Selumetinib (AZD6244)

For research use only. Not for use in humans.

Catalog No.S1008 Synonyms: ARRY-142886

398 publications

Selumetinib (AZD6244) Chemical Structure

Molecular Weight(MW): 457.68

Selumetinib (AZD6244) is a potent, highly selective MEK inhibitor with IC50 of 14 nM for MEK1 and Kd value of 530 nM for MEK2. It also inhibits ERK1/2 phosphorylation with IC50 of 10 nM, no inhibition to p38α, MKK6, EGFR, ErbB2, ERK2, B-Raf, etc. Phase 3.

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Selleck's Selumetinib (AZD6244) has been cited by 398 publications

Purity & Quality Control

Choose Selective MEK Inhibitors

Biological Activity

Description Selumetinib (AZD6244) is a potent, highly selective MEK inhibitor with IC50 of 14 nM for MEK1 and Kd value of 530 nM for MEK2. It also inhibits ERK1/2 phosphorylation with IC50 of 10 nM, no inhibition to p38α, MKK6, EGFR, ErbB2, ERK2, B-Raf, etc. Phase 3.
Features First MEK inhibitor being tested in Phase II clinical trials.
Targets
MEK1 [1]
(Cell-free assay)
MEK1 [13]
(Cell-free assay)
MEK2 [13]
(Cell-free assay)
14 nM 99 nM(Kd) 530 nM(Kd)
In vitro

AZD6244 is not competitive with ATP and inactivates the ERK1/2 phosphorylation with IC50 concentrations below 40 nM. AZD6244 also inhibits the growth of primary HCC cells through inhibition of ERK1/2 and p90RSK phosphorylation, accompanied with elevation of the cleavage of caspase-3 and caspase-7, and cleaved poly(ADP)ribose polymerase. AZD6244 has little effects on the p38, c-Jun-NH2-kinase, phosphatidylinositol 3-kinase, and MEK5/ERK5 pathways. [1] AZD6244 is sensitive to Raf mutations in breast cancer cell lines and Ras mutations in NSCLC cell lines. [2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human CHP-212 cell NV[zPI5HT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NHnnfZFKdmirYnn0bY9vKG:oIHj1cYFvKEOKUD2yNVIh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0{NjF3IH7NMi=> M1\1bXNCVkeHUh?=
human H9 cell M3fVOWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MoTSTY5pcWKrdHnvckBw\iCqdX3hckBJQSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTJ{Lki4JI5ONg>? M3GwOHNCVkeHUh?=
human HL-60 cell MWXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NF60XGZKdmirYnn0bY9vKG:oIHj1cYFvKEiOLU[wJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlQvPTlibl2u NInu[ZVUSU6JRWK=
human A375 cells M3nzenBzd2yrZnXyZZRqd25iYYPzZZk> Mof3O|IhcA>? MULBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEF|N{WgZ4VtdHNiZYjwdoV{e2mwZzDCVmFHKFZ4MEDFJI12fGGwdDDh[pRmeiB5MjDodpMh[nliQ3XscEB1cXSncj3ncI8h[XO|YYmsJGlEPTB;M{Ggcm0v NETCdVIzOzR5NEO4PC=>
human NOMO-1 cell Mon5S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? Mn\2TY5pcWKrdHnvckBw\iCqdX3hckBPV02RLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zNU46PyCwTT6= MV\TRW5ITVJ?
human DU-4475 cell NULqNHZiT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NGm0PWpKdmirYnn0bY9vKG:oIHj1cYFvKESXLUS0O|Uh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0{Oy54NzDuUU4> MWPTRW5ITVJ?
human M14 cell NFnNNodIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MYLJcohq[mm2aX;uJI9nKGi3bXHuJG0yPCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTN4Lki5JI5ONg>? M3jufXNCVkeHUh?=
human HT-144 cell Mk[0S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MXrJcohq[mm2aX;uJI9nKGi3bXHuJGhVNTF2NDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUi5MlA2KG6PLh?= MnWyV2FPT0WU
human SK-N-AS cell MUfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NELRXndKdmirYnn0bY9vKG:oIHj1cYFvKFONLV6tRXMh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF06Oi56MzDuUU4> M{LkNnNCVkeHUh?=
human LB2518-MEL cell NWj3Zpk6T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MWfJcohq[mm2aX;uJI9nKGi3bXHuJGxDOjVzOD3NSWwh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF06Oy56MjDuUU4> Mn\qV2FPT0WU
human C32 cell MVnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NGPadIZKdmirYnn0bY9vKG:oIHj1cYFvKEN|MjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUm4MlI{KG6PLh?= NHXq[JFUSU6JRWK=
human BHT-101 cell NYPK[G1oT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M1\MeGlvcGmkaYTpc44hd2ZiaIXtZY4hSkiWLUGwNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVExPi57MzDuUU4> NIL4SJZUSU6JRWK=
human KY821 cell NHzkc5FIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MYHJcohq[mm2aX;uJI9nKGi3bXHuJGt[QDJzIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUC3MlE5KG6PLh?= MUTTRW5ITVJ?
human CP50-MEL-B cell NXrSUI12T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MnPxTY5pcWKrdHnvckBw\iCqdX3hckBEWDVyLV3FUE1DKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTJ5Lkm0JI5ONg>? M2DUNnNCVkeHUh?=
human MEL-HO cell MnrKS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? Mn;ITY5pcWKrdHnvckBw\iCqdX3hckBOTUxvSF:gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xN|gvQDRibl2u NVy3e4tWW0GQR1XS
human MIAPaCa2 cells NFXnTYlRem:uaX\ldoF1cW:wIHHzd4F6 NV:0WmxQSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNTWFR[UOjMjDj[YxteyxiSVO1NF0yPDJibl2u MlHuNlM1PzR|OEi=
human EoL-1-cell cell M3zNd2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MkfnTY5pcWKrdHnvckBw\iCqdX3hckBGd0xvMT3j[YxtKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTR2Lke2JI5ONg>? MkD0V2FPT0WU
human DOK cell MXPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MnyyTY5pcWKrdHnvckBw\iCqdX3hckBFV0tiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zNEeuNFghdk1w MVjTRW5ITVJ?
human SH-4 cell NGDqWIhIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NV;qVXduUW6qaXLpeIlwdiCxZjDoeY1idiCVSD20JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVY3NjR6IH7NMi=> MlvLV2FPT0WU
human BPH-1 cell NFTzXZdIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MXjJcohq[mm2aX;uJI9nKGi3bXHuJGJRUC1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUiyMlMyKG6PLh?= NUfVNmhEW0GQR1XS
human HuP-T4 cell NUTYb4h2T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MXjJcohq[mm2aX;uJI9nKGi3bXHuJGh2WC2WNDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUG5OU4{OiCwTT6= M{jVWHNCVkeHUh?=
human KU812 cell M{Gzfmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MnLaTY5pcWKrdHnvckBw\iCqdX3hckBMXThzMjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUKxNU43QCCwTT6= Moj4V2FPT0WU
human A549 cell MnvJS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NVzadIh[UW6qaXLpeIlwdiCxZjDoeY1idiCDNUS5JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlE1NjF|IH7NMi=> NX;qWllLW0GQR1XS
human HTC-C3 cell MV\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MnLsTY5pcWKrdHnvckBw\iCqdX3hckBJXENvQ{OgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yNVQvPjFibl2u NH;STZBUSU6JRWK=
human A101D cell M33sfmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MVTJcohq[mm2aX;uJI9nKGi3bXHuJGEyODGGIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MkSwMlM{KG6PLh?= M2\aU3NCVkeHUh?=
human ONS-76 cell NVnWXZN[T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M2\1b2lvcGmkaYTpc44hd2ZiaIXtZY4hV06VLUe2JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlQ1NjV|IH7NMi=> NWTVcVRpW0GQR1XS
human RKO cell MonOS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NYLZZldDUW6qaXLpeIlwdiCxZjDoeY1idiCUS1:gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yOFgvOzhibl2u NWjUOVVFW0GQR1XS
human WM-115 cell NH;hSFdIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NWLkU3VwUW6qaXLpeIlwdiCxZjDoeY1idiCZTT2xNVUh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zPjdwNUSgcm0v NWHCS4V1W0GQR1XS
human HCC2998 cell NFPvNllIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NHmyNXBKdmirYnn0bY9vKG:oIHj1cYFvKEiFQ{K5PVgh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zPjlwMEegcm0v MoTkV2FPT0WU
human C2BBe1 cell NVPGepVzT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M1uyW2lvcGmkaYTpc44hd2ZiaIXtZY4hSzKEQnWxJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlczNjV7IH7NMi=> NXLlNIxRW0GQR1XS
human RVH-421 cell NHXufZRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MYLJcohq[mm2aX;uJI9nKGi3bXHuJHJXUC12MkGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yO|kvOzlibl2u Mo\UV2FPT0WU
human H-EMC-SS cell MlziS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NXLvOYtuUW6qaXLpeIlwdiCxZjDoeY1idiCKLVXNR{1UWyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTJ7MD65PUBvVS5? MnXtV2FPT0WU
human ML-2 cell MknnS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? Mnn4TY5pcWKrdHnvckBw\iCqdX3hckBOVC1{IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MkmzMlY{KG6PLh?= NYjEbXFMW0GQR1XS
human SW620 cell NYnCSWs2T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M2DLSmlvcGmkaYTpc44hd2ZiaIXtZY4hW1d4MkCgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zNFIvOiCwTT6= MYfTRW5ITVJ?
human UACC-257 cell NU\GWphnT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NH3qT4lKdmirYnn0bY9vKG:oIHj1cYFvKFWDQ1OtNlU4KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OzJzLki0JI5ONg>? NFX6fVlUSU6JRWK=
human AsPC-1 cell M2TpW2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MkjUTY5pcWKrdHnvckBw\iCqdX3hckBCe1CFLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zNlQvOzlibl2u M3PLdnNCVkeHUh?=
human CAL-39 cell MnHGS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NFP2flZKdmirYnn0bY9vKG:oIHj1cYFvKEODTD2zPUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVM{Oi5{NjDuUU4> NHj6dFlUSU6JRWK=
human COLO-679 cell MnfpS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NFGyTJVKdmirYnn0bY9vKG:oIHj1cYFvKEORTF:tOlc6KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OzRzLkG5JI5ONg>? NVLIb5ROW0GQR1XS
human NCI-H747 cell Ml\nS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NWXITnlZUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFc1PyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTN3MD65PEBvVS5? NV2yZ5JtW0GQR1XS
human NCI-H1437 cell MmjyS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NFz1SWhKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3INVQ{PyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTN3Mj64OUBvVS5? NUfxRVc5W0GQR1XS
human PSN1 cell MmjvS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MkXYTY5pcWKrdHnvckBw\iCqdX3hckBRW05zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;M{[2MlA6KG6PLh?= MkjaV2FPT0WU
human NKM-1 cell NYOySWZJT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NWntbll5UW6qaXLpeIlwdiCxZjDoeY1idiCQS12tNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVM5PS56IH7N NUL5TVZtW0GQR1XS
human MZ2-MEL cell MYXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MUjJcohq[mm2aX;uJI9nKGi3bXHuJG1bOi2PRVygZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zPVQvOzdibl2u NGnUUG1USU6JRWK=
human SK-MEL-2 cell NImzTGNIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NH7CSGRKdmirYnn0bY9vKG:oIHj1cYFvKFONLV3FUE0zKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PDB3LkC2JI5ONg>? NE\Cd3hUSU6JRWK=
human LAMA-84 cell NHvuVJRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= Ml;RTY5pcWKrdHnvckBw\iCqdX3hckBNSU2DLUi0JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OFU3NjJ{IH7NMi=> M3\NVHNCVkeHUh?=
human U-266 cell NWDQWWFCT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= Mnz3TY5pcWKrdHnvckBw\iCqdX3hckBWNTJ4NjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUS4O{44PCCwTT6= MkTnV2FPT0WU
human RCM-1 cell M{LnR2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M1jzcGlvcGmkaYTpc44hd2ZiaIXtZY4hWkOPLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME20PVMvQDVibl2u NUe5PGg{W0GQR1XS

... 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
In vivo AZD6244 significantly inhibits phosphorylation of ERK1/2 in 2-1318, 5-1318, 26-1004 and 4-1318 xenografts and induces apoptosis in primary 2-1318 cells by activating the caspase pathway. [1] AZD6244 could inhibit the tumor growth in HT-29 xenograft, which is a colorectal tumor model carrying a B-Raf mutation, at a dose of 100 mg/kg and the tumor growth inhibition of AZD6244 is better than it of Gemcitabine. [3] Otherwise AZD6244 could inhibit HCC xenografts tumor growth, which associated with increased apoptosis and down-regulation of cell cycle regulators, including cyclin D1, Cdc-2, CDK2 and 4, cyclin B1, and c-Myc. [4]

Protocol

Kinase Assay:

[1]

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Assay of MEK Kinase Activity:

Anti-MEK1 antibody is used to immunoprecipitate MEK1 molecules. MEK kinase activity is measured as the ability of immuno-isolated MEK1 to activate recombinant ERK1 in a coupled assay using MBP as the end point of the assay. Phosphorylated MBP is resolved on a 14% SDS-PAGE gel and vacuum-dried before exposure to X-ray film.
Cell Research:

[1]

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  • Cell lines: Primary HCC cell lines including 2-1318, 4-1318 and 26-1004 cells
  • Concentrations: ~ 10 μM
  • Incubation Time: 24 or 48 hours
  • Method:

    Cells are seeded at a density of 2.0 × 104. After 48 hours incubation, the cells are rinsed twice with culture media. Cells are treated with various concentrations of AZD6244 for 24 or 48 hours. Cell viability is determined by the 3-(4,5-dimethylthiazol-2y1)-2,5-diphenyltetrazolium bromide (MTT) assay. Cell proliferation is assayed using a bromodeoxyuridine kit.


    (Only for Reference)
Animal Research:

[1]

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  • Animal Models: HCC xenografts in mice homozygous for the SCID (severe combined immunodeficiency) mutation
  • Formulation: In water
  • Dosages: 50 or 100mg/kg
  • Administration: Administered via p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 91 mg/mL warmed (198.82 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
4% DMSO+30% PEG 300+5% Tween 80+ddH2O
For best results, use promptly after mixing.
5mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 457.68
Formula

C17H15BrClFN4O3

CAS No. 606143-52-6
Storage powder
in solvent
Synonyms ARRY-142886
Smiles C[N]1C=NC2=C(F)C(=C(C=C12)C(=O)NOCCO)NC3=CC=C(Br)C=C3Cl

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • 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):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

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

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

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Frequently Asked Questions

  • Question 1:

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

  • Answer:

    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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID