Selumetinib (AZD6244)

For research use only. Not for use in humans.

目录号:S1008 别名: ARRY-142886

Selumetinib (AZD6244) Chemical Structure

Molecular Weight(MW): 457.68

Selumetinib (AZD6244)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磷酸化,IC50为10 nM,对p38α, MKK6, EGFR, ErbB2, ERK2, B-Raf等没有抑制作用。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 1062.09 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398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)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磷酸化,IC50为10 nM,对p38α, MKK6, EGFR, ErbB2, ERK2, B-Raf等没有抑制作用。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
human CHP-212 cell M2LOPGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MnzRTY5pcWKrdHnvckBw\iCqdX3hckBEUFBvMkGyJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N{4yPSCwTT6= M1LZWXNCVkeHUh?=
human H9 cell NVfvUI1oT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NU\zN4lPUW6qaXLpeIlwdiCxZjDoeY1idiCKOTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUKyMlg5KG6PLh?= MnW4V2FPT0WU
human HL-60 cell NIO1d3pIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M1rseWlvcGmkaYTpc44hd2ZiaIXtZY4hUExvNkCgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yOE42QSCwTT6= M4XLN3NCVkeHUh?=
human A375 cells MoW5VJJwdGmoZYLheIlwdiCjc4PhfS=> Mn\sO|IhcA>? M2[zSWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQUO3OUBk\WyuczDlfJBz\XO|aX7nJGJTSUZiVk[wNGUhdXW2YX70JIFnfGW{IEeyJIhzeyCkeTDD[YxtKHSrdHXyMYdtdyCjc4PhfUwhUUN3ME2zNUBvVS5? MlrmNlM1PzR|OEi=
human NOMO-1 cell M4TXW2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MXjJcohq[mm2aX;uJI9nKGi3bXHuJG5QVU9vMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUOxMlk4KG6PLh?= MoPEV2FPT0WU
human DU-4475 cell MkPRS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M{\hTGlvcGmkaYTpc44hd2ZiaIXtZY4hTFVvNES3OUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVM{NjZ5IH7NMi=> MUPTRW5ITVJ?
human M14 cell M1nKcGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MYPJcohq[mm2aX;uJI9nKGi3bXHuJG0yPCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTN4Lki5JI5ONg>? NY\UXpJSW0GQR1XS
human HT-144 cell M2HvPGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NIXL[olKdmirYnn0bY9vKG:oIHj1cYFvKEiWLUG0OEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVg6NjB3IH7NMi=> NYLnT49wW0GQR1XS
human SK-N-AS cell NH6xNFRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NGf5cVNKdmirYnn0bY9vKG:oIHj1cYFvKFONLV6tRXMh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF06Oi56MzDuUU4> MXTTRW5ITVJ?
human LB2518-MEL cell NIni[XBIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MXjJcohq[mm2aX;uJI9nKGi3bXHuJGxDOjVzOD3NSWwh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF06Oy56MjDuUU4> NYTP[GdXW0GQR1XS
human C32 cell NE\YTpdIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MXXJcohq[mm2aX;uJI9nKGi3bXHuJGM{OiClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTl6LkKzJI5ONg>? M{juVnNCVkeHUh?=
human BHT-101 cell MXnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NX6yXlVkUW6qaXLpeIlwdiCxZjDoeY1idiCESGStNVAyKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTB4LkmzJI5ONg>? NYLTUlNKW0GQR1XS
human KY821 cell MYrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MnT3TY5pcWKrdHnvckBw\iCqdX3hckBMYTh{MTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGwO{4yQCCwTT6= MYHTRW5ITVJ?
human CP50-MEL-B cell M1HNUGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NXPBboJJUW6qaXLpeIlwdiCxZjDoeY1idiCFUEWwMW1GVC2EIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUK3Mlk1KG6PLh?= M3v6NXNCVkeHUh?=
human MEL-HO cell NF63cnRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MVXJcohq[mm2aX;uJI9nKGi3bXHuJG1GVC2KTzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGzPE45PCCwTT6= NWLnSWxZW0GQR1XS
human MIAPaCa2 cells M3LXNHBzd2yrZnXyZZRqd25iYYPzZZk> NGfXW2pCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3JRXBiS2F{IHPlcIx{NCCLQ{WwQVE1OiCwTT6= NF[0fJozOzR5NEO4PC=>
human EoL-1-cell cell M2fD[2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NILDXXpKdmirYnn0bY9vKG:oIHj1cYFvKEWxTD2xMYNmdGxiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zNESuO|Yhdk1w NWe3U2R[W0GQR1XS
human DOK cell M3OzXmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NVPyb4x2UW6qaXLpeIlwdiCxZjDoeY1idiCGT1ugZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xOFcvODhibl2u M1zEXnNCVkeHUh?=
human SH-4 cell NVjufYR4T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NVXFcZo4UW6qaXLpeIlwdiCxZjDoeY1idiCVSD20JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVY3NjR6IH7NMi=> M4L4bXNCVkeHUh?=
human BPH-1 cell NWDFT5ZiT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MWrJcohq[mm2aX;uJI9nKGi3bXHuJGJRUC1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUiyMlMyKG6PLh?= NEWxZ45USU6JRWK=
human HuP-T4 cell NH3zXXVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MVvJcohq[mm2aX;uJI9nKGi3bXHuJGh2WC2WNDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUG5OU4{OiCwTT6= MX3TRW5ITVJ?
human KU812 cell M2jUOmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MnHQTY5pcWKrdHnvckBw\iCqdX3hckBMXThzMjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUKxNU43QCCwTT6= M1LQbHNCVkeHUh?=
human A549 cell NVjUWoFtT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NULIfHY1UW6qaXLpeIlwdiCxZjDoeY1idiCDNUS5JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlE1NjF|IH7NMi=> NX\LXIN{W0GQR1XS
human HTC-C3 cell MUHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NF\IR2tKdmirYnn0bY9vKG:oIHj1cYFvKEiWQz3DN{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVIyPC54MTDuUU4> Ml;QV2FPT0WU
human A101D cell M2\W[Wdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MnO1TY5pcWKrdHnvckBw\iCqdX3hckBCOTBzRDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUK0NE4{OyCwTT6= NGm5NpdUSU6JRWK=
human ONS-76 cell NV3id4xRT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NY\oepNuUW6qaXLpeIlwdiCxZjDoeY1idiCRTmOtO|Yh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zPDRwNUOgcm0v NVjHZmZnW0GQR1XS
human RKO cell M3;FS2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NETPR4VKdmirYnn0bY9vKG:oIHj1cYFvKFKNTzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUK0PE4{QCCwTT6= NV3IVpYzW0GQR1XS
human WM-115 cell MX3Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NEnhVnJKdmirYnn0bY9vKG:oIHj1cYFvKFePLUGxOUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVI3Py53NDDuUU4> MV\TRW5ITVJ?
human HCC2998 cell M160eGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 Mn\2TY5pcWKrdHnvckBw\iCqdX3hckBJS0N{OUm4JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlY6NjB5IH7NMi=> MYnTRW5ITVJ?
human C2BBe1 cell MV\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NGnqN2lKdmirYnn0bY9vKG:oIHj1cYFvKEN{QlLlNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVI4Oi53OTDuUU4> NWX4SJFPW0GQR1XS
human RVH-421 cell NHnnVlNIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MkjOTY5pcWKrdHnvckBw\iCqdX3hckBTXkhvNEKxJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9Nlc6NjN7IH7NMi=> NUjjSWdMW0GQR1XS
human H-EMC-SS cell M2rBe2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NVzsc3N3UW6qaXLpeIlwdiCxZjDoeY1idiCKLVXNR{1UWyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTJ7MD65PUBvVS5? MV;TRW5ITVJ?
human ML-2 cell MVHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M1Wy[GlvcGmkaYTpc44hd2ZiaIXtZY4hVUxvMjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUK5N{43OyCwTT6= NGPqfHpUSU6JRWK=
human SW620 cell NYP4boNQT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NEWxTlVKdmirYnn0bY9vKG:oIHj1cYFvKFOZNkKwJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N|AzNjJibl2u M2jaUnNCVkeHUh?=
human UACC-257 cell MYLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M1TZemlvcGmkaYTpc44hd2ZiaIXtZY4hXUGFQz2yOVch[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0{OjFwOESgcm0v MVvTRW5ITVJ?
human AsPC-1 cell MYTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NFzFXoZKdmirYnn0bY9vKG:oIHj1cYFvKEG|UFOtNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVMzPC5|OTDuUU4> NIjtTlFUSU6JRWK=
human CAL-39 cell MUjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M4TOPWlvcGmkaYTpc44hd2ZiaIXtZY4hS0GOLUO5JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N|MzNjJ4IH7NMi=> MkX4V2FPT0WU
human COLO-679 cell NGrYTJVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NWCyWYJrUW6qaXLpeIlwdiCxZjDoeY1idiCFT1zPMVY4QSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTN2MT6xPUBvVS5? MlzBV2FPT0WU
human NCI-H747 cell MV\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? Mn\DTY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEe0O{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVM2OC57ODDuUU4> NVTvd5I3W0GQR1XS
human NCI-H1437 cell NX7FO|FST3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NUDnOmVbUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFE1OzdiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1|NUKuPFUhdk1w MlvEV2FPT0WU
human PSN1 cell MnL3S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M16z[mlvcGmkaYTpc44hd2ZiaIXtZY4hWFOQMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUO2Ok4xQSCwTT6= M1j2S3NCVkeHUh?=
human NKM-1 cell MmfIS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M4m2XWlvcGmkaYTpc44hd2ZiaIXtZY4hVkuPLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zPFUvQCCwTR?= NIm3NmpUSU6JRWK=
human MZ2-MEL cell NIrKVldIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MVnJcohq[mm2aX;uJI9nKGi3bXHuJG1bOi2PRVygZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zPVQvOzdibl2u NGrGUHdUSU6JRWK=
human SK-MEL-2 cell NUm2cItUT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MlHhTY5pcWKrdHnvckBw\iCqdX3hckBUUy2PRVytNkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQxPS5yNjDuUU4> NFzxVGRUSU6JRWK=
human LAMA-84 cell NVfhXJJYT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NInSXpFKdmirYnn0bY9vKG:oIHj1cYFvKEyDTVGtPFQh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF01PTZwMkKgcm0v M3;ydnNCVkeHUh?=
human U-266 cell MWHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? Ml\ITY5pcWKrdHnvckBw\iCqdX3hckBWNTJ4NjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUS4O{44PCCwTT6= M17GbHNCVkeHUh?=
human RCM-1 cell NGHQeZhIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M1LZd2lvcGmkaYTpc44hd2ZiaIXtZY4hWkOPLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME20PVMvQDVibl2u MV3TRW5ITVJ?

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-ERK / ERK / β-catenin / E-cadherin / Vimentin / Fibronection; 

PubMed: 26384399     


MDA-MB-231 and SUM149 cells were treated with selumetinib for 48 hours, and western blot analysis was performed, with β-actin used as a loading control. 

pS6(235/236) / pS6(240/244); 

PubMed: 26137449     


Selumetinib (Sel) in combination with BEZ235 or ZSTK474 inhibits pS6 expression in BRAF-mutant melanoma cell lines that are highly sensitive (NZM3, NZM11, NZM20) or moderately sensitive (NZM6, NZM7, NZM12) to single agent selumetinib. Cells were treated with 500 nM of each compound as indicated for 1 or 24 h. Blots are representative images of two independent determinations.

pVEGFR(Y1175) / VEGFR2 / pPDGFRβ(Y751) / pPDGFRβ / pAXL(Y702) / AXL / pMEK / MEK; 

PubMed: 22500798     


Dose-dependent RTK reprogramming in response to AZD6244. Dose-dependent induction of RTK expression and activity in 24h-treated SUM159 cells was determined by western blot.

Bak / Bad / Bcl-xl / BimEL / BimL / BimS / PUMA / NOXA ; 

PubMed: 20885957     


Human lung cancer cell lines (Calu-6, H2347, and H3122) were treated with 3 µM AZD6244 for 4, 8, 24, 48, and 72 hours.  Western blots of Bcl-2 family members after treatment with AZD6244.

26384399 26137449 22500798 20885957
Immunofluorescence
β-catenin; 

PubMed: 26384399     


MDA-MB-231 and SUM149 cells were treated with selumetinib in a 3D culture for 48 hours. Immunofluorescence staining was done to detect β-catenin-FITC (fluorescein isothiocyanate), and nuclei were stained with DAPI. Images were taken under 60× magnification.

FOXO3a; 

PubMed: 20885957     


Subcellular localization of FOXO3a in Calu-6 and H522 cells was detected with immunofluorescence staining after AZD6244 treatment. 

26384399 20885957
Growth inhibition assay
Cell viability; 

PubMed: 26384399     


MDA-MB-231 and SUM149 cells were treated with selumetinib for 72 hours, and then cell viability was measured using the WST-1 assay.

26384399
体内研究 活体研究显示AZD6244在2-1318, 5-1318, 及26-1004 4-1318移植物中明显抑制ERK1/2的磷酸化,并且在原代2-1318细胞中通过激活caspase通路诱导细胞凋亡。[1]HT-29移植瘤是携带B-raf突变的直肠瘤模型,AZD6244 在100mg/kg剂量时可以抑制HT-29移植瘤中肿瘤的增长,并且AZD6244作用下的肿瘤指数比吉西他滨作用下的肿瘤指数要好[3]。另外,AZD6244可以抑制HCC移植瘤的增长,HCC移植瘤的增长与细胞凋亡的增多,及细胞周期调控的减量调节有关。包括:cyclin D1, cdc-2, CDK 2 ,CDK4, cyclin B1, 及 c-Myc。[4]

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:

[3]

- 合并

激酶实验:

在杆状病毒感染的hi5昆虫细胞中表达的组成型的氮端用六聚组氨酸标记的MEK1,通过金属亲和层析、离子交换及凝胶过滤纯化。MEK1的活性评估通过测量[γ-33P]ATP 作用于ERK2的示踪[γ-33P]磷酸的渗透率。实验在96孔板中进行,保温混合物由25 mM HEPES (pH 7.4), 10 mM MgCl2, 5 mM β-甘油磷酸 100 μM 原钒酸钠, 5 mM DTT, 5 nM MEK1, 1 μM ERK2, 和AZD6244 (溶解在 1% DMSO)组成。加入10 μM ATP (0.5 μC k[γ-33P]ATP/每孔)反应开始,然后在室温下温育45分钟。加入同等量的25%的三氯乙酸反应停止,使蛋白沉淀。沉淀的蛋白加到玻璃纤维过滤板上,用0.5%的磷酸冲洗掉过量的示踪ATP,然后在液体闪烁计数管中计算放射性。通过在反应混合物中改变ATP的量来决定ATP相关性。
细胞实验:

[1]

- 合并
  • Cell lines: 原代HCC细胞系包括2-1318, 4-1318和26-1004细胞
  • Concentrations: 10 μM 左右
  • Incubation Time: 24或48小时
  • Method:

    肿瘤细胞按2.0×104密度接种,温育48小时,然后用培养基清洗细胞两次。用不同浓度的AZD6244处理细胞24小时或者48小时。细胞活力通过MTT实验来测定。用溴脱氧核苷尿嘧啶试剂盒测定细胞增殖。


    (Only for Reference)
动物实验:

[1]

- 合并
  • Animal Models: 携带HCC移植瘤的SCID鼠
  • Formulation: 溶于水中
  • Dosages: 50或100mg/kg
  • Administration: 口服处理
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 91 mg/mL warmed (198.82 mM)
Water Insoluble
Ethanol 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):
4% DMSO+30% PEG 300+5% Tween 80+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 457.68
化学式

C17H15BrClFN4O3

CAS号 606143-52-6
储存条件 粉状
溶于溶剂
别名 ARRY-142886

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
NCT03433183 Recruiting Drug: Selumetinib|Drug: Sirolimus Malignant Peripheral Nerve Sheath Tumors|Neurofibromatosis 1 Sarcoma Alliance for Research through Collaboration|United States Department of Defense|AstraZeneca October 2 2019 Phase 2
NCT03833427 Recruiting Drug: Selumetinib|Biological: Pembrolizumab Advanced/Metastatic Solid Tumors Merck Sharp & Dohme Corp. March 18 2019 Phase 1
NCT03745989 Recruiting Drug: MK-8353|Drug: Selumetinib Solid Tumors Merck Sharp & Dohme Corp. February 22 2019 Phase 1
NCT03326388 Not yet recruiting Drug: Selumetinib Neurofibromatosis Type 1|Plexiform Neurofibroma|Optic Nerve Glioma Great Ormond Street Hospital for Children NHS Foundation Trust|AstraZeneca February 2019 Phase 1|Phase 2
NCT03705507 Recruiting Drug: Selumetinib|Drug: Dexamethasone Acute Lymphoblastic Leukemia|Acute Lymphoblastic Leukemia Adult|Acute Lymphoblastic Leukemia Pediatric|Acute Lymphoblastic Leukemia in Relapse|Acute Lymphoblastic Leukemia Recurrent University of Birmingham|Cancer Research UK|AstraZeneca April 17 2018 Phase 1|Phase 2
NCT00553332 Completed Drug: selumetinib|Other: laboratory biomarker analysis Liver and Intrahepatic Biliary Tract Cancer|Recurrent Extrahepatic Bile Duct Cancer|Unresectable Extrahepatic Bile Duct Cancer National Cancer Institute (NCI) November 2007 Phase 2

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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:

    How about the solubility of S1008? How to prepare for the solution if I need to do the in vivo experiments?

  • 回答:

    S1008 AZD6244 in vehicle 5% DMSO+30% PEG 300+ddH2O will be a suspension for oral administration. If you want a clear solution for injection, you can dissolve it in 4% DMSO+30% PEG 300+5% Tween 80+ddH2O.

MEK Signaling Pathway Map

MEK Inhibitors with Unique Features

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID