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 117 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.

    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.

    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 MnP5S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NH7INXVKdmirYnn0bY9vKG:oIHj1cYFvKEOKUD2yNVIh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0{NjF3IH7NMi=> NW\oTmZnW0GQR1XS
human H9 cell MUnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NGnWNY5KdmirYnn0bY9vKG:oIHj1cYFvKEh7IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MkKuPFghdk1w MnTuV2FPT0WU
human HL-60 cell MWDHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NVn2R|lsUW6qaXLpeIlwdiCxZjDoeY1idiCKTD22NEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVI1NjV7IH7NMi=> MYrTRW5ITVJ?
human A375 cells NUP3[Yx4WHKxbHnm[ZJifGmxbjDhd5NigQ>? NEO2XIk4OiCq NVr0dpd1SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDBN|c2KGOnbHzzJIV5eHKnc4PpcochSlKDRjDWOlAxTSCvdYThcpQh[W[2ZYKgO|IhcHK|IHL5JGNmdGxidHn0[ZIu\2yxIHHzd4F6NCCLQ{WwQVMyKG6PLh?= NYHTelRQOjN2N{SzPFg>
human NOMO-1 cell MXLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MWfJcohq[mm2aX;uJI9nKGi3bXHuJG5QVU9vMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUOxMlk4KG6PLh?= NYLxb4ZDW0GQR1XS
human DU-4475 cell MoeyS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NGHGc3JKdmirYnn0bY9vKG:oIHj1cYFvKESXLUS0O|Uh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0{Oy54NzDuUU4> Mm\zV2FPT0WU
human M14 cell M{\SNmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NV\JeZpyUW6qaXLpeIlwdiCxZjDoeY1idiCPMUSgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zOk45QSCwTT6= NYD2NVhkW0GQR1XS
human HT-144 cell M1;VPGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MUDJcohq[mm2aX;uJI9nKGi3bXHuJGhVNTF2NDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUi5MlA2KG6PLh?= MnrvV2FPT0WU
human SK-N-AS cell Mlf4S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MnzuTY5pcWKrdHnvckBw\iCqdX3hckBUUy2QLVHTJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9PVIvQDNibl2u MVfTRW5ITVJ?
human LB2518-MEL cell Ml3LS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M2rvOmlvcGmkaYTpc44hd2ZiaIXtZY4hVEJ{NUG4MW1GVCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTl|LkiyJI5ONg>? MUjTRW5ITVJ?
human C32 cell NILZTI9Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= M2Gz[WlvcGmkaYTpc44hd2ZiaIXtZY4hSzN{IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;OUiuNlMhdk1w NX:2TVluW0GQR1XS
human BHT-101 cell MVzHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NX7SS45pUW6qaXLpeIlwdiCxZjDoeY1idiCESGStNVAyKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTB4LkmzJI5ONg>? MVLTRW5ITVJ?
human KY821 cell MXjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M2i3c2lvcGmkaYTpc44hd2ZiaIXtZY4hU1l6MkGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xNFcvOThibl2u MkjnV2FPT0WU
human CP50-MEL-B cell M{jw[mdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NWLxVYVlUW6qaXLpeIlwdiCxZjDoeY1idiCFUEWwMW1GVC2EIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUK3Mlk1KG6PLh?= MkG2V2FPT0WU
human MEL-HO cell NX\ldppsT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NUnqUIc2UW6qaXLpeIlwdiCxZjDoeY1idiCPRVytTG8h[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yOzhwOESgcm0v NWDXOIxWW0GQR1XS
human MIAPaCa2 cells MXLQdo9tcW[ncnH0bY9vKGG|c3H5 MVzBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2LQWDhR4EzKGOnbHzzMEBKSzVyPUG0NkBvVS5? M3n5fFI{PDd2M{i4
human EoL-1-cell cell MULHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MonYTY5pcWKrdHnvckBw\iCqdX3hckBGd0xvMT3j[YxtKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTR2Lke2JI5ONg>? Mm\5V2FPT0WU
human DOK cell MknYS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M13lU2lvcGmkaYTpc44hd2ZiaIXtZY4hTE:NIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUS3MlA5KG6PLh?= Mn;jV2FPT0WU
human SH-4 cell Mk\YS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MX3Jcohq[mm2aX;uJI9nKGi3bXHuJHNJNTRiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zNk[uOFghdk1w NWT1RZM5W0GQR1XS
human BPH-1 cell NUTzVndzT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NUPXdJdLUW6qaXLpeIlwdiCxZjDoeY1idiCEUFitNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVE5Oi5|MTDuUU4> NU\rUYc5W0GQR1XS
human HuP-T4 cell NEfYNZVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NGe4RYdKdmirYnn0bY9vKG:oIHj1cYFvKEi3UD3UOEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVE6PS5|MjDuUU4> MmLLV2FPT0WU
human KU812 cell NV7YTmxST3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MmTjTY5pcWKrdHnvckBw\iCqdX3hckBMXThzMjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUKxNU43QCCwTT6= M4nDXnNCVkeHUh?=
human A549 cell M2jjTGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MWHJcohq[mm2aX;uJI9nKGi3bXHuJGE2PDliY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1{MUSuNVMhdk1w NUTtVWhMW0GQR1XS
human HTC-C3 cell NIHBe3BIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NYC2[Ih4UW6qaXLpeIlwdiCxZjDoeY1idiCKVFOtR|Mh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zOTRwNkGgcm0v NEfnPW5USU6JRWK=
human A101D cell MUXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MnXmTY5pcWKrdHnvckBw\iCqdX3hckBCOTBzRDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUK0NE4{OyCwTT6= MkezV2FPT0WU
human ONS-76 cell MnLqS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MULJcohq[mm2aX;uJI9nKGi3bXHuJG9PWy15NjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUK0OE42OyCwTT6= NXXHXnZ6W0GQR1XS
human RKO cell Mn\BS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NHPsPZZKdmirYnn0bY9vKG:oIHj1cYFvKFKNTzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUK0PE4{QCCwTT6= NX\CV|VsW0GQR1XS
human WM-115 cell NHrtVWVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MVjJcohq[mm2aX;uJI9nKGi3bXHuJHdONTFzNTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUK2O{42PCCwTT6= MoHaV2FPT0WU
human HCC2998 cell M1fH[Gdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NGnMPVZKdmirYnn0bY9vKG:oIHj1cYFvKEiFQ{K5PVgh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zPjlwMEegcm0v MUDTRW5ITVJ?
human C2BBe1 cell M13vUmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NHrIVXVKdmirYnn0bY9vKG:oIHj1cYFvKEN{QlLlNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVI4Oi53OTDuUU4> Mmn1V2FPT0WU
human RVH-421 cell MVXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NUL3dJR[UW6qaXLpeIlwdiCxZjDoeY1idiCUVlitOFIyKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:Ojd7LkO5JI5ONg>? M2fFRnNCVkeHUh?=
human H-EMC-SS cell NGXLcFVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M3TnVWlvcGmkaYTpc44hd2ZiaIXtZY4hUC2HTVOtV3Mh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zQTBwOUmgcm0v NIfXRYVUSU6JRWK=
human ML-2 cell M4HKZWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NF\idnVKdmirYnn0bY9vKG:oIHj1cYFvKE2OLUKgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yPVMvPjNibl2u M3Ly[HNCVkeHUh?=
human SW620 cell NH\qdm1Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= NWHZenNwUW6qaXLpeIlwdiCxZjDoeY1idiCVV{[yNEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVMxOi5{IH7NMi=> NWO5c2pHW0GQR1XS
human UACC-257 cell MoX5S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NHfCZodKdmirYnn0bY9vKG:oIHj1cYFvKFWDQ1OtNlU4KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OzJzLki0JI5ONg>? NXXDXmNwW0GQR1XS
human AsPC-1 cell MWPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NXfGbmhuUW6qaXLpeIlwdiCxZjDoeY1idiCDc2DDMVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0{OjRwM{mgcm0v NFPDZ5RUSU6JRWK=
human CAL-39 cell MnT1S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NHnkbGNKdmirYnn0bY9vKG:oIHj1cYFvKEODTD2zPUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVM{Oi5{NjDuUU4> M3rBWnNCVkeHUh?=
human COLO-679 cell M{DnU2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NF;MeHlKdmirYnn0bY9vKG:oIHj1cYFvKEORTF:tOlc6KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OzRzLkG5JI5ONg>? NWTQSFR7W0GQR1XS
human NCI-H747 cell M37IRmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 Mn7nTY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEe0O{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVM2OC57ODDuUU4> MWHTRW5ITVJ?
human NCI-H1437 cell NGPTS2RIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M4PYT2lvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLVixOFM4KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OzV{Lki1JI5ONg>? Mo\6V2FPT0WU
human PSN1 cell NGrwS4dIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MXLJcohq[mm2aX;uJI9nKGi3bXHuJHBUVjFiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1|Nk[uNFkhdk1w MWTTRW5ITVJ?
human NKM-1 cell M{OzO2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NXjqVW1nUW6qaXLpeIlwdiCxZjDoeY1idiCQS12tNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVM5PS56IH7N NFnVZYJUSU6JRWK=
human MZ2-MEL cell M2PzOWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MXrJcohq[mm2aX;uJI9nKGi3bXHuJG1bOi2PRVygZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zPVQvOzdibl2u NV\MS2R3W0GQR1XS
human SK-MEL-2 cell M4W3XGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NWjlZ3ZZUW6qaXLpeIlwdiCxZjDoeY1idiCVSz3NSWwuOiClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTRyNT6wOkBvVS5? NVq4[W83W0GQR1XS
human LAMA-84 cell M3npW2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MVPJcohq[mm2aX;uJI9nKGi3bXHuJGxCVUFvOESgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME20OVYvOjJibl2u NGXWNHNUSU6JRWK=
human U-266 cell NFrIRYpIem:5dHigbY5pcWKrdHnvckBie3OjeR?= Ml3PTY5pcWKrdHnvckBw\iCqdX3hckBWNTJ4NjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUS4O{44PCCwTT6= MV\TRW5ITVJ?
human RCM-1 cell MVnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NYG5OJFlUW6qaXLpeIlwdiCxZjDoeY1idiCUQ12tNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQ6Oy56NTDuUU4> Ml3yV2FPT0WU

... 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:
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
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.

  • * 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