Selumetinib (AZD6244)

Catalog No.S1008 Synonyms: ARRY-142886

Selumetinib (AZD6244) Chemical Structure

Molecular Weight(MW): 457.68

Selumetinib (AZD6244) is a potent, highly selective MEK1 inhibitor with IC50 of 14 nM in cell-free assays, 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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In DMSO USD 117 In stock
USD 90 In stock
USD 130 In stock
USD 170 In stock
USD 370 In stock
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Cited by 116 Publications

13 Customer Reviews

  • Left: BRAFV600E A375 cells expressing pLKO or shMED12 vectors were cultured in the absence or presence of 2.5 μM PLX4032 or 0.5 μM AZD6244. The cells were fixed, stained, and photographed after 10 (untreated) or 28 days (treated). Right: A375 cells expressing pLKO or shMED12 vectors were grown in the absence or presence of 1 μM PLX4032 or 0.5 μM AZD6244 for 6 hr.

    Cell, 2012, 151(5): 937–950. Selumetinib (AZD6244) purchased from Selleck.

    Left: KRASV12 SKCO-1 cells expressing pLKO or shMED12 vectors were cultured in the absence or presence of 0.5 μM AZD6244. The cells were fixed, stained, and photographed after 14 (untreated) or 28 days (treated). Right: SK-CO-1 cells expressing pLKO or shMED12 vectors were grown in the absence or presence of 1 μM AZD6244 for 6 hr.

    Cell, 2012, 151(5): 937–950. Selumetinib (AZD6244) purchased from Selleck.

  • A,ERK phosphorylation in A375 expressing indicated ORFs following treatment with DMSO or 1 μM of PLX4720, RAF265, CI-1040 or AZD6244. B,ERK phosphorylation in A375 expressing indicated ORFs following treatment with DMSO, PLX4720 (1 μM) or PLX4720 in combination with CI-1040 or AZD6244 (all 1 μM).

    Nature 2010 468, 968-972. Selumetinib (AZD6244) purchased from Selleck.

    Survival curves for isogenic cell line pairs and melanoma cultures treated with the indicated AZD6244 concentration for 72 h (relative to DMSO treated controls; mean6s.e.m., n55). PLX4032 resistant cells were grown with PLX4032. Dashed line, 50% cell killing.

    Nature 2010 468, 973-977. Selumetinib (AZD6244) purchased from Selleck.

  • a-c, Inhibitors of BRAFV600E (PLX4032) and MEK1/2 (PD98059 or AZD6244) increase PGC1α and ID2 expression (a, b) and repress integrin expression and signalling (b, c). Cells were treated with indicated concentration of inhibitors for 6 h (a, b) or 24 h (c). d, e, PLX4032 increases the interaction between ID2 and TCF4 (d) and decreases the occupancy of TCF4 at the promoters of integrin genes (e). f–g, PGC1α and ID2 are partially required for PLX4032-mediated inhibition of invasion and metastasis. For in vitro assays (f), A375 cells were incubated with 1 μM PLX4032 for 10 h. Images represent one picture captured per membrane with the scale bar representing 200 μm. Values in a, b, e and f represent mean±s.d. of independent biological triplicates; *P<0.05 and **P<0.01 by Student's t-test  in a, b, e, f.

    Nature, 2016, 537(7620):422-428.. Selumetinib (AZD6244) purchased from Selleck.

    Ex vivo and functional characterization of MEK1(P124L). (A) AZD6244-mediated growth inhibition ex vivo of treatment-naïve BRAFV600E melanoma cells (black and blue) or cells cultured from an AZD6244-resistant metastatic focus (red). (B) ERK phosphorylation (p-ERK) andMEKphosphorylation (p-MEK) are shown following treatment with increasing concentrations of AZD6244 in treatment-naïve or AZD6244-resistant melanoma cells cultured ex vivo. The tubulin loading control (-tubulin) is also shown. (C) AZD6244 growth inhibition curves of parental A375 (solid black), A375 cells expressing MEK-DD (grey), wild-type MEK1 (hatched black), or MEK1(P124L) (red) are shown. In each instance n6 anderrorstandard deviation. (D) p-ERK and p-MEK are shown following treatment with increasing AZD6244 concentrations in the cell lines described in C, Above. The -tubulin control is also shown.

    Proc Natl Acad Sci USA 2009 106, 20411-20416. Selumetinib (AZD6244) purchased from Selleck.

  • AZD6244 enhanced FOXO3a expression and induced suppression of cancer cell proliferation. A, tumor volume of the HCT116 xenografts treated with Placebo or AZD6244 was measured for 21 d. The tumor sections of four individual DMSO or AZD6244-treated HCT116 xenografts were subjected to immunohistochemistry with a FOXO3a antibody. Relative percentages of nuclear FOXO3a expression of individual xenograft tumors from B were analyzed and the mean values of FOXO3a expression in Placebo or AZD6244-treated group were indicated as bars.

    Cancer Res 2010 70, 4709-4718. Selumetinib (AZD6244) purchased from Selleck.

    lysates from various cancer cell lines: breast cancer (MDA-MB-435), colon cancer (HCT116, SW620, and HT29), and melanoma (WM793) treated with DMSO or AZD6244 (10 μmol/L) for 4 h were subjected to immunoblotting with the indicated antibodies.

    Cancer Res 2010 70, 4709-4718. Selumetinib (AZD6244) purchased from Selleck.

  • A and B, clonogenic assays in 2 melanoma cell lines (YUVON and YUSIK) treated with NVPBEZ235 (BEZ) and AZD6244 (AZD) alone and in combination. Combinations were more effective in inhibiting colony formation at lower concentrations than either drug alone.

    Clin Cancer Res 2010 16, 6029-6039. Selumetinib (AZD6244) purchased from Selleck.

    Stimulation response of p37d-expressing cells. (c) Western blot of 5 min serum stimulated HEK-293 cells stably expressing p37d, p110d or control, with the presence of inhibitors as indicated at the top.

    Oncogene 2012 31, 3277–3286. Selumetinib (AZD6244) purchased from Selleck.

  • INA-6 MM cells were treated with AS703026 or AZD6244 for 2 d, followed by [3H]thymidine uptake assay. PBMCs isolated from normal donors (n = 3) were incubated with M-CSF and RANKL, in the presence or absence of AS703026 or AZD6244 for 14 d. The TRAP assay was performed to measure the formation of multinuclear osteoclast cells (OC).

    Br J Haematol 2010 149, 537–549. Selumetinib (AZD6244) purchased from Selleck.

    B-RafV600E mutated melanoma line,A375, was treated with different doses of AZD6244 for 1hour or 24 hours.Cell lysates were analyzed by Western Blotting to determine the levels of phosphorylated ERK1/2(Perk1/2)

    Dr. Jong-In Park of Medical College of Wisconsin. Selumetinib (AZD6244) purchased from Selleck.

  • Selumetinib (AZD6244) purchased from Selleck.

Purity & Quality Control

Choose Selective MEK Inhibitors

Biological Activity

Description Selumetinib (AZD6244) is a potent, highly selective MEK1 inhibitor with IC50 of 14 nM in cell-free assays, 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)
14 nM
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 MVLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? Mn3wTY5pcWKrdHnvckBw\iCqdX3hckBEUFBvMkGyJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N{4yPSCwTT6= M{joT3NCVkeHUh?=
human H9 cell Mn;ES5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NUXidFM1UW6qaXLpeIlwdiCxZjDoeY1idiCKOTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUKyMlg5KG6PLh?= M13GTnNCVkeHUh?=
human HL-60 cell NEHBbYhIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M{XacmlvcGmkaYTpc44hd2ZiaIXtZY4hUExvNkCgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yOE42QSCwTT6= MYLTRW5ITVJ?
human A375 cells NWrNU2puWHKxbHnm[ZJifGmxbjDhd5NigQ>? NUmydJlJPzJiaB?= M4P1W2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQUO3OUBk\WyuczDlfJBz\XO|aX7nJGJTSUZiVk[wNGUhdXW2YX70JIFnfGW{IEeyJIhzeyCkeTDD[YxtKHSrdHXyMYdtdyCjc4PhfUwhUUN3ME2zNUBvVS5? M3nSTVI{PDd2M{i4
human NOMO-1 cell MXPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MoTRTY5pcWKrdHnvckBw\iCqdX3hckBPV02RLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zNU46PyCwTT6= M{m4RnNCVkeHUh?=
human DU-4475 cell MmXqS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NHjpXVJKdmirYnn0bY9vKG:oIHj1cYFvKESXLUS0O|Uh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0{Oy54NzDuUU4> M17XZ3NCVkeHUh?=
human M14 cell MVfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MUPJcohq[mm2aX;uJI9nKGi3bXHuJG0yPCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTN4Lki5JI5ONg>? MV7TRW5ITVJ?
human HT-144 cell NX7n[4NkT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M{X0T2lvcGmkaYTpc44hd2ZiaIXtZY4hUFRvMUS0JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9PFkvODVibl2u MnHZV2FPT0WU
human SK-N-AS cell M{jw[2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 Mkf1TY5pcWKrdHnvckBw\iCqdX3hckBUUy2QLVHTJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9PVIvQDNibl2u MYHTRW5ITVJ?
human LB2518-MEL cell M1Lve2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NHLDTm1KdmirYnn0bY9vKG:oIHj1cYFvKEyEMkWxPE1OTUxiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD17Mz64NkBvVS5? M3;ZRnNCVkeHUh?=
human C32 cell NXK1Z5FVT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NH7lOGZKdmirYnn0bY9vKG:oIHj1cYFvKEN|MjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUm4MlI{KG6PLh?= MWXTRW5ITVJ?
human BHT-101 cell MVfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NIDKVoVKdmirYnn0bY9vKG:oIHj1cYFvKEKKVD2xNFEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yODZwOUOgcm0v NUDWTYpxW0GQR1XS
human KY821 cell M3PkdGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NFrycHVKdmirYnn0bY9vKG:oIHj1cYFvKEu\OEKxJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVA4NjF6IH7NMi=> M2nC[nNCVkeHUh?=
human CP50-MEL-B cell NEO4W25Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= NEXPXIhKdmirYnn0bY9vKG:oIHj1cYFvKEOSNUCtUWVNNUJiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zMkeuPVQhdk1w NI\PclRUSU6JRWK=
human MEL-HO cell MVPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M2K4SGlvcGmkaYTpc44hd2ZiaIXtZY4hVUWOLVjPJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVM5Njh2IH7NMi=> MUnTRW5ITVJ?
human MIAPaCa2 cells NHuxNG9Rem:uaX\ldoF1cW:wIHHzd4F6 NEPYNVVCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3JRXBiS2F{IHPlcIx{NCCLQ{WwQVE1OiCwTT6= MnqzNlM1PzR|OEi=
human EoL-1-cell cell MoK4S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M4XB[WlvcGmkaYTpc44hd2ZiaIXtZY4hTW:OLUGtZ4VtdCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTF2ND63OkBvVS5? NW\uVZJvW0GQR1XS
human DOK cell M3vtZWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MoDLTY5pcWKrdHnvckBw\iCqdX3hckBFV0tiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zNEeuNFghdk1w MULTRW5ITVJ?
human SH-4 cell MnjTS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MonaTY5pcWKrdHnvckBw\iCqdX3hckBUUC12IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MU[2MlQ5KG6PLh?= M3nMbnNCVkeHUh?=
human BPH-1 cell MVTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M3XC[WlvcGmkaYTpc44hd2ZiaIXtZY4hSlCKLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xPFIvOzFibl2u MoC3V2FPT0WU
human HuP-T4 cell MoTYS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NWn5c4VDUW6qaXLpeIlwdiCxZjDoeY1idiCKdWCtWFQh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yQTVwM{Kgcm0v NIjUS4dUSU6JRWK=
human KU812 cell MkHHS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MXfJcohq[mm2aX;uJI9nKGi3bXHuJGtWQDF{IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MkGxMlY5KG6PLh?= Mk[1V2FPT0WU
human A549 cell NWnndmtsT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MoPHTY5pcWKrdHnvckBw\iCqdX3hckBCPTR7IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MkG0MlE{KG6PLh?= NVKwUXdmW0GQR1XS
human HTC-C3 cell M1\BW2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M2DnWWlvcGmkaYTpc44hd2ZiaIXtZY4hUFSFLVOzJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlE1NjZzIH7NMi=> NV\4Z4tUW0GQR1XS
human A101D cell MWLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NGq1dFNKdmirYnn0bY9vKG:oIHj1cYFvKEFzMEHEJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlQxNjN|IH7NMi=> MoDYV2FPT0WU
human ONS-76 cell Mn;1S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NIrYe2FKdmirYnn0bY9vKG:oIHj1cYFvKE:QUz23OkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVI1PC53MzDuUU4> MV3TRW5ITVJ?
human RKO cell NIPyemFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MYjJcohq[mm2aX;uJI9nKGi3bXHuJHJMVyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTJ2OD6zPEBvVS5? MorGV2FPT0WU
human WM-115 cell NHXRbJFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M1;YNGlvcGmkaYTpc44hd2ZiaIXtZY4hX01vMUG1JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlY4NjV2IH7NMi=> NEDHTpZUSU6JRWK=
human HCC2998 cell M{H0OWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NYPHTFNNUW6qaXLpeIlwdiCxZjDoeY1idiCKQ1OyPVk5KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OjZ7LkC3JI5ONg>? NWXpRYs{W0GQR1XS
human C2BBe1 cell NWT2ZpBKT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MYHJcohq[mm2aX;uJI9nKGi3bXHuJGMzSkKnMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUK3Nk42QSCwTT6= NHvxVIdUSU6JRWK=
human RVH-421 cell M{K5eWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 Mn7LTY5pcWKrdHnvckBw\iCqdX3hckBTXkhvNEKxJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9Nlc6NjN7IH7NMi=> MlvNV2FPT0WU
human H-EMC-SS cell NI[z[XdIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M4W1cWlvcGmkaYTpc44hd2ZiaIXtZY4hUC2HTVOtV3Mh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zQTBwOUmgcm0v MXLTRW5ITVJ?
human ML-2 cell M3frR2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NFnWemxKdmirYnn0bY9vKG:oIHj1cYFvKE2OLUKgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yPVMvPjNibl2u NWXKXHRqW0GQR1XS
human SW620 cell MkTFS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M3\zfGlvcGmkaYTpc44hd2ZiaIXtZY4hW1d4MkCgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zNFIvOiCwTT6= M2niWHNCVkeHUh?=
human UACC-257 cell M3rFPGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MmDuTY5pcWKrdHnvckBw\iCqdX3hckBWSUOFLUK1O{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVMzOS56NDDuUU4> M3LFRnNCVkeHUh?=
human AsPC-1 cell MVfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MW\Jcohq[mm2aX;uJI9nKGi3bXHuJGF{WENvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUOyOE4{QSCwTT6= MVPTRW5ITVJ?
human CAL-39 cell Mn;4S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MYnJcohq[mm2aX;uJI9nKGi3bXHuJGNCVC1|OTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUOzNk4zPiCwTT6= NGHOXI1USU6JRWK=
human COLO-679 cell M1ezTmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M3TX[GlvcGmkaYTpc44hd2ZiaIXtZY4hS0:OTz22O|kh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0{PDFwMUmgcm0v MkjpV2FPT0WU
human NCI-H747 cell MmjKS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M33jUWlvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLVi3OFch[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0{PTBwOUigcm0v MnjKV2FPT0WU
human NCI-H1437 cell NHTr[opIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M325XmlvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLVixOFM4KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OzV{Lki1JI5ONg>? M1\odXNCVkeHUh?=
human PSN1 cell MYHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NHToS2RKdmirYnn0bY9vKG:oIHj1cYFvKFCVTkGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zOlYvODlibl2u NF\2[JVUSU6JRWK=
human NKM-1 cell MmGyS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M4XzU2lvcGmkaYTpc44hd2ZiaIXtZY4hVkuPLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zPFUvQCCwTR?= MnLmV2FPT0WU
human MZ2-MEL cell Mni3S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NXf3WZV5UW6qaXLpeIlwdiCxZjDoeY1idiCPWkKtUWVNKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:Ozl2LkO3JI5ONg>? NIq2Z4xUSU6JRWK=
human SK-MEL-2 cell Ml;4S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NHXrSY5KdmirYnn0bY9vKG:oIHj1cYFvKFONLV3FUE0zKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PDB3LkC2JI5ONg>? Mo\iV2FPT0WU
human LAMA-84 cell NYjJZmFjT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NV;tc2p[UW6qaXLpeIlwdiCxZjDoeY1idiCOQV3BMVg1KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PDV4LkKyJI5ONg>? NYfqUIZ3W0GQR1XS
human U-266 cell MnHmS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M1PZfmlvcGmkaYTpc44hd2ZiaIXtZY4hXS1{Nk[gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME20PFcvPzRibl2u MVjTRW5ITVJ?
human RCM-1 cell M{TZN2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M2r3ZWlvcGmkaYTpc44hd2ZiaIXtZY4hWkOPLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME20PVMvQDVibl2u NHL3bm5USU6JRWK=

... Click to View More Cell Line Experimental Data

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 individually and in order:
4% DMSO+30% PEG 300+5% Tween 80+ddH2O
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
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)

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*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 )

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    C2
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* 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):
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    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:

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Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

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Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01287130 Completed Colonic Neoplasms|Cancer of the Colon|Colon Cancer|Colon Neoplasms|Colonic Cancer National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) January 7, 2011 Phase 1
NCT01134601 Terminated Non-Metastatic Adenocarcinoma of the Rectum National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) May 24, 2010 Phase 1
NCT01306045 Recruiting Carcinoma, Non-Small-Cell Lung|Carcinoma, Small Cell Lung|Carcinoma, Thymic National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) January 21, 2011 Phase 2
NCT03040986 Not yet recruiting KRAS NP_004976.2:p.G12R|Stage II Pancreatic Cancer|Stage IIA Pancreatic Cancer|Stage IIB Pancreatic Cancer|Stage III Pancreatic Cancer|Stage IV Pancreatic Cancer National Cancer Institute (NCI) July 2017 Phase 2
NCT03004105 Not yet recruiting Malignant Neoplasm of Respiratory and Intrathoracic Organ Carcinoma|Advanced Lung Cancer|Recurrent Nonsmall Cell Lung Cancer M.D. Anderson Cancer Center|AstraZeneca|MedImmune LLC April 2017 Phase 2
NCT02839720 Not yet recruiting Appearance Distress|Bothered by Itching Skin|Cafe Au Lait Spot|Cutaneous Neurofibroma|Disfigurement|Dysplasia|Lisch Nodule|Neurofibromatosis Type 1|NF1 Gene Mutation|Optic Nerve Glioma National Cancer Institute (NCI) January 2017 --

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