PD98059

目录号:S1177

PD98059 Chemical Structure

Molecular Weight(MW): 267.28

PD98059是一种非ATP竞争性的MEK抑制剂,无细胞试验中IC50为2 μM,特异性抑制MEK-1介导的MAPK激活;不直接抑制ERK1或ERK2。

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客户使用Selleck该产品发表文献50篇:

客户使用该产品的10个实验数据:

  • 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):422-427.. PD98059 purchased from Selleck.

     

    Melanoma cell viability and in vivo growth by cyclindependent kinase 2/4 inhibition. Western blot analysis for c-Jun, phosphorylated-ERK1/2 (Thr202/Tyr204) (p-ERK1/2), and total ERK1/2 protein levels was done for human melanoma cell lines treated with the BRAFV600E inhibitor GDC-0879 (1 μM), or MEK inhibitors CI-1040 (1 μM), U0126 (1 μM), and PD98059 (10 μM) for 18 hours.

    J Natl Cancer Inst 2012 104(21), 1673-9. PD98059 purchased from Selleck.

  •  

    Melanoma cell viability and in vivo growth by cyclindependent kinase 2/4 inhibition. In vivo growth of LOXIMVI xenografts in athymic nude Foxn1nu mice is shown. Tumors were allowed to grow to a maximum volume of 250 mm3, and the mice were subsequently treated daily at the indicated dose levels with CDK2/4 inhibitors by intraperitoneal injection in combination with a BRAFV600E- or MEK-inhibitor. CDK2/4 inhibitor (CVT-313/indolocarbazole CDK4-I) treatment sensitizes tumors to GDC-0879 and CI1040.

    J Natl Cancer Inst 2012 104(21), 1673-9. PD98059 purchased from Selleck.

    effect of ERK1/2 inhibitor PD98059 (1, 5, and 10 μM) on SRP72 protein expression was evaluated on Jurkat cells stimulated with rhIL-1. The cells were harvested at 0,120, and 240 min, and the protein expression was verified by WB using antibodies against human SRP72, human SRP54 (nonphosphorylated SRP protein), and humanGAPDHas constitutive protein.Adecreased SRP72 expression at 10 μM and 240 min was found.

     

     

    J Biol Chem 2010 285, 32824-32833. PD98059 purchased from Selleck.

  • C, effect of ERK1/2 inhibitor PD98059 (1, 5, and 10 μM) was evaluated in SRP72-immunoprecipitated cell lysates. WB using anti-phosphoserine antibody showed a decreased SRP72 band when used as the inhibitor at concentrations of 1 μM at 240 min, 5 μM at 120 min, and 10 μM at 120 and 240 min (lanes 3, 5, 8, and 9). D, results were analyzed and RUA illustrated, finding significant results at 1 μM at 240 versus 0, 5 μM at 120 versus 0, and 10 μM at 120 versus 0 min.

     

     

    J Biol Chem 2010 285, 32824-32833. PD98059 purchased from Selleck.

    We used real time RT-PCR to investigate the effects of PD98059 on SRP72 mRNA expression. All the samples were treated under the same experimental conditions used in protein tests done by WB, and phosphorylation was measured indirectly by IP-WB. The results did not show significant changes on the mRNA expression of SRP72 after the treatment with these inhibitors.

     

     

    J Biol Chem 2010 285, 32824-32833. PD98059 purchased from Selleck.

  •  

    Activation of a TLR2eERK1/2 pathway in MDDC. (C) MDDC were either untreated or treated with C. pneumoniae alone or in the presence of the ERK1/2 inhibitor PD98059 for 48 h. IL-12p70 and IL-10 release in culture media was assessed by ELISA. (D) MDDC were treated as in panel C for 48 h and then cocultured with purified allogeneic CD3t T cells. On day 12, supernatants were collected, and secreted cytokines were measured by ELISA.

    Microbes Infect 2013 15, 105-14. PD98059 purchased from Selleck.

    HepG2 cells, “Pnt-2” primary HCC cells or THLE-2 normal liver cells were pretreated with PD-98059 (1 mM) or MEK-162 (“MEK”, 1 mM) for 1 h prior toWAY-600 (“WAY”, 100 nM) treatment, after applied period, cell viability and apoptosis were tested by MTT assay (F and H).

    Biochem Biophys Res Commun, 2016, 474(2):330-7.. PD98059 purchased from Selleck.

  • Collagen I and α-SMA are conducive for S. aureus adhesion to and invasion into BMFBs. BMFBs were treated with PD98059 2 h before the addition of 5 ng/ml TGF-β1; 24 h later, the adhesion (A) and invasion (B) assays were performed as previously described. The results are expressed as the mean cfu/ml ± SD from experiments performed in triplicate (*P < 0.05, **P < 0.01).

    Microb Pathog, 2017, 106:25-29. PD98059 purchased from Selleck.

    After starved in serum-free medium for 24h,T47D cells incubated with the indicated concentrations of  PD98059 for 3h,followed by 20-minute  stimolation of 100ng/ml EGF.

     

    2010 Dr. Zhang of Tianjin Medical University. PD98059 purchased from Selleck.

产品安全说明书

MEK抑制剂选择性比较

生物活性

产品描述 PD98059是一种非ATP竞争性的MEK抑制剂,无细胞试验中IC50为2 μM,特异性抑制MEK-1介导的MAPK激活;不直接抑制ERK1或ERK2。
特性 PD98059不会抑制已经被c-Raf磷酸化的 MEK1
靶点
MEK1 [1]
(Cell-free assay)
2 μM
体外研究

PD98059 要么抑制本底的MEK1,要么抑制一种被部分激活的MEK突变体,该突变体是 218 和 222号位上丝氨酸突变为谷氨酸后形成的(MEK-2E), IC50 为2 μM. PD98059 不会抑制JNK和P38这两个 MAPK 的同系物. PD98059会高度选择性的抑制MEK, 因为对其它包括Raf 激酶, cAMP-依赖性激酶, 蛋白激酶C, v-Src, 表皮生长因子 (EGF) 受体激酶, 胰岛素受体激酶, PDGF 受体激酶, 和磷脂酰肌醇(-3)激酶等在内的一系列激酶都没有抑制性。 PD98059 会抑制经过PDGF刺激而活化的MAPK 和胸苷 进入 3T3 细胞, IC50分别为 ~10 μM 和 ~7 μM [1]。PD98059可以有效地阻止 MEK1 被Raf 或者MEK 激酶活化, IC50为4 μM, 可以微弱地 抑制MEK2被 Raf 活化, IC50 为50 μM。 在KB 和 PC12 细胞中, PD98059 不会抑制MKK4 和RK激酶这两个参与压力和白细胞介素-1介导的激酶级联反应的MEK的同系物的活化,在Swiss 3T3 细胞中也不会通过胰岛素或者表皮生长因子抑制p70 S6 激酶的活化[2]。PD98059会在不改变细胞生存能力的情况下完全阻断 神经生长因子(NGF)诱导的 PC12 细胞的分化[3] 。PD98059会以剂量依赖性的方式抑制培养在含有破骨细胞分化因子培养基中的 RAW264.7细胞的增值,进而导致TRAP阳性细胞数量明显下降[6]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
H1355 M{D5bGZ2dmO2aX;uJGF{e2G7 M3rEOFI2KM7:TR?= NH7BS2YyKGh? Mn\qZox2dnS|IITo[UBDY2GfUD3pcoR2[2WmIHnuZ5Jm[XOnIHnuJJBpd3OyaH:tR4hsOSCjbnSgdIhwe3Cqbz3FVmsh\XiycnXzd4lwdg>? MWSyOVc3QTF6MR?=
MCF-7  NUHtclcyTnWwY4Tpc44hSXO|YYm= NXHJXlRWOTBizszN MYSxJIg> MknSbY5pcWKrdIOgTWwuOThvZX7oZY5k\WRiY3XscEBucWe{YYTpc44> MmLDNlU4OjdyMUG=
HepG2  M1:1XWZ2dmO2aX;uJGF{e2G7 Mn\PNVAh|ryP MWq1JIg> NHTWT2RjdG:la4OgdIhwe3Cqb4L5cIF1\WRiTVHQT5MhcW6mdXPl[EBjgSCneH;n[Y5wfXNiVFfGMe6zOQ>? M4DmclI2PTZyNEi4
HepG2  NEmxfGNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX6yNEDPxE1? MXeyOEBp MU\zeZBxemW|c3XzJHRITi4QskGtbY5lfWOnZDDj[YxtKHC{b3zp[oVz[XSrb36gZY5lKGmwdnHzbY9v M3TMeVI2PTZyNEi4
MDA-MB-231 MoPNSpVv[3Srb36gRZN{[Xl? MVuyOUDPxE1? MmXSNk0{KGh? NF;NWW1l\WO{ZXHz[ZMheC2HUluxM|Ih[W6mIGOxNFBCPCCneIDy[ZN{cW:w NHLMWmIzPTV3NUi3OS=>
SW480 NI\PdGJHfW6ldHnvckBCe3OjeR?= MmfVNlDDqM7:TR?= M3;wcVHDqGh? NXO0NYxGemWmdXPld{B1cGViZYjwdoV{e2mxbjDv[kBCXEZ|IIDyc5RmcW5? MXmyOVQ1PzhzNh?=
HCT-15 MkH3SpVv[3Srb36gRZN{[Xl? NIPHTm4yKGh? NHfpdIhifHSnboXheIV{KFCJRUKtbY5lfWOnZDDwbI9{eGixconsZZRqd25ib3[gSZJsyqB? M2TrTFI2PDNzNEK1
HCT-15 MofnRZBweHSxc3nzJGF{e2G7 MlzuNUBp MlvtZYJwdGm|aHXzJJRp\SCycn;0[YN1cX[nIHXm[oVkfHNib3[gVGdGOsLiYXfhbY5{fCCldYLjeY1qdi2rbnT1Z4VlKGGyb4D0c5Nqew>? Mmf5NlU1OzF2MkW=
786-O NXr4cFBESXCxcITvd4l{KEG|c3H5 MW[1NOKh|ryP NFvBc5AzPCCq NVTpVXp6eG:2ZX70bYF1\XQEoITo[UBxem9vYYDvdJRwfGmlIHXm[oVkfHNib3[gUmM> NVv0UXg4OjR3MEi0O|Y>
A498 MV3BdI9xfG:|aYOgRZN{[Xl? NYLK[YRMPTEEoN88US=> MYSyOEBp NX24V3lieG:2ZX70bYF1\XQEoITo[UBxem9vYYDvdJRwfGmlIHXm[oVkfHNib3[gUmM> M4i0eVI1PTB6NEe2
NHBE M3;SO2Z2dmO2aX;uJGF{e2G7 NWPZUJJ3Oi9{MDFOwG0> MV2yJIg> NYTUXW56[XS2ZX71ZZRmeyCLTD2zN{B{fGmvdXzheIVlKEO[Q1y4M2lNNThic3XjdoV1cW:w MmnRNlQ1Pzl3Mk[=
A375 NFH6UpVE\WyuIFnueoF{cW:wIFHzd4F6 NIfie2QyOOLCk{KwJOK2VQ>? MVSyOEBp M4i5cJJm\HWlZYOgcYVt[W6xbXGgZ4VtdCCrbo\hd4lwdg>? MVGyOFQ3PjB|Nh?=
HBMEC M4HFVGZ2dmO2aX;uJGF{e2G7 NFHCNJoyOCEQvF2= NGPofJAyKGh? NH60NlljdG:la4OgWmVITi2rbnT1Z4VlKEWyaFGyJIV5eHKnc4Ppc44> MnTaNlQ1PTh7OEK=
HPAEpiCs  MXHGeY5kfGmxbjDBd5NigQ>? NImzZYs{OCEQvF2= MX6xJIg> NV7YSlFpcW6qaXLpeJMhXE6ILd8xJJN1cW23bHH0[YQheDR{L4C0OEBOSVCNIIDoc5NxcG:{eXzheIlwdg>? NF\DTWgzPDR2MUi3NC=>
BeWo NFzhc|hHfW6ldHnvckBCe3OjeR?= NFHrfJcyOMLizszN M1v2bFIhcA>? MkHObY5pcWKrdIOgSXJMOS9{ MoPUNlQ1OzN6NE[=
PC3  NUHsO4dQSXCxcITvd4l{KEG|c3H5 MYe1NEDPxE1? NFO1cWsxNjViaB?= NGDhcpZqdmirYnn0d{BOUFlvNES5MYlv\HWlZXSgZZBweHSxc3nzxsA> M3XVe|I1PDJ2OEi5
HGC-27 MUTBdI9xfG:|aYOgRZN{[Xl? MofLNUDDvU1? MV2xJIg> NEXpfll{fXCycnXzd4V{KFKDRECwNUBxdHW|IF3LMVIzODZvaX7keYNm\CClZXzsJJZq[WKrbHn0fUBtd3O| MVeyOFQyPjN2OR?=
MCF-7 NWf4T4prTnWwY4Tpc44hSXO|YYm= NYfRU5RWOTEEoN88US=> NH71[2YyOC9|MDDtbY4> Ml[1doVlfWOnczD0bIUhXVSSLXTldIVv\GWwdDDFVmsheGixc4Doc5J6dGG2aX;u NUjG[mo3OjR|OUC4NVk>
HUVECs M{LaZmZ2dmO2aX;uJGF{e2G7 NYe4dYdIOTEEoN88US=> NH\yNoEyKGh? M2rqPYlvcGmkaYTzJJRp\SCKRFygdoVlfWOnZDDDU3guOiCneIDy[ZN{cW:wIHHu[EBRT0lvMjDy[Yxm[XOn M36welI1Ozh3MUC5
HeLa MlPXSpVv[3Srb36gRZN{[Xl? NXLpb5JlPTBizszN NETCRXgxNjViaB?= M{DCPYJtd2OtczDUVnguOSCwdXPs[YFzKG2rZ4LheIlwdiCjbnSgWHhPUVBiZH;3ck1z\We3bHH0bY9v NXq5RlVROjR|N{[4Nlc>
HL-60  NVjR[IU3TnWwY4Tpc44hSXO|YYm= MorKNVAwOjBizszN MkjUNUBp M4jPfYlvcGmkaYTzJJRp\cLiTj6gZ4hqdmWwc3nz[Zh1emGldNMgbY5lfWOnZDDkbYZn\XKnboTpZZRqd25iaX70c{BoemGwdXzvZ5l1\XN? MknXNlQ{PTdyMkC=
HL-60 MWPGeY5kfGmxbjDBd5NigQ>? NVTBSlRxOiEEtV2= MmrJNVYhcA>? MXLEUXNQ NX7Mc|dFcW6qaXLpeJMhfGinIHHzd49kcWG2aX;uJI9nKHCVNkKxJHJi\i1zIHHu[EBPTkGWY{OsJIFv\CC2aHWgVmEucW6mdXPl[EBxcG:|cHjvdplt[XSrb36gc4YhdnWlbHXhdkBPTkGWY{O= MknqNlQ{OzByNki=
HEK 293 Mm\lSpVv[3Srb36gRZN{[Xl? M4LJc|ExKM7:TR?= M4nWWlUhcA>? NXX0OJU4TE2VTx?= M3v2cIlvcGmkaYTzJHdvfC2rbnT1Z4VlKM7{LXPheIVvcW5xVFPGOEBi[3Srdnn0fUBidmRiboXjcIVieiEQsj3jZZRmdmmwIHHjZ5VufWyjdHnvci=> Mn[4NlQ{OjR|Nk[=
HEK 293 NFfmbYxHfW6ldHnvckBCe3OjeR?= MYmxNEDPxE1? NYPxfml6PSCq M2XFSWROW09? MmTRd5VxeHKnc4Pld{B1cGViQ2LUJIFkfGm4aYT5 M3G5eFI1OzJ2M{[2
SW480 NHrTPWVHfW6ldHnvckBCe3OjeR?= NWH5OlN1OTBizszN MV6yNEBp MWTEUXNQ Ml:wd5VxeHKnc4Pld{B1cGViQ2LUJIFkfGm4aYT5 NYPTNFFPOjR|MkSzOlY>
HCSMCs NF\rSJVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH;KfJYyOCEQvF2= MX2yOEBp NVXp[2cy[myxY3vzJGZCSlB2LXnu[JVk\WRiSFPBV21EKHC{b3zp[oVz[XSrb36= M3\nUlI1OzF{M{ix
PANC-1 MWHGeY5kfGmxbjDBd5NigQ>? M4PUOVIxKM7:TR?= MXu0PEBp MkL4bY5pcWKrdIOgeIhmKGW6cILld5Nqd25ib3[g{rQ3TCCrbjDy[ZNxd26|ZTD0c{B1cGViUGDBVu61yqCjZ3;ubZN1yqB? MlTNNlQzQTRzM{O=
A549 M1\sTmZ2dmO2aX;uJGF{e2G7 MnXmN|Ah|ryP MojNNE42KGh? NWDnOFlYTE2VTx?= M2TKSYlvcGmkaYTzJJRp\SC2aILvcYJqdi2rbnT1Z4VlKEmOLUivR3hEVDhvTIXjJIFkfGm4aYT5 MlzjNlQzPzd4OU[=
A549 NEHhXplHfW6ldHnvckBCe3OjeR?= M1LxV|MxKM7:TR?= M3HsUVAvPSCq NVPSTHRtTE2VTx?= MkTrbY5pcWKrdIOgeIhzd22kaX6tbY5lfWOnZDDDM2VDWM7{IGTodlI{PcLicHjvd5Bpd3K7bHH0bY9v M{jBUlI1Ojd5Nkm2
MC-3 NV7OeJlqSXCxcITvd4l{KEG|c3H5 NXf5[odLOTBizszN M{DF[|I1KGh? MULwc5RmdnSrYYTl[EBOTVOFLXnu[JVk\WRiYYDvdJRwe2m|IHnuJEBk\Wyucx?= NH;sWYgzPDJ5MEWyNy=>
Raji  MoqxSpVv[3Srb36gRZN{[Xl? MVixNEDPxE1? MnzBNUBp NUfZOGUx[myxY3vzJIh{SkGIRjDpcoR2[2WmIFXyb|EwOiCyaH;zdIhwenmuYYTpc44> MoizNlQzPjl4M{C=
Raji  NWTpeZZnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MY[xNEDPxE1? M3vvZVEhcA>? M4DzeIlvcGmkaYTzJJRp\SCkYYPhcEBweiCqc1LBSmYue3SrbYXsZZRm\CClZXzsJJBzd2yrZnXyZZRqd25iYX7kJJZq[WKrbHn0fS=> NV3oW3BlOjR{Nkm2N|A>
HT29 M1;iZWZ2dmO2aX;uJGF{e2G7 MXqxNEDPxE1? NHju[XozKGh? MWLpcohq[mm2czDv[kBLSUt{LDDFVmsyNzJiYX7kJHNVSVR|IIDoc5NxcG:{eXzheIlwdg>? MkLqNlQzPjV{OUO=
HepG2 Mn;TRZBweHSxc3nzJGF{e2G7 NYfxblBjOjBizszN M3rtfFI1KGh? Mor3bY5pcWKrdIOgSXJMOS9{IIDoc5NxcG:{eXzheIlwdiCjbnSg[Y5p[W6lZYOgWmIyNWmwZIXj[YQh[XCxcITvd4l{ NWDhOnRSOjR{NEe5NFk>
HepG2 NEXlVItHfW6ldHnvckBCe3OjeR?= M3fkN|IxKM7:TR?= MX:yJIg> M1;RNYVvcGGwY3XzJHZDOS2rbnT1Z4VlKE[RWF:zZUB1emGwc3PybZB1cW:wYXygZYN1cX[rdIm= M2S2bFI1OjR5OUC5
TE4 MonySpVv[3Srb36gRZN{[Xl? MVuyNE82OC9zMECg{txO NIDJXIw1QCCq MYTEUXNQ M3r3NYlvcGmkaYTzJJAuTXKtIHHu[EB4d3K2bXHucolvKGSxd37y[Yd2dGG2ZXSgdE1Cc3RiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? M2D6O|I1OjR2MEKz
TE1 NHG5eIZHfW6ldHnvckBCe3OjeR?= MVWyNE82OC9zMECg{txO NFTEV241QCCq M4LnfGROW09? MV\pcohq[mm2czDwMWVzcyCjbnSge49zfG2jbn7pckBld3ewcnXneYxifGWmIICtRYt1KGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NIjaXW8zPDJ2NECyNy=>
KYSE30 NVLNTVhzTnWwY4Tpc44hSXO|YYm= M4jDZVIxNzVyL{GwNEDPxE1? NGDONFA1QCCq M1fBWmROW09? NF;BRo9qdmirYnn0d{BxNUW{azDhcoQhf2:{dH3hco5qdiCmb4fudoVofWyjdHXkJJAuSWu2IHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ NXvpfFJ2OjR{NESwNlM>
TE1 NVvQeoZ6TnWwY4Tpc44hSXO|YYm= NYjyb5dVPTBizszN NGnybZc1QCCq NWLSVVBUTE2VTx?= MX\1dJJm\3WuYYTld{B1cGViZYjwdoV{e2mxbjDv[kBJVEFiY3zhd5MhUQ>? NWLibmlEOjR{NESwNlM>
TE3 MkS1SpVv[3Srb36gRZN{[Xl? NEm2fYM2OCEQvF2= MXu0PEBp M2HPcGROW09? MVf1dJJm\3WuYYTld{B1cGViZYjwdoV{e2mxbjDv[kBJVEFiY3zhd5MhUQ>? NVHwS5o{OjR{NESwNlM>
TE4 NVqyUnZNTnWwY4Tpc44hSXO|YYm= M4S4OlUxKM7:TR?= M{m3VVQ5KGh? MV\EUXNQ NUn6SnR4fXC{ZXf1cIF1\XNidHjlJIV5eHKnc4Ppc44hd2ZiSFzBJINt[XO|IFm= NHK4SJMzPDJ2NECyNy=>
TE5 NWn1TVN1TnWwY4Tpc44hSXO|YYm= MVu1NEDPxE1? MnjuOFghcA>? NX\ISlFbTE2VTx?= NFTZSZR2eHKnZ4XsZZRmeyC2aHWg[ZhxemW|c3nvckBw\iCKTFGgZ4xie3NiSR?= M{HUU|I1OjR2MEKz
KYSE30 MkK1SpVv[3Srb36gRZN{[Xl? NIfpOFM2OCEQvF2= MYm0PEBp NH7Ud5BFVVOR NX;nTXM2fXC{ZXf1cIF1\XNidHjlJIV5eHKnc4Ppc44hd2ZiSFzBJINt[XO|IFm= NVHWbXBTOjR{NESwNlM>
MKN7 M4rCPGZ2dmO2aX;uJGF{e2G7 M4LDclUxKM7:TR?= NUPCd3BQPDhiaB?= NYnhclFYTE2VTx?= MoXlbY5kemWjc3XzJIV5eHKnc4Ppc44hd2ZiSFzBMWExOiCxcjDIUGEuSTJ2IH3vcIVkfWyncx?= NFXTR2QzPDJ2NECyNy=>
OE19 MkjCSpVv[3Srb36gRZN{[Xl? M4H3PFUxKM7:TR?= M1v4N|Q5KGh? MXHEUXNQ NXvXZYt{cW6lcnXhd4V{KGW6cILld5Nqd25ib3[gTGxCNUFyMjDvdkBJVEFvQUK0JI1wdGWldXzldy=> MnvwNlQzPDRyMkO=
KATOIII  M2\zfWZ2dmO2aX;uJGF{e2G7 NF7sZVQ2OCEQvF2= NUmyZmpQPDhiaB?= NHnDUHJFVVOR MkLGbY5kemWjc3XzJIV5eHKnc4Ppc44hd2ZiSFzBMWExOiCxcjDIUGEuSTJ2IH3vcIVkfWyncx?= M3Hpc|I1OjR2MEKz
NCI-N87  M3;XdWZ2dmO2aX;uJGF{e2G7 NX\iVGZnPTBizszN M3n4SlQ5KGh? MWjEUXNQ M1XKdYlv[3KnYYPld{BmgHC{ZYPzbY9vKG:oIFjMRU1CODJib4KgTGxCNUF{NDDtc4xm[3WuZYO= M1jCV|I1OjR2MEKz
NUGC3 MWnGeY5kfGmxbjDBd5NigQ>? NH;sfZQ2OCEQvF2= NGXyUpY1QCCq NYS4UVlnTE2VTx?= NUT6VVRKcW6lcnXhd4V{KGW6cILld5Nqd25ib3[gTGxCNUFyMjDvdkBJVEFvQUK0JI1wdGWldXzldy=> Mmf2NlQzPDRyMkO=
NUGC2 MULGeY5kfGmxbjDBd5NigQ>? MXe1NEDPxE1? NWf6PJhxPDhiaB?= NEf2OZJFVVOR MXLpcoNz\WG|ZYOg[ZhxemW|c3nvckBw\iCKTFGtRVAzKG:{IFjMRU1COjRibX;s[YN2dGW| MmHYNlQzPDRyMkO=
SGC-7901  NYTVV|I5SXCxcITvd4l{KEG|c3H5 MoqwNlAh|ryP M4rkTFI1KGh? MnrrbY5pcWKrdIOgR3AudWWmaXH0[YQh[XCxcITvd4l{ NWXweHRnOjR{NEGzOVE>
MG-63 NGnmdppHfW6ldHnvckBCe3OjeR?= NYHyS49EOjBizszN MlPuNE42KGh? MXnicI9kc3NidHjlJGNJNWmwZIXj[YQheGixc4Doc5J6dGG2ZXSgSWxMOSCycn;0[YlvKGW6cILld5Nqd25? M4q5N|I1OjN7NkSw
ARPE-19 NFrKcGpHfW6ldHnvckBCe3OjeR?= MnXPNlAh|ryP NEHxSmsxNjViaB?= M4r4[olvcGmkaYTzJGFx\Wyrbj3pcoR2[2WmIIDoc5NxcG:{eXzheIlwdiCxZjDFdosh[W6mIFHreC=> MnjGNlQzOjd7MUi=
CRL-2302 M{PsVmZ2dmO2aX;uJGF{e2G7 M1LRUlIxKM7:TR?= MX:wMlUhcA>? NI[4XGZqdmirYnn0d{BCeGWuaX6tbY5lfWOnZDDwbI9{eGixconsZZRqd25ib3[gSZJsKGGwZDDBb5Q> NHvHNVAzPDJ{N{mxPC=>
MCF-7 MX\GeY5kfGmxbjDBd5NigQ>? NFzlfJMzOCEQvF2= M{nVN|EhcA>? M{\ZTYFjd2yrc3jld{BmgHC{ZYPzbY9vKG:oIIDoc5NxcG:{eXzheIVlKEWUSzDjc{11emWjdH3lcpQhf2m2aDDjc45rfWejdHW= NVXEelJIOjR{MU[yPFk>
MCF-7 NHL2XnBCeG:ydH;zbZMhSXO|YYm= NWjhPJBtOjBizszN NF36[WsyKGh? MYDpcoNz\WG|ZYOgZ4F{eGG|ZT25JIVvgnmvZTDhZ5Rqfmm2eR?= MY[yOFIyPjJ6OR?=
DLD-1  NF3DV2lHfW6ldHnvckBCe3OjeR?= NIjzNGEzOMLizszN Mn\XOFghcA>? NV\pb2lWemWmdXPld{B1cGViQl7JVFMh\XiycnXzd4lwdiCycnWteJJm[XSnZDD3bZRpKDVvYYrhMYRE M4LCZlI1OjFzNUix
HT-29 NVvtZXMxTnWwY4Tpc44hSXO|YYm= NVy0OZU6OjEEoN88US=> NFrre5Y1QCCq NUXRWIZ1emWmdXPld{B1cGViQl7JVFMh\XiycnXzd4lwdiCycnWteJJm[XSnZDD3bZRpKDVvYYrhMYRE MUmyOFIyOTV6MR?=
7402 M4KyUWFxd3C2b4Ppd{BCe3OjeR?= NGHKdJg{OCEQvF2= NIW3dZU2KGR? NYnDUYl2\GWlcnXhd4V{KGOnbHygdJJwdGmoZYLheIlwdg>? M3LlZlI1OjFzMkWz
7721 MYjBdI9xfG:|aYOgRZN{[Xl? MnvXN|Ah|ryP M4rub|Uh\A>? NV[3bphm\GWlcnXhd4V{KGOnbHygdJJwdGmoZYLheIlwdg>? M{Pjd|I1OjFzMkWz
SGC7901  M2KzNWFxd3C2b4Ppd{BCe3OjeR?= MW[1NOKh|ryP NGq3ZmQzPC92OD:3NkBp M3jBfmROW09? MWjpcoR2[2W|IHHwc5B1d3OrczDjc41jcW6nZDD3bZRpKEqDS{Kgd4hTVkF? NV3nVo42OjRzN{iyOFA>
SMMC7721 MmixSpVv[3Srb36gRZN{[Xl? Mk\NNlUwPTBizszN NGjiNZAzPCCq NHL3ZYp{fXCycnXzd4V{KHSqZTDlfJBz\XO|aX;uJI9nKHBvQXv0JI9zKHBvRWLLNU8zyqB? MYeyOFE3QDB3Nh?=
MCF-7 Mlq3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX6xNEDPxE1? Mnf6OFhp MVrEUXNQ NYjPfY1VemW4ZYLz[ZMhSk6ILXnu[JVk\WRiY3XscEBkgWOuZTDhdpJme3R? MmHzNlQyPjN2MES=
Caco-2 M3mwS2Z2dmO2aX;uJGF{e2G7 MYm1NOKh|ryP NYjOOIsxPDiq NX;HSIE6TE2VTx?= M4O5UIVvcGGwY3XzJJRp\SCvUl7BJIxmfmWuczDv[uKhW0OQTkHBMGZZYUR|LNMgUGNVNMLiTF;YMOKhUEmIM1GsxsBbTzF4LNMgVGRGPkIEoHHu[OKhVEeDTGOxOuKh\2WwZYRCpINwNXS{ZXH0[YQhf2m2aDDE[Zg> M4[5VFI1OTZzNkm1
HAECs M4G5OmZ2dmO2aX;uJGF{e2G7 MkToNVAh|ryP MkfTNUBp MnSxxsBifHSnboXheIV{KFSQRj5OtU1{fGmvdXzheIVlKEmFQV2tNUBidmRiVlPBUU0yKGW6cILld5Nqd25? MYGyOFE{PDZ3Nx?=
Ca9-22 NH3oSYRHfW6ldHnvckBCe3OjeR?= MYGzJO69VQ>? NWjmc2RpOSCq NVT1OVh1[WKxbHnzbIV{KHSqZTDhZoltcXS7IH;mJGhjWiC2bzDpcoR2[2ViSVytPEBxem:mdXP0bY9v M{fvTVI1OTJ4NUOy
Ca9-22 NUXKRZMxTnWwY4Tpc44hSXO|YYm= NYXV[I1ROyEQvF2= MX2xM|IhcA>? NGDpTYpz\WS3Y3XzJGhjWi2rbnT1Z4VlKEGWRj2yJJBpd3OyaH;yfYxifGmxbh?= NHfQfJAzPDF{NkWzNi=>
AGS MmLvSpVv[3Srb36gRZN{[Xl? MUOxNEDPxE4EoB?= MWGwMlUhcA>? NYnSNpZpcW6qaXLpeJMhfGinIIXwdoVofWyjdHnvckBw\iC2aHWgTWwuQCCpZX7l MYCyOFExPjF4Nh?=
Caco-2  MkPSRZBweHSxc3nzJGF{e2G7 NYTZW|F6OTEEoN88US=> MojmNlTDqGh? M3n1eIRm[3KnYYPld{Bk\WyuIHHwc5B1d3OrczDpcoR2[2WmIHL5JFUuTlV? NHOxepozPDB7NUi2Ny=>
HCT-8 NIraRmtCeG:ydH;zbZMhSXO|YYm= NXrIOY1[OTEEoN88US=> Mn62NlTDqGh? NWPZU2tP\GWlcnXhd4V{KGOnbHygZZBweHSxc3nzJIlv\HWlZXSgZpkhPS2IVR?= MXyyOFA6PTh4Mx?=
A549 NF75PZpHfW6ldHnvckBCe3OjeR?= MnrFOVDDqM7:TR?= NV3Lb3ptOiCq MoH0Zoxw[2u|IFXST{BxcG:|cHjvdplt[XSrb36gcYVlcWG2ZXSgZpkhOSx{LV7R NYi2UWJrOjRyNke3Nlc>
HPMC M2rUN2Z2dmO2aX;uJGF{e2G7 MmrjNVDDqM7:TR?= M2X6eVQ5KGh? NYfIZWtIemW4ZYLz[ZMhfGinIHPoZY5o\XNiaX6gZ4VtdCCvb4LwbI9td2e7IHnu[JVk\WRiYomgTGdRTFN? NVTyZnA{OjRyNEK4N|g>
HPMC NGrrWHNCeG:ydH;zbZMhSXO|YYm= MYmxNOKh|ryP MmLBNlTDqGh? MYry[ZZmenOnczDk[YNz\WG|ZTDpckBk\WyuII\pZYJqdGm2eTDpcoR2[2WmIHL5JGhIWESV MWOyOFA1Ojh|OB?=
MGC803  MlOwRZBweHSxc3nzJGF{e2G7 M3rEZ|IxyqEQvF2= Ml\TNUBp M1jSW4lvcGmkaYTzJIFxd3C2b4Ppd{BqdmS3Y3XkJIJ6KEmITj5OteKh[W6mIEZihNIuTE[XUh?= M376flI1ODJ5N{Ww
SGC7901 NGmybFFCeG:ydH;zbZMhSXO|YYm= MX[yNOKh|ryP Mnr0NUBp M3zWZ4lvcGmkaYTzJIFxd3C2b4Ppd{BqdmS3Y3XkJIJ6KEmITj5OteKh[W6mIEZihNIuTE[XUh?= M{D5U|I1ODJ5N{Ww
COLO205 MknFRZBweHSxc3nzJGF{e2G7 NEjPcVgyOC9{MD:0NEDPxE1? NWLNWYM5OjRiaB?= MkjEbY5lfWOnczDEUmEhdGGmZHXyJIZwem2jdHnvci=> MYSyOFAyQTFyOB?=
G292  MUjBdI9xfG:|aYOgRZN{[Xl? MVWzNOKh|ryP MlPoNkBp MU\y[ZN1d3KnczDjZZB{[WmlaX6tbY5lfWOnZDDj[YxtKGSnYYTo NUHqVm9{OjRyMUK5N|A>
BxPC-3 NVfOVZdqTnWwY4Tpc44hSXO|YYm= MYKxNEDPxE4EoB?= NYnHZWwzPiCq MnnLbY5kemWjc3WgcYlTNTF2MzDlfJBz\XO|aX;u NF31ZoczOzl5M{exNC=>
HPAF-II MnO3SpVv[3Srb36gRZN{[Xl? MVixNEDPxE4EoB?= NF;Rcnc3KGh? NVPOXJV{cW6lcnXhd4UhdWmULUG0N{BmgHC{ZYPzbY9v M4r5O|I{QTd|N{Gw
HL-60 NXXOT3pqSXCxcITvd4l{KEG|c3H5 MnzxOVDDqM7:TR?= MUCxJIg> NHnHbGxz\XOldXXzJGJCOTR3IH3l[IlifGWmIHHwc5B1d3Orcx?= MoTjNlM6PDh5NUG=
HepG2 NImwOIFHfW6ldHnvckBCe3OjeR?= NHW1UFA1OCEQvF2= MXi2M|EzKGh? MVfpcohq[mm2czD0bIUhcW6lcnXhd4Uhd2ZicD3FVmsyKGGwZDDwMYMuUnWwIIDyc5RmcW5iZYjwdoV{e2mxbjDifUBRVA>? MmrxNlM6PDJ6NUG=
HUVECs NWnGU4EyTnWwY4Tpc44hSXO|YYm= M2PKbFI2KM7:TR?= MUKxJIg> MnG2bY5kemWjc3WgUmYu|rqEIIC2OUBvfWOuZXHyJJRz[W6|bH;jZZRqd25? MX:yN|kxOTByOB?=
LNCaP  Mmi5SpVv[3Srb36gRZN{[Xl? NGL6VpIyOCEQvF5CpC=> NYfy[lRUOSCq MYrk[YNz\WG|ZYOgeIhmKEWJRjD1dJJm\3WuYYTl[EBxNVmELUG= NFv1XpczOzh|OEOxPC=>
HL60  Mki0SpVv[3Srb36gRZN{[Xl? MkXrNlDDqM7:TR?= Mmr4O|IhcA>? M2rCdWROW09? MkTubY5pcWKrdIOg[IF{[XSrbnniMYlv\HWlZXSgR2QyOWJiZYjwdoV{e2mxbh?= MkLINlM5OjV3OEW=
NB4  MlXvSpVv[3Srb36gRZN{[Xl? MU[xNEDPxE4EoB?= MnzSO|IhcA>? M2jIemROW09? MVPpcohq[mm2czDkZZNifGmwaXKtbY5lfWOnZDDDSFEy[iCneIDy[ZN{cW:w NGLn[lQzOzh{NUW4OS=>
EPOR/CR3 MXPGeY5kfGmxbjDBd5NigQ>? MVO1NOKh|ryP M4HtVVMhcA>? NGrvNFhz\WS3Y3XzJGVRVyCjbnSvc5IhUUxvMz3pcoR2[2WmIITo[UB1gXKxc3nu[UBxcG:|cHjvdplt[XSrb39CpC=> M1fldFI{QDJyN{Ox
HUASMCs Mn\MSpVv[3Srb36gRZN{[Xl? NFLle2gyOCEQvF5CpC=> NYHHW2NVOjRiaB?= NVzUepk2\GmvaX7pd4hmeyCDbnegTWku[2G3c3XkJHNQS1N|IH3SUmEh[W6mIIDyc5RmcW5iZYjwdoV{e2mxbtMg NIf3RYMzOzhzNkS2PC=>
HUASMCs MVLGeY5kfGmxbjDBd5NigQ>? NIq4em4yOCEQvF5CpC=> NVfQRlB7OjRiaB?= NUD0bWZUcW6qaXLpeJMhSW6pIFnJMYlv\HWlZXSgSXJMOS9{IIDoc5NxcG:{eXzheIlwdiCuZY\lcC=> NEewR4MzOzhzNkS2PC=>
SGC7901 MVXGeY5kfGmxbjDBd5NigQ>? NU\S[XVTOTBizszNxsA> MXqyOEBp MorvbY5pcWKrdIOgeIhmKGW6cILld5Nqd25ib3[gdIhwe3Cqb4L5cIF1\WRiRWLLNU8z NHPWdpozOzd7MkW4PC=>
MKN45 MnfuSpVv[3Srb36gRZN{[Xl? MWGxNEDPxE4EoB?= M2PCWlI1KGh? MUXpcohq[mm2czD0bIUh\XiycnXzd4lwdiCxZjDwbI9{eGixconsZZRm\CCHUluxM|I> MUmyN|c6OjV6OB?=
SGC7901 NH;tUnNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlrXNVAh|ryPwrC= MoDPNlQwPDhxN{KgbC=> MXzpcohq[mm2czDj[YxtKGe{b4f0bEBkdy22cnXheIVlKHerdHigSGFRXA>? NHzRb28zOzd7MkW4PC=>
MKN45 NGG5ZoxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkfKNVAh|ryPwrC= NIfZb2ozPC92OD:3NkBp M1nBS4lvcGmkaYTzJINmdGxiZ4Lve5RpKGOxLYTy[YF1\WRid3n0bEBFSVCW NXfzfIdvOjN5OUK1PFg>
SGC7901 MoC3RZBweHSxc3nzJGF{e2G7 MY[xNEDPxE4EoB?= MXKyOEBp MlPhbY5kemWjc3XzJJRp\SCGQWDUMYlv\HWlZXSgZ4VtdCCjcH;weI9{cXN? M3zVc|I{Pzl{NUi4
MKN45 NHv0Z3JCeG:ydH;zbZMhSXO|YYm= NHfKS|EyOCEQvF5CpC=> NIjWVYgzPCCq M37CeIlv[3KnYYPld{B1cGViRFHQWE1qdmS3Y3XkJINmdGxiYYDvdJRwe2m| MnTCNlM4QTJ3OEi=
BxPC-3 cells M1XsVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2DBVlIxyqEQvF2= MW[wMlUhcA>? NHLOVmpqdmirYnn0d{BXTUeILVGtdoVofWyjdHXkJGhWXkWFIHfyc5d1cCCjbnSgeJVj\SCob4LtZZRqd25iaX7keYNm\CCkeTDQRXIuOiCDUB?= MVOyN|c3PDB2Nh?=
NB4  NWTG[|NZSXCxcITvd4l{KEG|c3H5 M1njR|ExNzJyL{[wJO69VQ>? M4KwXlEvPSCq MWTEUXNQ M3Xn[IRm[3KnYYPld{Bk\WyuII\pZYJqdGm2eTDjc{11emWjdHXkJJdqfGhiUHHjcIl1[XinbB?= MYOyN|c{PTV2MR?=
HepG2  NWHjfVFiTnWwY4Tpc44hSXO|YYm= NWPxXVZSOjEEoN88US=> MYWyOEBp M1K1RYlvcGmkaYTzJJRp\SCKTz2xJJBzd3SnaX6g[ZhxemW|c3nvckBkdy22cnXheIVlKHerdHigcYV1\m:{bXnu MYKyN|cxPzZyOR?=
HUVECs NEHWe5dCeG:ydH;zbZMhSXO|YYm= MYmyM|Qh|ryP M2\rXFI1NzR6IHi= NXjVOmtycW6mdXPld{Bk\WyuIHTlZZRp M{TrN|I{PzB5NUKw
KG-1  NInuT3JCeG:ydH;zbZMhSXO|YYm= M{\DcVIxyqEQvF2= MkixNVIhcA>? M324coVvcGGwY3XzJINmdGxiYYDvdJRwe2m|IHnu[JVk\WRiYomgV|E> MWGyN|cxPjZ7MR?=
AML 1# MV7BdI9xfG:|aYOgRZN{[Xl? M{jJWlIxyqEQvF2= M1m2ZVEzKGh? MUDlcohidmOnczDj[YxtKGGyb4D0c5NqeyCrbnT1Z4VlKGK7IGOx MmjzNlM4ODZ4OUG=
A2780  M2HYcWZ2dmO2aX;uJGF{e2G7 M4LSdFIxyqEQvF2= NFPndIsyKGh? NF;JNnRjdG:la4OgSHRETC2rbnT1Z4VlKESUNTDlfJBz\XO|aX;u MV:yN|Y6Pjh4Mh?=

... Click to View More Cell Line Experimental Data

体内研究 在大脑缺血前30分钟用PD98059处理小鼠可以明显减轻伤害, 使脑梗塞的体积减小[4]。基于胰腺的湿重和组织学研究发现,提前30分钟用PD98059预处理 (10 mg/kg 静脉注射) 然后每小时注射一次蛙皮素连续三次的小鼠可以明显改善蛙皮素诱导的急性胰腺炎[7]。卡拉胶损伤一小时后用PD98059 (10 mg/kg) 对小鼠进行治疗可以发现与炎症相关的所有指标均有所下降[11]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

激酶实验:[1]
+ 展开

体外MEK激酶活性测定:

在含有44-kDa GST-MAPK 或者45-kDa GST-MEK1的体系中检测32P被掺入蛋白 MBP中的情况。 反应体系50 μL ,含有50 mM Tris, pH 7.4/10 mM MgCl2/2 mM EGTA/10 μM [γ-32P]ATP, 加入10 μg GST-MEK1, 0.5 μg GST-MAPK和 40 μg MBP。30°C 孵育15 分钟, 加入Laemmli SDS 样品缓冲液终止反应。磷酸化的MBP 进行10% SDS-PAGE分析
细胞实验:[1]
+ 展开
  • Cell lines: K-Balb, KNRK, v-raf-3Y1, SRA/3Y1, EGFR/3T3, 和K562
  • Concentrations: 溶于DMSO, 终浓度~100 μM
  • Incubation Time: 3 天, 或者7-10天
  • Method: 细胞按10,000-20,000个/mL的密度接种在多孔平板中进行单层生长。48小时后把不同浓度的PD98059 加到细胞培养基孵育3天。 然后通过胰酶将细胞从平板中消化下来并用Coulter 计数器计数。 将细胞按5,000-10,000每皿的浓度接种在35 mm的培养皿中,培养基中含有0.3% 的琼脂和期望浓度的PD98059,让细胞在软琼脂上生长.经过7-10天的生长, 可以借助解剖显微镜将可见的菌落数出来。
    (Only for Reference)
动物实验:[7]
+ 展开
  • Animal Models: 患有急性胰腺炎的雄性Sprague–Dawley 大鼠
  • Formulation: 溶于 DMSO, 用生理盐水稀释
  • Dosages: 10 mg/kg
  • Administration: 静脉注射
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 14 mg/mL warmed (52.37 mM)
Water Insoluble
Ethanol Insoluble
体内 从左到右依次将纯溶剂加入产品,现配现用(数据来自Selleck实验检测而非文献):
4% DMSO+30% PEG 300+5% Tween 80+ddH2O
1mg/mL

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 267.28
化学式

C16H13NO3

CAS号 167869-21-8
稳定性 powder
in solvent
别名 N/A

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • 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):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

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操作手册

如果有其他问题,请给我们留言。

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常见问题及建议解决方法

  • 问题 1:

    How to formulate this inhibitor for i.p. injection?

  • 回答:

    You can prepare the stock by the vehicle 30% PEG400/0.5% Tween80/5% Propylene glycol, 0.5% CMC.

MEK Signaling Pathway Map

MEK Inhibitors with Unique Features

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID