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582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 NUXXfHAzT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NFK5cIJKdmirYnn0bY9vKG:oIHj1cYFvKEOKUD2yNVIh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NEA:KDBwMECzNVU{KM7:TT6= MnvGQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVYyPDdyMT:nQnNCVkeHUkyvZV4>
H9 NUThTXNnT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= Mlz3TY5pcWKrdHnvckBw\iCqdX3hckBJQSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxKD1iMD6wNlI5QCEQvF2u MUG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxOlE1PzBzLze+V2FPT0WUPD;hQi=>
HL-60 Ml;BS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NUDDd3A5UW6qaXLpeIlwdiCxZjDoeY1idiCKTD22NEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwJF0hOC5yMkS1PUDPxE1w NI\MV2g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyPjF2N{CxM{c,W0GQR1XSQE9iRg>?
NOMO-1 MlTtS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M3vQU2lvcGmkaYTpc44hd2ZiaIXtZY4hVk:PTz2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUCgQUAxNjB|MUm3JO69VS5? NWfURoxPRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTZzNEewNU8oRlODTlfFVlww[T5?
DU-4475 M{fDc2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M3G4[GlvcGmkaYTpc44hd2ZiaIXtZY4hTFVvNES3OUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwJF0hOC5yM{O2O{DPxE1w M4D2TFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE3OTR5MEGvK|5USU6JRWK8M4E,
M14 MV;Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NEK0VlZKdmirYnn0bY9vKG:oIHj1cYFvKE1zNDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyIE2gNE4xOzZ6OTFOwG0v NXLoXXQ{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTZzNEewNU8oRlODTlfFVlww[T5?
HT-144 NXzDblBRT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NF\xOmtKdmirYnn0bY9vKG:oIHj1cYFvKEiWLUG0OEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwJF0hOC5yOEmwOUDPxE1w NYfmb3lwRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTZzNEewNU8oRlODTlfFVlww[T5?
SK-N-AS MnPKS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M4q5fWlvcGmkaYTpc44hd2ZiaIXtZY4hW0tvTj3BV{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwJF0hOC5yOUK4N{DPxE1w NWrvUJNGRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTZzNEewNU8oRlODTlfFVlww[T5?
LB2518-MEL MUDHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MnX3TY5pcWKrdHnvckBw\iCqdX3hckBNSjJ3MUitUWVNKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVAhRSByLkC5N|gzKM7:TT6= MVG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxOlE1PzBzLze+V2FPT0WUPD;hQi=>
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KY821 NEXE[oVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NUHQV3NZUW6qaXLpeIlwdiCxZjDoeY1idiCNWUiyNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwJF0hOC5zMEexPEDPxE1w M3HiWFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE3OTR5MEGvK|5USU6JRWK8M4E,
CP50-MEL-B MVfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NYe5WXJrUW6qaXLpeIlwdiCxZjDoeY1idiCFUEWwMW1GVC2EIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTBiPTCwMlEzPzl2IN88UU4> NGX3U449[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyPjF2N{CxM{c,W0GQR1XSQE9iRg>?
MEL-HO M2HSW2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NUKwO4pqUW6qaXLpeIlwdiCxZjDoeY1idiCPRVytTG8h[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NEA:KDBwMUO4PFQh|ryPLh?= M1i3dVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE3OTR5MEGvK|5USU6JRWK8M4E,
EoL-1-cell Mn:wS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NG\HPHVKdmirYnn0bY9vKG:oIHj1cYFvKEWxTD2xMYNmdGxiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OCB;IECuNVQ1PzZizszNMi=> NYDLdodyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTZzNEewNU8oRlODTlfFVlww[T5?
DOK MXTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NXXBSWRkUW6qaXLpeIlwdiCxZjDoeY1idiCGT1ugZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3MDC9JFAvOTR5MEig{txONg>? M{j6dFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE3OTR5MEGvK|5USU6JRWK8M4E,
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BPH-1 MXXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M365SGlvcGmkaYTpc44hd2ZiaIXtZY4hSlCKLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3MDC9JFAvOTh{M{Gg{txONg>? NEjKPGs9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyPjF2N{CxM{c,W0GQR1XSQE9iRg>?
HuP-T4 MnrpS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NXz6PWw3UW6qaXLpeIlwdiCxZjDoeY1idiCKdWCtWFQh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NEA:KDBwMUm1N|Ih|ryPLh?= NX3N[XJzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTZzNEewNU8oRlODTlfFVlww[T5?
KU812 Mnq1S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M2f6W2lvcGmkaYTpc44hd2ZiaIXtZY4hU1V6MUKgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3MDC9JFAvOjFzNkig{txONg>? MnjWQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVYyPDdyMT:nQnNCVkeHUkyvZV4>
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HTC-C3 NY\OOYxtT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MkjqTY5pcWKrdHnvckBw\iCqdX3hckBJXENvQ{OgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3MDC9JFAvOjF2NkGg{txONg>? NELkWXg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyPjF2N{CxM{c,W0GQR1XSQE9iRg>?
A101D MUTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MmXSTY5pcWKrdHnvckBw\iCqdX3hckBCOTBzRDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyIE2gNE4zPDB|MzFOwG0v NWjZb3BuRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTZzNEewNU8oRlODTlfFVlww[T5?
ONS-76 M1vsbWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NUCxWJV4UW6qaXLpeIlwdiCxZjDoeY1idiCRTmOtO|Yh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NEA:KDBwMkS0OVMh|ryPLh?= M16xSlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE3OTR5MEGvK|5USU6JRWK8M4E,
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WM-115 NHjReGRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MV3Jcohq[mm2aX;uJI9nKGi3bXHuJHdONTFzNTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyIE2gNE4zPjd3NDFOwG0v MmXyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVYyPDdyMT:nQnNCVkeHUkyvZV4>
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