Selumetinib (AZD6244)

Catalog No.S1008 Synonyms: ARRY-142886

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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Cited by 145 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 M2n0OGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MYTJcohq[mm2aX;uJI9nKGi3bXHuJGNJWC1{MUKgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zMlE2KG6PLh?= MVnTRW5ITVJ?
human H9 cell NYHMdpN1T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NITST49KdmirYnn0bY9vKG:oIHj1cYFvKEh7IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MkKuPFghdk1w NGHmcJNUSU6JRWK=
human HL-60 cell MoO4S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NXO3R4pDUW6qaXLpeIlwdiCxZjDoeY1idiCKTD22NEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVI1NjV7IH7NMi=> NXTIO242W0GQR1XS
human A375 cells MUDQdo9tcW[ncnH0bY9vKGG|c3H5 MmrMO|IhcA>? NUeyTlR4SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDBN|c2KGOnbHzzJIV5eHKnc4PpcochSlKDRjDWOlAxTSCvdYThcpQh[W[2ZYKgO|IhcHK|IHL5JGNmdGxidHn0[ZIu\2yxIHHzd4F6NCCLQ{WwQVMyKG6PLh?= MlPDNlM1PzR|OEi=
human NOMO-1 cell NUnJPFhHT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M3G5V2lvcGmkaYTpc44hd2ZiaIXtZY4hVk:PTz2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N|EvQTdibl2u M1v5VXNCVkeHUh?=
human DU-4475 cell NVzxfWdbT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M{LnXmlvcGmkaYTpc44hd2ZiaIXtZY4hTFVvNES3OUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVM{NjZ5IH7NMi=> MXfTRW5ITVJ?
human M14 cell NXTEd3BTT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NEjyZnRKdmirYnn0bY9vKG:oIHj1cYFvKE1zNDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUO2Mlg6KG6PLh?= M3PKeXNCVkeHUh?=
human HT-144 cell MVnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NHXIdJZKdmirYnn0bY9vKG:oIHj1cYFvKEiWLUG0OEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVg6NjB3IH7NMi=> MX3TRW5ITVJ?
human SK-N-AS cell M4\UT2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MmHyTY5pcWKrdHnvckBw\iCqdX3hckBUUy2QLVHTJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9PVIvQDNibl2u MX;TRW5ITVJ?
human LB2518-MEL cell NFXkeGNIem:5dHigbY5pcWKrdHnvckBie3OjeR?= Mon5TY5pcWKrdHnvckBw\iCqdX3hckBNSjJ3MUitUWVNKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:QTNwOEKgcm0v NEPQSnlUSU6JRWK=
human C32 cell NHjVNmpIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NWnxNVZQUW6qaXLpeIlwdiCxZjDoeY1idiCFM{KgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME25PE4zOyCwTT6= MmXpV2FPT0WU
human BHT-101 cell M3qwW2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NF;RPZNKdmirYnn0bY9vKG:oIHj1cYFvKEKKVD2xNFEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yODZwOUOgcm0v NFLadoxUSU6JRWK=
human KY821 cell M{m4Tmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MojTTY5pcWKrdHnvckBw\iCqdX3hckBMYTh{MTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGwO{4yQCCwTT6= MlzNV2FPT0WU
human CP50-MEL-B cell NE\TSndIem:5dHigbY5pcWKrdHnvckBie3OjeR?= Ml3HTY5pcWKrdHnvckBw\iCqdX3hckBEWDVyLV3FUE1DKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTJ5Lkm0JI5ONg>? MVvTRW5ITVJ?
human MEL-HO cell NILRbZlIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NWjrWnYxUW6qaXLpeIlwdiCxZjDoeY1idiCPRVytTG8h[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yOzhwOESgcm0v MVHTRW5ITVJ?
human MIAPaCa2 cells MVTQdo9tcW[ncnH0bY9vKGG|c3H5 NFvQeoJCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3JRXBiS2F{IHPlcIx{NCCLQ{WwQVE1OiCwTT6= NG\PbGwzOzR5NEO4PC=>
human EoL-1-cell cell MX;Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MWLJcohq[mm2aX;uJI9nKGi3bXHuJGVwVC1zLXPlcIwh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yPDRwN{[gcm0v NGfzV4xUSU6JRWK=
human DOK cell NUnHcm0xT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M4nhcGlvcGmkaYTpc44hd2ZiaIXtZY4hTE:NIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUS3MlA5KG6PLh?= MXHTRW5ITVJ?
human SH-4 cell NHLoeVZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NF7NdHJKdmirYnn0bY9vKG:oIHj1cYFvKFOKLUSgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xOlYvPDhibl2u MkDsV2FPT0WU
human BPH-1 cell MYXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MmPkTY5pcWKrdHnvckBw\iCqdX3hckBDWEhvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUG4Nk4{OSCwTT6= NFP0SlBUSU6JRWK=
human HuP-T4 cell Ml3MS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MkDYTY5pcWKrdHnvckBw\iCqdX3hckBJfVBvVESgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xPVUvOzJibl2u MnfRV2FPT0WU
human KU812 cell NWruSVd2T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= Mn74TY5pcWKrdHnvckBw\iCqdX3hckBMXThzMjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUKxNU43QCCwTT6= NE[ybIRUSU6JRWK=
human A549 cell M{XBeGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MmX3TY5pcWKrdHnvckBw\iCqdX3hckBCPTR7IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MkG0MlE{KG6PLh?= NEPmfJRUSU6JRWK=
human HTC-C3 cell Mo\lS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NEL0WJJKdmirYnn0bY9vKG:oIHj1cYFvKEiWQz3DN{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVIyPC54MTDuUU4> NW\BeZVoW0GQR1XS
human A101D cell NFfBOXlIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MVrJcohq[mm2aX;uJI9nKGi3bXHuJGEyODGGIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MkSwMlM{KG6PLh?= MmjiV2FPT0WU
human ONS-76 cell MXXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NEDYRmZKdmirYnn0bY9vKG:oIHj1cYFvKE:QUz23OkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVI1PC53MzDuUU4> NVHENHJbW0GQR1XS
human RKO cell NInmRm9Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= MVjJcohq[mm2aX;uJI9nKGi3bXHuJHJMVyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTJ2OD6zPEBvVS5? NWXyU24zW0GQR1XS
human WM-115 cell M2nzdGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MUPJcohq[mm2aX;uJI9nKGi3bXHuJHdONTFzNTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUK2O{42PCCwTT6= MVXTRW5ITVJ?
human HCC2998 cell M{S5dWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MlThTY5pcWKrdHnvckBw\iCqdX3hckBJS0N{OUm4JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlY6NjB5IH7NMi=> NGjzR4FUSU6JRWK=
human C2BBe1 cell NHf0e4dIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MYHJcohq[mm2aX;uJI9nKGi3bXHuJGMzSkKnMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUK3Nk42QSCwTT6= MWjTRW5ITVJ?
human RVH-421 cell M2nQSWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MojzTY5pcWKrdHnvckBw\iCqdX3hckBTXkhvNEKxJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9Nlc6NjN7IH7NMi=> NGDQZVNUSU6JRWK=
human H-EMC-SS cell MoT5S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NHzVSWNKdmirYnn0bY9vKG:oIHj1cYFvKEhvRV3DMXNUKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OjlyLkm5JI5ONg>? MYPTRW5ITVJ?
human ML-2 cell Mn23S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MUnJcohq[mm2aX;uJI9nKGi3bXHuJG1NNTJiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1{OUOuOlMhdk1w NXPEVFRiW0GQR1XS
human SW620 cell M4nQWGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M2DaTWlvcGmkaYTpc44hd2ZiaIXtZY4hW1d4MkCgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zNFIvOiCwTT6= M{j4TnNCVkeHUh?=
human UACC-257 cell MWXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NH;wcXhKdmirYnn0bY9vKG:oIHj1cYFvKFWDQ1OtNlU4KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OzJzLki0JI5ONg>? NFjXRmtUSU6JRWK=
human AsPC-1 cell MWrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NYfZd4VlUW6qaXLpeIlwdiCxZjDoeY1idiCDc2DDMVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0{OjRwM{mgcm0v MoTyV2FPT0WU
human CAL-39 cell NXX5dGNYT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NXHldGRYUW6qaXLpeIlwdiCxZjDoeY1idiCFQVytN|kh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0{OzJwMk[gcm0v Ml;WV2FPT0WU
human COLO-679 cell MWfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? Mn7qTY5pcWKrdHnvckBw\iCqdX3hckBEV0yRLU[3PUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVM1OS5zOTDuUU4> NVew[IdtW0GQR1XS
human NCI-H747 cell Mn3TS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NIfyW5VKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3IO|Q4KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OzVyLkm4JI5ONg>? M3HFV3NCVkeHUh?=
human NCI-H1437 cell Mne0S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NXLsOHhuUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFE1OzdiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1|NUKuPFUhdk1w NWfDNlEzW0GQR1XS
human PSN1 cell MoTpS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MkXmTY5pcWKrdHnvckBw\iCqdX3hckBRW05zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;M{[2MlA6KG6PLh?= M{DPVHNCVkeHUh?=
human NKM-1 cell NHHUdo1Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= MWnJcohq[mm2aX;uJI9nKGi3bXHuJG5MVS1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;M{i1Mlghdk1? M3PGUXNCVkeHUh?=
human MZ2-MEL cell NYO1bYZ6T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NWXuT|FPUW6qaXLpeIlwdiCxZjDoeY1idiCPWkKtUWVNKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:Ozl2LkO3JI5ONg>? NEL0XpBUSU6JRWK=
human SK-MEL-2 cell NGH1bItIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MULJcohq[mm2aX;uJI9nKGi3bXHuJHNMNU2HTD2yJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OFA2NjB4IH7NMi=> MYfTRW5ITVJ?
human LAMA-84 cell M4nNVmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MX\Jcohq[mm2aX;uJI9nKGi3bXHuJGxCVUFvOESgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME20OVYvOjJibl2u NXzVS3pFW0GQR1XS
human U-266 cell NXXiUZZKT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NV;ocWZGUW6qaXLpeIlwdiCxZjDoeY1idiCXLUK2OkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQ5Py55NDDuUU4> MnXFV2FPT0WU
human RCM-1 cell NX7KWnl{T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MlHkTY5pcWKrdHnvckBw\iCqdX3hckBTS01vMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUS5N{45PSCwTT6= MVXTRW5ITVJ?

... 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]

+ Expand

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]

+ Expand
  • 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]

+ Expand
  • 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

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 (g) = Concentration (mol/L) × Volume (L) × 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 Conditions Sponsor/Collaborators Start Date Phases
NCT03871257 Not yet recruiting Low Grade Glioma|Neurofibromatosis Type 1|Visual Pathway Glioma National Cancer Institute (NCI) May 3 2019 Phase 3
NCT03871257 Not yet recruiting Low Grade Glioma|Neurofibromatosis Type 1|Visual Pathway Glioma National Cancer Institute (NCI) May 3 2019 Phase 3
NCT03581487 Not yet recruiting Recurrent Non-Small Cell Lung Carcinoma|Stage IV Lung Cancer|Stage IVA Lung Cancer|Stage IVB Lung Cancer M.D. Anderson Cancer Center|National Cancer Institute (NCI) April 15 2019 Phase 1|Phase 2
NCT03581487 Not yet recruiting Recurrent Non-Small Cell Lung Carcinoma|Stage IV Lung Cancer|Stage IVA Lung Cancer|Stage IVB Lung Cancer M.D. Anderson Cancer Center|National Cancer Institute (NCI) April 15 2019 Phase 1|Phase 2
NCT03433183 Not yet recruiting Malignant Peripheral Nerve Sheath Tumors|Neurofibromatosis 1 Sarcoma Alliance for Research through Collaboration|United States Department of Defense|AstraZeneca March 2019 Phase 2
NCT03109301 Recruiting Neoplasms Nerve Tissue|Neurofibromatosis 1|Heredodegenerative Disorders Nervous System|Peripheral Nervous System Diseases National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) March 28 2019 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