Selumetinib (AZD6244)

製品コードS1008 別名:ARRY-142886

Selumetinib (AZD6244)化学構造


Selumetinib (AZD6244)は一種の有効で、高度選択性的なMEK1阻害剤で、無細胞試験でIC50値が14 nMですが、ERK1/2リン酸化も抑制する時のIC50値が10 nMになって、p38α、MKK6、EGFR、ErbB2、ERK2とB-Raf等を抑制する作用がありません。臨床3期。

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JPY 19422.00 あり
JPY 14940.00 あり
JPY 21580.00 あり
JPY 28220.00 あり
JPY 61420.00 あり



  • 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.




製品説明 Selumetinib (AZD6244)は一種の有効で、高度選択性的なMEK1阻害剤で、無細胞試験でIC50値が14 nMですが、ERK1/2リン酸化も抑制する時のIC50値が10 nMになって、p38α、MKK6、EGFR、ErbB2、ERK2とB-Raf等を抑制する作用がありません。臨床3期。
特性 First MEK inhibitor being tested in Phase II clinical trials.
MEK1 [1]
(Cell-free assay)
14 nM

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 Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human CHP-212 cell MkjWS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NHTSdnhKdmirYnn0bY9vKG:oIHj1cYFvKEOKUD2yNVIh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0{NjF3IH7NMi=> M4D6OHNCVkeHUh?=
human H9 cell MV7Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NUDGbVZkUW6qaXLpeIlwdiCxZjDoeY1idiCKOTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUKyMlg5KG6PLh?= NU\VSlB3W0GQR1XS
human HL-60 cell NGH4cmNIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NWDqfWdKUW6qaXLpeIlwdiCxZjDoeY1idiCKTD22NEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVI1NjV7IH7NMi=> NV7RXYpNW0GQR1XS
human A375 cells MoC4VJJwdGmoZYLheIlwdiCjc4PhfS=> NX[3RlVPPzJiaB?= NIjhe5NCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFGzO|Uh[2WubIOg[ZhxemW|c3nu[{BDWkGIIG[2NFBGKG23dHHueEBi\nSncjC3NkBpenNiYomgR4VtdCC2aYTldk1odG9iYYPzZZktKEmFNUC9N|Ehdk1w NUPXb3FtOjN2N{SzPFg>
human NOMO-1 cell NIfXeIhIem:5dHigbY5pcWKrdHnvckBie3OjeR?= Mnv2TY5pcWKrdHnvckBw\iCqdX3hckBPV02RLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zNU46PyCwTT6= NF23V5VUSU6JRWK=
human DU-4475 cell MmHNS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M1rsemlvcGmkaYTpc44hd2ZiaIXtZY4hTFVvNES3OUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVM{NjZ5IH7NMi=> MUfTRW5ITVJ?
human M14 cell NUn5XldkT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NHTIVI1KdmirYnn0bY9vKG:oIHj1cYFvKE1zNDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUO2Mlg6KG6PLh?= NF;yWopUSU6JRWK=
human HT-144 cell NUT2blR1T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MkfoTY5pcWKrdHnvckBw\iCqdX3hckBJXC1zNESgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME24PU4xPSCwTT6= MmP0V2FPT0WU
human SK-N-AS cell MXjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NFP6boFKdmirYnn0bY9vKG:oIHj1cYFvKFONLV6tRXMh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF06Oi56MzDuUU4> MXrTRW5ITVJ?
human LB2518-MEL cell NYPZ[pY4T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MWDJcohq[mm2aX;uJI9nKGi3bXHuJGxDOjVzOD3NSWwh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF06Oy56MjDuUU4> NHzpe3JUSU6JRWK=
human C32 cell MUTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M2\HUWlvcGmkaYTpc44hd2ZiaIXtZY4hSzN{IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;OUiuNlMhdk1w MX;TRW5ITVJ?
human BHT-101 cell NVK0OVNzT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NYjkfZZlUW6qaXLpeIlwdiCxZjDoeY1idiCESGStNVAyKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTB4LkmzJI5ONg>? M2CxTXNCVkeHUh?=
human KY821 cell MUDHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MYnJcohq[mm2aX;uJI9nKGi3bXHuJGt[QDJzIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUC3MlE5KG6PLh?= NXPX[Jp5W0GQR1XS
human CP50-MEL-B cell NY\Uc5NuT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MnjxTY5pcWKrdHnvckBw\iCqdX3hckBEWDVyLV3FUE1DKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTJ5Lkm0JI5ONg>? M1;Qb3NCVkeHUh?=
human MEL-HO cell MoLrS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MnGyTY5pcWKrdHnvckBw\iCqdX3hckBOTUxvSF:gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xN|gvQDRibl2u M1nmdnNCVkeHUh?=
human MIAPaCa2 cells M3n2SnBzd2yrZnXyZZRqd25iYYPzZZk> NGn6ZZhCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3JRXBiS2F{IHPlcIx{NCCLQ{WwQVE1OiCwTT6= Mk\SNlM1PzR|OEi=
human EoL-1-cell cell M1nCVWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MW\Jcohq[mm2aX;uJI9nKGi3bXHuJGVwVC1zLXPlcIwh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yPDRwN{[gcm0v MWfTRW5ITVJ?
human DOK cell NV\nR2M4T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NUnWXWR{UW6qaXLpeIlwdiCxZjDoeY1idiCGT1ugZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xOFcvODhibl2u M3;rZXNCVkeHUh?=
human SH-4 cell M{XkVGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NV;lcW5WUW6qaXLpeIlwdiCxZjDoeY1idiCVSD20JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVY3NjR6IH7NMi=> MYTTRW5ITVJ?
human BPH-1 cell M4f2NWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NIW3UoFKdmirYnn0bY9vKG:oIHj1cYFvKEKSSD2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVgzNjNzIH7NMi=> MWrTRW5ITVJ?
human HuP-T4 cell Mn63S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MXTJcohq[mm2aX;uJI9nKGi3bXHuJGh2WC2WNDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUG5OU4{OiCwTT6= NY\wPVZVW0GQR1XS
human KU812 cell NGr5dIVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MYLJcohq[mm2aX;uJI9nKGi3bXHuJGtWQDF{IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MkGxMlY5KG6PLh?= M{fEd3NCVkeHUh?=
human A549 cell MoTnS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NIjGNGpKdmirYnn0bY9vKG:oIHj1cYFvKEF3NEmgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yNVQvOTNibl2u M1HYVnNCVkeHUh?=
human HTC-C3 cell M{XBUWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NVqxOpBZUW6qaXLpeIlwdiCxZjDoeY1idiCKVFOtR|Mh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zOTRwNkGgcm0v MlLQV2FPT0WU
human A101D cell NWfwUo5MT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MV;Jcohq[mm2aX;uJI9nKGi3bXHuJGEyODGGIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MkSwMlM{KG6PLh?= NVrwdGtqW0GQR1XS
human ONS-76 cell NF3pSppIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NVjUU|ZmUW6qaXLpeIlwdiCxZjDoeY1idiCRTmOtO|Yh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zPDRwNUOgcm0v NFTYTJJUSU6JRWK=
human RKO cell M2O2SGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NWfYc2tNUW6qaXLpeIlwdiCxZjDoeY1idiCUS1:gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yOFgvOzhibl2u NHvjXWFUSU6JRWK=
human WM-115 cell MWnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MYTJcohq[mm2aX;uJI9nKGi3bXHuJHdONTFzNTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUK2O{42PCCwTT6= MXXTRW5ITVJ?
human HCC2998 cell Mn7PS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? Mn;3TY5pcWKrdHnvckBw\iCqdX3hckBJS0N{OUm4JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlY6NjB5IH7NMi=> NWrJWIU3W0GQR1XS
human C2BBe1 cell NEf4bm5Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= M37oTmlvcGmkaYTpc44hd2ZiaIXtZY4hSzKEQnWxJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlczNjV7IH7NMi=> NEH6UpRUSU6JRWK=
human RVH-421 cell MofIS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NEDIeFNKdmirYnn0bY9vKG:oIHj1cYFvKFKYSD20NlEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zPzlwM{mgcm0v NWDpdG1DW0GQR1XS
human H-EMC-SS cell MmfES5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MoD5TY5pcWKrdHnvckBw\iCqdX3hckBJNUWPQz3TV{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVI6OC57OTDuUU4> MnfmV2FPT0WU
human ML-2 cell NV7HS282T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M{nBXmlvcGmkaYTpc44hd2ZiaIXtZY4hVUxvMjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUK5N{43OyCwTT6= M1;qfHNCVkeHUh?=
human SW620 cell NH7C[lFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NVP2fmI1UW6qaXLpeIlwdiCxZjDoeY1idiCVV{[yNEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVMxOi5{IH7NMi=> MWrTRW5ITVJ?
human UACC-257 cell MYjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NHrzclRKdmirYnn0bY9vKG:oIHj1cYFvKFWDQ1OtNlU4KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OzJzLki0JI5ONg>? MV7TRW5ITVJ?
human AsPC-1 cell MYfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M2ToN2lvcGmkaYTpc44hd2ZiaIXtZY4hSXOSQz2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N|I1NjN7IH7NMi=> NYLLbVJGW0GQR1XS
human CAL-39 cell NF7CU45Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= MnXiTY5pcWKrdHnvckBw\iCqdX3hckBESUxvM{mgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zN|IvOjZibl2u NFu4d5pUSU6JRWK=
human COLO-679 cell M4fTN2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MVXJcohq[mm2aX;uJI9nKGi3bXHuJGNQVE9vNke5JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N|QyNjF7IH7NMi=> NHrqOZFUSU6JRWK=
human NCI-H747 cell MnjTS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NX7qWFZDUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFc1PyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTN3MD65PEBvVS5? NVTFRmU2W0GQR1XS
human NCI-H1437 cell M3fVbmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MXfJcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KMUSzO{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVM2Oi56NTDuUU4> NHr5T2xUSU6JRWK=
human PSN1 cell NYDnZ3NLT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NFv1eVZKdmirYnn0bY9vKG:oIHj1cYFvKFCVTkGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zOlYvODlibl2u NInn[IZUSU6JRWK=
human NKM-1 cell M3XUe2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M2HTbGlvcGmkaYTpc44hd2ZiaIXtZY4hVkuPLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zPFUvQCCwTR?= NFrJZYxUSU6JRWK=
human MZ2-MEL cell NY[z[WFWT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MoXCTY5pcWKrdHnvckBw\iCqdX3hckBOYjJvTVXMJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N|k1NjN5IH7NMi=> MULTRW5ITVJ?
human SK-MEL-2 cell NFS0d|BIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MWHJcohq[mm2aX;uJI9nKGi3bXHuJHNMNU2HTD2yJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OFA2NjB4IH7NMi=> M4XPe3NCVkeHUh?=
human LAMA-84 cell NFTHVYZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MVLJcohq[mm2aX;uJI9nKGi3bXHuJGxCVUFvOESgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME20OVYvOjJibl2u NX\UeJA3W0GQR1XS
human U-266 cell NUfRN|d1T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NEKxfFBKdmirYnn0bY9vKG:oIHj1cYFvKFVvMk[2JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OFg4Njd2IH7NMi=> MlPOV2FPT0WU
human RCM-1 cell M4n0N2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NInHT|FKdmirYnn0bY9vKG:oIHj1cYFvKFKFTT2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OFk{Njh3IH7NMi=> NV\LbXFlW0GQR1XS


体内試験 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]




+ 展開

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.


+ 展開
  • 細胞株: Primary HCC cell lines including 2-1318, 4-1318 and 26-1004 cells
  • 濃度: ~ 10 μM
  • 反応時間: 24 or 48 hours
  • 実験の流れ:

    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.



+ 展開
  • 動物モデル: HCC xenografts in mice homozygous for the SCID (severe combined immunodeficiency) mutation
  • 製剤: In water
  • 投薬量: 50 or 100mg/kg
  • 投与方法: Administered via p.o.

溶解度 (25°C)

体外 DMSO 91 mg/mL (198.82 mM) warming
Water Insoluble
Ethanol Insoluble
体内 順序で溶剤を入れること:
4% DMSO+30% PEG 300+5% Tween 80+ddH2O

* 溶解度検測はSelleck技術部門によって行いますので、文献より提供された溶解度と差異がある可能性がありますが、生産工芸と不同ロット(lot)で起きる正常な現象ですから、ご安心ください。


分子量 457.68


CAS No. 606143-52-6
別名 ARRY-142886





マス (g) = 濃度 (mol/L) x ボリューム (L) x 分子量 (g/mol)


  • マス




貯蔵液を準備することを要求される希釈剤を計算してください. セレック希釈計算器は、以下の方程式に基づきます:

開始濃度 x 開始体積 = 最終濃度 x 最終体積


この方程式は、一般に略語を使われます:C1V1 = C2V2 ( 輸入 輸出 )

  • C1



  • 連続希釈剤

  • 計算結果

  • 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):




チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2


マス 濃度 ボリューム 分子量


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 --



Handling Instructions


  • * 必須


  • 問題1:

    How about the solubility of S1008? How to prepare for the solution if I need to do the in vivo experiments?

  • 回答:

    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 Inhibitors with Unique Features


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細胞株 試験類型 濃度 培養時間 溶剤類型 活性叙述 PMID