Selumetinib (AZD6244)

For research use only. Not for use in humans.

目录号:S1008 别名: ARRY-142886 中文名称:司美替尼

Selumetinib (AZD6244) Chemical Structure

CAS No. 606143-52-6

Selumetinib (AZD6244, ARRY-142886)是一种有效,高选择性的MEK抑制剂,对MEK1的IC50为14 nM,对MEK2的Kd值为530 nM。它也抑制ERK1/2磷c酸化,IC50为10 nM,对p38α, MKK6, EGFR, ErbB2, ERK2, B-Raf等没有抑制作用。Selumetinib可抑制细胞增殖、迁移并诱导凋亡。Phase 3。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 956.17 现货
RMB 741.25 现货
RMB 1395.14 现货
RMB 3011.75 现货
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客户使用Selleck生产的Selumetinib (AZD6244)发表文献550篇:

产品安全说明书

MEK抑制剂选择性比较

生物活性

产品描述 Selumetinib (AZD6244, ARRY-142886)是一种有效,高选择性的MEK抑制剂,对MEK1的IC50为14 nM,对MEK2的Kd值为530 nM。它也抑制ERK1/2磷c酸化,IC50为10 nM,对p38α, MKK6, EGFR, ErbB2, ERK2, B-Raf等没有抑制作用。Selumetinib可抑制细胞增殖、迁移并诱导凋亡。Phase 3。
特性 AZD6244是第一个处于随机二期研究的MEK抑制剂。
靶点
MEK1 [1]
(Cell-free assay)
MEK1 [13]
(Cell-free assay)
MEK2 [13]
(Cell-free assay)
14 nM 99 nM(Kd) 530 nM(Kd)
体外研究

AZD6244是ATP非竞争性的抑制剂,在IC50浓度小于40 nM时使ERK1/2的磷酸化作用失活。AZD6244也通过抑制ERK1/2和p90RSK的磷酸化抑制原代HCC细胞的生长,同时伴随着caspase-3和caspase-7分裂的加强, 及断裂的聚腺苷二磷酸核糖聚合酶的增多。AZD6244在P38,JNK,PI3K,及MEK5/ERK5通路中的作用不大。[1]AZD6244对感知乳腺癌细胞系中的raf突变和非小细胞肺癌细胞系中的ras突变很灵敏。[2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
CHP-212 MYrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NF7wToVKdmirYnn0bY9vKG:oIHj1cYFvKEOKUD2yNVIh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NEA:KDBwMECzNVU{KM7:TT6= NEPaRXo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyPjF2N{CxM{c,W0GQR1XSQE9iRg>?
H9 M4PEXGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NWnzOlNYUW6qaXLpeIlwdiCxZjDoeY1idiCKOTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyIE2gNE4xOjJ6ODFOwG0v NF3xeYk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyPjF2N{CxM{c,W0GQR1XSQE9iRg>?
HL-60 NY\KPWZ7T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MnmzTY5pcWKrdHnvckBw\iCqdX3hckBJVC14MDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyIE2gNE4xOjR3OTFOwG0v MYi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxOlE1PzBzLze+V2FPT0WUPD;hQi=>
NOMO-1 MmC4S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M3K2PWlvcGmkaYTpc44hd2ZiaIXtZY4hVk:PTz2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUCgQUAxNjB|MUm3JO69VS5? NF;tOWc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyPjF2N{CxM{c,W0GQR1XSQE9iRg>?
DU-4475 M4K5c2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MlfqTY5pcWKrdHnvckBw\iCqdX3hckBFXS12NEe1JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUCgQUAxNjB|M{[3JO69VS5? MV[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxOlE1PzBzLze+V2FPT0WUPD;hQi=>
M14 MVLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NFLUS2lKdmirYnn0bY9vKG:oIHj1cYFvKE1zNDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyIE2gNE4xOzZ6OTFOwG0v NFm1RlY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyPjF2N{CxM{c,W0GQR1XSQE9iRg>?
HT-144 NXzGeZFnT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M{S4bGlvcGmkaYTpc44hd2ZiaIXtZY4hUFRvMUS0JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUCgQUAxNjB6OUC1JO69VS5? NFfac5k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyPjF2N{CxM{c,W0GQR1XSQE9iRg>?
SK-N-AS NELWboVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NWrnWWdvUW6qaXLpeIlwdiCxZjDoeY1idiCVSz3OMWFUKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVAhRSByLkC5Nlg{KM7:TT6= NWjjOVFYRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTZzNEewNU8oRlODTlfFVlww[T5?
LB2518-MEL NX\jTVlST3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MXLJcohq[mm2aX;uJI9nKGi3bXHuJGxDOjVzOD3NSWwh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NEA:KDBwMEmzPFIh|ryPLh?= NGr4TlE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyPjF2N{CxM{c,W0GQR1XSQE9iRg>?
C32 M3r0XGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NFXPbZNKdmirYnn0bY9vKG:oIHj1cYFvKEN|MjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyIE2gNE4xQTh{MzFOwG0v NYexSodGRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTZzNEewNU8oRlODTlfFVlww[T5?
BHT-101 NVjGVHNxT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MWnJcohq[mm2aX;uJI9nKGi3bXHuJGJJXC1zMEGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3MDC9JFAvOTB4OUOg{txONg>? NIK2c3Q9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyPjF2N{CxM{c,W0GQR1XSQE9iRg>?
KY821 M3Gycmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NUTFW49qUW6qaXLpeIlwdiCxZjDoeY1idiCNWUiyNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwJF0hOC5zMEexPEDPxE1w M{X2W|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE3OTR5MEGvK|5USU6JRWK8M4E,
CP50-MEL-B M{K3c2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M{\RRmlvcGmkaYTpc44hd2ZiaIXtZY4hS1B3MD3NSWwuSiClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxKD1iMD6xNlc6PCEQvF2u NHzjSoE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyPjF2N{CxM{c,W0GQR1XSQE9iRg>?
MEL-HO NG\NdmhIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NVW4UYw5UW6qaXLpeIlwdiCxZjDoeY1idiCPRVytTG8h[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NEA:KDBwMUO4PFQh|ryPLh?= NH;kTVI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyPjF2N{CxM{c,W0GQR1XSQE9iRg>?
EoL-1-cell MmjOS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MYnJcohq[mm2aX;uJI9nKGi3bXHuJGVwVC1zLXPlcIwh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NEA:KDBwMUS0O|Yh|ryPLh?= NUDTfINDRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTZzNEewNU8oRlODTlfFVlww[T5?
DOK M{XNfWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NX\N[4hWUW6qaXLpeIlwdiCxZjDoeY1idiCGT1ugZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3MDC9JFAvOTR5MEig{txONg>? MX:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxOlE1PzBzLze+V2FPT0WUPD;hQi=>
SH-4 NILYXmlIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M17mU2lvcGmkaYTpc44hd2ZiaIXtZY4hW0hvNDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyIE2gNE4yPjZ2ODFOwG0v NV24eJV3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTZzNEewNU8oRlODTlfFVlww[T5?
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HuP-T4 MlPCS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NHjQendKdmirYnn0bY9vKG:oIHj1cYFvKEi3UD3UOEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwJF0hOC5zOUWzNkDPxE1w MVO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxOlE1PzBzLze+V2FPT0WUPD;hQi=>
KU812 NVXzS2VWT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M1LEeGlvcGmkaYTpc44hd2ZiaIXtZY4hU1V6MUKgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3MDC9JFAvOjFzNkig{txONg>? NHLyNJY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyPjF2N{CxM{c,W0GQR1XSQE9iRg>?
A549 M3T5S2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M3\mTWlvcGmkaYTpc44hd2ZiaIXtZY4hSTV2OTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyIE2gNE4zOTRzMzFOwG0v NV2yU49RRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTZzNEewNU8oRlODTlfFVlww[T5?
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HCC2998 MkPBS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MXjJcohq[mm2aX;uJI9nKGi3bXHuJGhESzJ7OUigZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3MDC9JFAvOjZ7MEeg{txONg>? MX68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxOlE1PzBzLze+V2FPT0WUPD;hQi=>
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CAL-54 MUXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MmnqTY5pcWKrdHnvckBw\iCqdX3hckBESUxvNUSgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3MDC9JFEvPDl|MUSg{txONg>? NXTufWg1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTZzNEewNU8oRlODTlfFVlww[T5?
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CAL-33 NFXOUpdIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M4DYU2lvcGmkaYTpc44hd2ZiaIXtZY4hS0GOLUOzJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUCgQUAyNjV2Nkm0JO69VS5? NVWwepF1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTZzNEewNU8oRlODTlfFVlww[T5?
COLO-678 NIfCWGxIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MV;Jcohq[mm2aX;uJI9nKGi3bXHuJGNQVE9vNke4JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUCgQUAyNjZ{M{iyJO69VS5? M4Llb|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE3OTR5MEGvK|5USU6JRWK8M4E,
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