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。

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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 NHXSdFJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHvFfFNKSzVyPUCuNFYyPDNizszN M2n6PXNCVkeHUh?=
LAMA-84 NHzjeWRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{Xpd2lEPTB;MD6xOVk6KM7:TR?= M1\KZXNCVkeHUh?=
MEG-01 MmXPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2PiS2lEPTB;MD6yN|Y5QCEQvF2= MmHSV2FPT0WU
EM-2 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYLLeY9vUUN3ME2wMlI3PSEQvF2= NVrZcYlGW0GQR1XS
TE-15 Mn7rS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmPVTWM2OD1yLkK3OFEzKM7:TR?= M3S3ZnNCVkeHUh?=
NCI-H1648 M4LFS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmjITWM2OD1yLkK4NVE3KM7:TR?= MYrTRW5ITVJ?
TE-12 MlfwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYfEPXAxUUN3ME2wMlMzPjhizszN NFfIfHNUSU6JRWK=
LB996-RCC M3fIdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXLWPJlsUUN3ME2wMlQ1OTl4IN88US=> M1vHOHNCVkeHUh?=
K-562 NH[1SZNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnHFTWM2OD1yLkS0PVY4KM7:TR?= M3nkXXNCVkeHUh?=
D-336MG M4nNZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXvFcY92UUN3ME2wMlUxOzB2IN88US=> MVjTRW5ITVJ?
NOS-1 M1v3RWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX\JR|UxRTBwNkC1Nlkh|ryP NVnFdYV2W0GQR1XS
EW-24 Mnj1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUHIdmpjUUN3ME2wMlYzPjl|IN88US=> M3TQcXNCVkeHUh?=
BV-173 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkfCTWM2OD1yLk[1NlQ6KM7:TR?= NGLxXVdUSU6JRWK=
NCCIT M2\WV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml7wTWM2OD1yLkezNlE5KM7:TR?= MVHTRW5ITVJ?
NCI-H1436 NFG0VY5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYXJR|UxRTBwN{mwOFkh|ryP Mk\GV2FPT0WU
BB30-HNC M4Dxc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF;C[XBKSzVyPUCuPFYzODNizszN Mnz5V2FPT0WU
TE-8 NYfydIQ2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mm\yTWM2OD1yLki3Nlc2KM7:TR?= NF;mZZNUSU6JRWK=
A704 NHniTXdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWPJR|UxRTBwOEmyNUDPxE1? NFfCSYZUSU6JRWK=
TK10 M1Xhemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEHSWVVKSzVyPUCuPVA3PjlizszN NFn1S5BUSU6JRWK=
KS-1 MnzPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3XGe2lEPTB;MT6xPVc4QSEQvF2= MoWwV2FPT0WU
C2BBe1 M3HsXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV3JR|UxRTFwMkC1NFch|ryP M3v4VXNCVkeHUh?=
RXF393 NUXpXGExT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHLkfHBKSzVyPUGuNlQ{PiEQvF2= NF3nS4tUSU6JRWK=
KGN NFXrR3hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1jnTGlEPTB;MT6yO|Y5PyEQvF2= MmTBV2FPT0WU
NB69 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX;JR|UxRTFwM{e0PVch|ryP NXjE[oI2W0GQR1XS
TE-11 MkGxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoXhTWM2OD1zLkSzOFE5KM7:TR?= MVXTRW5ITVJ?
TE-1 NIqz[VZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVe2bI1MUUN3ME2xMlQ1OTB3IN88US=> NVHQNIJ4W0GQR1XS
ST486 M1WzWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIrMe2NKSzVyPUGuOFU5PTJizszN M3PDT3NCVkeHUh?=
HOP-62 M3LKOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYLJR|UxRTFwNUCyOFYh|ryP M4TjcXNCVkeHUh?=
EW-16 NGLwfpBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV3kU5UzUUN3ME2xMlU2ODh|IN88US=> NWf5UVBiW0GQR1XS
LB1047-RCC MkHRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUfJR|UxRTFwNUW0OVMh|ryP NIe5cGtUSU6JRWK=
TE-10 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmHkTWM2OD1zLk[2NlUzKM7:TR?= MX;TRW5ITVJ?
RL95-2 MlzkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUPJR|UxRTFwNk[5NFIh|ryP NF\0dmVUSU6JRWK=
DOHH-2 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVHJR|UxRTFwN{G3PFIh|ryP NWLmSZV7W0GQR1XS
MFH-ino Mn3PS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkTSTWM2OD1zLke3PFch|ryP NFvJZYhUSU6JRWK=
GB-1 NELGWFFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFu1bGhKSzVyPUGuO|k5OzNizszN NXr1fIpoW0GQR1XS
SK-N-DZ NH\WW|lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1npVmlEPTB;MT64OFY5QCEQvF2= NVXCSVRtW0GQR1XS
OS-RC-2 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXr3VI1iUUN3ME2xMlg5PTd2IN88US=> Ml6xV2FPT0WU
SW982 NHW0NJVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4H0[2lEPTB;MT65NlA6OyEQvF2= NVfqSIZ5W0GQR1XS
KALS-1 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{fqPGlEPTB;MT65PFczOiEQvF2= MkXvV2FPT0WU
TGBC24TKB Ml;tS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUXJR|UxRTJwMEW5OVgh|ryP M4jSXXNCVkeHUh?=
GI-1 M2izNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV;JR|UxRTJwMU[wPFQh|ryP MnXrV2FPT0WU
SW962 M4P4UWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmSzTWM2OD1{LkG3NVc5KM7:TR?= NHXkfHRUSU6JRWK=
SW872 MnzqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEO5TW9KSzVyPUKuNVg2ODdizszN NVHIS2g2W0GQR1XS
NCI-H747 NX[2WZZqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{j1OGlEPTB;Mj6yOVcyPCEQvF2= NH\RO3pUSU6JRWK=
MZ1-PC NUj5VG05T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnLnTWM2OD1{LkK5N|U3KM7:TR?= NYLk[IlTW0GQR1XS
MSTO-211H NGPNSGpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVLXeWc1UUN3ME2yMlM2PzJ|IN88US=> NET3XXNUSU6JRWK=
BL-70 M1;jPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVPJR|UxRTJwNEe0NlIh|ryP NEXVPWxUSU6JRWK=
SW954 Mn7LS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M17PWmlEPTB;Mj61O|QxQCEQvF2= NIXUWo1USU6JRWK=
SNB75 NHq3WZBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVLJR|UxRTJwNki1PVQh|ryP MkDuV2FPT0WU
IST-SL2 NImwfVJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVLJR|UxRTJwN{KzO|kh|ryP MV\TRW5ITVJ?
GCIY MkPCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NU\aV4JtUUN3ME2yMlg4ODB3IN88US=> MlH0V2FPT0WU
KU812 MkLrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIC4OnZKSzVyPUOuNFUzQTlizszN M{nRbHNCVkeHUh?=
LXF-289 MlWzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIjIUJVKSzVyPUOuNVIyODlizszN M3v6WnNCVkeHUh?=
ETK-1 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkH3TWM2OD1|LkKwO|Y4KM7:TR?= NFnNfYRUSU6JRWK=
SF126 M{XESWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYjYUnJmUUN3ME2zMlMyOTd2IN88US=> MWXTRW5ITVJ?
LC-2-ad MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkLVTWM2OD1|LkW1O{DPxE1? NHe0XZFUSU6JRWK=
KNS-42 M{\CVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWTJR|UxRTNwNkWg{txO MoXGV2FPT0WU
OVCAR-4 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWXJR|UxRTNwN{O0N|Mh|ryP NIDndoxUSU6JRWK=
PF-382 M4PpPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXnJR|UxRTNwOEO2PVgh|ryP M{\aTHNCVkeHUh?=
SH-4 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXHkZnR5UUN3ME20MlI2OjV7IN88US=> Ml3DV2FPT0WU
KM12 MonmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1\6NWlEPTB;ND6zNlQyPiEQvF2= NIXNd4NUSU6JRWK=
NB5 M1vRdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3vBdWlEPTB;ND60NVg3PCEQvF2= MX;TRW5ITVJ?
KURAMOCHI NXLFUFN4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MljkTWM2OD12Lk[1NlU3KM7:TR?= M3HaTXNCVkeHUh?=
Becker MmG5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXL0eWZZUUN3ME20MlY3PDF4IN88US=> NVPWNmFmW0GQR1XS
MV-4-11 M1TZPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYXJR|UxRTRwOEGzOFQh|ryP MYHTRW5ITVJ?
KINGS-1 NYHmeVEzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYmyPVZzUUN3ME20MlgzOzd|IN88US=> M4nrZXNCVkeHUh?=
LS-123 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFnBeoFKSzVyPUWuOFk3QDRizszN M4HoUnNCVkeHUh?=
SF268 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYDJR|UxRTVwNkGyOlIh|ryP Mn34V2FPT0WU
A388 NGmySIVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{L6NmlEPTB;NT62N|Y3PyEQvF2= NFO3O3hUSU6JRWK=
NMC-G1 NIXEUZRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWHqdIR6UUN3ME22MlAyQDFzIN88US=> M3rBVHNCVkeHUh?=
CGTH-W-1 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUDpeo1sUUN3ME22MlAzODd3IN88US=> M2fuSnNCVkeHUh?=
ES4 MoLXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlLPTWM2OD14LkWzNFc1KM7:TR?= MXnTRW5ITVJ?
SR NWjpR2Z{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGHYR|lKSzVyPU[uOVg5ODdizszN MYHTRW5ITVJ?
BB49-HNC NFzT[m1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn7DTWM2OD14LkezNlA3KM7:TR?= NFu2d4ZUSU6JRWK=
KLE NIjwR2JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUHJR|UxRTZwN{izO|ch|ryP MlvlV2FPT0WU
HUTU-80 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml7iTWM2OD14Lkm4OFY3KM7:TR?= MoHSV2FPT0WU
SNU-C2B MkSwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmrTTWM2OD15LkiyO|M4KM7:TR?= NXG0NYdUW0GQR1XS
BB65-RCC NILVTFVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYDMZmhoUUN3ME23Mlk1QTB2IN88US=> NXXt[IIyW0GQR1XS
QIMR-WIL M1TmdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1jzNmlEPTB;OD60NlgxQCEQvF2= NInsPINUSU6JRWK=
GDM-1 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXXIeZQ2UUN3ME24Mlk4Ojl{IN88US=> MmmzV2FPT0WU
LC4-1 M1XHPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml;tTWM2OD17LkCwPVEyKM7:TR?= MXnTRW5ITVJ?
MLMA NUW5fnMyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnTFTWM2OD17LkG1NFA3KM7:TR?= M4eycXNCVkeHUh?=
EoL-1-cell MoW1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV;SV2U4UUN3ME25MlMxOTl{IN88US=> NH7KbVlUSU6JRWK=
BOKU NEXzXXZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV3ZWmptUUN3ME25Mlk3PDZ4IN88US=> M1PMe3NCVkeHUh?=
EVSA-T MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEfwUJhKSzVyPUGwMlY2PjhizszN NXzNSZpnW0GQR1XS
D-283MED MlH6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NInxUlVKSzVyPUGwMlkyPzZizszN NF7re4FUSU6JRWK=
NB1 NFPqV4NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml;ETWM2OD1zMT6wNlQzKM7:TR?= M4LHb3NCVkeHUh?=
RPMI-8402 NInHSZFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEfkS5ZKSzVyPUGxMlE4QCEQvF2= NI\5SppUSU6JRWK=
NCI-H1355 M3PmW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYnzfmxEUUN3ME2xNU4yQDB4IN88US=> NELaTmJUSU6JRWK=
NB7 MkHUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkTxTWM2OD1zMT6zNlk4KM7:TR?= MYfTRW5ITVJ?
RPMI-6666 NXTrcXRVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYXJR|UxRTF{Lkm1Olch|ryP M1Lu[HNCVkeHUh?=
697 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2jaS2lEPTB;MUOuNlcxOSEQvF2= NEHUcllUSU6JRWK=
CTB-1 NYnmRodlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3PtfGlEPTB;MUOuOVk1QCEQvF2= NV3HeVlIW0GQR1XS
VA-ES-BJ NE\tclJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXW3bHRDUUN3ME2xN{46OjN2IN88US=> NHn0THlUSU6JRWK=
BE-13 NFKyNXlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M321cmlEPTB;MUSuN|kyPSEQvF2= M{nLVnNCVkeHUh?=
SKM-1 NGTMRVZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3LkRWlEPTB;MUSuOFQ6QSEQvF2= NV7ndlE2W0GQR1XS
TE-6 M3jSN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4HXVGlEPTB;MUSuO|U6OSEQvF2= NYPD[HUyW0GQR1XS
LB771-HNC Mn3yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mkm3TWM2OD1zND63PFk5KM7:TR?= Mlv1V2FPT0WU
ECC4 M4\aV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUPJR|UxRTF5LkCyO|ch|ryP MnPjV2FPT0WU
ES3 NV22NlMzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHT6XFZKSzVyPUG3MlQ3PTVizszN Ml\hV2FPT0WU
LB647-SCLC NIXCRm1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoDDTWM2OD1zNz60PVQ6KM7:TR?= M2OweXNCVkeHUh?=
NB10 MkjZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXO1WoV[UUN3ME2xPE42OjV4IN88US=> M4XT[nNCVkeHUh?=
L-540 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M17kNmlEPTB;MUiuPFExQSEQvF2= MkL3V2FPT0WU
NCI-H2126 NWDkbmY5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFP1XphKSzVyPUG5MlUyKM7:TR?= MXTTRW5ITVJ?
HH MoT0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX;I[2NRUUN3ME2yNE4xODl7IN88US=> M2XZdnNCVkeHUh?=
MPP-89 NGnFNGJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYDJR|UxRTJ|LkKyPFkh|ryP NGezTlFUSU6JRWK=
IST-MEL1 MoPsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVnxZ4NQUUN3ME2yN{45PjV6IN88US=> NITM[VhUSU6JRWK=
KP-N-YS MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFrWUlBKSzVyPUKzMlkzPTVizszN NV;MNmJnW0GQR1XS
EC-GI-10 NYTmOFV{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NELje2NKSzVyPUK0MlU6QDlizszN NYrNdYtHW0GQR1XS
EKVX MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWe0S|hHUUN3ME2yOk4xOjB|IN88US=> MmDBV2FPT0WU
TGBC1TKB MkjwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NG\UcmpKSzVyPUK2MlQ{PCEQvF2= MlLmV2FPT0WU
Daudi MoLIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXrJR|UxRTJ5LkC3O|Mh|ryP MlPmV2FPT0WU
ALL-PO NGDvN4pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{HSV2lEPTB;MkeuNFgyKM7:TR?= NXrGWGRIW0GQR1XS
NB6 Mnf5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoXjTWM2OD1{Nz60PFgh|ryP MmXvV2FPT0WU
ES6 Mk\nS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXPJR|UxRTJ5LkmxNlMh|ryP NUXWOVFiW0GQR1XS
COLO-320-HSR M4HNRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmLWTWM2OD1{OD6wN|c{KM7:TR?= M4PWZXNCVkeHUh?=
K5 NYnxPVdxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVnJR|UxRTJ6LkGyPFch|ryP MX;TRW5ITVJ?
ES1 NHzQcFFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHnqZldKSzVyPUK4Mlc4PzNizszN Mny4V2FPT0WU
LC-1F NH\x[GFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXP0V3A4UUN3ME2yPU44OzR4IN88US=> M{\kTXNCVkeHUh?=
SCLC-21H NXvZUXRRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NG\TeY5KSzVyPUOwMlc{OTdizszN NV20e|NnW0GQR1XS
SK-PN-DW MmfyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUHJR|UxRTN{LkW1PVgh|ryP NH3HPWdUSU6JRWK=
D-247MG MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXnjfllmUUN3ME2zNk46Pzd|IN88US=> MlfDV2FPT0WU
TE-5 MmHIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mm[0TWM2OD1|Mz6wN|YzKM7:TR?= M1m0RnNCVkeHUh?=
MONO-MAC-6 MnjvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVjJR|UxRTN|LkWwOFgh|ryP M3HQfHNCVkeHUh?=
LB2518-MEL M3r4dmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFfocZNKSzVyPUOzMlc3PjZizszN MVPTRW5ITVJ?
LOXIMVI MlHkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUPJR|UxRTN|Lke5Nlgh|ryP NFn3T3BUSU6JRWK=
NCI-H209 NYHPc2NFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGnISmpKSzVyPUO1MlE1PCEQvF2= MUPTRW5ITVJ?
A253 NGOxTGFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M17Me2lEPTB;M{WuO|QzQSEQvF2= MY\TRW5ITVJ?
HCC1599 MkH5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGfXbXlKSzVyPUO2MlcxPTNizszN MkHNV2FPT0WU
EB-3 MkTiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoDSTWM2OD1|Nj65OVE5KM7:TR?= Moe2V2FPT0WU
GOTO MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M37ZeGlEPTB;M{euN|IzPCEQvF2= M2nGfnNCVkeHUh?=
SW684 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXHzbnVnUUN3ME20NU45PDl3IN88US=> NISxdIFUSU6JRWK=
DEL M161fWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NITSSZJKSzVyPUSyMlA2OjJizszN NEfVT3RUSU6JRWK=
HT-144 M133W2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUjJR|UxRTR{LkG2O|Yh|ryP M3vJNXNCVkeHUh?=
TE-9 MoexS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHLN[pZKSzVyPUSzMlQ2QTZizszN NHvaco5USU6JRWK=
KARPAS-45 M2TWUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVPJR|UxRTR2LkO5NlUh|ryP NHK1[VBUSU6JRWK=
HAL-01 NIfsUIxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3TtS2lEPTB;NESuOVA{PCEQvF2= M2nvfHNCVkeHUh?=
RCC10RGB M2Tiemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2rWcmlEPTB;NESuO|M6OiEQvF2= NUPOXZBsW0GQR1XS
CP67-MEL MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmjQTWM2OD12NT62NlQyKM7:TR?= MX\TRW5ITVJ?
NB17 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml:xTWM2OD12NT62OlQ{KM7:TR?= NE\tbGFUSU6JRWK=
SK-UT-1 NYnpbo13T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3GyPWlEPTB;NEWuPVQ3PCEQvF2= MYjTRW5ITVJ?
JiyoyeP-2003 MnLLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVPDVpJ3UUN3ME20Ok4xOTF7IN88US=> NI\jU4dUSU6JRWK=
HCE-4 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVXLd2xUUUN3ME20Ok42QTZ6IN88US=> MXzTRW5ITVJ?
NCI-H720 M3HwUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1O1SmlEPTB;NE[uO|Y5OiEQvF2= MkH1V2FPT0WU
KARPAS-422 NWXxSWJLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NULDSGpFUUN3ME20O{4xQDl3IN88US=> NVTiZnNDW0GQR1XS
Ramos-2G6-4C10 M2D3eWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn7VTWM2OD12Nz6xOlIzKM7:TR?= NXLmWFRQW0GQR1XS
HCE-T M2TQVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIDabYVKSzVyPUS3MlY5OjhizszN M2O1NnNCVkeHUh?=
PSN1 NWPNc3JJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NViwNIpVUUN3ME20O{44QDF|IN88US=> MV3TRW5ITVJ?

... Click to View More Cell Line Experimental Data

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]

+ 展开

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]

+ 展开
  • 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]

+ 展开
  • 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
稳定性 powder
in solvent
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 (g) = 浓度 (mol/L) x 体积 (L) 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 Conditions Sponsor/Collaborators Start Date Phases
NCT03661125 Not yet recruiting Parkinson Disease Psychosis King''s College London|AstraZeneca|King''s College Hospital NHS Trust April 11 2019 Early Phase 1
NCT03661125 Not yet recruiting Parkinson Disease Psychosis King''s College London|AstraZeneca|King''s College Hospital NHS Trust April 11 2019 Early Phase 1
NCT02955186 Recruiting Alcohol Drinking Yale University May 9 2017 Phase 2
NCT02955186 Recruiting Alcohol Drinking Yale University May 9 2017 Phase 2
NCT02737202 Recruiting Pulmonary Lymphangioleiomyomatosis Baylor College of Medicine|University of Cincinnati|Brigham and Women''s Hospital|Stanford University|Loyola University|University of South Florida|National Institutes of Health (NIH) April 2016 Phase 2
NCT02737202 Recruiting Pulmonary Lymphangioleiomyomatosis Baylor College of Medicine|University of Cincinnati|Brigham and Women''s Hospital|Stanford University|Loyola University|University of South Florida|National Institutes of Health (NIH) April 2016 Phase 2

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