Panobinostat (LBH589)

製品コードS1030 別名:NVP-LBH589

Panobinostat (LBH589)化学構造

分子量(MW):349.43

Panobinostat (LBH589) is a novel broad-spectrum HDAC inhibitor with IC50 of 5 nM in a cell-free assay. Phase 3.

サイズ 価格(税別)  
JPY 14940.00
JPY 44820.00
JPY 111220.00

文献中Selleckの製品使用例(52)

カスタマーフィードバック(12)

  • (G) A375 parental and BRAFi-resistant ex vivo clones were treated with a panel of HDACi (1 μM vorinostat, 0.5 μM belinostat, and 6 nM panobinostat) in single treatment or in combination with 1 μM vemurafenib in a long-term colony formation assay.

    Cell, 2018, 173(6):1413-1425. Panobinostat (LBH589) purchased from Selleck.

    LSD1 and HDAC inhibitors exhibit synergistic growth inhibition. Cells were simultaneously treated with pargyline or HDAC inhibitors for 48 h.

     

     

    Breast Cancer Res Treat 2012 131, 777-789. Panobinostat (LBH589) purchased from Selleck.

  • Using CRISPR-Cas9 technology, ERα was silenced at the genomic level in ECC1 cells. Ishikawa, parental ECC1 cells and individual ESR1 KO ECC1 clones were treated with 20 nM LBH589 for 24 hr. Expression of ERα, PR, FOXO1, and Myc were evaluated by Western blotting. β-actin serves as a loading control.

    PLoS One, 2016, 11(2):e0148912.. Panobinostat (LBH589) purchased from Selleck.

    HDACIs That Simultaneously Inhibit HDACs 1 and 6 Showed Greater Antileukemic Activities than HDACIs that Don’t at Cmax Concentrations. THP-1 cells were treated with LBH-589, PXD101, SAHA, VPA, MS-275 and MGCD0103 at Cmax concentrations for 3 h and 24 h, respectively. The cells post 3 h treatments were washed three times with complete medium and divided into two halves. One half of the cells was resuspended in complete media and cultured for up to 24 h to determine the effects of the 3 h treatments on cell proliferation and apoptosis. The other half of the cells was used to prepare whole cell lysates. Whole cell lysates from the 3 h and 24 h treatments were extracted and subjected to Western blots probed by anti-ac-tubulin or –b-actin antibody (panels A&B), or subjected to HDAC1 enzymatic assays post IP as described in the Materials and Methods (Panels C&D). The effects of the 3 h and 24 h HDACI treatments on cell proliferation, as reflected by percent decrease of live cells relative to untreated cells (panel E), and apoptosis (panel F) were determined by flow cytometry analysis as described in the Materials and Methods.

     

     

    PLoS One 2011 6, e17138. Panobinostat (LBH589) purchased from Selleck.

  • Induction of DNA Damage and Bim Is Critical for HDACI-Induced Apoptosis in Pediatric AML Cells. THP-1 cells were treated with the HDACIs at Cmax concentrations for 3 (panel A) and 24 h (panel B), respectively. Whole cell lysates were extracted and subjected to Western blots probed by anti-p21, -c-Myc, -cH2AX, -Bim, or -b-actin antibody.

     

     

    PLoS One 2011 6, e17138. Panobinostat (LBH589) purchased from Selleck.

    Cell death induction by LBH589 as a single agent was detected in control or MTDH knockdown Hec50co cells. After 3 days, cell death was determined by the WST-1 method.

    PLoS One 2011 6, e20920. Panobinostat (LBH589) purchased from Selleck.

  • Expression of pro-/anti-apoptosis genes. Control or MTDH knockdown Hec50co cells were treated for 24 hours with vehicle control, 20 nM LBH589, 25 ng/ml TRAIL or LBH589 and TRAIL at the concentrations noted. Lysates were collected. Expression of DR4, DR5, and apoptosis related caspase-3, caspase-8, PARP-1, BID, FLIP, XIAP, Bim, MCL-1 and BCL-XL was analyzed by Western blotting.

    PLoS One 2011 6, e20920. Panobinostat (LBH589) purchased from Selleck.

    p53(+/+) and (/) HCT116 cells were treated with TSA (1–5 lM),LBH589 (2–5 lM), valproate (2.5–5 mM), MS-275 (20 lM) and sodium butyrate (2 mM). TAp63 expression was compared in both cell lines after 24 h of treatment. Consistent with the above data, all HDAC inhibitors failed to induce significant levels of TAp63 in p53(/) HCT116 cells.

     

     

    Biochem Bioph Res Co 2009 391, 1748-1751. Panobinostat (LBH589) purchased from Selleck.

  • Effect of panobinostat on the viability of cervical cancer cells. HeLa (A) and SiHa (B) cells were treated with increasing concentrations of panobinostat for 24, 48 and 72 h. Cell viability was determined by MTT assay. The results are presented as percentage; calculated from the reduction in cell viability at a given concentration of drug compared to the untreated control (untreated control being 100%). The IC5072h values were calculated from sigmoidal dose-response curves generated in Prism 5.0 (GraphPad). (C) Cytotoxic effects of panobinostat on HeLa and SiHa cells measured at 72 h and expressed as% cell death. Each value is the mean ± SD of three independent experiments performed in triplicates.

    Biomed Pharmacother, 2016, 84:1393-1405. Panobinostat (LBH589) purchased from Selleck.

    Western blot analysis of Acetyl-H3 and H3. 0-10μM Panobinostat was added.

    Dr.Zhang of Tianjin Medical University. Panobinostat (LBH589) purchased from Selleck.

  • HDAC inhibitors induce p63a expression (A) HCT116 cells were treated with TSA (1 lM), LBH589 (2 lM), valproate (2.5 mM), MS-275 (20 lM) and sodium butyrate(2 mM) for 24 h. Expression of p63 was assessed by Western blotting with the H129 pan-anti-p63 antibody. Although TSA and LBH589 induced p63 efficiently, valproate, MS-275 and sodium butyrate were much less efficient. The lower panel shows the actin loading control. Arrow indicates TAp63. (B) The HDAC inhibitors used in this study are shown, grouped according to their structure and with their HDAC specificity. The efficiency of TAp63 expression is shown in the last column.

     

     

    Dr. Berna S. Sayan of Leicester University. Panobinostat (LBH589) purchased from Selleck.

    U266 and KMS-11 were treated with 20 nM panobinostat for 48 h followed by Western blot analysis. Actin served as a loading control. Nine (U266) and 3 (KMS-11) biologically independent experiments were performed. To determine the expression of PPP3CA mRNA in treated cells for 24 h, we performed relative quantification real-time PCR (n = 6). Four (U266) and 2 (KMS-11) biologically independent experiments were performed.

    JCI Insight, 2016, 1(5):e85061. Panobinostat (LBH589) purchased from Selleck.

製品安全説明書

HDAC阻害剤の選択性比較

生物活性

製品説明 Panobinostat (LBH589) is a novel broad-spectrum HDAC inhibitor with IC50 of 5 nM in a cell-free assay. Phase 3.
ターゲット
HDAC (MOLT-4 cells) [1] HDAC (Reh cells) [1]
5 nM 20 nM
体外試験

LBH589 induces apoptosis among MOLT-4 and Reh cells in a time- and dose-dependent manner. Moreover, LBH589 is more potent in MOLT-4 than in Reh cells. LBH589 markedly prevents the growth of both MOLT-4 and Reh cells in a dose-dependent manner at 48 hours. LBH589 treatment causes a 2- to 3-fold increase in the number of cells in the G2/M phase of the cell cycle compared with the control cells. LBH589 is associated with induction of histone H3K9 and histone H4K8 acetylation as well as decreasing levels of c-Myc expression in a dose-dependent manner. LBH589 treatment also increases the levels of p21 expression. LBH589 treatment also decreases the levels of c-Myc after an initial increase at the lowest dose (10 nM) in Reh cells. In addition, LBH589 gives rise to substantial increases in mRNA levels of proapoptosis and DNA repair genes. LBH589 induces increased levels of acetylated histone H3 and H4 at the GADD45G promoter. [1] Besides, LBH589 inhibits growth of non small cell lung cancer cell lines (such as human H1299, L55 and A549 with IC50 of 5 nM, 11 nM and 30 nM, respectively), mesothelioma (such as human OK-6 and Ok-5 with IC50 of 5 nM and 7 nM, respectively) and small cell lung cancer cell lines (such as human RG-1 and LD-T with IC50 of 4 nM and 5 nM, respectively). [2]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HT29 MnGwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUC5OYpoOC1zMDFOwG0> NXPIZZFoOC12IHS= M3rycYlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHLveIghfGmvZT2gZY5lKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= Ml\CNlY4ODJ5OES=
HepG2 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlHnNE0yOCEQvF2= NF6wT2YxNTRiZB?= MUfpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCkb4ToJJRqdWVvIHHu[EBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MXmyOlcxOjd6NB?=
HT29 NXXBPWZDTnWwY4Tpc44hSXO|YYm= NWi0[|lMPTEEoH7N Mn3xNlQuPzJiaB?= M1OxRolv\HWlZXSgZYN1cX[jdHnvckBw\iClYYPwZZNmKDNiYX\0[ZIhPDkEoHlCpC=> M{e5XVI3PzB{N{i0
HepG2 NF;3cYdHfW6ldHnvckBCe3OjeR?= MoD2OVDDqG6P M{\XblI1NTd{IHi= NFPHToxqdmS3Y3XkJIFkfGm4YYTpc44hd2ZiY3HzdIF{\SB|IHHmeIVzKDJ2wrDoxsA> MkPUNlY4ODJ5OES=
HCC827 Mn75S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUnIfmFJPS95LkWvNVAhdk1? M1vqfVczyqCq M1fxSGROW09? NIHq[oFmdmijbnPld{B1cGViYX70bZBzd2yrZnXyZZRqfmViZX\m[YN1KG:oIHXycI91cW6rYh?= M3fUSlI3Pjd3NEi0
A549  MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoLtNVAwOTVxMkCgcm0> NH7HPFU4OsLiaB?= NEO5c4FFVVOR MmHY[Y5p[W6lZYOgeIhmKGGwdHnwdo9tcW[ncnH0bZZmKGWoZnXjeEBw\iCncnzveIlvcWJ? Mln1NlY3PzV2OES=
NCI-H460  M3y1XWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV[xNE8zOC9|MDDuUS=> Mle4O|LDqGh? MYfEUXNQ NWf6b5hE\W6qYX7j[ZMhfGinIHHueIlxem:uaX\ldoF1cX[nIHXm[oVkfCCxZjDldoxwfGmwaXK= MlTrNlY3PzV2OES=
J89GFP MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWrVZVdZTE2VT9Mg MXzFR|UxRTR7Lki1JOKyKDF{Lk[1JI5O NXfMUWk5OjZ3NkO1Olg>
THP89GFP MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4faOmROW00EoB?= NFj3XG1GSzVyPUG5MlM1KMLzIE[uOFMhdk1? NUTxU3RZOjZ3NkO1Olg>
SK-NEP-1 M4DyW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYqwMlAy6oDVMUCuNEDPxE1? M3Sw[VI1KGh? MnTRSG1UV8Li NX2yS5F4UUN3ME23Ok4{PCCwTR?= MVyyOlE4PjJzOR?=
G401 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXuwMlAy6oDVMUCuNEDPxE1? NIC0cHQzPCCq MlPWSG1UV8Li M4ezbmlEPTB;MUSzMlAzKG6P NH;we44zPjF5NkKxPS=>
SK-NEP-1 M{T3NmNmdGxiVnnhZoltcXS7IFHzd4F6 MnvaOVAhdk1? MUWx5qCUPCCm Mn3XSG1UV8Li NX\p[Is4emWmdXPld{Bk\WyuIIP1dpZqfmGuIHnuJIEhfGmvZTDk[ZBmdmSnboSgcYFvdmW{ M2Gwe|I3OTd4MkG5
G401 MXXD[YxtKF[rYXLpcIl1gSCDc4PhfS=> M17CVlUxKG6P NFPyOlgy6oDVNDDk NImzcVFFVVORwrC= MWPy[YR2[2W|IHPlcIwhe3W{dnn2ZYwhcW5iYTD0bY1mKGSncHXu[IVvfCCvYX7u[ZI> NGnTXlczPjF5NkKxPS=>
SK-NEP-1 MVrBdI9xfG:|aYOgRZN{[Xl? NX7oW5FZPTBxMUCwJI5O M{XQXlI1KGh? MmfYSG1UV8Li MXHpcoR2[2W|IHPlcIwh[XCxcITvd4l{KGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz M2X2clI3OTd4MkG5
G401 M3Lx[WFxd3C2b4Ppd{BCe3OjeR?= NUjJPId5PTBxMUCwJI5O NXnuOHZJOjRiaB?= MlTsSG1UV8Li NXy2TI54cW6mdXPld{Bk\WyuIHHwc5B1d3OrczDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= NXv1PIVTOjZzN{[yNVk>
SK-NEP-1 M4fqOWZ2dmO2aX;uJGF{e2G7 M{PVV|UxNzFyMDDuUS=> NFzSTXYzPCCq MojwSG1UV8Li NGjOZ|d{cG:5czD0bIUhcW6mdXP0bY9vKG:oIFTORUBnemGpbXXueIF1cW:w NGDsOmEzPjF5NkKxPS=>
G401 MYjGeY5kfGmxbjDBd5NigQ>? MmfCOVAwOTByIH7N NWraWIRoOjRiaB?= M1i5PGROW00EoB?= M4C0bZNpd3e|IITo[UBqdmS3Y4Tpc44hd2ZiRF7BJIZz[WevZX70ZZRqd25? MUeyOlE4PjJzOR?=
SK-NEP-1 M4nvd2Z2dmO2aX;uJGF{e2G7 MYm1NE8yODBibl2= NIDST2EzPCCq MVrEUXNQyqB? M{LUeolv\HWlZYOgZ4VtdCCleXPs[UBlcXOxcnTlduKh Mlf1NlYyPzZ{MUm=
G401 M4TUfGZ2dmO2aX;uJGF{e2G7 NVexeHh{PTBxMUCwJI5O Mlq0NlQhcA>? M2LwcWROW00EoB?= MUHpcoR2[2W|IHPlcIwh[3mlbHWg[Il{d3KmZYNCpC=> NYjEOZdzOjZzN{[yNVk>
RPMI 8226 M1vnW2NmdGxiU4Xyeol3[WxiQYPzZZk> Mn\yNk81NzZibl2= MkfZOFjjiImq MmHwbY5lfWOnczDhJJNq\26rZnnjZY51KGSnY4LlZZNmKGmwIITo[UBk\WyuIHfyc5d1cA>? NYPG[IprOjZyMECyPVI>
OPM2 M{Lx[GNmdGxiU4Xyeol3[WxiQYPzZZk> MoGwNk81NzZibl2= MojHOFjjiImq MVzpcoR2[2W|IHGgd4lodmmoaXPhcpQh\GWlcnXhd4UhcW5idHjlJINmdGxiZ4Lve5Rp MnzENlYxODB{OUK=
U266 NF;5XohE\WyuIGP1dpZqfmGuIFHzd4F6 NG[3bGozNzRxNjDuUS=> Mn\YOFjjiImq NID0c4FqdmS3Y3XzJIEhe2mpbnnmbYNidnRiZHXjdoVie2ViaX6geIhmKGOnbHyg[5Jwf3Sq MUOyOlAxODJ7Mh?=
H929 NWP0cGcyS2WubDDTeZJ3cX[jbDDBd5NigQ>? M3rOU|IwPC94IH7N NXjveFRHPDkkgJno MUnpcoR2[2W|IHGgd4lodmmoaXPhcpQh\GWlcnXhd4UhcW5idHjlJINmdGxiZ4Lve5Rp M{X5XVI3ODByMkmy
RPMI 8226  NX;BTm9VSXCxcITvd4l{KEG|c3H5 NGjtUVc16oDLbl2= M3nZeFI1NzR6IHi= NGjvbYFqdmS3Y3XzJINmdGxiYYDvdJRwe2m|IHnuJIEhfGmvZT3k[ZBmdmSnboSgcYFvdmW{ NYfKO2t2OjZyMECyPVI>
HCC827 MlHnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIPMVnUyOCCwTR?= NY\hO2RTPDhiaB?= NVnYR|VsTE2VTx?= MU\lcohidmOnczDjbZNxdGG2aX6gd4Vve2m2aY\peJnDqA>? M37ObVI2QTR2NkG3
NCI-H23 Mn6yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFTWc3EyOCCwTR?= NXO3cm03PDhiaB?= MWfEUXNQ NILMc|RmdmijbnPld{BkcXOybHH0bY4he2Wwc3n0bZZqfHoEoB?= MVyyOVk1PDZzNx?=
AML3 MVjGeY5kfGmxbjDBd5NigQ>? MnrNNE0yKM7:TR?= NWSzXZFqOjUEoHi= MXfpcoR2[2W|IFTORUBnemGpbXXueIF1cW:wwrDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= M3f1eFI2PjF{OUSx
ML-1 NUPpT2lLTnWwY4Tpc44hSXO|YYm= NEXkfGQxNTFizszN MknpNlTDqGh? NHXMVo1qdmS3Y3XzJGRPSSCocnHncYVvfGG2aX;uxsBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MWWyOVYyOjl2MR?=
RPMI-8226vr10  NIfxR2VHfW6ldHnvckBCe3OjeR?= NWr0W4M5OC1zIN88US=> NIHVbpEzPMLiaB?= M2LrN4lv\HWlZYOgSG5CKG[{YXft[Y51[XSrb39CpIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy M{XneVI2PjF{OUSx
ML-1 M3X5R2Z2dmO2aX;uJGF{e2G7 NViwcVI6OSEQvF2= M4TZXVI1yqCq MW\pcoNz\WG|ZYOgZ4F{eGG|ZT2zJIFkfGm4aYT5JFQu\m:uZB?= MXSyOVYyOjl2MR?=
RPMI-8226vr10  NF3QTZVHfW6ldHnvckBCe3OjeR?= MlnlNUDPxE1? Mmj5NlTDqGh? NF7hZ4VqdmO{ZXHz[ZMh[2G|cHHz[U0{KGGldHn2bZR6KDJwNT3mc4xl M{HBXVI2PjF{OUSx
SK-N-BE (2) NX\NS3ZXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGjNWGkzPOLCiXi= M2Ps[mlEPTB;MUC0MlDjiIoEsfMAjVcvQCCwTR?= NF3ydpkzPTNyOEmxOi=>
SK-N-BE (2), PAN  MK MlHLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkLhNlTjiImq MnTCTWM2OD1zMESuNQKBkcLz4pEJO{45KG6P NHXtfm8zPTNyOEmxOi=>
SK-N-BE (2), MK  PAN MoraS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NW\T[5ZzOjUkgJno MoGyTWM2OD1|OEKuNQKBkcLz4pEJOFMvOiCwTR?= MnmxNlU{ODh7MU[=
SK-N-AS NEHuZVVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUiyOQKBkWh? MoPjTWM2OD1|Nz6x5qCKyrIkgJmyMlQhdk1? MmLkNlU{ODh7MU[=
SK-N-DZ M4TnWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXOyOQKBkWh? Ml3RTWM2OD1zNz6x5qCKyrIkgJmwMlQhdk1? NEPheVEzPTNyOEmxOi=>
Caki-1 M3;yTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3L4blExNzJ3L{WwJI5O MWW0PEBp Mo[xbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZIhe3mwZYLnbZN1cWOjbHz5JJdqfGhicnn0c45ifmm{ NGTMNpczPTJ5OUG5NS=>
ACHN MkL0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWqxNE8zPS93MDDuUS=> NW\kW4tPPDhiaB?= MWjpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldkB{gW6ncnfpd5Rq[2GubImge4l1cCC{aYTvcoF3cXJ? NWG2e|M4OjV{N{mxPVE>
769-P NH\u[W9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVexNE8zPS93MDDuUS=> M{DnXFQ5KGh? MnLIbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZIhe3mwZYLnbZN1cWOjbHz5JJdqfGhicnn0c45ifmm{ MnXYNlUzPzlzOUG=
786-O  MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYqxNE8zPS93MDDuUS=> Mn[3OFghcA>? NVWyS5N2cW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJic4nu[ZJocXO2aXPhcIx6KHerdHigdol1d26jdnny M3j5RVI2Ojd7MUmx
Caki-1 M2nFc2Fxd3C2b4Ppd{BCe3OjeR?= MnPpOVAhdk1? NVHDR5NLPDhiaB?= MmPObY5lfWOnczDj[YxtKGGyb4D0c5NqeyClb33ibY5m\CC{aYTvcoF3cXJ? NVHYUWNUOjV{N{mxPVE>
ACHN NVHVeIszSXCxcITvd4l{KEG|c3H5 NYrRTHVNPTBibl2= M3Pj[FQ5KGh? NF6xR2RqdmS3Y3XzJINmdGxiYYDvdJRwe2m|IHPvcYJqdmWmIILpeI9v[X[rch?= MVSyOVI4QTF7MR?=
769-P NIe0S|JCeG:ydH;zbZMhSXO|YYm= MnrBOVAhdk1? M3n1[FQ5KGh? MoHabY5lfWOnczDj[YxtKGGyb4D0c5NqeyClb33ibY5m\CC{aYTvcoF3cXJ? NY\heGg2OjV{N{mxPVE>
786-O  MV;BdI9xfG:|aYOgRZN{[Xl? MnPwOVAhdk1? M17uV|Q5KGh? MnXjbY5lfWOnczDj[YxtKGGyb4D0c5NqeyClb33ibY5m\CC{aYTvcoF3cXJ? MXOyOVI4QTF7MR?=
Caki-1 M2KyV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXmyOU82OCCwTR?= MWi0PEBp NYT4[ZF3TE2VTx?= NXfFPHdGcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJic4nu[ZJocXO2aXPhcIx6KHerdHigZo9zfGW8b33pZi=> MlyzNlUyPzZ|NUS=
ACHN M1rZRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUn2fId2OjVxNUCgcm0> NUjY[XJyPDhiaB?= NH3k[ZRFVVOR NVHBd2RKcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJic4nu[ZJocXO2aXPhcIx6KHerdHigZo9zfGW8b33pZi=> MYWyOVE4PjN3NB?=
769-P M{nZUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEDoN|czPS93MDDuUS=> MmG2OFghcA>? MUfEUXNQ NWnLcWg{cW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJic4nu[ZJocXO2aXPhcIx6KHerdHigZo9zfGW8b33pZi=> NEDTXoMzPTF5NkO1OC=>
Caki-1 MnK1R49td267IF\vdo1ifGmxbjDBd5NigQ>? M{LRNlUxKG6P NVfaUItUPy1zNDDk M1\aVmROW09? M2DtdpN2eHC{ZYPz[YQh[2:ub375JIZwem2jdHnvckB{cWewaX\pZ4FvfGy7IHPvcYJqdmWmIIfpeIghf2m2aDDic5J1\XqxbXniJOKh NIjW[o8zPTF5NkO1OC=>
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HSC4  M3n0fmFxd3C2b4Ppd{BCe3OjeR?= NE\xRWgxNTJyIH7N MnHrOFghcA>? M{DTbWROW09? MVLpcoR2[2W|IHPlcIwh[XCxcITvd4l{ NIfyepUzOzh5N{KzOS=>
HN22 NHLtUoNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFG1ZoMxNTJyIH7N M2iyflQ5KGh? MYTEUXNQ NV7I[FVVcW6mdXPld{BIOSCyaHHz[UBk\WyuIHP5Z4xmKGG{cnXzeOKh NIXMVGMzOzh5N{KzOS=>
HSC4  MmTiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGjXUVIxNTJyIH7N NXjqPYd3PDhiaB?= NUC4fpBPTE2VTx?= NXzYeodOcW6mdXPld{BIOSCyaHHz[UBk\WyuIHP5Z4xmKGG{cnXzeOKh MVWyN|g4PzJ|NR?=
HN22 MYrGeY5kfGmxbjDBd5NigQ>? NGX3UpoxNTJyIH7N M2noR|Q5KGh? NEPrNXBFVVOR MYXzeZBxemW|c3XzJHNxOSCneIDy[ZN{cW:wwrC= Moj4NlM5Pzd{M{W=
HSC4  MV\GeY5kfGmxbjDBd5NigQ>? NE\oPHAxNTJyIH7N NH;1U3I1QCCq MnyxSG1UVw>? NHTWb3V{fXCycnXzd4V{KFOyMTDlfJBz\XO|aX;uxsA> MUCyN|g4PzJ|NR?=
Cal62 NYPJNYlbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHm1VVVKSzVyPUOzJOKyKDRibl2= M{HqZlI{QDJ2ME[0
Hth7 NILRTlFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYGwTHEyUUN3ME2xOUDDuSB{IH7N NX;WelJoOjN6MkSwOlQ>
Hth83 M3PRdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYHJR|UxRTN2INMxJFUhdk1? M1i5dVI{QDJ2ME[0
C643 M{HUNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV;JR|UxRTdzINMxJFExKG6P NYLkNnFVOjN6MkSwOlQ>
SW1736 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoXETWM2OD1|NTFCtUA5KG6P MmewNlM5OjRyNkS=
T241 MmGyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXrJR|UxRTZ3INMxJFchdk1? MlXlNlM5OjRyNkS=
T351 M4q1PWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF75SnFKSzVyPUWwJOKyKDFyIH7N M2X3VVI{QDJ2ME[0
BHP2-7 M3HGN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoHGTWM2OD1|NzFCtUA3KG6P NHvoW2EzOzh{NEC2OC=>
T238 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUHlfFJ7UUN3ME2xMFUxOCEEsTCyNFAhdk1? NVSz[291OjN6MkSwOlQ>
HCT8 NXvTW|NFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4r0Z|czKGh? MnHKSG1UVw>? M4T0[WlEPTB;MUKuPgKBkcLz4pEJNU46KG6P NUXQSlhtOjN{OUmzPFg>
H630 MlH0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUHYR4lqPzJiaB?= NWnENJdbTE2VTx?= M33TVWlEPTB;MUKuOQKBkcLz4pEJN{4yKG6P M2fCXVI{Ojl7M{i4
cH630 5-FU-res NEjYdHVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVu3NkBp NUf4VJZjTE2VTx?= M3rTV2lEPTB;MUWuOgKBkcLz4pEJNU4zKG6P Ml;sNlMzQTl|OEi=
HCT116 NVTzcY9XT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1rqNlczKGh? NF:1e5dFVVOR NH\hXnZKSzVyPUGwMlfjiIoEsfMAjVIvOiCwTR?= MVSyN|I6QTN6OB?=
HCT116 p53−/− M17aPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX23NkBp NE\TeGVFVVOR M1rlXWlEPTB;OD625qCKyrIkgJmxMlchdk1? M1;ZSlI{Ojl7M{i4
dHCT116 p21−/− MkP6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{W5VVczKGh? MnXLSG1UVw>? Mo\mTWM2OD13LkpihKnDueLCiUGuN{BvVQ>? MkHqNlMzQTl|OEi=
HT29 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVvNXohiPzJiaB?= M3HOOWROW09? MkfpTWM2OD1zNj6z5qCKyrIkgJmyMlMhdk1? NH:2VmEzOzJ7OUO4PC=>
LoVo NFXIPYhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYq3NkBp M2HGPGROW09? M4fW[GlEPTB;NT6x5qCKyrIkgJmwMlYhdk1? NVnMSJJROjN{OUmzPFg>
RKO M1PWUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkXFO|IhcA>? MYfEUXNQ MkToTWM2OD15LkpihKnDueLCiUKuNkBvVQ>? MYCyN|I6QTN6OB?=
SW480 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkXZO|IhcA>? NUTT[VhJTE2VTx?= NV7ZWlBnUUN3ME2xO{426oDLwsJihKkxNjhibl2= NYTxdYRJOjN{OUmzPFg>
eSW620 M1XLSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn;SO|IhcA>? NWHzVplnTE2VTx?= NHK4RmxKSzVyPUmuNgKBkcLz4pEJNk4yKG6P NUX4SG4zOjN{OUmzPFg>

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体内試験 In lung cancer and mesothelioma animal models, LBH589 markedly decreases tumor growth by 62%. LBH589 is equally effective in immunocompetent and severe combined immunodeficien-cymice, suggesting that the inhibition of tumor growth by LBH589 is not due to direct immunologic effects. Daily LBH589, given i.p. at 20 mg/kg for 5 days per week, leading to an average decrease in growth of 70%. Compared with the corresponding control tumors, LBH589 leads to a 53% decrease for H526-derived tumors, an 81% decrease for BK-T-derived tumors, a 76% decrease for RG-1- derived tumors, and a 70% decrease for H69-derived tumors. In contrast to the lack of tumor regression notes in NSCLC and Meso-derived xenografted tumors that are treated under identical conditions and doses, LBH589 results in dramatic tumor regression in SCLC-derived tumors and RG-1-derived tumor. [2]

お薦めの試験操作(参考用のみ)

細胞試験: [1]
+ 展開
  • 細胞株: MOLT-4 cell lines and Reh (pre-B cells)
  • 濃度: 50 nM
  • 反応時間: 48 hours
  • 実験の流れ: Untreated and LBH589-treated cells [human Ph- acute lymphoblastic leukemia MOLT-4 (T cells) and Reh (pre-B cells)] are stained with annexin V and propidium iodide using annexin V-FITC apoptosis detection kit I. The percentage of apoptotic and nonviable cells is determined by flow cytometry. At least 5 × 104 cells are collected with a CyAn ADP Violet cytometer. Percentage apoptosis is calculated considering all the annexin V-positive plus the annexin V/PI-positive cells; percentage loss of cell viability is calculated considering all the annexin V-positive plus the PI-positive and the annexinV/PI-positive cells.
    (参考用のみ)
動物試験:[2]
+ 展開
  • 動物モデル: Severe combined immunodeficiency (SCID) mice with M30 (107 cells) or A549 (5 × 106 cells), H69 (2.5 × 106 cells), BK-T (6.5 × 106), H526 (10 × 106), and RG1 (10 × 106) cells
  • 製剤: Dextrose 5% in water
  • 投薬量: 10 mg/kg, 20 mg/kg
  • 投与方法: Administered via i.p. injection
    (参考用のみ)

溶解度 (25°C)

体外 DMSO 69 mg/mL (197.46 mM)
Water Insoluble
Ethanol Insoluble
体内 左から(NMPから)右の順に溶剤を製品に加えます(文献ではなく、Selleckの実験によるデータ):
2% DMSO+48% PEG 300+2% Tween 80+ddH2O
混合させたのち直ちに使用することを推奨します。
5mg/mL

* 溶解度測定はSelleck技術部門によって行われており、その他文献に示されている溶解度と差異がある可能性がありますが、同一ロットの生産工程で起きる正常な現象ですからご安心ください。

化学情報

分子量 349.43
化学式

C21H23N3O2

CAS No. 404950-80-7
保管
in solvent
別名 NVP-LBH589

便利ツール

モル濃度計算器

モル濃度計算器

求めたい質量、体積または濃度を計算してください。

質量 (g) = 濃度 (mol/L) x 体積 (L) x 分子量 (g/mol)

モル濃度計算器方程式

  • 質量
    濃度
    体積
    分子量

*貯蔵液を準備するとき、常に、オンであるとわかる製品のバッチに特有の分子量を使って、を通してラベルとMSDS/COA(製品ページで利用可能な)。

希釈計算器

希釈計算器

貯蔵液を準備するために必要な希釈率を計算してください。Selleck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

希釈の計算式

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

  • C1
    V1
    C2
    V2

常に貯蔵液を準備するとき、小びんラベルとMSDS/COA(オンラインで利用できる)で見つかる製品のバッチに特有の分子量を使ってください。

連続希釈計算器方程式

  • 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):
分子量計算器

分子量计算器

そのモル質量と元素組成を計算するために、合成物の化学式を入力してください:

総分子量:g/mol

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

モル濃度計算器

質量 濃度 体積 分子量

臨床試験

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03632317 Recruiting Glioma|Diffuse Intrinsic Pontine Glioma University of Michigan Cancer Center September 2018 Phase 2
NCT03566199 Recruiting Diffuse Intrinsic Pontine Glioma Sabine Mueller MD PhD|Midatech Pharma US Inc.|Pacific Pediatric Neuro-Oncology Consortium|University of California San Francisco May 22 2018 Phase 1|Phase 2
NCT03256045 Recruiting Recurrent Plasma Cell Myeloma|Refractory Plasma Cell Myeloma University of Washington|National Cancer Institute (NCI) February 8 2018 Phase 2
NCT02961816 Withdrawn Lymphoma M.D. Anderson Cancer Center June 2017 Phase 2
NCT02802163 Withdrawn Multiple Myeloma H. Lee Moffitt Cancer Center and Research Institute|Novartis|Amgen June 2017 Phase 1|Phase 2
NCT02756663 Withdrawn Multiple Myeloma Novartis Pharmaceuticals|Novartis December 2016 Phase 2

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

  • * 必須

よくある質問(FAQ)

  • 質問1:

    How to reconstitute the compound for in vivo mice study?

  • 回答:

    We recommend the vehicle is 2 % DMSO, 2 % Tween 80, 48%PEG300, 48% water. The compound is first dissolved in DMSO, then add Tween, PEG300, water in sequence.

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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