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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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 118 Publications

14 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.

    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.

  • Parental murine KRasG12V;p53-/- lung cancer cells or the same cell lines stably expressing exogenous KRASWT or KRASD154Q were injected intravenously into nude mice. After one week, animals were treated with selumetinib (50 mg/kg daily) and sacrificed at the indicated time points. Lungs were lysed and analyzed by western blot with the indicated antibodies.

    Cell, 2018, 172(4):857-868. 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.

  • 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.

    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.

  • Concentration equilibrium transport assays (CETAs) for selumetinib using parental and (murine) Mdr1a or (human) MDR1 overexpressing LLC cells. Zosuquidar (5 μM) was used to specifically inhibit P-gp mediated transport. Data are means ± SD; n = 6; ** p < 0.01, *** p < 0.001.

    Int J Cancer, 2018, 142(2):381-391. 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 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 M2PocWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MnrSTY5pcWKrdHnvckBw\iCqdX3hckBEUFBvMkGyJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N{4yPSCwTT6= M3zHOnNCVkeHUh?=
human H9 cell MmD5S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M3TGXWlvcGmkaYTpc44hd2ZiaIXtZY4hUDliY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1{Mj64PEBvVS5? NVS1[GkxW0GQR1XS
human HL-60 cell MU\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NXPNWJRLUW6qaXLpeIlwdiCxZjDoeY1idiCKTD22NEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVI1NjV7IH7NMi=> MmnUV2FPT0WU
human A375 cells M3LtVHBzd2yrZnXyZZRqd25iYYPzZZk> NWHvTmlyPzJiaB?= NGDEUHFCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFGzO|Uh[2WubIOg[ZhxemW|c3nu[{BDWkGIIG[2NFBGKG23dHHueEBi\nSncjC3NkBpenNiYomgR4VtdCC2aYTldk1odG9iYYPzZZktKEmFNUC9N|Ehdk1w MUSyN|Q4PDN6OB?=
human NOMO-1 cell NGDEOHFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= Mlj4TY5pcWKrdHnvckBw\iCqdX3hckBPV02RLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zNU46PyCwTT6= NYPBTFdRW0GQR1XS
human DU-4475 cell MVfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M1rINWlvcGmkaYTpc44hd2ZiaIXtZY4hTFVvNES3OUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVM{NjZ5IH7NMi=> MXPTRW5ITVJ?
human M14 cell MoriS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MXvJcohq[mm2aX;uJI9nKGi3bXHuJG0yPCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTN4Lki5JI5ONg>? Ml\4V2FPT0WU
human HT-144 cell MojPS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NYTYcodKUW6qaXLpeIlwdiCxZjDoeY1idiCKVD2xOFQh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF05QS5yNTDuUU4> M{K4[HNCVkeHUh?=
human SK-N-AS cell MlTTS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MV;Jcohq[mm2aX;uJI9nKGi3bXHuJHNMNU5vQWOgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME25Nk45OyCwTT6= MXnTRW5ITVJ?
human LB2518-MEL cell MW\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M3;NfmlvcGmkaYTpc44hd2ZiaIXtZY4hVEJ{NUG4MW1GVCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTl|LkiyJI5ONg>? MWnTRW5ITVJ?
human C32 cell MVTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NWf1fFBSUW6qaXLpeIlwdiCxZjDoeY1idiCFM{KgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME25PE4zOyCwTT6= MkTvV2FPT0WU
human BHT-101 cell NXnWOlNXT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NIm3fZRKdmirYnn0bY9vKG:oIHj1cYFvKEKKVD2xNFEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yODZwOUOgcm0v NIS2eIdUSU6JRWK=
human KY821 cell NIPrPIdIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M2XWemlvcGmkaYTpc44hd2ZiaIXtZY4hU1l6MkGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xNFcvOThibl2u NXjvOZVIW0GQR1XS
human CP50-MEL-B cell NVf3W4F2T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MnvqTY5pcWKrdHnvckBw\iCqdX3hckBEWDVyLV3FUE1DKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTJ5Lkm0JI5ONg>? NH7BfHdUSU6JRWK=
human MEL-HO cell MVjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MlHYTY5pcWKrdHnvckBw\iCqdX3hckBOTUxvSF:gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xN|gvQDRibl2u NWrUV45oW0GQR1XS
human MIAPaCa2 cells NVXsWYRWWHKxbHnm[ZJifGmxbjDhd5NigQ>? NEjFVnRCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3JRXBiS2F{IHPlcIx{NCCLQ{WwQVE1OiCwTT6= NX3odZQ3OjN2N{SzPFg>
human EoL-1-cell cell M3rYdGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M2X2N2lvcGmkaYTpc44hd2ZiaIXtZY4hTW:OLUGtZ4VtdCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTF2ND63OkBvVS5? NUHq[Ip1W0GQR1XS
human DOK cell NIr6dmNIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M3vPd2lvcGmkaYTpc44hd2ZiaIXtZY4hTE:NIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUS3MlA5KG6PLh?= MX\TRW5ITVJ?
human SH-4 cell NYftV|hoT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M2O4cGlvcGmkaYTpc44hd2ZiaIXtZY4hW0hvNDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUG2Ok41QCCwTT6= NF7qR|hUSU6JRWK=
human BPH-1 cell MkjLS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? Mm\YTY5pcWKrdHnvckBw\iCqdX3hckBDWEhvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUG4Nk4{OSCwTT6= NHz5WGhUSU6JRWK=
human HuP-T4 cell NXLicHFCT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NH;hbJhKdmirYnn0bY9vKG:oIHj1cYFvKEi3UD3UOEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVE6PS5|MjDuUU4> MlrQV2FPT0WU
human KU812 cell MnSwS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MVLJcohq[mm2aX;uJI9nKGi3bXHuJGtWQDF{IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MkGxMlY5KG6PLh?= M3z0UnNCVkeHUh?=
human A549 cell M3L3Zmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MoHwTY5pcWKrdHnvckBw\iCqdX3hckBCPTR7IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MkG0MlE{KG6PLh?= MX3TRW5ITVJ?
human HTC-C3 cell NGfFcmJIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NGjZPGNKdmirYnn0bY9vKG:oIHj1cYFvKEiWQz3DN{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVIyPC54MTDuUU4> MXHTRW5ITVJ?
human A101D cell M1W1TGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NVLyc3ZtUW6qaXLpeIlwdiCxZjDoeY1idiCDMUCxSEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVI1OC5|MzDuUU4> MXPTRW5ITVJ?
human ONS-76 cell MnS2S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NWTr[GppUW6qaXLpeIlwdiCxZjDoeY1idiCRTmOtO|Yh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zPDRwNUOgcm0v M{fhb3NCVkeHUh?=
human RKO cell NVfOTHR{T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M2PPTWlvcGmkaYTpc44hd2ZiaIXtZY4hWkuRIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MkS4MlM5KG6PLh?= M4PRR3NCVkeHUh?=
human WM-115 cell M13ZNmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NYDhclFXUW6qaXLpeIlwdiCxZjDoeY1idiCZTT2xNVUh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zPjdwNUSgcm0v NFX4dIpUSU6JRWK=
human HCC2998 cell MUjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MXPJcohq[mm2aX;uJI9nKGi3bXHuJGhESzJ7OUigZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yOlkvODdibl2u MmnsV2FPT0WU
human C2BBe1 cell NYH0SHl4T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M13vcmlvcGmkaYTpc44hd2ZiaIXtZY4hSzKEQnWxJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlczNjV7IH7NMi=> M{nQb3NCVkeHUh?=
human RVH-421 cell NFr3PXZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NVHwSVh6UW6qaXLpeIlwdiCxZjDoeY1idiCUVlitOFIyKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:Ojd7LkO5JI5ONg>? NVnHcWJ5W0GQR1XS
human H-EMC-SS cell NFGwd2VIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MV\Jcohq[mm2aX;uJI9nKGi3bXHuJGguTU2FLWPTJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlkxNjl7IH7NMi=> MmPOV2FPT0WU
human ML-2 cell M2DCUGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M3zoSWlvcGmkaYTpc44hd2ZiaIXtZY4hVUxvMjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUK5N{43OyCwTT6= NH[yeXFUSU6JRWK=
human SW620 cell NFu5fo9Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= M1PjTGlvcGmkaYTpc44hd2ZiaIXtZY4hW1d4MkCgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zNFIvOiCwTT6= NXG2eZpDW0GQR1XS
human UACC-257 cell MlS3S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MkHkTY5pcWKrdHnvckBw\iCqdX3hckBWSUOFLUK1O{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVMzOS56NDDuUU4> MlPYV2FPT0WU
human AsPC-1 cell M1fsSGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MXHJcohq[mm2aX;uJI9nKGi3bXHuJGF{WENvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUOyOE4{QSCwTT6= NILZc5dUSU6JRWK=
human CAL-39 cell M1v4[Gdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NV\ORmNRUW6qaXLpeIlwdiCxZjDoeY1idiCFQVytN|kh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0{OzJwMk[gcm0v MYPTRW5ITVJ?
human COLO-679 cell M3\Bcmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M2PMfWlvcGmkaYTpc44hd2ZiaIXtZY4hS0:OTz22O|kh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0{PDFwMUmgcm0v M3ry[HNCVkeHUh?=
human NCI-H747 cell NFLlW2xIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NGnFUYpKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3IO|Q4KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OzVyLkm4JI5ONg>? M4PMOHNCVkeHUh?=
human NCI-H1437 cell NWH4Z|FtT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NHnw[nVKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3INVQ{PyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTN3Mj64OUBvVS5? NYTIXoJxW0GQR1XS
human PSN1 cell NGDqNZhIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MlTZTY5pcWKrdHnvckBw\iCqdX3hckBRW05zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;M{[2MlA6KG6PLh?= MmX2V2FPT0WU
human NKM-1 cell MVTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M4rSRWlvcGmkaYTpc44hd2ZiaIXtZY4hVkuPLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zPFUvQCCwTR?= M{\0TnNCVkeHUh?=
human MZ2-MEL cell NYLHWnFpT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M1LSU2lvcGmkaYTpc44hd2ZiaIXtZY4hVVp{LV3FUEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVM6PC5|NzDuUU4> NXG5b2F2W0GQR1XS
human SK-MEL-2 cell NE\Cd2dIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MV;Jcohq[mm2aX;uJI9nKGi3bXHuJHNMNU2HTD2yJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OFA2NjB4IH7NMi=> NFXxU3JUSU6JRWK=
human LAMA-84 cell M4f3Wmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MXvJcohq[mm2aX;uJI9nKGi3bXHuJGxCVUFvOESgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME20OVYvOjJibl2u NETXcnZUSU6JRWK=
human U-266 cell NYH6fHNpT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= Mo[0TY5pcWKrdHnvckBw\iCqdX3hckBWNTJ4NjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUS4O{44PCCwTT6= MlTXV2FPT0WU
human RCM-1 cell M1Ps[Wdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M3zmWWlvcGmkaYTpc44hd2ZiaIXtZY4hWkOPLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME20PVMvQDVibl2u MX7TRW5ITVJ?

... 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 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)

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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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* 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):
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    C4=C3/X C4: LOG(C4):
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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
NCT03095248 Recruiting Neurofibromatosis 2|Vestibular Schwannoma|Meningioma|Ependymoma|Glioma Children''s Hospital Medical Center Cincinnati|AstraZeneca May 8 2017 Phase 2
NCT00463814 Active not recruiting Tumor|Cancer AstraZeneca March 8 2007 Phase 1
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
NCT03649165 Recruiting Neurofibromatosis Type 1 (NF1)-Related Plexiform Neurofibromas (PNs)|Healthy Participants AstraZeneca September 5 2018 Phase 1
NCT02337530 Active not recruiting Non-Small Cell Lung Cancer Canadian Cancer Trials Group|AstraZeneca February 5 2015 Phase 2
NCT02188264 Active not recruiting Recurrent Colorectal Carcinoma|Solid Neoplasm|Stage IIIA Colorectal Cancer AJCC v7|Stage IIIB Colorectal Cancer AJCC v7|Stage IIIC Colorectal Cancer AJCC v7|Stage IVA Colorectal Cancer AJCC v7|Stage IVB Colorectal Cancer AJCC v7 National Cancer Institute (NCI) August 5 2014 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.

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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.

MEK Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID