Selumetinib (AZD6244)

For research use only.

Catalog No.S1008 Synonyms: ARRY-142886

446 publications

Selumetinib (AZD6244) Chemical Structure

Molecular Weight(MW): 457.68

Selumetinib (AZD6244, ARRY-142886) 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. Selumetinib suppresses cell proliferation, migration and trigger apoptosis. Phase 3.

Size Price Stock Quantity  
10mM (1mL 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.

Selleck's Selumetinib (AZD6244) has been cited by 446 publications

Purity & Quality Control

Choose Selective MEK Inhibitors

Biological Activity

Description Selumetinib (AZD6244, ARRY-142886) 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. Selumetinib suppresses cell proliferation, migration and trigger apoptosis. 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 NGrwNI9Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= M1zJS2lvcGmkaYTpc44hd2ZiaIXtZY4hS0iSLUKxNkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVMvOTVibl2u NW[ydmJiW0GQR1XS
human H9 cell NYfWU4gxT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M4\KSGlvcGmkaYTpc44hd2ZiaIXtZY4hUDliY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1{Mj64PEBvVS5? Ml\aV2FPT0WU
human HL-60 cell Ml\IS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NV;HN3NoUW6qaXLpeIlwdiCxZjDoeY1idiCKTD22NEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVI1NjV7IH7NMi=> MoDFV2FPT0WU
human A375 cells NYrWW4pEWHKxbHnm[ZJifGmxbjDhd5NigQ>? M1u1PVczKGh? MkDGRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCDM{e1JINmdGy|IHX4dJJme3OrbnegRnJCTiCYNkCwSUBufXSjboSgZYZ1\XJiN{KgbJJ{KGK7IFPlcIwhfGm2ZYKt[4xwKGG|c3H5MEBKSzVyPUOxJI5ONg>? NWDL[oR4OjN2N{SzPFg>
human NOMO-1 cell MoPUS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MXnJcohq[mm2aX;uJI9nKGi3bXHuJG5QVU9vMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUOxMlk4KG6PLh?= M2[3UXNCVkeHUh?=
human DU-4475 cell MkHDS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MWfJcohq[mm2aX;uJI9nKGi3bXHuJGRWNTR2N{WgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zN{43PyCwTT6= M4[3NXNCVkeHUh?=
human M14 cell NVq1OJRMT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MkXqTY5pcWKrdHnvckBw\iCqdX3hckBOOTRiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1|Nj64PUBvVS5? NF3KR4hUSU6JRWK=
human HT-144 cell MlPZS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MmDQTY5pcWKrdHnvckBw\iCqdX3hckBJXC1zNESgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME24PU4xPSCwTT6= MWrTRW5ITVJ?
human SK-N-AS cell M4TTVWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 Mlz4TY5pcWKrdHnvckBw\iCqdX3hckBUUy2QLVHTJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9PVIvQDNibl2u M1vudHNCVkeHUh?=
human LB2518-MEL cell MW\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MkP4TY5pcWKrdHnvckBw\iCqdX3hckBNSjJ3MUitUWVNKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:QTNwOEKgcm0v NYfhe5NjW0GQR1XS
human C32 cell NUX3[|F4T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NIjZdWxKdmirYnn0bY9vKG:oIHj1cYFvKEN|MjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUm4MlI{KG6PLh?= M1u3XHNCVkeHUh?=
human BHT-101 cell Mk[2S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M3fuSGlvcGmkaYTpc44hd2ZiaIXtZY4hSkiWLUGwNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVExPi57MzDuUU4> M1TkcXNCVkeHUh?=
human KY821 cell NWXiXmsyT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M{[2b2lvcGmkaYTpc44hd2ZiaIXtZY4hU1l6MkGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xNFcvOThibl2u NV73NpA2W0GQR1XS
human CP50-MEL-B cell NVfje2I1T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M4TXT2lvcGmkaYTpc44hd2ZiaIXtZY4hS1B3MD3NSWwuSiClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTF{Nz65OEBvVS5? MVfTRW5ITVJ?
human MEL-HO cell MmPKS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MkjMTY5pcWKrdHnvckBw\iCqdX3hckBOTUxvSF:gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xN|gvQDRibl2u MYPTRW5ITVJ?
human MIAPaCa2 cells M3jHcnBzd2yrZnXyZZRqd25iYYPzZZk> M2HtdmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVnBVIFE[TJiY3XscJMtKEmFNUC9NVQzKG6PLh?= NWP5W3J{OjN2N{SzPFg>
human EoL-1-cell cell MXfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MlzoTY5pcWKrdHnvckBw\iCqdX3hckBGd0xvMT3j[YxtKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTR2Lke2JI5ONg>? NHjONXhUSU6JRWK=
human DOK cell NHS5cXhIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NGDKcoVKdmirYnn0bY9vKG:oIHj1cYFvKESRSzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUG0O{4xQCCwTT6= MnW1V2FPT0WU
human SH-4 cell MXTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NGTS[3RKdmirYnn0bY9vKG:oIHj1cYFvKFOKLUSgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xOlYvPDhibl2u MYrTRW5ITVJ?
human BPH-1 cell MmfnS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NH7wT|BKdmirYnn0bY9vKG:oIHj1cYFvKEKSSD2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVgzNjNzIH7NMi=> M4XIS3NCVkeHUh?=
human HuP-T4 cell MVTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NIHrSllKdmirYnn0bY9vKG:oIHj1cYFvKEi3UD3UOEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVE6PS5|MjDuUU4> NITZVYhUSU6JRWK=
human KU812 cell NV3aN4JwT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NWjlTopCUW6qaXLpeIlwdiCxZjDoeY1idiCNVUixNkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVIyOS54ODDuUU4> M4fv[XNCVkeHUh?=
human A549 cell M{PRVmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M{ji[mlvcGmkaYTpc44hd2ZiaIXtZY4hSTV2OTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUKxOE4yOyCwTT6= NUX1XXQ{W0GQR1XS
human HTC-C3 cell MXjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MoXGTY5pcWKrdHnvckBw\iCqdX3hckBJXENvQ{OgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yNVQvPjFibl2u NGfVN2JUSU6JRWK=
human A101D cell NF3JOYhIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M3LSfWlvcGmkaYTpc44hd2ZiaIXtZY4hSTFyMVSgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yOFAvOzNibl2u M2jsS3NCVkeHUh?=
human ONS-76 cell MmH4S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NFjG[JJKdmirYnn0bY9vKG:oIHj1cYFvKE:QUz23OkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVI1PC53MzDuUU4> NUD2OJRmW0GQR1XS
human RKO cell M2LGVmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NYrIU4FiUW6qaXLpeIlwdiCxZjDoeY1idiCUS1:gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yOFgvOzhibl2u MoLYV2FPT0WU
human WM-115 cell MnvZS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MoS5TY5pcWKrdHnvckBw\iCqdX3hckBYVS1zMUWgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yOlcvPTRibl2u NWK1W2RvW0GQR1XS
human HCC2998 cell MXzHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M4LCTmlvcGmkaYTpc44hd2ZiaIXtZY4hUEOFMkm5PEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVI3QS5yNzDuUU4> MYHTRW5ITVJ?
human C2BBe1 cell NH63cIFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MoDvTY5pcWKrdHnvckBw\iCqdX3hckBEOkKEZUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yO|IvPTlibl2u Mmn2V2FPT0WU
human RVH-421 cell NWnjcJdET3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NFfKZppKdmirYnn0bY9vKG:oIHj1cYFvKFKYSD20NlEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zPzlwM{mgcm0v NYmzOHlbW0GQR1XS
human H-EMC-SS cell MUfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MkjpTY5pcWKrdHnvckBw\iCqdX3hckBJNUWPQz3TV{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVI6OC57OTDuUU4> MlO0V2FPT0WU
human ML-2 cell NV\Td2ZLT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M3rVPGlvcGmkaYTpc44hd2ZiaIXtZY4hVUxvMjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUK5N{43OyCwTT6= M3;XZnNCVkeHUh?=
human SW620 cell M33vbmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M3vucmlvcGmkaYTpc44hd2ZiaIXtZY4hW1d4MkCgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zNFIvOiCwTT6= NEDjZnZUSU6JRWK=
human UACC-257 cell NHKxeXFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M3PJWWlvcGmkaYTpc44hd2ZiaIXtZY4hXUGFQz2yOVch[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0{OjFwOESgcm0v M4L3bHNCVkeHUh?=
human AsPC-1 cell Ml7TS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M1fjdmlvcGmkaYTpc44hd2ZiaIXtZY4hSXOSQz2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N|I1NjN7IH7NMi=> MX7TRW5ITVJ?
human CAL-39 cell MV\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M{LsZmlvcGmkaYTpc44hd2ZiaIXtZY4hS0GOLUO5JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N|MzNjJ4IH7NMi=> MUDTRW5ITVJ?
human COLO-679 cell MlrNS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MlO5TY5pcWKrdHnvckBw\iCqdX3hckBEV0yRLU[3PUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVM1OS5zOTDuUU4> Mk\GV2FPT0WU
human NCI-H747 cell M{LaeGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NWH2c3puUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFc1PyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTN3MD65PEBvVS5? MV;TRW5ITVJ?
human NCI-H1437 cell M3vxfWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M33GOWlvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLVixOFM4KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OzV{Lki1JI5ONg>? NIj2dYhUSU6JRWK=
human PSN1 cell NVLWS4kyT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NF;VTZVKdmirYnn0bY9vKG:oIHj1cYFvKFCVTkGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zOlYvODlibl2u MWHTRW5ITVJ?
human NKM-1 cell MlXlS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NF3aTFdKdmirYnn0bY9vKG:oIHj1cYFvKE6NTT2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N|g2Njhibl2= MVjTRW5ITVJ?
human MZ2-MEL cell NFjuWJZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MoO1TY5pcWKrdHnvckBw\iCqdX3hckBOYjJvTVXMJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N|k1NjN5IH7NMi=> MWfTRW5ITVJ?
human SK-MEL-2 cell NXrkW3pET3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MVzJcohq[mm2aX;uJI9nKGi3bXHuJHNMNU2HTD2yJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OFA2NjB4IH7NMi=> M4\nUnNCVkeHUh?=
human LAMA-84 cell NFPqV3ZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MX;Jcohq[mm2aX;uJI9nKGi3bXHuJGxCVUFvOESgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME20OVYvOjJibl2u MVLTRW5ITVJ?
human U-266 cell MoX6S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NYDHemdzUW6qaXLpeIlwdiCxZjDoeY1idiCXLUK2OkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQ5Py55NDDuUU4> MnfmV2FPT0WU
human RCM-1 cell NWnWOow2T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MVzJcohq[mm2aX;uJI9nKGi3bXHuJHJEVS1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;NEmzMlg2KG6PLh?= MVvTRW5ITVJ?

... 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]

- Collapse

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]

- Collapse
  • 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]

- Collapse
  • Animal Models: HCC xenografts in mice homozygous for the SCID (severe combined immunodeficiency) mutation
  • 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
Smiles CN1C=NC2=C1C=C(C(=C2F)NC3=C(C=C(C=C3)Br)Cl)C(=O)NOCCO

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O
CalculateReset

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 (mg) = Concentration (mM) × Volume (mL) × 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
NCT03326388 Recruiting Drug: Selumetinib Neurofibromatosis Type 1|Plexiform Neurofibroma|Optic Nerve Glioma Great Ormond Street Hospital for Children NHS Foundation Trust|AstraZeneca September 26 2019 Phase 1|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
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 May 18 2018 Phase 1|Phase 2

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