Saracatinib (AZD0530)

For research use only. Not for use in humans.

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。Saracatinib可诱导自噬。Phase 2/3。

规格 价格 库存 购买数量  
10mM (1mL 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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客户使用Selleck生产的Saracatinib (AZD0530)发表文献187篇：

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。Saracatinib可诱导自噬。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 NWLnW5gxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1fXN2lEPTB;MD6wOlE1OyEQvF2= NV\pS3FMW0GQR1XS
LAMA-84 NHvSdZdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn7oTWM2OD1yLkG1PVkh|ryP M4rSWnNCVkeHUh?=
MEG-01 M2DMe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1izcWlEPTB;MD6yN|Y5QCEQvF2= Mk\lV2FPT0WU
EM-2 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NE\jSWxKSzVyPUCuNlY2KM7:TR?= NU\RfXpMW0GQR1XS
TE-15 MmHhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXnJR|UxRTBwMke0NVIh|ryP NV;oPXRtW0GQR1XS
NCI-H1648 M1uxe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVTkNYRFUUN3ME2wMlI5OTF4IN88US=> NYH6U2ZuW0GQR1XS
TE-12 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV;JR|UxRTBwM{K2PEDPxE1? MUPTRW5ITVJ?
LB996-RCC MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX21Zo9YUUN3ME2wMlQ1OTl4IN88US=> M2nofHNCVkeHUh?=
K-562 M1XmUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mnj3TWM2OD1yLkS0PVY4KM7:TR?= MnjOV2FPT0WU
D-336MG NGm0OFFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoLZTWM2OD1yLkWwN|A1KM7:TR?= M{DNVnNCVkeHUh?=
NOS-1 M3W3Vmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml\4TWM2OD1yLk[wOVI6KM7:TR?= MVjTRW5ITVJ?
EW-24 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mle3TWM2OD1yLk[yOlk{KM7:TR?= NF3aNVFUSU6JRWK=
BV-173 NIfzVVlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVTOUHF7UUN3ME2wMlY2OjR7IN88US=> MofIV2FPT0WU
NCCIT NX7PZm8{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVruN41[UUN3ME2wMlc{OjF6IN88US=> M3XvZnNCVkeHUh?=
NCI-H1436 M3fpUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGnzUXFKSzVyPUCuO|kxPDlizszN NHLhb49USU6JRWK=
BB30-HNC MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIrZOoNKSzVyPUCuPFYzODNizszN NFnxdlFUSU6JRWK=
TE-8 M4DreWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlPnTWM2OD1yLki3Nlc2KM7:TR?= MX;TRW5ITVJ?
A704 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1XTUmlEPTB;MD64PVIyKM7:TR?= MX\TRW5ITVJ?
TK10 NUK1WYcyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGC2eoNKSzVyPUCuPVA3PjlizszN MlrwV2FPT0WU
KS-1 M{XLWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGTGXWpKSzVyPUGuNVk4PzlizszN MkL3V2FPT0WU
C2BBe1 M3H1cWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVGyepZoUUN3ME2xMlIxPTB5IN88US=> M{XscHNCVkeHUh?=
RXF393 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYGyN5hRUUN3ME2xMlI1OzZizszN NW\QXJhZW0GQR1XS
KGN NGKzfGpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmnpTWM2OD1zLkK3Olg4KM7:TR?= MmPLV2FPT0WU
NB69 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVzJR|UxRTFwM{e0PVch|ryP NE\tPVZUSU6JRWK=
TE-11 NHu5TmhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIPSV4dKSzVyPUGuOFM1OThizszN MnHTV2FPT0WU
TE-1 M1TGfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYrWSXptUUN3ME2xMlQ1OTB3IN88US=> NHPRe|ZUSU6JRWK=
ST486 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUXJR|UxRTFwNEW4OVIh|ryP MoDlV2FPT0WU
HOP-62 M{[xXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYTJR|UxRTFwNUCyOFYh|ryP M1PHZnNCVkeHUh?=
EW-16 MnTVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXnlN2E{UUN3ME2xMlU2ODh|IN88US=> NXj0fZlXW0GQR1XS
LB1047-RCC NHOzeo5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX7JR|UxRTFwNUW0OVMh|ryP NGKyemZUSU6JRWK=
TE-10 NHTneXpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M37TbGlEPTB;MT62OlI2OiEQvF2= MYXTRW5ITVJ?
RL95-2 NEjHe2hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXjJR|UxRTFwNk[5NFIh|ryP NFrvS3BUSU6JRWK=
DOHH-2 M{e3Wmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVf4coZqUUN3ME2xMlcyPzh{IN88US=> M3LqS3NCVkeHUh?=
MFH-ino M4nyTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHraZ4NKSzVyPUGuO|c5PyEQvF2= MWrTRW5ITVJ?
GB-1 NHOz[YNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MluyTWM2OD1zLke5PFM{KM7:TR?= Ml3DV2FPT0WU
SK-N-DZ MkTZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXjJR|UxRTFwOES2PFgh|ryP MnGxV2FPT0WU
OS-RC-2 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlL4TWM2OD1zLki4OVc1KM7:TR?= MnLjV2FPT0WU
SW982 MmjwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NITBNG1KSzVyPUGuPVIxQTNizszN NEf4eJFUSU6JRWK=
KALS-1 NV3l[o55T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFPxNHpKSzVyPUGuPVg4OjJizszN MnjCV2FPT0WU
TGBC24TKB MlzOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFLFRnNKSzVyPUKuNFU6PThizszN NIL2OWJUSU6JRWK=
GI-1 MlrWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NE\UZ2hKSzVyPUKuNVYxQDRizszN M1jMdnNCVkeHUh?=
SW962 M3yzT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIHiSGhKSzVyPUKuNVcyPzhizszN M{HVb3NCVkeHUh?=
SW872 M2XKUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlzsTWM2OD1{LkG4OVA4KM7:TR?= M{HHcXNCVkeHUh?=
NCI-H747 NXPsSZhbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVPPNWc2UUN3ME2yMlI2PzF2IN88US=> NXrsWnJGW0GQR1XS
MZ1-PC MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGrNOFhKSzVyPUKuNlk{PTZizszN NF7V[opUSU6JRWK=
MSTO-211H M3:yWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWG3WHREUUN3ME2yMlM2PzJ|IN88US=> MmHCV2FPT0WU
BL-70 M3\Q[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkfGTWM2OD1{LkS3OFIzKM7:TR?= M4TjdXNCVkeHUh?=
SW954 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVrJR|UxRTJwNUe0NFgh|ryP NEHuZ|BUSU6JRWK=
SNB75 NVu2SJNJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlTETWM2OD1{Lk[4OVk1KM7:TR?= MkfYV2FPT0WU
IST-SL2 M{C4Tmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2fwRWlEPTB;Mj63NlM4QSEQvF2= NFjrNJJUSU6JRWK=
GCIY NVrzT3JiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MU\JR|UxRTJwOEewNFUh|ryP NVTWZ5FQW0GQR1XS
KU812 NG\LcFZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEXsVVRKSzVyPUOuNFUzQTlizszN M4LYU3NCVkeHUh?=
LXF-289 NUTm[FNsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkT5TWM2OD1|LkGyNVA6KM7:TR?= M3LJZ3NCVkeHUh?=
ETK-1 NI\Xc4JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUfMfXpKUUN3ME2zMlIxPzZ5IN88US=> MVHTRW5ITVJ?
SF126 MoPkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlXsTWM2OD1|LkOxNVc1KM7:TR?= MVLTRW5ITVJ?
LC-2-ad M3;JTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkTiTWM2OD1|LkW1O{DPxE1? M3T6OnNCVkeHUh?=
KNS-42 M2LZS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUHJR|UxRTNwNkWg{txO NFmwZpRUSU6JRWK=
OVCAR-4 M3:yNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWHSeIgzUUN3ME2zMlc{PDN|IN88US=> MUnTRW5ITVJ?
PF-382 M2LEO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV3JR|UxRTNwOEO2PVgh|ryP NHrjb5BUSU6JRWK=
SH-4 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVy5OYhHUUN3ME20MlI2OjV7IN88US=> MWDTRW5ITVJ?
KM12 NY\VTmx6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVrJR|UxRTRwM{K0NVYh|ryP NVH2W5Q6W0GQR1XS
NB5 M4PPd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFzTUY5KSzVyPUSuOFE5PjRizszN M2jYdXNCVkeHUh?=
KURAMOCHI MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{PsfmlEPTB;ND62OVI2PiEQvF2= M1W4UnNCVkeHUh?=
Becker NGnsVZhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYjxNWlOUUN3ME20MlY3PDF4IN88US=> MmL6V2FPT0WU
MV-4-11 MlvTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEHUOJpKSzVyPUSuPFE{PDRizszN M4jFfXNCVkeHUh?=
KINGS-1 M4fmfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{jOdWlEPTB;ND64NlM4OyEQvF2= MmDXV2FPT0WU
LS-123 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWLJR|UxRTVwNEm2PFQh|ryP MUTTRW5ITVJ?
SF268 M{TmPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1LrNmlEPTB;NT62NVI3OiEQvF2= M4HYdnNCVkeHUh?=
A388 MnL3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX;rSploUUN3ME21MlY{PjZ5IN88US=> NVHhU3hPW0GQR1XS
NMC-G1 NFzlcHJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXHJR|UxRTZwMEG4NVEh|ryP MU\TRW5ITVJ?
CGTH-W-1 NXfsUXU{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWTDfHBQUUN3ME22MlAzODd3IN88US=> M{H1VXNCVkeHUh?=
ES4 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGjBPFVKSzVyPU[uOVMxPzRizszN MXjTRW5ITVJ?
SR M3X4U2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{T5cGlEPTB;Nj61PFgxPyEQvF2= NVPrVoY1W0GQR1XS
BB49-HNC NYr5O3RqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4G0SGlEPTB;Nj63N|IxPiEQvF2= MUPTRW5ITVJ?
KLE NHToRotIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUfJR|UxRTZwN{izO|ch|ryP MkXCV2FPT0WU
HUTU-80 MmPBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mlv5TWM2OD14Lkm4OFY3KM7:TR?= NIKxfWdUSU6JRWK=
SNU-C2B M2f6Zmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NW\TN|J3UUN3ME23MlgzPzN5IN88US=> NX\3WZpJW0GQR1XS
BB65-RCC NUmyemNuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWL2dGJ2UUN3ME23Mlk1QTB2IN88US=> MlXNV2FPT0WU
QIMR-WIL M1mxVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnvaTWM2OD16LkSyPFA5KM7:TR?= MYfTRW5ITVJ?
GDM-1 MlvjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3i1bWlEPTB;OD65O|I6OiEQvF2= M1WwU3NCVkeHUh?=
LC4-1 NY\3cI9KT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUHJR|UxRTlwMEC5NVEh|ryP NU\wRoRkW0GQR1XS
MLMA MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXrJR|UxRTlwMUWwNFYh|ryP MonaV2FPT0WU
EoL-1-cell NIfDXG9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXfJR|UxRTlwM{CxPVIh|ryP NI\lUWNUSU6JRWK=
BOKU MnTvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXnob|dvUUN3ME25Mlk3PDZ4IN88US=> MWTTRW5ITVJ?
EVSA-T NVPQe2pmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH3kfHpKSzVyPUGwMlY2PjhizszN NVS1W29oW0GQR1XS
D-283MED MkWxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUfJR|UxRTFyLkmxO|Yh|ryP MULTRW5ITVJ?
NB1 NYDQUm9ET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlH2TWM2OD1zMT6wNlQzKM7:TR?= MlnBV2FPT0WU
RPMI-8402 M3;Ifmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkPFTWM2OD1zMT6xO|gh|ryP M3W4TXNCVkeHUh?=
NCI-H1355 MoHxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUTJR|UxRTFzLkG4NFYh|ryP Mkn5V2FPT0WU
NB7 NWTvNmd1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnvJTWM2OD1zMT6zNlk4KM7:TR?= M{\sdHNCVkeHUh?=
RPMI-6666 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGfSSohKSzVyPUGyMlk2PjdizszN MoPVV2FPT0WU
697 MnH1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUXJR|UxRTF|LkK3NFEh|ryP MXnTRW5ITVJ?
CTB-1 NHXUTIVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MojhTWM2OD1zMz61PVQ5KM7:TR?= NEDTNHNUSU6JRWK=
VA-ES-BJ MonkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mm[5TWM2OD1zMz65NlM1KM7:TR?= NVjFRZh1W0GQR1XS
BE-13 MmDtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2KzVWlEPTB;MUSuN|kyPSEQvF2= NYLkZYhWW0GQR1XS
SKM-1 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFnUdotKSzVyPUG0MlQ1QTlizszN NYjiNYV2W0GQR1XS
TE-6 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{\z[GlEPTB;MUSuO|U6OSEQvF2= MlyxV2FPT0WU
LB771-HNC M4\heWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFuyfodKSzVyPUG0Mlc5QThizszN MmnIV2FPT0WU
ECC4 NETyN4lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWfXe5M2UUN3ME2xO{4xOjd5IN88US=> NXLYcYptW0GQR1XS
ES3 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIiyco1KSzVyPUG3MlQ3PTVizszN NV3RVphQW0GQR1XS
LB647-SCLC MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWrJR|UxRTF5LkS5OFkh|ryP MX3TRW5ITVJ?
NB10 M3\FfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX3VUoJTUUN3ME2xPE42OjV4IN88US=> M4TRNXNCVkeHUh?=
L-540 NVzuT3lET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVHJR|UxRTF6LkixNFkh|ryP MWrTRW5ITVJ?
NCI-H2126 M{\admdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGryeHdKSzVyPUG5MlUyKM7:TR?= NHXyZVRUSU6JRWK=
HH NIj6[pJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFTmWVNKSzVyPUKwMlAxQTlizszN MmGwV2FPT0WU
MPP-89 NUf1SlBOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWfJR|UxRTJ|LkKyPFkh|ryP MlHCV2FPT0WU
IST-MEL1 NEK4TI5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3PTdWlEPTB;MkOuPFY2QCEQvF2= M3HmWnNCVkeHUh?=
KP-N-YS M2n0[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1fsS2lEPTB;MkOuPVI2PSEQvF2= NXrWVWN3W0GQR1XS
EC-GI-10 MmLVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH\E[2RKSzVyPUK0MlU6QDlizszN NHzEU|BUSU6JRWK=
EKVX M2flNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUTlfmlqUUN3ME2yOk4xOjB|IN88US=> M2HRbXNCVkeHUh?=
TGBC1TKB NEjIboVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGjMXphKSzVyPUK2MlQ{PCEQvF2= MYXTRW5ITVJ?
Daudi NY\FPJVmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFntSnJKSzVyPUK3MlA4PzNizszN NHfqS4ZUSU6JRWK=
ALL-PO MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWrJR|UxRTJ5LkC4NUDPxE1? M{PaSHNCVkeHUh?=
NB6 NXrmUFZsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVzJR|UxRTJ5LkS4PEDPxE1? MnLMV2FPT0WU
ES6 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYm5NGhzUUN3ME2yO{46OTJ|IN88US=> M1fZO3NCVkeHUh?=
COLO-320-HSR MoXxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NULJOZA6UUN3ME2yPE4xOzd|IN88US=> M1jaVHNCVkeHUh?=
K5 M4Tsemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVTXOW9NUUN3ME2yPE4yOjh5IN88US=> MWPTRW5ITVJ?
ES1 NUX5UolFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVHRV3d6UUN3ME2yPE44Pzd|IN88US=> NGXMNFJUSU6JRWK=
LC-1F NHjhWmZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX2yPGx3UUN3ME2yPU44OzR4IN88US=> NWDScHo{W0GQR1XS
SCLC-21H Mmj4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlvxTWM2OD1|MD63N|E4KM7:TR?= NW[zRYdkW0GQR1XS
SK-PN-DW NEGxW4xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWW5doJzUUN3ME2zNk42PTl6IN88US=> MVnTRW5ITVJ?
D-247MG NInJUWRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXnJR|UxRTN{Lkm3O|Mh|ryP MXfTRW5ITVJ?
TE-5 MljUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4DwemlEPTB;M{OuNFM3OiEQvF2= M{WwZXNCVkeHUh?=
MONO-MAC-6 Mlf5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYHJR|UxRTN|LkWwOFgh|ryP M1z6[nNCVkeHUh?=
LB2518-MEL NGSw[XZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4LMXGlEPTB;M{OuO|Y3PiEQvF2= MmjkV2FPT0WU
LOXIMVI M1HnVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXTJR|UxRTN|Lke5Nlgh|ryP NYjySY5NW0GQR1XS
NCI-H209 NIqyW2pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4HGc2lEPTB;M{WuNVQ1KM7:TR?= NFHMb|lUSU6JRWK=
A253 MmrpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3juN2lEPTB;M{WuO|QzQSEQvF2= M1HKe3NCVkeHUh?=
HCC1599 M3\SXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{TieGlEPTB;M{[uO|A2OyEQvF2= Mn\nV2FPT0WU
EB-3 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV\ZeWtSUUN3ME2zOk46PTF6IN88US=> Mn\TV2FPT0WU
GOTO M1u2ZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIrMV2NKSzVyPUO3MlMzOjRizszN M17nfXNCVkeHUh?=
SW684 MoTkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXjJR|UxRTRzLki0PVUh|ryP NV;CTHZoW0GQR1XS
DEL MnfzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1W4RmlEPTB;NEKuNFUzOiEQvF2= NU\yTlZnW0GQR1XS
HT-144 M{TPWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXnJR|UxRTR{LkG2O|Yh|ryP Moi2V2FPT0WU
TE-9 M1XZRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1r0c2lEPTB;NEOuOFU6PiEQvF2= Ml\RV2FPT0WU
KARPAS-45 NYT5RYh[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWXyeGgyUUN3ME20OE4{QTJ3IN88US=> NWXkXVJTW0GQR1XS
HAL-01 Moe0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkLYTWM2OD12ND61NFM1KM7:TR?= NYflSm5ZW0GQR1XS
RCC10RGB NGDJWJFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGf1c4lKSzVyPUS0Mlc{QTJizszN Ml[3V2FPT0WU
CP67-MEL NILWVoxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXXJR|UxRTR3Lk[yOFEh|ryP MUTTRW5ITVJ?
NB17 NGS3[pZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NULON5REUUN3ME20OU43PjR|IN88US=> MkL0V2FPT0WU
SK-UT-1 MkLBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX7ybHVUUUN3ME20OU46PDZ2IN88US=> NY\y[JZ[W0GQR1XS
JiyoyeP-2003 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MorWTWM2OD12Nj6wNVE6KM7:TR?= MnzoV2FPT0WU
HCE-4 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1G0RWlEPTB;NE[uOVk3QCEQvF2= NIDKZo9USU6JRWK=
NCI-H720 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYDCd3BDUUN3ME20Ok44Pjh{IN88US=> MoPFV2FPT0WU
KARPAS-422 Mk\NS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV60RYFZUUN3ME20O{4xQDl3IN88US=> Ml3YV2FPT0WU
Ramos-2G6-4C10 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVPsOIdyUUN3ME20O{4yPjJ{IN88US=> MYTTRW5ITVJ?
HCE-T M4DVO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4LROGlEPTB;NEeuOlgzQCEQvF2= NGDTZ5FUSU6JRWK=
PSN1 M{jQPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4TiSmlEPTB;NEeuO|gyOyEQvF2= M2XKdnNCVkeHUh?=

... 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
  • 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)
Water Insoluble
Ethanol '31 mg/mL
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

动物体内配方计算器 (澄清溶液)

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量 只
第二步：请输入动物体内配方组成（不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
% DMSO % % Tween 80 % ddH2O
计算重置

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
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

Selleck产品目录册

Src Signaling Pathway Map

Src Inhibitors with Unique Features

  • 活性最高的Src抑制剂

    Dasatinib : Src, IC50=0.8 nM.

  • FDA批准的Src抑制剂

    Bosutinib (SKI-606) : Approved by FDA for Ph+ chronic myelogenous leukemia (CML).

  • 最新的Src抑制剂

    PP1 : Potent and selective Src inhibitor for Lck/Fyn with IC50 of 5 nM/ 6 nM.

  • 经典的Src抑制剂

    KX2-391 : The first clinical Src inhibitor (peptidomimetic class) that targets the peptide substrate site of Src, with GI50 of 9-60 nM in cancer cell lines.

相关Src产品

  • Dasatinib Monohydrate New

    Dasatinib Monohydrate 是一种新型有效的多靶点抑制剂，作用于靶点Abl，Src 和 c-Kit，IC50分别为 <1 nM，0.8 nM 和 79 nM。

  • SU6656 New

    SU 6656 是一种选择性 Src 家族激酶抑制剂，对Src，Yes，Lyn，和 Fyn 的 IC50 分别为 280 nM，20 nM，130 nM，和 170 nM。

  • PX-478 2HCl New

    PX-478 2HCl 是一种具有口服活性的选择性hypoxia-inducible factor-1α (HIF-1α)抑制剂。PX-478 2HCl可诱导凋亡并具有抗肿瘤的活性。Phase 1。

  • Bosutinib (SKI-606)

    Bosutinib (SKI-606) 是一种新型的双重Src/Abl抑制剂，在无细胞试验中IC50分别为1.2 nM 和 1 nM。Bosutinib也可通过阻滞p-ERK、p-S6和p-STAT3的磷酸化来有效地降低PI3K/AKT/mTOR、MAPK/ERK和JAK/STAT3信号通路的活性。Bosutinib可促进自噬。

  • Dasatinib

    Dasatinib 是一种新型有效的多靶点抑制剂，作用于Abl、Src和 c-Kit，在无细胞试验中IC50分别为 <1 nM、0.8 nM 和 79 nM。Dasatinib 可诱导自噬和凋亡并具有抗肿瘤的活性。

  • KX2-391（Tirbanibulin）

    KX2-391是第一个临床Src抑制剂(拟肽类)，靶向作用于Src的肽底物位点，在癌细胞系中GI50为9-60 nM。Phase 2。

  • PP1

    PP1是一种有效的Src选择性抑制剂，作用于Lck/Fyn时，IC50为5 nM/6 nM。

  • PP2

    PP2是一种Src家族激酶抑制剂，有效抑制Lck/Fyn，无细胞试验中IC50为4 nM/5 nM，作用于EGFR效果低100倍左右，对ZAP-70，JAK2和PKA没有活性。

  • WH-4-023

    WH-4-023是一种有效的，口服具有活性的Lck/Src抑制剂，无细胞试验中IC50分别为2 nM 和 6 nM。对p38α和KDR的选择性低300倍以上，还能有效抑制SIK（对SIK1、2、3的IC50分别为10、22、60 nM）。

  • Ibrutinib (PCI-32765)

    Ibrutinib (PCI-32765)是一种有效的，高选择性的Brutons tyrosine kinase (Btk)抑制剂，无细胞试验中IC50为0.5 nM，对Bmx， CSK， FGR， BRK及HCK适度有效，对EGFR， Yes， ErbB2， JAK3等作用效果较弱。Ibrutinib 可作为Btk配体用于合成包括P13I在内的一系列PROTAC。

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID