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。

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10mM (1mL in DMSO)	RMB 746.35	现货
10mg	RMB 569.55	现货
25mg	RMB 1395.95	现货
200mg	RMB 5472.84	现货
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客户使用Selleck生产的Saracatinib (AZD0530)发表文献243篇：

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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

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)	点击更多
2.7 nM	<4 nM	4 nM	4 nM	5 nM	点击更多

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	Activity Description	PMID
CTV-1	NVH4VVZFT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=			NV\WNFBbUUN3ME2wMlA3OTR\|IN88US=>	MYW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVcxQTJxJ{7TRW5ITVJ:L3G+
LAMA-84	MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?			NFTqPXdKSzVyPUCuNVU6QSEQvF2=	MWm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVcxQTJxJ{7TRW5ITVJ:L3G+
MEG-01	NFvBUpFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=			MXjJR\|UxRTBwMkO2PFgh\|ryP	M4WxTFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyPzB7Mj:nQnNCVkeHUkyvZV4>
EM-2	NIHBXnhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=			NVvUVmplUUN3ME2wMlI3PSEQvF2=	NYW2TnNjRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjF5MEmyM{c,W0GQR1XSQE9iRg>?
TE-15	Mlj4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?			NVzCVlY1UUN3ME2wMlI4PDF{IN88US=>	MYi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVcxQTJxJ{7TRW5ITVJ:L3G+
NCI-H1648	M1;ad2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7			M{H3UWlEPTB;MD6yPFEyPiEQvF2=	NH3UO2k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTdyOUKvK\|5USU6JRWK8M4E,
TE-12	NGfEXFBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=			MUfJR\|UxRTBwM{K2PEDPxE1?	MUW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVcxQTJxJ{7TRW5ITVJ:L3G+
LB996-RCC	NUS5PXVMT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=			MlTJTWM2OD1yLkS0NVk3KM7:TR?=	MnjBQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlE4ODl{Lze+V2FPT0WUPD;hQi=>
K-562	NWfBN405T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=			MlrxTWM2OD1yLkS0PVY4KM7:TR?=	MY[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVcxQTJxJ{7TRW5ITVJ:L3G+
D-336MG	NHf1eGRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=			NY\iSJh1UUN3ME2wMlUxOzB2IN88US=>	MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVcxQTJxJ{7TRW5ITVJ:L3G+
NOS-1	NUfMTHk1T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=			MoGyTWM2OD1yLk[wOVI6KM7:TR?=	MX:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVcxQTJxJ{7TRW5ITVJ:L3G+
EW-24	NV;LS5c1T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=			NFPzeXJKSzVyPUCuOlI3QTNizszN	NHPMW4U9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTdyOUKvK\|5USU6JRWK8M4E,
BV-173	NH33[oRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=			MUXJR\|UxRTBwNkWyOFkh\|ryP	NIDtPJo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTdyOUKvK\|5USU6JRWK8M4E,
NCCIT	M37DbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7			NHfmZXVKSzVyPUCuO\|MzOThizszN	NVfXNpZJRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjF5MEmyM{c,W0GQR1XSQE9iRg>?
NCI-H1436	M2Lrdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7			NYexZZBvUUN3ME2wMlc6ODR7IN88US=>	MUO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVcxQTJxJ{7TRW5ITVJ:L3G+
BB30-HNC	MmK2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?			M2PMZ2lEPTB;MD64OlIxOyEQvF2=	MVO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVcxQTJxJ{7TRW5ITVJ:L3G+
TE-8	NVrRcpZmT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=			NIH3UXlKSzVyPUCuPFczPzVizszN	NH6wOHQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTdyOUKvK\|5USU6JRWK8M4E,
A704	M{Gye2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7			NVjWT2xIUUN3ME2wMlg6OjFizszN	MX[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVcxQTJxJ{7TRW5ITVJ:L3G+
TK10	NGjLfHFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=			M1nYOGlEPTB;MD65NFY3QSEQvF2=	MoLDQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlE4ODl{Lze+V2FPT0WUPD;hQi=>
KS-1	NXXjZ5FZT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=			Ml\kTWM2OD1zLkG5O\|c6KM7:TR?=	MXy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVcxQTJxJ{7TRW5ITVJ:L3G+
C2BBe1	M1LY[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7			NXzXS3BTUUN3ME2xMlIxPTB5IN88US=>	MVe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVcxQTJxJ{7TRW5ITVJ:L3G+
RXF393	NYXzZ4s1T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=			NYn0SXZyUUN3ME2xMlI1OzZizszN	NHzkUnM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTdyOUKvK\|5USU6JRWK8M4E,
KGN	MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?			NWD5d2J4UUN3ME2xMlI4Pjh5IN88US=>	NHrye2Q9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTdyOUKvK\|5USU6JRWK8M4E,
NB69	MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?			MojrTWM2OD1zLkO3OFk4KM7:TR?=	NUDROnNGRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjF5MEmyM{c,W0GQR1XSQE9iRg>?
TE-11	NX;tXmRKT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=			MYLJR\|UxRTFwNEO0NVgh\|ryP	MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVcxQTJxJ{7TRW5ITVJ:L3G+
TE-1	M1PvWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7			NGjFcGVKSzVyPUGuOFQyODVizszN	M{LGVFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyPzB7Mj:nQnNCVkeHUkyvZV4>
ST486	M{XhcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7			MXTJR\|UxRTFwNEW4OVIh\|ryP	MkjxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlE4ODl{Lze+V2FPT0WUPD;hQi=>
HOP-62	MnHuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?			NYPSSGMxUUN3ME2xMlUxOjR4IN88US=>	M4Hpc\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyPzB7Mj:nQnNCVkeHUkyvZV4>
EW-16	NFzmNYFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=			M1nMNGlEPTB;MT61OVA5OyEQvF2=	MVO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVcxQTJxJ{7TRW5ITVJ:L3G+
LB1047-RCC	NV7pfZUyT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=			NUnke\|RYUUN3ME2xMlU2PDV\|IN88US=>	NVPoTHh6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjF5MEmyM{c,W0GQR1XSQE9iRg>?
TE-10	NUX3PYlwT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=			M2H1bmlEPTB;MT62OlI2OiEQvF2=	MXi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVcxQTJxJ{7TRW5ITVJ:L3G+
RL95-2	NFO2OYlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=			NWKzPG5bUUN3ME2xMlY3QTB{IN88US=>	NIfpbmg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTdyOUKvK\|5USU6JRWK8M4E,
DOHH-2	NH7GfYVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=			MX;JR\|UxRTFwN{G3PFIh\|ryP	NVrw[lJlRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjF5MEmyM{c,W0GQR1XSQE9iRg>?
MFH-ino	NWfRd3RqT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=			MmjYTWM2OD1zLke3PFch\|ryP	MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVcxQTJxJ{7TRW5ITVJ:L3G+
GB-1	NUW4dJFKT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=			NYHuO3lCUUN3ME2xMlc6QDN\|IN88US=>	MknWQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlE4ODl{Lze+V2FPT0WUPD;hQi=>
SK-N-DZ	Ml;5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?			NGnXUIJKSzVyPUGuPFQ3QDhizszN	NVHwcWxYRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjF5MEmyM{c,W0GQR1XSQE9iRg>?
OS-RC-2	NFPLPVFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=			M1TZS2lEPTB;MT64PFU4PCEQvF2=	NUT6elNsRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjF5MEmyM{c,W0GQR1XSQE9iRg>?
SW982	NIC1SlNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=			MXLJR\|UxRTFwOUKwPVMh\|ryP	NV3ne3N2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjF5MEmyM{c,W0GQR1XSQE9iRg>?
KALS-1	MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?			MY\JR\|UxRTFwOUi3NlIh\|ryP	NVHVZoVXRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjF5MEmyM{c,W0GQR1XSQE9iRg>?
TGBC24TKB	M4fFTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7			MVjJR\|UxRTJwMEW5OVgh\|ryP	MmHCQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlE4ODl{Lze+V2FPT0WUPD;hQi=>
GI-1	NIn3V3hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=			MoLYTWM2OD1{LkG2NFg1KM7:TR?=	MWG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVcxQTJxJ{7TRW5ITVJ:L3G+
SW962	M1\XOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7			NHnHXVJKSzVyPUKuNVcyPzhizszN	NVWy[2lMRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjF5MEmyM{c,W0GQR1XSQE9iRg>?
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Becker	Mk\DS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?			NXfj[XFYUUN3ME20MlY3PDF4IN88US=>	MnztQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlE4ODl{Lze+V2FPT0WUPD;hQi=>
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KINGS-1	M13wZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7			NW\ud4tbUUN3ME20MlgzOzd\|IN88US=>	M13mRVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyPzB7Mj:nQnNCVkeHUkyvZV4>
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SF268	MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?			Ml3STWM2OD13Lk[xNlYzKM7:TR?=	MXe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVcxQTJxJ{7TRW5ITVJ:L3G+
A388	M1jjdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7			Mn;wTWM2OD13Lk[zOlY4KM7:TR?=	NYDtN4NbRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjF5MEmyM{c,W0GQR1XSQE9iRg>?
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CGTH-W-1	NX\BO45lT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=			NYrSRpdqUUN3ME22MlAzODd3IN88US=>	M2GzNFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyPzB7Mj:nQnNCVkeHUkyvZV4>
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BB49-HNC	Ml62S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?			M4HuTWlEPTB;Nj63N\|IxPiEQvF2=	MVq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVcxQTJxJ{7TRW5ITVJ:L3G+
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HUTU-80	M4nydWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7			NWPZdXF1UUN3ME22Mlk5PDZ4IN88US=>	MoDLQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlE4ODl{Lze+V2FPT0WUPD;hQi=>
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BB65-RCC	MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?			NFzE[WlKSzVyPUeuPVQ6ODRizszN	Ml7pQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlE4ODl{Lze+V2FPT0WUPD;hQi=>
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EoL-1-cell	MknTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?			NYXsOmd6UUN3ME25MlMxOTl{IN88US=>	MVS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVcxQTJxJ{7TRW5ITVJ:L3G+
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BT-37	NVrwc\|BLeUiWUzDhd5NigQ>?			M{HJe5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCEVD2zO{Bk\Wyucx?=	MWC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-
RD	MnT3dWhVWyCjc4PhfS=>			NWPnc5JteUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC\|Y4Ll[Y4h\m:{IGLEJINmdGy\|	MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-
SK-N-SH	MkjldWhVWyCjc4PhfS=>			M2P6eJFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCVSz3OMXNJKGOnbHzz	NGr5eGI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N\|UyOzl:L3G+
OHS-50	MlPQdWhVWyCjc4PhfS=>			NXzJVWpUeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC\|Y4Ll[Y4h\m:{IF;IV{02OCClZXzsdy=>	NUC0Z2lLRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N\|UyOzlpPkK5OFM2OTN7PD;hQi=>
SJ-GBM2	MVjxTHRUKGG\|c3H5			MoDldWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[\|ohWHKrbXHyfUB{[3KnZX6g[o9zKFOMLVfCUVIh[2WubIO=	MXS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-
SK-N-MC	NUW5NmdjeUiWUzDhd5NigQ>?			MYXxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhW0tvTj3NR{Bk\Wyucx?=	MXO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-
LAN-5	NV\TT5k2eUiWUzDhd5NigQ>?			MmLOdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[\|ohWHKrbXHyfUB{[3KnZX6g[o9zKEyDTj21JINmdGy\|	M2XtdlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
HEK293	M3LmTmZ2dmO2aX;uJIF{e2G7	MoXZNE4yKHSxIEGgeW0>	M4HXO\|E3KGi{cx?=	MVvJcohq[mm2aX;uJI9nKGOxbHzh[4VvKElvaX7keYNm\CCGRGKyJGk3OziIIH31eIFvfCBqdX7rco94diCxcnnnbY4qKHCqb4PwbI9zgWyjdHnvckBmgHC{ZYPz[YQhcW5iSFXLNlk{KGOnbHzzJIF1KDBwMTD0c{AyKHWPIHHmeIVzKDF4IHjyd{BjgSCZZYP0[ZJvKGKub4T0bY5o	M2HFOVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4MUmxN\|Y6Lz5{NkG5NVM3QTxxYU6=

... Click to View More Cell Line Experimental Data

Assay

Methods	Test Index	PMID
Western blot	pY576-FAK / pY861-FAK / FAK; PubMed: 20551056 Cancer Res (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 J Cancer Sci Ther 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 Genes Cancer 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 PLoS One 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]

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（K_m）。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)

参考文献

- 合并

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 Download Saracatinib (AZD0530) SDF

分子量	542.03
化学式	C₂₇H₃₂ClN₅O₅
CAS号	379231-04-6
储存条件	3年-20°C 粉状 2年-80°C 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

每只动物给药体积

动物数量

只

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

计算结果:

工作液浓度： mg/ml；

DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；

体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL ddH₂O，混匀澄清。

注意：1. 首先保证母液是澄清的；
2. 一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。

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、SDS / 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

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、SDS / 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
初始浓度:
稀释倍数:

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

通过输入化合物的化学式来计算其分子量：

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 (data from https://clinicaltrials.gov, updated on 2022-01-17)

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\|National Institute of Neurological Disorders and Stroke (NINDS)\|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。

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

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.

研究领域

产品类型

定制您的化合物库

Saracatinib (AZD0530)

客户使用Selleck生产的Saracatinib (AZD0530)发表文献243篇：

产品安全说明书

Src抑制剂选择性比较

生物活性

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)

参考文献

溶解度 (25°C)

化学数据 Download Saracatinib (AZD0530) SDF

动物体内配方计算器 (澄清溶液)

计算器

摩尔浓度计算器

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

摩尔浓度计算公式

稀释计算器

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

连续稀释计算器方程

连续稀释

计算结果

分子量计算器

总分子量：g/mol

摩尔浓度计算器

临床试验信息 (data from https://clinicaltrials.gov, updated on 2022-01-17)

技术支持

常见问题及建议解决方法

Src Signaling Pathway Map

Src Inhibitors with Unique Features

相关Src产品