Saracatinib (AZD0530)

For research use only. Not for use in humans.

目录号:S1006 中文名称:塞卡替尼

Saracatinib (AZD0530) Chemical Structure

CAS No. 379231-04-6

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 5472.84 现货
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客户使用Selleck生产的Saracatinib (AZD0530)发表文献223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 NXX2RXZRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXfHfmVZUUN3ME2wMlA3OTR|IN88US=> MkXIQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlE4ODl{Lze+V2FPT0WUPD;hQi=>
LAMA-84 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{X2PGlEPTB;MD6xOVk6KM7:TR?= M1ToZlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyPzB7Mj:nQnNCVkeHUkyvZV4>
MEG-01 NWqxRoNzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NILKPG9KSzVyPUCuNlM3QDhizszN Ml\pQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlE4ODl{Lze+V2FPT0WUPD;hQi=>
EM-2 M3vaWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWDJR|UxRTBwMk[1JO69VQ>? M{LrS|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyPzB7Mj:nQnNCVkeHUkyvZV4>
TE-15 NFO5NIJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWPJR|UxRTBwMke0NVIh|ryP M{PmdFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyPzB7Mj:nQnNCVkeHUkyvZV4>
NCI-H1648 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUnhb2ZGUUN3ME2wMlI5OTF4IN88US=> M3vhUlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyPzB7Mj:nQnNCVkeHUkyvZV4>
TE-12 NV2wPHRUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2X5bGlEPTB;MD6zNlY5KM7:TR?= NF30N3k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTdyOUKvK|5USU6JRWK8M4E,
LB996-RCC M2jLW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWXLXlFQUUN3ME2wMlQ1OTl4IN88US=> MXS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVcxQTJxJ{7TRW5ITVJ:L3G+
K-562 MnzJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3;2NmlEPTB;MD60OFk3PyEQvF2= MVq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVcxQTJxJ{7TRW5ITVJ:L3G+
D-336MG NXnKWmFqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2j1emlEPTB;MD61NFMxPCEQvF2= MU[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVcxQTJxJ{7TRW5ITVJ:L3G+
NOS-1 Ml[3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlOyTWM2OD1yLk[wOVI6KM7:TR?= MV28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVcxQTJxJ{7TRW5ITVJ:L3G+
EW-24 NEOwT3ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3nq[GlEPTB;MD62NlY6OyEQvF2= MonYQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlE4ODl{Lze+V2FPT0WUPD;hQi=>
BV-173 NHfQcmdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIP2OWNKSzVyPUCuOlUzPDlizszN NIjRblU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTdyOUKvK|5USU6JRWK8M4E,
NCCIT MluyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXG4SGR[UUN3ME2wMlc{OjF6IN88US=> NXT5[5FzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjF5MEmyM{c,W0GQR1XSQE9iRg>?
NCI-H1436 M4n6eWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4[weWlEPTB;MD63PVA1QSEQvF2= NEfYeXI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTdyOUKvK|5USU6JRWK8M4E,
BB30-HNC MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnjWTWM2OD1yLki2NlA{KM7:TR?= NIG2U2k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTdyOUKvK|5USU6JRWK8M4E,
TE-8 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYLhZmtLUUN3ME2wMlg4Ojd3IN88US=> MmPQQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlE4ODl{Lze+V2FPT0WUPD;hQi=>
A704 M4D5PWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkTOTWM2OD1yLki5NlEh|ryP NHzuPIY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTdyOUKvK|5USU6JRWK8M4E,
TK10 M4HzTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NILPZ3hKSzVyPUCuPVA3PjlizszN M1nuRVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyPzB7Mj:nQnNCVkeHUkyvZV4>
KS-1 MoO4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M33YUGlEPTB;MT6xPVc4QSEQvF2= M4\MdVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyPzB7Mj:nQnNCVkeHUkyvZV4>
C2BBe1 NEPjNXRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mo\LTWM2OD1zLkKwOVA4KM7:TR?= MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVcxQTJxJ{7TRW5ITVJ:L3G+
RXF393 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlTZTWM2OD1zLkK0N|Yh|ryP M33uSlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyPzB7Mj:nQnNCVkeHUkyvZV4>
KGN MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUnoRVVXUUN3ME2xMlI4Pjh5IN88US=> NHO1[Gs9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTdyOUKvK|5USU6JRWK8M4E,
NB69 NFXB[5dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkXZTWM2OD1zLkO3OFk4KM7:TR?= NE\MUVQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTdyOUKvK|5USU6JRWK8M4E,
TE-11 NHvVblhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnrtTWM2OD1zLkSzOFE5KM7:TR?= MlfhQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlE4ODl{Lze+V2FPT0WUPD;hQi=>
TE-1 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mk\RTWM2OD1zLkS0NVA2KM7:TR?= NFTxVoQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTdyOUKvK|5USU6JRWK8M4E,
ST486 NFvTbXlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEnUO4tKSzVyPUGuOFU5PTJizszN M1TK[FxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyPzB7Mj:nQnNCVkeHUkyvZV4>
HOP-62 M{mydmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFn0eWRKSzVyPUGuOVAzPDZizszN MluyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlE4ODl{Lze+V2FPT0WUPD;hQi=>
EW-16 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVXlbmdsUUN3ME2xMlU2ODh|IN88US=> MU[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVcxQTJxJ{7TRW5ITVJ:L3G+
LB1047-RCC M3LOOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnTUTWM2OD1zLkW1OFU{KM7:TR?= NGDQS4Q9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTdyOUKvK|5USU6JRWK8M4E,
TE-10 NFzVflRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXT1bI9uUUN3ME2xMlY3OjV{IN88US=> NX;sRnVORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjF5MEmyM{c,W0GQR1XSQE9iRg>?
RL95-2 MnvlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIDpRW1KSzVyPUGuOlY6ODJizszN M2\QPFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyPzB7Mj:nQnNCVkeHUkyvZV4>
DOHH-2 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYrJR|UxRTFwN{G3PFIh|ryP NYT6UodORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjF5MEmyM{c,W0GQR1XSQE9iRg>?
MFH-ino M1y0Zmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4DnNGlEPTB;MT63O|g4KM7:TR?= M{f1W|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyPzB7Mj:nQnNCVkeHUkyvZV4>
GB-1 MmHGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1LaSWlEPTB;MT63PVg{OyEQvF2= NF7Cd2k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTdyOUKvK|5USU6JRWK8M4E,
SK-N-DZ NHi2SJVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGXPSnlKSzVyPUGuPFQ3QDhizszN M{Xmc|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyPzB7Mj:nQnNCVkeHUkyvZV4>
OS-RC-2 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkX6TWM2OD1zLki4OVc1KM7:TR?= M{D4dlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyPzB7Mj:nQnNCVkeHUkyvZV4>
SW982 NIjuNoNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkDoTWM2OD1zLkmyNFk{KM7:TR?= NVroRppXRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjF5MEmyM{c,W0GQR1XSQE9iRg>?
KALS-1 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3Lrd2lEPTB;MT65PFczOiEQvF2= NEDaUXI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTdyOUKvK|5USU6JRWK8M4E,
TGBC24TKB M1vkfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmnPTWM2OD1{LkC1PVU5KM7:TR?= M3yyNVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyPzB7Mj:nQnNCVkeHUkyvZV4>
GI-1 NUTlcVZwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWHJR|UxRTJwMU[wPFQh|ryP MXi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVcxQTJxJ{7TRW5ITVJ:L3G+
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SJ-GBM2 MVTxTHRUKGG|c3H5 NYKzRoo1eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGPKMWdDVTJiY3XscJM> Mn;GQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
SK-N-MC MU\xTHRUKGG|c3H5 MUHxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhW0tvTj3NR{Bk\Wyucx?= MUO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
LAN-5 NGDBeG5yUFSVIHHzd4F6 MlPrdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKEyDTj21JINmdGy| M1XkdFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
HEK293 NIPJcoJHfW6ldHnvckBie3OjeR?= NEXyboQxNjFidH:gNUB2VQ>? Ml[0NVYhcHK| NUm0Z3dMUW6qaXLpeIlwdiCxZjDjc4xt[WenbjDJMYlv\HWlZXSgSGRTOiCLNkO4SkBufXSjboSgLJVvc26xd36gc5Jq\2mwKTDwbI9{eGixconsZZRqd25iZYjwdoV{e2WmIHnuJGhGUzJ7MzDj[YxteyCjdDCwMlEhfG9iMTD1UUBi\nSncjCxOkBpenNiYomgW4V{fGW{bjDicI91fGmwZx?= MoXKQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZzOUGzOlkoRjJ4MUmxN|Y6RC:jPh?=

... 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)
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

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
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;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
NCT04598919 Recruiting Drug: Saracatinab|Drug: Placebo Idiopathic Pulmonary Fibrosis (IPF) National Jewish Health|Yale University|Icahn School of Medicine at Mount Sinai|AstraZeneca|National Center for Advancing Translational Science (NCATS) November 12 2020 Phase 1|Phase 2
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 August 5 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

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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID