR?= NHG2dYdUSU6JRWK=
TGBC24TKB MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1TseGlEPTB;Mj6wOVk2QCEQvF2= NFy4[mhUSU6JRWK=
GI-1 M1Prbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGe5bWxKSzVyPUKuNVYxQDRizszN MYfTRW5ITVJ?
SW962 MmmwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUftS29nUUN3ME2yMlE4OTd6IN88US=> MWPTRW5ITVJ?
SW872 Mki3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWjS[FRYUUN3ME2yMlE5PTB5IN88US=> NVfldJp7W0GQR1XS
NCI-H747 M4Wxc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUi4NXdIUUN3ME2yMlI2PzF2IN88US=> MVLTRW5ITVJ?
MZ1-PC NVv1TXdlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUDyeHlFUUN3ME2yMlI6OzV4IN88US=> NGPyeo1USU6JRWK=
MSTO-211H NUDhOnJET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUXJR|UxRTJwM{W3NlMh|ryP MlfuV2FPT0WU
BL-70 MlPJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYTJR|UxRTJwNEe0NlIh|ryP MVTTRW5ITVJ?
SW954 MnK1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYDJR|UxRTJwNUe0NFgh|ryP MoLIV2FPT0WU
SNB75 Mm\ES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MW\JR|UxRTJwNki1PVQh|ryP MmHjV2FPT0WU
IST-SL2 NIPIelRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUjN[2lIUUN3ME2yMlczOzd7IN88US=> MUPTRW5ITVJ?
GCIY MmrvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX;R[5V3UUN3ME2yMlg4ODB3IN88US=> MYjTRW5ITVJ?
KU812 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3LrS2lEPTB;Mz6wOVI6QSEQvF2= MV;TRW5ITVJ?
LXF-289 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2f4OWlEPTB;Mz6xNlExQSEQvF2= MkjLV2FPT0WU
ETK-1 M1WxeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYXTUoY5UUN3ME2zMlIxPzZ5IN88US=> NX3BRlB7W0GQR1XS
SF126 MmTLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFSyc41KSzVyPUOuN|EyPzRizszN NGi3TmpUSU6JRWK=
LC-2-ad NWrVe2NyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWfJR|UxRTNwNUW3JO69VQ>? NH7GSVdUSU6JRWK=
KNS-42 NYrqOo5TT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mmf3TWM2OD1|Lk[1JO69VQ>? Mn7hV2FPT0WU
OVCAR-4 Mo[4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWLJR|UxRTNwN{O0N|Mh|ryP NF:1eWpUSU6JRWK=
PF-382 NGrpdW1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3rCZWlEPTB;Mz64N|Y6QCEQvF2= NGX2dXBUSU6JRWK=
SH-4 MoO1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M33qU2lEPTB;ND6yOVI2QSEQvF2= MXnTRW5ITVJ?
KM12 NXrBfWlWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH:zd29KSzVyPUSuN|I1OTZizszN MmnzV2FPT0WU
NB5 MnvzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlXFTWM2OD12LkSxPFY1KM7:TR?= NGfJVnFUSU6JRWK=
KURAMOCHI MlvZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUfJR|UxRTRwNkWyOVYh|ryP MVXTRW5ITVJ?
Becker M{XvRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlW1TWM2OD12Lk[2OFE3KM7:TR?= NIrEdHBUSU6JRWK=
MV-4-11 MlvnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFzVfY9KSzVyPUSuPFE{PDRizszN NHHPZmhUSU6JRWK=
KINGS-1 NHv3SnRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFHQdlBKSzVyPUSuPFI{PzNizszN MoXvV2FPT0WU
LS-123 NYPmXok6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkLuTWM2OD13LkS5Olg1KM7:TR?= NELnN|ZUSU6JRWK=
SF268 NVXVUnRtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHG0SmdKSzVyPUWuOlEzPjJizszN M2jJbnNCVkeHUh?=
A388 NH7EV45Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2S2SGlEPTB;NT62N|Y3PyEQvF2= MnTxV2FPT0WU
NMC-G1 NYLxOHcxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4XuVmlEPTB;Nj6wNVgyOSEQvF2= NH;SZmpUSU6JRWK=
CGTH-W-1 NUTKVmNTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmjaTWM2OD14LkCyNFc2KM7:TR?= NHXtWYVUSU6JRWK=
ES4 MkniS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXXJR|UxRTZwNUOwO|Qh|ryP M{W5O3NCVkeHUh?=
SR MonSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{PROmlEPTB;Nj61PFgxPyEQvF2= MlzwV2FPT0WU
BB49-HNC NXnXVIY1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWD1cJEzUUN3ME22Mlc{OjB4IN88US=> NEm1OFhUSU6JRWK=
KLE M3rXZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIT3WFVKSzVyPU[uO|g{PzdizszN Ml;GV2FPT0WU
HUTU-80 NYmzeGtqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXTJR|UxRTZwOUi0OlYh|ryP MVvTRW5ITVJ?
SNU-C2B NFfRUGFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH;GN2tKSzVyPUeuPFI4OzdizszN MVPTRW5ITVJ?
BB65-RCC MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnnjTWM2OD15Lkm0PVA1KM7:TR?= MVXTRW5ITVJ?
QIMR-WIL NFLye25Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGTWNGRKSzVyPUiuOFI5ODhizszN NWDjOnFiW0GQR1XS
GDM-1 NGPO[nlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4\q[mlEPTB;OD65O|I6OiEQvF2= MV\TRW5ITVJ?
LC4-1 NIjKWHlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWHNTIVCUUN3ME25MlAxQTFzIN88US=> NXm0Toh6W0GQR1XS
MLMA MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1;jZ2lEPTB;OT6xOVAxPiEQvF2= NV;OXHFUW0GQR1XS
EoL-1-cell NFTxSoFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFvPXYJKSzVyPUmuN|AyQTJizszN MXrTRW5ITVJ?
BOKU MmPmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmrSTWM2OD17Lkm2OFY3KM7:TR?= NUWzWZFHW0GQR1XS
EVSA-T MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWfJR|UxRTFyLk[1Olgh|ryP MWTTRW5ITVJ?
D-283MED NEPh[3dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnPOTWM2OD1zMD65NVc3KM7:TR?= NGLWSoxUSU6JRWK=
NB1 M2e5dWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnjvTWM2OD1zMT6wNlQzKM7:TR?= MUTTRW5ITVJ?
RPMI-8402 M2frRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{nHN2lEPTB;MUGuNVc5KM7:TR?= NXu2bJdZW0GQR1XS
NCI-H1355 NF6zRZVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVXyfmJ7UUN3ME2xNU4yQDB4IN88US=> M3TSSnNCVkeHUh?=
NB7 NUnJRppUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NE\mcpVKSzVyPUGxMlMzQTdizszN NFHGcXFUSU6JRWK=
RPMI-6666 M13CWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUDJR|UxRTF{Lkm1Olch|ryP NFS3WXhUSU6JRWK=
697 NG\uU21Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{Tyb2lEPTB;MUOuNlcxOSEQvF2= MmDTV2FPT0WU
CTB-1 NW\ZOGU{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXvIfZlnUUN3ME2xN{42QTR6IN88US=> Moi1V2FPT0WU
VA-ES-BJ Mo[0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M37RT2lEPTB;MUOuPVI{PCEQvF2= NInT[2RUSU6JRWK=
BE-13 M{nlSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2\VUmlEPTB;MUSuN|kyPSEQvF2= MYrTRW5ITVJ?
SKM-1 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWjJR|UxRTF2LkS0PVkh|ryP NU\BcoF7W0GQR1XS
TE-6 Ml\GS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{nCZWlEPTB;MUSuO|U6OSEQvF2= NGracYVUSU6JRWK=
LB771-HNC NF3oN2RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUDJR|UxRTF2Lke4PVgh|ryP NGDBbXpUSU6JRWK=
ECC4 M4LlWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEn5XnRKSzVyPUG3MlAzPzdizszN NFvCSFBUSU6JRWK=
ES3 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYnLPIFlUUN3ME2xO{41PjV3IN88US=> M1L2SHNCVkeHUh?=
LB647-SCLC NWPweopHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmH4TWM2OD1zNz60PVQ6KM7:TR?= NHrMZpVUSU6JRWK=
NB10 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{P6fmlEPTB;MUiuOVI2PiEQvF2= M{HwNHNCVkeHUh?=
L-540 NGr3OldIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3fqWGlEPTB;MUiuPFExQSEQvF2= M{jJN3NCVkeHUh?=
NCI-H2126 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2fCSWlEPTB;MUmuOVEh|ryP NHn3TopUSU6JRWK=
HH MkG4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIP2R5hKSzVyPUKwMlAxQTlizszN MWnTRW5ITVJ?
MPP-89 M{DNe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlXpTWM2OD1{Mz6yNlg6KM7:TR?= M4PmTHNCVkeHUh?=
IST-MEL1 M1Xzc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH;zZlZKSzVyPUKzMlg3PThizszN M4TzfXNCVkeHUh?=
KP-N-YS MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXnSTZAxUUN3ME2yN{46OjV3IN88US=> NVS0Z25PW0GQR1XS
EC-GI-10 NXiweG9GT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2LXW2lEPTB;MkSuOVk5QSEQvF2= NEWzdnNUSU6JRWK=
EKVX NHyyOGRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYr3VHBOUUN3ME2yOk4xOjB|IN88US=> M1Lh[3NCVkeHUh?=
TGBC1TKB NEXie5dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1LDXmlEPTB;Mk[uOFM1KM7:TR?= M1O4VXNCVkeHUh?=
Daudi MlX5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlXlTWM2OD1{Nz6wO|c{KM7:TR?= MX\TRW5ITVJ?
ALL-PO NW\DTmFbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVzBNnV6UUN3ME2yO{4xQDFizszN NF7ufVNUSU6JRWK=
NB6 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4jifGlEPTB;MkeuOFg5KM7:TR?= MUPTRW5ITVJ?
ES6 MlvBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkTjTWM2OD1{Nz65NVI{KM7:TR?= MlXOV2FPT0WU
COLO-320-HSR MmPYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX;JR|UxRTJ6LkCzO|Mh|ryP MXrTRW5ITVJ?
K5 MkD0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX32[XZJUUN3ME2yPE4yOjh5IN88US=> Mkm5V2FPT0WU
ES1 M17icWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2rqR2lEPTB;MkiuO|c4OyEQvF2= MkHkV2FPT0WU
LC-1F MlHXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4HqOWlEPTB;MkmuO|M1PiEQvF2= M3;WNXNCVkeHUh?=
SCLC-21H MnPUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmfrTWM2OD1|MD63N|E4KM7:TR?= NXHMZmJOW0GQR1XS
SK-PN-DW MojkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYPJR|UxRTN{LkW1PVgh|ryP NUjSXoJlW0GQR1XS
D-247MG MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MY\JR|UxRTN{Lkm3O|Mh|ryP M2HrRnNCVkeHUh?=
TE-5 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoHrTWM2OD1|Mz6wN|YzKM7:TR?= MUXTRW5ITVJ?
MONO-MAC-6 M1[0RWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHTzOXRKSzVyPUOzMlUxPDhizszN MoHzV2FPT0WU
LB2518-MEL MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NULze|A2UUN3ME2zN{44PjZ4IN88US=> M4ruPHNCVkeHUh?=
LOXIMVI NHrJZ3JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXzlSXdYUUN3ME2zN{44QTJ6IN88US=> NXOwVWVlW0GQR1XS
NCI-H209 MmHoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlvmTWM2OD1|NT6xOFQh|ryP MVHTRW5ITVJ?
A253 NV\He4hqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NU\rS2VKUUN3ME2zOU44PDJ7IN88US=> Mkj3V2FPT0WU
HCC1599 NYq0dIdIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWDJR|UxRTN4LkewOVMh|ryP NGruVnlUSU6JRWK=
EB-3 M4Dx[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkP2TWM2OD1|Nj65OVE5KM7:TR?= NYLTd|h2W0GQR1XS
GOTO MmflS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYfJR|UxRTN5LkOyNlQh|ryP NUnGSXJWW0GQR1XS
SW684 MljtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlfwTWM2OD12MT64OFk2KM7:TR?= MlLOV2FPT0WU
DEL NUfzN|ZST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{TiZ2lEPTB;NEKuNFUzOiEQvF2= NVfDZmY1W0GQR1XS
HT-144 M2\GSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYrPV3d7UUN3ME20Nk4yPjd4IN88US=> M2C0WXNCVkeHUh?=
TE-9 Mnr5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmX2TWM2OD12Mz60OVk3KM7:TR?= NFPZZYxUSU6JRWK=
KARPAS-45 M1LwR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2nvd2lEPTB;NESuN|kzPSEQvF2= M{TwV3NCVkeHUh?=
HAL-01 M{HjcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2faeWlEPTB;NESuOVA{PCEQvF2= NVmwXFl{W0GQR1XS
RCC10RGB MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUXJR|UxRTR2LkezPVIh|ryP NV7tdFFXW0GQR1XS
CP67-MEL MkXyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{fYUGlEPTB;NEWuOlI1OSEQvF2= MmnKV2FPT0WU
NB17 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVPJR|UxRTR3Lk[2OFMh|ryP NIfrbVVUSU6JRWK=
SK-UT-1 NVm2T29yT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NE\sc|VKSzVyPUS1Mlk1PjRizszN M{DUSnNCVkeHUh?=
JiyoyeP-2003 NYT6e4EzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX3JUFZLUUN3ME20Ok4xOTF7IN88US=> Ml;UV2FPT0WU
HCE-4 MoXNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2P6WWlEPTB;NE[uOVk3QCEQvF2= MUPTRW5ITVJ?
NCI-H720 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYjJR|UxRTR4Lke2PFIh|ryP M37ES3NCVkeHUh?=
KARPAS-422 NU\x[I43T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV;JR|UxRTR5LkC4PVUh|ryP MUTTRW5ITVJ?
Ramos-2G6-4C10 NWO1b4d7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVLJR|UxRTR5LkG2NlIh|ryP M17MTnNCVkeHUh?=
HCE-T NWO3UWF6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHztNnZKSzVyPUS3MlY5OjhizszN M3vUXnNCVkeHUh?=
PSN1 NXLudYRoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3S5N2lEPTB;NEeuO|gyOyEQvF2= Ml\nV2FPT0WU

... Click to View More Cell Line Experimental Data

Assay
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
体内研究

Saracatinib作用于Src3T3异体移植物显示出强的肿瘤生长抑制率,且Saracatinib造成Calu-6, MDA-MB-231, AsPc-1和BT474C移植瘤生长适当延迟。[1]Saracatinib处理常位DU145鼠,按鼠体重,每千克每天口服处理25mg Saracatinib,结果显示出强的抗癌活性。[2]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

激酶实验:

[1]

- 合并

激酶实验:

使用受体和非受体酪氨酸激酶的重组催化区,通过酶联免疫吸附法测定酪氨酸激酶活性的IC50值。加入的Saracatinib剂量从0.001到10 mM不等。针对丝氨酸/苏氨酸激酶的特定实验是加32P 的渗透捕捉实验。在加入10 μL 20mM Mg.ATP开始反应前,包含0.5 μL Saracatinib或DMSO(作对照) 或pH 3.0 buffer(作对照)的多支路384孔板加入15 μL酶和肽/蛋白底物温育5分钟。 所有酶的最终浓度都接近米氏常数(Km)。实验在室温下进行30分钟,然后加入5 μL正磷酸终止反应。混合后,孔中的内含物加到P81联合板上,使用正磷酸作为洗涤缓冲液,然后计算IC50值。
细胞实验:

[2]

- 合并
  • Cell lines: PC3, DU145, CWR22Rv1, LNCaP, LAPC-4, PZ-HPV7,和RWPE-1细胞
  • Concentrations: 62.5 nM-16 mM
  • Incubation Time: 1, 3,和5天
  • Method:

    PC3, DU145, CWR22Rv1, LNCaP, LAPC-4, PZ-HPV7 及RWPE-1细胞按2×103密度接种在96孔板上,温育过夜。加入浓度不等(62.5 nM-16 mM)的Saracatinib。1,3,5天后分离培养基,每孔加入0.2 mL DMSO,按每分钟200轮持续震荡96孔板15分钟。MTT实验测IC50值。


    (Only for Reference)
动物实验:

[2]

- 合并
  • Animal Models: 移植DU145细胞的CB17鼠
  • Formulation: 溶于0.5% 羟丙基甲基纤维素和0.1% Tween-80中
  • Dosages: 25 mg/kg
  • Administration: 每天口服处理
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 35 mg/mL warmed (64.57 mM)
Ethanol 31 mg/mL (57.19 mM)
Water Insoluble
体内 从左到右依次将纯溶剂加入产品,现配现用(数据来自Selleck实验检测而非文献):
2% DMSO+30% PEG 300+ddH2O
5mg/mL

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 542.03
化学式

C27H32ClN5O5

CAS号 379231-04-6
储存条件 粉状
溶于溶剂
别名 N/A

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • 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):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

临床试验信息

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
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
NCT00752206 Completed Drug: Saracatinib|Drug: Placebo Osteosarcoma Sarcoma Alliance for Research through Collaboration|AstraZeneca March 2009 Phase 2
NCT00771979 Completed Drug: AZD0530 Healthy AstraZeneca November 2008 Phase 1

技术支持

在订购、运输、储存和使用我们的产品的任何阶段,您遇到的任何问题,均可以通过拨打我们的热线电话400-668-6834,或者技术支持邮箱tech@selleck.cn,直接联系到我们。我们会在24小时内尽快联系您。

操作手册

如果有其他问题,请给我们留言。

  • * 必填项

常见问题及建议解决方法

  • 问题 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 Signaling Pathway Map

Src Inhibitors with Unique Features

相关Src产品

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID