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.

Size Price Stock Quantity  
In DMSO USD 117 In stock
USD 90 In stock
USD 130 In stock
USD 170 In stock
USD 370 In stock
Bulk Discount

Free Overnight Delivery on orders over $ 500
Next day delivery by 10:00 a.m. Order now.

Cited by 210 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 NE\JVGtIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NXzTNGkyUW6qaXLpeIlwdiCxZjDoeY1idiCFSGCtNlEzKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:Oy5zNTDuUU4> MUTTRW5ITVJ?
human H9 cell NIHhOGJIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M1fw[WlvcGmkaYTpc44hd2ZiaIXtZY4hUDliY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1{Mj64PEBvVS5? NIDQ[21USU6JRWK=
human HL-60 cell NGT4RmVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NES4XnNKdmirYnn0bY9vKG:oIHj1cYFvKEiOLU[wJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlQvPTlibl2u NVzLfW11W0GQR1XS
human A375 cells M3XYNnBzd2yrZnXyZZRqd25iYYPzZZk> M2fyelczKGh? M2O5VGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQUO3OUBk\WyuczDlfJBz\XO|aX7nJGJTSUZiVk[wNGUhdXW2YX70JIFnfGW{IEeyJIhzeyCkeTDD[YxtKHSrdHXyMYdtdyCjc4PhfUwhUUN3ME2zNUBvVS5? MY[yN|Q4PDN6OB?=
human NOMO-1 cell M2i5RWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MkLmTY5pcWKrdHnvckBw\iCqdX3hckBPV02RLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zNU46PyCwTT6= M{XnVnNCVkeHUh?=
human DU-4475 cell NULSWWlDT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M{HQ[mlvcGmkaYTpc44hd2ZiaIXtZY4hTFVvNES3OUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVM{NjZ5IH7NMi=> NYnmOlVtW0GQR1XS
human M14 cell MV3Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MkexTY5pcWKrdHnvckBw\iCqdX3hckBOOTRiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1|Nj64PUBvVS5? MUXTRW5ITVJ?
human HT-144 cell NIi5c3hIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NW\LdZJSUW6qaXLpeIlwdiCxZjDoeY1idiCKVD2xOFQh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF05QS5yNTDuUU4> MXTTRW5ITVJ?
human SK-N-AS cell NF20TFdIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NW\6cXRzUW6qaXLpeIlwdiCxZjDoeY1idiCVSz3OMWFUKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:QTJwOEOgcm0v NGDxUXNUSU6JRWK=
human LB2518-MEL cell Mk\0S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NFriW5lKdmirYnn0bY9vKG:oIHj1cYFvKEyEMkWxPE1OTUxiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD17Mz64NkBvVS5? MUDTRW5ITVJ?
human C32 cell NUntPZBVT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NGLXNJZKdmirYnn0bY9vKG:oIHj1cYFvKEN|MjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUm4MlI{KG6PLh?= MXvTRW5ITVJ?
human BHT-101 cell MXvHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NFT3UYZKdmirYnn0bY9vKG:oIHj1cYFvKEKKVD2xNFEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yODZwOUOgcm0v M3T6TXNCVkeHUh?=
human KY821 cell M4nTOWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MmHPTY5pcWKrdHnvckBw\iCqdX3hckBMYTh{MTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGwO{4yQCCwTT6= MonlV2FPT0WU
human CP50-MEL-B cell Mk\SS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M3;5d2lvcGmkaYTpc44hd2ZiaIXtZY4hS1B3MD3NSWwuSiClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTF{Nz65OEBvVS5? Ml62V2FPT0WU
human MEL-HO cell MWPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NX7I[mxtUW6qaXLpeIlwdiCxZjDoeY1idiCPRVytTG8h[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yOzhwOESgcm0v M3zObnNCVkeHUh?=
human MIAPaCa2 cells MoPiVJJwdGmoZYLheIlwdiCjc4PhfS=> MWLBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2LQWDhR4EzKGOnbHzzMEBKSzVyPUG0NkBvVS5? M1\JSlI{PDd2M{i4
human EoL-1-cell cell M13kZ2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NGfOfIpKdmirYnn0bY9vKG:oIHj1cYFvKEWxTD2xMYNmdGxiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zNESuO|Yhdk1w NI\3codUSU6JRWK=
human DOK cell NV\PNWp4T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MlS0TY5pcWKrdHnvckBw\iCqdX3hckBFV0tiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zNEeuNFghdk1w MUPTRW5ITVJ?
human SH-4 cell NEnoVIpIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NWjiSZFYUW6qaXLpeIlwdiCxZjDoeY1idiCVSD20JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVY3NjR6IH7NMi=> NH71WXNUSU6JRWK=
human BPH-1 cell MnzJS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? Mnn6TY5pcWKrdHnvckBw\iCqdX3hckBDWEhvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUG4Nk4{OSCwTT6= MYnTRW5ITVJ?
human HuP-T4 cell NEPSS2tIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MV7Jcohq[mm2aX;uJI9nKGi3bXHuJGh2WC2WNDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUG5OU4{OiCwTT6= NF;IOHJUSU6JRWK=
human KU812 cell NX60ZnEzT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M3y1eWlvcGmkaYTpc44hd2ZiaIXtZY4hU1V6MUKgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yNVEvPjhibl2u MV\TRW5ITVJ?
human A549 cell MXTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MnqzTY5pcWKrdHnvckBw\iCqdX3hckBCPTR7IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MkG0MlE{KG6PLh?= M4fO[3NCVkeHUh?=
human HTC-C3 cell NWTWbopKT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MmfnTY5pcWKrdHnvckBw\iCqdX3hckBJXENvQ{OgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yNVQvPjFibl2u NHO3N5hUSU6JRWK=
human A101D cell NVznSItFT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MnTlTY5pcWKrdHnvckBw\iCqdX3hckBCOTBzRDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUK0NE4{OyCwTT6= NYXKXG5kW0GQR1XS
human ONS-76 cell NV3ado1LT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= Mn61TY5pcWKrdHnvckBw\iCqdX3hckBQVlNvN{[gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yOFQvPTNibl2u MWjTRW5ITVJ?
human RKO cell NEjLV4NIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NVrUc4dVUW6qaXLpeIlwdiCxZjDoeY1idiCUS1:gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yOFgvOzhibl2u NGXyOYxUSU6JRWK=
human WM-115 cell NGriVZhIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MlvFTY5pcWKrdHnvckBw\iCqdX3hckBYVS1zMUWgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yOlcvPTRibl2u MoL4V2FPT0WU
human HCC2998 cell NE\ofFFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M4P0[WlvcGmkaYTpc44hd2ZiaIXtZY4hUEOFMkm5PEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVI3QS5yNzDuUU4> MVzTRW5ITVJ?
human C2BBe1 cell MlXiS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? Mn36TY5pcWKrdHnvckBw\iCqdX3hckBEOkKEZUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yO|IvPTlibl2u NFnuS5JUSU6JRWK=
human RVH-421 cell NVSxN3RDT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M4fNPWlvcGmkaYTpc44hd2ZiaIXtZY4hWl[KLUSyNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVI4QS5|OTDuUU4> MnO0V2FPT0WU
human H-EMC-SS cell NH\aR|dIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M2fZZmlvcGmkaYTpc44hd2ZiaIXtZY4hUC2HTVOtV3Mh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zQTBwOUmgcm0v MoL6V2FPT0WU
human ML-2 cell NUS0UmhQT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NXTwcnUyUW6qaXLpeIlwdiCxZjDoeY1idiCPTD2yJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9Nlk{NjZ|IH7NMi=> M2XkbHNCVkeHUh?=
human SW620 cell MYfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NFjFXIVKdmirYnn0bY9vKG:oIHj1cYFvKFOZNkKwJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N|AzNjJibl2u MoPFV2FPT0WU
human UACC-257 cell MnTrS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M{LjPGlvcGmkaYTpc44hd2ZiaIXtZY4hXUGFQz2yOVch[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0{OjFwOESgcm0v NXv4N5JVW0GQR1XS
human AsPC-1 cell M{O0XGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NWGzSJBSUW6qaXLpeIlwdiCxZjDoeY1idiCDc2DDMVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0{OjRwM{mgcm0v MWPTRW5ITVJ?
human CAL-39 cell NXLwZWlZT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NUT0RodJUW6qaXLpeIlwdiCxZjDoeY1idiCFQVytN|kh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0{OzJwMk[gcm0v Mn\QV2FPT0WU
human COLO-679 cell NHf3[pVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MXjJcohq[mm2aX;uJI9nKGi3bXHuJGNQVE9vNke5JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N|QyNjF7IH7NMi=> M{TuUHNCVkeHUh?=
human NCI-H747 cell MlvTS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MUTJcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KN{S3JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N|UxNjl6IH7NMi=> MlLCV2FPT0WU
human NCI-H1437 cell MWnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M4XnPWlvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLVixOFM4KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OzV{Lki1JI5ONg>? NW\4eGV5W0GQR1XS
human PSN1 cell MXXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MlPkTY5pcWKrdHnvckBw\iCqdX3hckBRW05zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;M{[2MlA6KG6PLh?= MlLaV2FPT0WU
human NKM-1 cell NF72WI1Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= NILy[mJKdmirYnn0bY9vKG:oIHj1cYFvKE6NTT2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N|g2Njhibl2= MWDTRW5ITVJ?
human MZ2-MEL cell MlrZS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NH3kNWtKdmirYnn0bY9vKG:oIHj1cYFvKE2cMj3NSWwh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0{QTRwM{egcm0v MlnIV2FPT0WU
human SK-MEL-2 cell NYPiV4dkT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MV7Jcohq[mm2aX;uJI9nKGi3bXHuJHNMNU2HTD2yJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OFA2NjB4IH7NMi=> Mnr4V2FPT0WU
human LAMA-84 cell MUDHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MoTYTY5pcWKrdHnvckBw\iCqdX3hckBNSU2DLUi0JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OFU3NjJ{IH7NMi=> M1:2XnNCVkeHUh?=
human U-266 cell MXPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NVXRe|l3UW6qaXLpeIlwdiCxZjDoeY1idiCXLUK2OkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQ5Py55NDDuUU4> MWHTRW5ITVJ?
human RCM-1 cell MV;Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MVXJcohq[mm2aX;uJI9nKGi3bXHuJHJEVS1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;NEmzMlg2KG6PLh?= M{\tc3NCVkeHUh?=

... 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 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
NCT03162627 Recruiting Drug: Selumetinib|Drug: Olaparib Malignant Neoplasm of Breast|Malignant Neoplasms of Digestive Organs|Malignant Neoplasms of Female Genital Organs|Malignant Neoplasms of Male Genital Organs|Malignant Neoplasms of Thyroid and Other Endocrine Glands M.D. Anderson Cancer Center|AstraZeneca August 4 2017 Phase 1

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.

  • * Indicates a Required Field

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.

MEK Signaling Pathway Map

MEK Inhibitors with Unique Features

Related MEK Products

Tags: buy Selumetinib (AZD6244) | Selumetinib (AZD6244) supplier | purchase Selumetinib (AZD6244) | Selumetinib (AZD6244) cost | Selumetinib (AZD6244) manufacturer | order Selumetinib (AZD6244) | Selumetinib (AZD6244) distributor
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID