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 NI\LR3RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV3UUW1KUUN3ME2wMlA3OTR|IN88US=> NXjoOXJDW0GQR1XS
LAMA-84 NHW5SIZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoLLTWM2OD1yLkG1PVkh|ryP MX7TRW5ITVJ?
MEG-01 M3XYRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFXicHRKSzVyPUCuNlM3QDhizszN NIjyR|JUSU6JRWK=
EM-2 MmjLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnH2TWM2OD1yLkK2OUDPxE1? MlzlV2FPT0WU
TE-15 MmP6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVjJR|UxRTBwMke0NVIh|ryP MXfTRW5ITVJ?
NCI-H1648 MmrZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFLZV5VKSzVyPUCuNlgyOTZizszN NX;PZo5bW0GQR1XS
TE-12 M3Tkd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoPUTWM2OD1yLkOyOlgh|ryP NImwNXVUSU6JRWK=
LB996-RCC NYDEW2ZsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX3NO3ZbUUN3ME2wMlQ1OTl4IN88US=> M1zZcnNCVkeHUh?=
K-562 M4T4Rmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFm4WIlKSzVyPUCuOFQ6PjdizszN MkfZV2FPT0WU
D-336MG MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV\JR|UxRTBwNUCzNFQh|ryP NF[0UndUSU6JRWK=
NOS-1 NYHrT2xjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVnJR|UxRTBwNkC1Nlkh|ryP NX:xXphWW0GQR1XS
EW-24 MoPjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYS3b3NyUUN3ME2wMlYzPjl|IN88US=> MX\TRW5ITVJ?
BV-173 NEW1dZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NILBZ5RKSzVyPUCuOlUzPDlizszN M4X3d3NCVkeHUh?=
NCCIT M2PCRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3TpZ2lEPTB;MD63N|IyQCEQvF2= MmrsV2FPT0WU
NCI-H1436 NVnqSllkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVWzS|dsUUN3ME2wMlc6ODR7IN88US=> NWfSVGxXW0GQR1XS
BB30-HNC NEfIXYpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXfQdIxzUUN3ME2wMlg3OjB|IN88US=> MWnTRW5ITVJ?
TE-8 Mn3xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NI\2fYpKSzVyPUCuPFczPzVizszN NUD5O|ZZW0GQR1XS
A704 MmPvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWLJR|UxRTBwOEmyNUDPxE1? M3rX[nNCVkeHUh?=
TK10 NUXBPFNnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYDHO|hFUUN3ME2wMlkxPjZ7IN88US=> M2DRSXNCVkeHUh?=
KS-1 M4THcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MljWTWM2OD1zLkG5O|c6KM7:TR?= NIfDfZdUSU6JRWK=
C2BBe1 NFXo[nlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIO0fGdKSzVyPUGuNlA2ODdizszN M13UTHNCVkeHUh?=
RXF393 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFvycmpKSzVyPUGuNlQ{PiEQvF2= MXLTRW5ITVJ?
KGN MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4L2NmlEPTB;MT6yO|Y5PyEQvF2= NYHQSpd5W0GQR1XS
NB69 Mkj3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYfWNHVFUUN3ME2xMlM4PDl5IN88US=> MoCwV2FPT0WU
TE-11 NF30TYlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mmi3TWM2OD1zLkSzOFE5KM7:TR?= M1;wcXNCVkeHUh?=
TE-1 M136fGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF\VXWJKSzVyPUGuOFQyODVizszN M4\nd3NCVkeHUh?=
ST486 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXruZo1YUUN3ME2xMlQ2QDV{IN88US=> MXTTRW5ITVJ?
HOP-62 M1rBTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnjPTWM2OD1zLkWwNlQ3KM7:TR?= M{LW[XNCVkeHUh?=
EW-16 NWnabmlNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXfIPJBUUUN3ME2xMlU2ODh|IN88US=> MUXTRW5ITVJ?
LB1047-RCC MlvKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXnJR|UxRTFwNUW0OVMh|ryP NVPxN5JoW0GQR1XS
TE-10 NVLBXlFkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXPJR|UxRTFwNk[yOVIh|ryP MX7TRW5ITVJ?
RL95-2 M4\NbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NE\mVVlKSzVyPUGuOlY6ODJizszN NYrCPGF2W0GQR1XS
DOHH-2 NXO3ZlFlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1vHdGlEPTB;MT63NVc5OiEQvF2= NHLrZphUSU6JRWK=
MFH-ino MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXzJR|UxRTFwN{e4O{DPxE1? NHnQeGRUSU6JRWK=
GB-1 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF3HW2JKSzVyPUGuO|k5OzNizszN NV\GSIxGW0GQR1XS
SK-N-DZ Mlv1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXnRN2tlUUN3ME2xMlg1Pjh6IN88US=> MVHTRW5ITVJ?
OS-RC-2 M4LSSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWHFcoNuUUN3ME2xMlg5PTd2IN88US=> NEjpbHBUSU6JRWK=
SW982 NXXIb4tmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWfYZYNKUUN3ME2xMlkzODl|IN88US=> Mn3YV2FPT0WU
KALS-1 M1TmVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3zjOWlEPTB;MT65PFczOiEQvF2= M3XKTHNCVkeHUh?=
TGBC24TKB NIfGbFlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlLwTWM2OD1{LkC1PVU5KM7:TR?= NHTHcZhUSU6JRWK=
GI-1 MoLvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYXJR|UxRTJwMU[wPFQh|ryP NHnzSHBUSU6JRWK=
SW962 NUHoN4JxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1W4e2lEPTB;Mj6xO|E4QCEQvF2= NGfEOVBUSU6JRWK=
SW872 MmrzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXrPZWZsUUN3ME2yMlE5PTB5IN88US=> M3rxenNCVkeHUh?=
NCI-H747 NUe1THJUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV[1O3RuUUN3ME2yMlI2PzF2IN88US=> MoG0V2FPT0WU
MZ1-PC Mn:0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFrZ[XRKSzVyPUKuNlk{PTZizszN MofFV2FPT0WU
MSTO-211H MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGrNPG1KSzVyPUKuN|U4OjNizszN MXTTRW5ITVJ?
BL-70 MlSxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mki0TWM2OD1{LkS3OFIzKM7:TR?= Mn34V2FPT0WU
SW954 NET0bFVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NULJZnk1UUN3ME2yMlU4PDB6IN88US=> MXjTRW5ITVJ?
SNB75 M330fGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{XpOmlEPTB;Mj62PFU6PCEQvF2= M1zpWnNCVkeHUh?=
IST-SL2 NWXTcIJ4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGrWXIxKSzVyPUKuO|I{PzlizszN NEfXNGtUSU6JRWK=
GCIY NEi5O5JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVvJR|UxRTJwOEewNFUh|ryP MnXrV2FPT0WU
KU812 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXrlSnVOUUN3ME2zMlA2Ojl7IN88US=> NH3vWJpUSU6JRWK=
LXF-289 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlnQTWM2OD1|LkGyNVA6KM7:TR?= NFnXdXpUSU6JRWK=
ETK-1 NETDbZdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGj4RWJKSzVyPUOuNlA4PjdizszN MWfTRW5ITVJ?
SF126 NF\QV|JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFflNZVKSzVyPUOuN|EyPzRizszN NIfsZ5pUSU6JRWK=
LC-2-ad MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXTJR|UxRTNwNUW3JO69VQ>? MkTuV2FPT0WU
KNS-42 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MorxTWM2OD1|Lk[1JO69VQ>? NHfLbWdUSU6JRWK=
OVCAR-4 NYTM[3Z3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGHPN|ZKSzVyPUOuO|M1OzNizszN NEjnN3JUSU6JRWK=
PF-382 M3L1Xmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF7td4FKSzVyPUOuPFM3QThizszN NIjFcpRUSU6JRWK=
SH-4 Mlv5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXmyeVlwUUN3ME20MlI2OjV7IN88US=> NHjk[mxUSU6JRWK=
KM12 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlnhTWM2OD12LkOyOFE3KM7:TR?= MUfTRW5ITVJ?
NB5 Mn3ZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGHYdGVKSzVyPUSuOFE5PjRizszN MkT5V2FPT0WU
KURAMOCHI NFfEXYlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUPER5g6UUN3ME20MlY2OjV4IN88US=> NVe0R|lDW0GQR1XS
Becker M1Xp[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWr3V5dNUUN3ME20MlY3PDF4IN88US=> M2nJR3NCVkeHUh?=
MV-4-11 M3XLZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWDJR|UxRTRwOEGzOFQh|ryP M17yUXNCVkeHUh?=
KINGS-1 MnrqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFWyOYNKSzVyPUSuPFI{PzNizszN Mn;kV2FPT0WU
LS-123 NYqxdmc1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmTjTWM2OD13LkS5Olg1KM7:TR?= NH\rSVNUSU6JRWK=
SF268 NIrBU2JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXHteHZ{UUN3ME21MlYyOjZ{IN88US=> NHHlTVBUSU6JRWK=
A388 NGDEUmlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYPJR|UxRTVwNkO2Olch|ryP MUfTRW5ITVJ?
NMC-G1 M1jjUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4nDOmlEPTB;Nj6wNVgyOSEQvF2= M2HLZ3NCVkeHUh?=
CGTH-W-1 NIn4W|hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2jL[mlEPTB;Nj6wNlA4PSEQvF2= NWPXVnloW0GQR1XS
ES4 Mne3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHjHWpBKSzVyPU[uOVMxPzRizszN MnfiV2FPT0WU
SR MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWDxe3BoUUN3ME22MlU5QDB5IN88US=> MlPUV2FPT0WU
BB49-HNC MoPoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkDXTWM2OD14LkezNlA3KM7:TR?= MYDTRW5ITVJ?
KLE MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkjlTWM2OD14Lke4N|c4KM7:TR?= NGTh[GlUSU6JRWK=
HUTU-80 MknvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnP5TWM2OD14Lkm4OFY3KM7:TR?= NXLtdppwW0GQR1XS
SNU-C2B M4TaSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkHTTWM2OD15LkiyO|M4KM7:TR?= MmjhV2FPT0WU
BB65-RCC NHHsVJBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3K5d2lEPTB;Nz65OFkxPCEQvF2= NYLJS21kW0GQR1XS
QIMR-WIL NX7BSG1{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX\IeGp2UUN3ME24MlQzQDB6IN88US=> Mn3QV2FPT0WU
GDM-1 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIK0TVZKSzVyPUiuPVczQTJizszN NGmyNYtUSU6JRWK=
LC4-1 Ml3qS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2f3UWlEPTB;OT6wNFkyOSEQvF2= NXSxWJhMW0GQR1XS
MLMA MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIfrdGlKSzVyPUmuNVUxODZizszN MX3TRW5ITVJ?
EoL-1-cell M4X2SWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUTJR|UxRTlwM{CxPVIh|ryP M1\j[3NCVkeHUh?=
BOKU NEnhS3JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{P3Z2lEPTB;OT65OlQ3PiEQvF2= NVzL[FFVW0GQR1XS
EVSA-T MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmjUTWM2OD1zMD62OVY5KM7:TR?= MXjTRW5ITVJ?
D-283MED NFHCOIdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXziUGU2UUN3ME2xNE46OTd4IN88US=> NVvVZ5ZlW0GQR1XS
NB1 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV3JR|UxRTFzLkCyOFIh|ryP M4DxUXNCVkeHUh?=
RPMI-8402 MlrVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVjodXA2UUN3ME2xNU4yPzhizszN MXnTRW5ITVJ?
NCI-H1355 Mlf4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVTJR|UxRTFzLkG4NFYh|ryP MYrTRW5ITVJ?
NB7 MkLnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmPHTWM2OD1zMT6zNlk4KM7:TR?= MnmyV2FPT0WU
RPMI-6666 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX7VVmF5UUN3ME2xNk46PTZ5IN88US=> M4PhfHNCVkeHUh?=
697 NVTq[VlIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmTrTWM2OD1zMz6yO|AyKM7:TR?= MnTyV2FPT0WU
CTB-1 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGPTRY5KSzVyPUGzMlU6PDhizszN MYPTRW5ITVJ?
VA-ES-BJ MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoLKTWM2OD1zMz65NlM1KM7:TR?= MojUV2FPT0WU
BE-13 M37EZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{HhZ2lEPTB;MUSuN|kyPSEQvF2= NEDYU5FUSU6JRWK=
SKM-1 NXXRRlAyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoDjTWM2OD1zND60OFk6KM7:TR?= NV;wVIpPW0GQR1XS
TE-6 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUDJR|UxRTF2Lke1PVEh|ryP Mk\LV2FPT0WU
LB771-HNC MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGTLbWdKSzVyPUG0Mlc5QThizszN MlvsV2FPT0WU
ECC4 M4HNUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFXDWXJKSzVyPUG3MlAzPzdizszN M3zrbXNCVkeHUh?=
ES3 NIXoRoFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFroNnJKSzVyPUG3MlQ3PTVizszN MnzwV2FPT0WU
LB647-SCLC MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXfJR|UxRTF5LkS5OFkh|ryP NYT1bWZpW0GQR1XS
NB10 M3;DUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVnJR|UxRTF6LkWyOVYh|ryP NIDwVYhUSU6JRWK=
L-540 NHfPPFBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoruTWM2OD1zOD64NVA6KM7:TR?= NG\BZ4VUSU6JRWK=
NCI-H2126 NG\4b5ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUPJR|UxRTF7LkWxJO69VQ>? NFu5PGpUSU6JRWK=
HH NIP3W|BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVnJR|UxRTJyLkCwPVkh|ryP MVLTRW5ITVJ?
MPP-89 MlPTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnTOTWM2OD1{Mz6yNlg6KM7:TR?= M4P2U3NCVkeHUh?=
IST-MEL1 MmjKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MULJR|UxRTJ|Lki2OVgh|ryP MW\TRW5ITVJ?
KP-N-YS MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGjEXZZKSzVyPUKzMlkzPTVizszN NYjON3NNW0GQR1XS
EC-GI-10 NU[wUGZDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHPEOVJKSzVyPUK0MlU6QDlizszN Mk\NV2FPT0WU
EKVX NV3hdIlZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3uzR2lEPTB;Mk[uNFIxOyEQvF2= MmLvV2FPT0WU
TGBC1TKB NEexPFRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVvKcGdVUUN3ME2yOk41OzRizszN NEPF[VNUSU6JRWK=
Daudi NWnDXXNzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1nWe2lEPTB;MkeuNFc4OyEQvF2= M4LqcnNCVkeHUh?=
ALL-PO NYq3RZdyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYDJR|UxRTJ5LkC4NUDPxE1? Mn\qV2FPT0WU
NB6 MmewS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3jMRWlEPTB;MkeuOFg5KM7:TR?= NIXm[Y5USU6JRWK=
ES6 NUTVPGlqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXvZRpZsUUN3ME2yO{46OTJ|IN88US=> NXTVR3ZIW0GQR1XS
COLO-320-HSR MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGjSZXBKSzVyPUK4MlA{PzNizszN NELYZoRUSU6JRWK=
K5 NGP0WlNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHzQWXhKSzVyPUK4MlEzQDdizszN Mn;rV2FPT0WU
ES1 MlnKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUfwXGFXUUN3ME2yPE44Pzd|IN88US=> MYTTRW5ITVJ?
LC-1F MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYTJR|UxRTJ7LkezOFYh|ryP NGTZVWFUSU6JRWK=
SCLC-21H NFfXTHBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3\OeGlEPTB;M{CuO|MyPyEQvF2= M1rWR3NCVkeHUh?=
SK-PN-DW NGrGSpVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3PtXGlEPTB;M{KuOVU6QCEQvF2= MkLrV2FPT0WU
D-247MG M1LZeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVrJR|UxRTN{Lkm3O|Mh|ryP Mn;ZV2FPT0WU
TE-5 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV25eIxEUUN3ME2zN{4xOzZ{IN88US=> MVHTRW5ITVJ?
MONO-MAC-6 NVTPVWZCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGHPOJBKSzVyPUOzMlUxPDhizszN NFraS5FUSU6JRWK=
LB2518-MEL MoXwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEL5UJVKSzVyPUOzMlc3PjZizszN MmPrV2FPT0WU
LOXIMVI Ml7LS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NE\XeZFKSzVyPUOzMlc6OjhizszN NXrqPWdSW0GQR1XS
NCI-H209 NFXnSXJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIXscYhKSzVyPUO1MlE1PCEQvF2= NFXuZ|FUSU6JRWK=
A253 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{nqbmlEPTB;M{WuO|QzQSEQvF2= NVXoOJdqW0GQR1XS
HCC1599 M1j6N2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXTKblBiUUN3ME2zOk44ODV|IN88US=> MlHIV2FPT0WU
EB-3 NF\vbIJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVK4[nE2UUN3ME2zOk46PTF6IN88US=> MXrTRW5ITVJ?
GOTO M{TIRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1zNWmlEPTB;M{euN|IzPCEQvF2= NH\tUZRUSU6JRWK=
SW684 M{joVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWPJR|UxRTRzLki0PVUh|ryP NETLXWlUSU6JRWK=
DEL NYHPZnhrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3K1XmlEPTB;NEKuNFUzOiEQvF2= NYnqXo1sW0GQR1XS
HT-144 NYjqVFlGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUfSN5BVUUN3ME20Nk4yPjd4IN88US=> MULTRW5ITVJ?
TE-9 M4T3S2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXX2eYN5UUN3ME20N{41PTl4IN88US=> NW\oeWh{W0GQR1XS
KARPAS-45 MljSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2\Db2lEPTB;NESuN|kzPSEQvF2= M3XSdnNCVkeHUh?=
HAL-01 M3;pcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2LIRmlEPTB;NESuOVA{PCEQvF2= NFLUToRUSU6JRWK=
RCC10RGB NW[3dXpUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4LlXWlEPTB;NESuO|M6OiEQvF2= NEHuUpJUSU6JRWK=
CP67-MEL NHK5e3lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3z1eGlEPTB;NEWuOlI1OSEQvF2= NVrGWHdxW0GQR1XS
NB17 NH3FcWhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUPJR|UxRTR3Lk[2OFMh|ryP NUH2OVhXW0GQR1XS
SK-UT-1 NWG5VZM1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2PGc2lEPTB;NEWuPVQ3PCEQvF2= MnTwV2FPT0WU
JiyoyeP-2003 NGf2e2dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnrPTWM2OD12Nj6wNVE6KM7:TR?= M37zR3NCVkeHUh?=
HCE-4 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{TGNGlEPTB;NE[uOVk3QCEQvF2= NVrJ[oh7W0GQR1XS
NCI-H720 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkW2TWM2OD12Nj63OlgzKM7:TR?= NHzmVVZUSU6JRWK=
KARPAS-422 NXvtRnRyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEe1[IVKSzVyPUS3MlA5QTVizszN MV7TRW5ITVJ?
Ramos-2G6-4C10 MlPKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIXaPXNKSzVyPUS3MlE3OjJizszN M4HrUHNCVkeHUh?=
HCE-T NH7wVHJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYrafG06UUN3ME20O{43QDJ6IN88US=> M4L1UHNCVkeHUh?=
PSN1 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXz1fmhMUUN3ME20O{44QDF|IN88US=> NHzybWhUSU6JRWK=

... 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