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566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 M3T4UGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NV3JO2drUW6qaXLpeIlwdiCxZjDoeY1idiCFSGCtNlEzKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVAhRSByLkCwN|E2OyEQvF2u MY[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxOlE1PzBzLze+V2FPT0WUPD;hQi=>
H9 NUDxfo4yT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MVHJcohq[mm2aX;uJI9nKGi3bXHuJGg6KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVAhRSByLkCyNlg5KM7:TT6= MYW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxOlE1PzBzLze+V2FPT0WUPD;hQi=>
HL-60 NYrZ[GJlT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M{j6Z2lvcGmkaYTpc44hd2ZiaIXtZY4hUExvNkCgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3MDC9JFAvODJ2NUmg{txONg>? NIjz[3M9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyPjF2N{CxM{c,W0GQR1XSQE9iRg>?
NOMO-1 MVjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NFrXTIhKdmirYnn0bY9vKG:oIHj1cYFvKE6RTV:tNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwJF0hOC5yM{G5O{DPxE1w NH3kS409[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyPjF2N{CxM{c,W0GQR1XSQE9iRg>?
DU-4475 MmnMS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M2DGXmlvcGmkaYTpc44hd2ZiaIXtZY4hTFVvNES3OUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwJF0hOC5yM{O2O{DPxE1w NGfDWFA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyPjF2N{CxM{c,W0GQR1XSQE9iRg>?
M14 NEO0R|VIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NHnpTXhKdmirYnn0bY9vKG:oIHj1cYFvKE1zNDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyIE2gNE4xOzZ6OTFOwG0v MknEQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVYyPDdyMT:nQnNCVkeHUkyvZV4>
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