Selumetinib (AZD6244)

For research use only.

Catalog No.S1008 Synonyms: ARRY-142886

495 publications

Selumetinib (AZD6244) Chemical Structure

CAS No. 606143-52-6

Selumetinib (AZD6244, ARRY-142886) 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. Selumetinib suppresses cell proliferation, migration and trigger apoptosis. Phase 3.

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Selleck's Selumetinib (AZD6244) has been cited by 495 publications

Purity & Quality Control

Choose Selective MEK Inhibitors

Biological Activity

Description Selumetinib (AZD6244, ARRY-142886) 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. Selumetinib suppresses cell proliferation, migration and trigger apoptosis. 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 Ml3iS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NGLvXo5KdmirYnn0bY9vKG:oIHj1cYFvKEOKUD2yNVIh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0{NjF3IH7NMi=> MnHhV2FPT0WU
human H9 cell NH[zboZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MV3Jcohq[mm2aX;uJI9nKGi3bXHuJGg6KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OjJwOEigcm0v MX\TRW5ITVJ?
human HL-60 cell MkXzS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M1jzS2lvcGmkaYTpc44hd2ZiaIXtZY4hUExvNkCgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yOE42QSCwTT6= MXrTRW5ITVJ?
human A375 cells MkfSVJJwdGmoZYLheIlwdiCjc4PhfS=> MVO3NkBp MVPBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEF|N{WgZ4VtdHNiZYjwdoV{e2mwZzDCVmFHKFZ4MEDFJI12fGGwdDDh[pRmeiB5MjDodpMh[nliQ3XscEB1cXSncj3ncI8h[XO|YYmsJGlEPTB;M{Ggcm0v MV6yN|Q4PDN6OB?=
human NOMO-1 cell NXi3V5FbT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MnHrTY5pcWKrdHnvckBw\iCqdX3hckBPV02RLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zNU46PyCwTT6= MkD5V2FPT0WU
human DU-4475 cell MYDHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NXfRclNwUW6qaXLpeIlwdiCxZjDoeY1idiCGVT20OFc2KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OzNwNkegcm0v MnzBV2FPT0WU
human M14 cell M3jZUmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NIPmNmhKdmirYnn0bY9vKG:oIHj1cYFvKE1zNDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUO2Mlg6KG6PLh?= NIXV[JNUSU6JRWK=
human HT-144 cell MVjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MmW5TY5pcWKrdHnvckBw\iCqdX3hckBJXC1zNESgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME24PU4xPSCwTT6= MWrTRW5ITVJ?
human SK-N-AS cell Mkm1S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MmLVTY5pcWKrdHnvckBw\iCqdX3hckBUUy2QLVHTJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9PVIvQDNibl2u MnPIV2FPT0WU
human LB2518-MEL cell NUns[5JOT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NE\Jd2VKdmirYnn0bY9vKG:oIHj1cYFvKEyEMkWxPE1OTUxiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD17Mz64NkBvVS5? M2XNdHNCVkeHUh?=
human C32 cell Mo\sS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NH\zRYVKdmirYnn0bY9vKG:oIHj1cYFvKEN|MjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUm4MlI{KG6PLh?= MnTnV2FPT0WU
human BHT-101 cell MWLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M4DFSGlvcGmkaYTpc44hd2ZiaIXtZY4hSkiWLUGwNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVExPi57MzDuUU4> MVXTRW5ITVJ?
human KY821 cell M{HrW2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NUn1cJdkUW6qaXLpeIlwdiCxZjDoeY1idiCNWUiyNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVExPy5zODDuUU4> NV6wT3BMW0GQR1XS
human CP50-MEL-B cell M3;SXmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MmjaTY5pcWKrdHnvckBw\iCqdX3hckBEWDVyLV3FUE1DKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTJ5Lkm0JI5ONg>? Mn7CV2FPT0WU
human MEL-HO cell MoHlS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NGPwUHRKdmirYnn0bY9vKG:oIHj1cYFvKE2HTD3IU{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVE{QC56NDDuUU4> MlLyV2FPT0WU
human MIAPaCa2 cells NVrScm1TWHKxbHnm[ZJifGmxbjDhd5NigQ>? MYLBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2LQWDhR4EzKGOnbHzzMEBKSzVyPUG0NkBvVS5? M4DyelI{PDd2M{i4
human EoL-1-cell cell MmLzS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M3PpSGlvcGmkaYTpc44hd2ZiaIXtZY4hTW:OLUGtZ4VtdCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTF2ND63OkBvVS5? M37o[HNCVkeHUh?=
human DOK cell NVnCXot6T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= Mo\5TY5pcWKrdHnvckBw\iCqdX3hckBFV0tiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zNEeuNFghdk1w MV7TRW5ITVJ?
human SH-4 cell M3fU[Wdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MlX3TY5pcWKrdHnvckBw\iCqdX3hckBUUC12IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MU[2MlQ5KG6PLh?= MW\TRW5ITVJ?
human BPH-1 cell NF3OWo1Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= MX\Jcohq[mm2aX;uJI9nKGi3bXHuJGJRUC1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUiyMlMyKG6PLh?= M3jHRnNCVkeHUh?=
human HuP-T4 cell MofWS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MoD3TY5pcWKrdHnvckBw\iCqdX3hckBJfVBvVESgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xPVUvOzJibl2u NWixcXd5W0GQR1XS
human KU812 cell NWXZb41UT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NVvEOnV7UW6qaXLpeIlwdiCxZjDoeY1idiCNVUixNkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVIyOS54ODDuUU4> M2PIUnNCVkeHUh?=
human A549 cell NHPXW25Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= M1f4Z2lvcGmkaYTpc44hd2ZiaIXtZY4hSTV2OTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUKxOE4yOyCwTT6= NXrnTXpxW0GQR1XS
human HTC-C3 cell MX3Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NWjmfHJFUW6qaXLpeIlwdiCxZjDoeY1idiCKVFOtR|Mh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zOTRwNkGgcm0v MVPTRW5ITVJ?
human A101D cell NVjIXoVkT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NGfZe5hKdmirYnn0bY9vKG:oIHj1cYFvKEFzMEHEJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlQxNjN|IH7NMi=> MoO3V2FPT0WU
human ONS-76 cell NEDIVopIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NXrRcmFvUW6qaXLpeIlwdiCxZjDoeY1idiCRTmOtO|Yh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zPDRwNUOgcm0v MoDIV2FPT0WU
human RKO cell Mmi1S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NYjQZ2NIUW6qaXLpeIlwdiCxZjDoeY1idiCUS1:gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yOFgvOzhibl2u Mm\nV2FPT0WU
human WM-115 cell NEPKUppIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M{faNWlvcGmkaYTpc44hd2ZiaIXtZY4hX01vMUG1JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlY4NjV2IH7NMi=> NHSyVZNUSU6JRWK=
human HCC2998 cell NUjMfGVQT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MlrZTY5pcWKrdHnvckBw\iCqdX3hckBJS0N{OUm4JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlY6NjB5IH7NMi=> NGrKNnlUSU6JRWK=
human C2BBe1 cell MljMS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MlXUTY5pcWKrdHnvckBw\iCqdX3hckBEOkKEZUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yO|IvPTlibl2u NUnTfIJWW0GQR1XS
human RVH-421 cell M{\3S2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MXPJcohq[mm2aX;uJI9nKGi3bXHuJHJXUC12MkGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yO|kvOzlibl2u M{Tk[3NCVkeHUh?=
human H-EMC-SS cell MVPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M1\Ee2lvcGmkaYTpc44hd2ZiaIXtZY4hUC2HTVOtV3Mh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zQTBwOUmgcm0v MnH0V2FPT0WU
human ML-2 cell NUHoR3IyT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M3HtVmlvcGmkaYTpc44hd2ZiaIXtZY4hVUxvMjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUK5N{43OyCwTT6= NGqwblhUSU6JRWK=
human SW620 cell NV;Cc5MzT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NH:z[G9KdmirYnn0bY9vKG:oIHj1cYFvKFOZNkKwJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N|AzNjJibl2u NGWzeYJUSU6JRWK=
human UACC-257 cell MkHYS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M1W1cmlvcGmkaYTpc44hd2ZiaIXtZY4hXUGFQz2yOVch[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0{OjFwOESgcm0v NW[5boN6W0GQR1XS
human AsPC-1 cell MY\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NYPkTlF5UW6qaXLpeIlwdiCxZjDoeY1idiCDc2DDMVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0{OjRwM{mgcm0v Mnu2V2FPT0WU
human CAL-39 cell NWHVUVZQT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MVnJcohq[mm2aX;uJI9nKGi3bXHuJGNCVC1|OTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUOzNk4zPiCwTT6= M1r2XHNCVkeHUh?=
human COLO-679 cell NHzVeZNIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NXTId|BPUW6qaXLpeIlwdiCxZjDoeY1idiCFT1zPMVY4QSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTN2MT6xPUBvVS5? NIjWPG9USU6JRWK=
human NCI-H747 cell M33JRWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M325UGlvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLVi3OFch[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0{PTBwOUigcm0v NYLpZXBnW0GQR1XS
human NCI-H1437 cell NX\nepdpT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NXK0b4xyUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFE1OzdiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1|NUKuPFUhdk1w NFOxUXBUSU6JRWK=
human PSN1 cell M37hTGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NXPGOHlRUW6qaXLpeIlwdiCxZjDoeY1idiCSU16xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N|Y3NjB7IH7NMi=> NFXrUFhUSU6JRWK=
human NKM-1 cell MX3Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MXzJcohq[mm2aX;uJI9nKGi3bXHuJG5MVS1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;M{i1Mlghdk1? MX3TRW5ITVJ?
human MZ2-MEL cell NHXySFFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MXTJcohq[mm2aX;uJI9nKGi3bXHuJG1bOi2PRVygZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zPVQvOzdibl2u MXXTRW5ITVJ?
human SK-MEL-2 cell MmLRS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NHHF[GdKdmirYnn0bY9vKG:oIHj1cYFvKFONLV3FUE0zKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PDB3LkC2JI5ONg>? MlvoV2FPT0WU
human LAMA-84 cell M1LuNmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MlvZTY5pcWKrdHnvckBw\iCqdX3hckBNSU2DLUi0JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OFU3NjJ{IH7NMi=> MWjTRW5ITVJ?
human U-266 cell MVTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NGK0SXZKdmirYnn0bY9vKG:oIHj1cYFvKFVvMk[2JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OFg4Njd2IH7NMi=> Mn\5V2FPT0WU
human RCM-1 cell M13WOGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MXfJcohq[mm2aX;uJI9nKGi3bXHuJHJEVS1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;NEmzMlg2KG6PLh?= M4n6eXNCVkeHUh?=

... 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
  • 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 CN1C=NC2=C1C=C(C(=C2F)NC3=C(C=C(C=C3)Br)Cl)C(=O)NOCCO

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O
CalculateReset

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
NCT03326388 Recruiting Drug: Selumetinib Neurofibromatosis Type 1|Plexiform Neurofibroma|Optic Nerve Glioma Great Ormond Street Hospital for Children NHS Foundation Trust|AstraZeneca September 26 2019 Phase 1|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
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 May 18 2018 Phase 1|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