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 MkLyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIXic2cxNTFyIN88US=> NGi5UlYxNTRiZB?= MYjpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCkb4ToJJRqdWVvIHHu[EBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NULU[JZ{OjZ5MEK3PFQ>
HepG2 NXTNcHRwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3fVdVAuOTBizszN M2DMdlAuPCCm M{fvSolvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHLveIghfGmvZT2gZY5lKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= NUXNcGx6OjZ5MEK3PFQ>
HT29 MoL2SpVv[3Srb36gRZN{[Xl? MXq1NOKhdk1? MVqyOE04OiCq MUHpcoR2[2WmIHHjeIl3[XSrb36gc4Yh[2G|cHHz[UA{KGGodHXyJFQ5yqCqwrC= M2\sWFI3PzB{N{i0
HepG2 NFHQeJBHfW6ldHnvckBCe3OjeR?= MXW1NOKhdk1? NFX5XHYzPC15MjDo M2S3cYlv\HWlZXSgZYN1cX[jdHnvckBw\iClYYPwZZNmKDNiYX\0[ZIhOjUEoHlCpC=> NIfVXVQzPjdyMke4OC=>
HCC827 Mn7rS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NG[xWpo2NzdwNT:xNEBvVQ>? MXO3NuKhcA>? M2fOXGROW09? MUDlcohidmOnczD0bIUh[W62aYDyc4xq\mW{YYTpeoUh\W[oZXP0JI9nKGW{bH;0bY5q[g>? NFfHeJczPjZ5NUS4OC=>
A549  MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYHrPWZqOTBxMUWvNlAhdk1? M3\3PFczyqCq MlTjSG1UVw>? NEPCOZZmdmijbnPld{B1cGViYX70bZBzd2yrZnXyZZRqfmViZX\m[YN1KG:oIHXycI91cW6rYh?= NG\tPI0zPjZ5NUS4OC=>
NCI-H460  NHvQSZpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2LHR|ExNzJyL{OwJI5O NYPsS5ptPzMEoHi= MkewSG1UVw>? NGribHpmdmijbnPld{B1cGViYX70bZBzd2yrZnXyZZRqfmViZX\m[YN1KG:oIHXycI91cW6rYh?= MlWzNlY3PzV2OES=
J89GFP Ml3RS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV7EUXNQyqB? NIXHVY9GSzVyPUS5Mlg2KMLzIEGyMlY2KG6P M3qwNlI3PTZ|NU[4
THP89GFP M{PoT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoXmSG1UV8Li NHf4[ZBGSzVyPUG5MlM1KMLzIE[uOFMhdk1? NF;McFQzPjV4M{W2PC=>
SK-NEP-1 M2rVWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYTVV2tzOC5yMfMAl|ExNjBizszN M{WybVI1KGh? MorXSG1UV8Li M3TMWmlEPTB;N{[uN|Qhdk1? MmPSNlYyPzZ{MUm=
G401 NEf6SmRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVu4Xm9nOC5yMfMAl|ExNjBizszN MVKyOEBp MkjKSG1UV8Li M3mwfGlEPTB;MUSzMlAzKG6P MofzNlYyPzZ{MUm=
SK-NEP-1 NXjab4NjS2WubDDWbYFjcWyrdImgRZN{[Xl? Mn7DOVAhdk1? NHXaWFIy6oDVNDDk MkHZSG1UV8Li MYHy[YR2[2W|IHPlcIwhe3W{dnn2ZYwhcW5iYTD0bY1mKGSncHXu[IVvfCCvYX7u[ZI> NWXiN2hUOjZzN{[yNVk>
G401 MWDD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MVW1NEBvVQ>? MmXRNgKBmzRiZB?= MlPKSG1UV8Li Mkj3doVlfWOnczDj[YxtKHO3co\peoFtKGmwIHGgeIlu\SCmZYDlcoRmdnRibXHucoVz MX:yOlE4PjJzOR?=
SK-NEP-1 MmGwRZBweHSxc3nzJGF{e2G7 MV61NE8yODBibl2= NH60Uo4zPCCq NUDHZ4k1TE2VT9Mg NFzZT2tqdmS3Y3XzJINmdGxiYYDvdJRwe2m|IHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ M2TnT|I3OTd4MkG5
G401 NVHxcG42SXCxcITvd4l{KEG|c3H5 M3z1bVUxNzFyMDDuUS=> NIXneFAzPCCq NHTyfY1FVVORwrC= M2L2Oolv\HWlZYOgZ4VtdCCjcH;weI9{cXNiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MYeyOlE4PjJzOR?=
SK-NEP-1 NHfSdoZHfW6ldHnvckBCe3OjeR?= MUS1NE8yODBibl2= NXPGS5dyOjRiaB?= MYrEUXNQyqB? NIiybo5{cG:5czD0bIUhcW6mdXP0bY9vKG:oIFTORUBnemGpbXXueIF1cW:w NWLNeZg3OjZzN{[yNVk>
G401 MkWwSpVv[3Srb36gRZN{[Xl? NWfu[5g4PTBxMUCwJI5O M2rDXlI1KGh? M4HFd2ROW00EoB?= NUnyfW5He2ixd4OgeIhmKGmwZIXjeIlwdiCxZjDEUmEh\nKjZ33lcpRifGmxbh?= M1frcFI3OTd4MkG5
SK-NEP-1 NUXifZpyTnWwY4Tpc44hSXO|YYm= MXe1NE8yODBibl2= M{HmdVI1KGh? M2TPc2ROW00EoB?= NVHYdnBlcW6mdXPld{Bk\WyuIHP5Z4xmKGSrc3;y[IVzyqB? MX2yOlE4PjJzOR?=
G401 NX[1e|kzTnWwY4Tpc44hSXO|YYm= NIjocGc2OC9zMECgcm0> NVTiPFliOjRiaB?= MWPEUXNQyqB? NHP5eZRqdmS3Y3XzJINmdGxiY4njcIUh\Gm|b4Lk[ZLDqA>? MlL3NlYyPzZ{MUm=
RPMI 8226 NUOxbphLS2WubDDTeZJ3cX[jbDDBd5NigQ>? NWjySGlvOi92L{[gcm0> NG\Ve|U1QOLCiXi= M2TreIlv\HWlZYOgZUB{cWewaX\pZ4FvfCCmZXPy[YF{\SCrbjD0bIUh[2WubDDndo94fGh? M33BcVI3ODByMkmy
OPM2 MXfD[YxtKFO3co\peoFtKEG|c3H5 MnHhNk81NzZibl2= NUf1S5BIPDkkgJno MnjVbY5lfWOnczDhJJNq\26rZnnjZY51KGSnY4LlZZNmKGmwIITo[UBk\WyuIHfyc5d1cA>? NUm2fHZIOjZyMECyPVI>
U266 M2nTfGNmdGxiU4Xyeol3[WxiQYPzZZk> NHzSdGwzNzRxNjDuUS=> NF\Md4g1QOLCiXi= NXztNpIycW6mdXPld{BiKHOrZ37p[olk[W62IHTlZ5Jm[XOnIHnuJJRp\SClZXzsJIdzd3e2aB?= NXO0eWM5OjZyMECyPVI>
H929 MVzD[YxtKFO3co\peoFtKEG|c3H5 MYCyM|QwPiCwTR?= NXTUTIN3PDkkgJno NIDnUoVqdmS3Y3XzJIEhe2mpbnnmbYNidnRiZHXjdoVie2ViaX6geIhmKGOnbHyg[5Jwf3Sq NV\YNGNWOjZyMECyPVI>
RPMI 8226  NIC3WG5CeG:ydH;zbZMhSXO|YYm= Mn70OQKBkW6P NG\YNY0zPC92ODDo NV3jV4x6cW6mdXPld{Bk\WyuIHHwc5B1d3OrczDpckBiKHSrbXWt[IVx\W6mZX70JI1idm6nch?= M2fGR|I3ODByMkmy
HCC827 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{f1XlExKG6P Mlq2OFghcA>? NVXxSIZpTE2VTx?= MUTlcohidmOnczDjbZNxdGG2aX6gd4Vve2m2aY\peJnDqA>? NXTOUnd{OjV7NES2NVc>
NCI-H23 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlXGNVAhdk1? NUXmflhlPDhiaB?= NF3yUJJFVVOR M2DSOYVvcGGwY3XzJINqe3CuYYTpckB{\W6|aYTpeol1gcLi NGrXS3QzPTl2NE[xOy=>
AML3 NUnYWWhLTnWwY4Tpc44hSXO|YYm= NYPsW|VSOC1zIN88US=> MXGyOOKhcA>? M1HBRolv\HWlZYOgSG5CKG[{YXft[Y51[XSrb39CpIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy NH\pNGozPTZzMkm0NS=>
ML-1 Mm[5SpVv[3Srb36gRZN{[Xl? MkG4NE0yKM7:TR?= M2DCbVI1yqCq MWnpcoR2[2W|IFTORUBnemGpbXXueIF1cW:wwrDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= MXGyOVYyOjl2MR?=
RPMI-8226vr10  NHe1eXRHfW6ldHnvckBCe3OjeR?= NVfqc2dbOC1zIN88US=> NF\Hb2IzPMLiaB?= MlvqbY5lfWOnczDEUmEh\nKjZ33lcpRifGmxbtMgbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK= M4n0[FI2PjF{OUSx
ML-1 NE[zVWFHfW6ldHnvckBCe3OjeR?= MmLxNUDPxE1? M4fqRlI1yqCq NYTzNXNMcW6lcnXhd4V{KGOjc4Dhd4UuOyCjY4Tpeol1gSB2LX\vcIQ> M3K0fVI2PjF{OUSx
RPMI-8226vr10  NU\mc|RNTnWwY4Tpc44hSXO|YYm= NFPq[lEyKM7:TR?= NH;kWm4zPMLiaB?= Mn;ZbY5kemWjc3XzJINie3Cjc3WtN{Bi[3Srdnn0fUAzNjVvZn;s[C=> MUOyOVYyOjl2MR?=
SK-N-BE (2) NX7wd29{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3rJe|I16oDLaB?= MWrJR|UxRTFyND6w5qCKyrIkgJm3Mlghdk1? NYfEb|ViOjV|MEi5NVY>
SK-N-BE (2), PAN  MK MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVSyOQKBkWh? NVnXNJBVUUN3ME2xNFQvOOLCidMx5qCKPy56IH7N Mn7xNlU{ODh7MU[=
SK-N-BE (2), MK  PAN M4LQWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmrwNlTjiImq MWXJR|UxRTN6Mj6w5qCKyrIkgJm0N{4zKG6P NYL0XJR{OjV|MEi5NVY>
SK-N-AS NYrrb3lsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M17ZcVI16oDLaB?= NF;CfYRKSzVyPUO3MlHjiIoEsfMAjVIvPCCwTR?= NFK3S5gzPTNyOEmxOi=>
SK-N-DZ MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1\ubFI16oDLaB?= Ml3UTWM2OD1zNz6x5qCKyrIkgJmwMlQhdk1? NFzqR|gzPTNyOEmxOi=>
Caki-1 NVyyPYNRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXzQfIhxOTBxMkWvOVAhdk1? MYi0PEBp MoPqbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZIhe3mwZYLnbZN1cWOjbHz5JJdqfGhicnn0c45ifmm{ NILIXXgzPTJ5OUG5NS=>
ACHN NH3pc|JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1TqUVExNzJ3L{WwJI5O MX60PEBp MWnpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldkB{gW6ncnfpd5Rq[2GubImge4l1cCC{aYTvcoF3cXJ? NUPRe|kyOjV{N{mxPVE>
769-P MnjKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4rES|ExNzJ3L{WwJI5O MWW0PEBp NGTJZoJqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meiC|eX7ldodqe3SrY3HscJkhf2m2aDDybZRwdmG4aYK= NIXZfowzPTJ5OUG5NS=>
786-O  NWG5[oh1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3XNSlExNzJ3L{WwJI5O MUK0PEBp NEHhfpRqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meiC|eX7ldodqe3SrY3HscJkhf2m2aDDybZRwdmG4aYK= MXKyOVI4QTF7MR?=
Caki-1 NH\GSpJCeG:ydH;zbZMhSXO|YYm= NW[zd|dLPTBibl2= NWLFRmRoPDhiaB?= NYrjeIdNcW6mdXPld{Bk\WyuIHHwc5B1d3OrczDjc41jcW6nZDDybZRwdmG4aYK= MVeyOVI4QTF7MR?=
ACHN NGjJTIdCeG:ydH;zbZMhSXO|YYm= MV21NEBvVQ>? M{DqPFQ5KGh? MW\pcoR2[2W|IHPlcIwh[XCxcITvd4l{KGOxbXLpcoVlKHKrdH;uZZZqeg>? M3rjXVI2Ojd7MUmx
769-P MXXBdI9xfG:|aYOgRZN{[Xl? NYXvZ2ZGPTBibl2= NGG5TIo1QCCq NHmzOoRqdmS3Y3XzJINmdGxiYYDvdJRwe2m|IHPvcYJqdmWmIILpeI9v[X[rch?= NIf4RlczPTJ5OUG5NS=>
786-O  NWiyR2VuSXCxcITvd4l{KEG|c3H5 MUm1NEBvVQ>? M1fPZ|Q5KGh? M4nFNolv\HWlZYOgZ4VtdCCjcH;weI9{cXNiY3;tZolv\WRicnn0c45ifmm{ Mmj3NlUzPzlzOUG=
Caki-1 M13wNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWrzNXNxOjVxNUCgcm0> MorxOFghcA>? NVfvXm56TE2VTx?= MnSybY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZIhe3mwZYLnbZN1cWOjbHz5JJdqfGhiYn;yeIV7d22rYh?= NGC0[JAzPTF5NkO1OC=>
ACHN M4fseWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1\XTVI2NzVyIH7N MkH6OFghcA>? NE\qWYJFVVOR MWLpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldkB{gW6ncnfpd5Rq[2GubImge4l1cCCkb4L0[ZpwdWmk Mn7UNlUyPzZ|NUS=
769-P MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXSyOU82OCCwTR?= NXvMXXhCPDhiaB?= NIjsfJFFVVOR NUXWTHU4cW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJic4nu[ZJocXO2aXPhcIx6KHerdHigZo9zfGW8b33pZi=> M3jsNVI2OTd4M{W0
Caki-1 NFPhbmxEd2yxbomgSo9zdWG2aX;uJGF{e2G7 NETBNmM2OCCwTR?= NGLLfGM4NTF2IHS= M{HFZWROW09? NGr2T4V{fXCycnXzd4VlKGOxbH;ufUBnd3KvYYTpc44he2mpbnnmbYNidnSueTDjc41jcW6nZDD3bZRpKHerdHigZo9zfGW8b33pZkDDqA>? NYfLUnNGOjVzN{[zOVQ>
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OCI-AML3  MnO3RZBweHSxc3nzJGF{e2G7 M3fU[VDjiJN2MDDuUeKh M17qflQ5KGh? M4S1R4lv\HWlZYOgZZBweHSxc3nzJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy NVzSeI52OjR{NES0Nlk>
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PC3 MVjBdI9xfG:|aYOgRZN{[Xl? NHy3cXkxNTFyMDDuUS=> NGnmOoEzPC92ODDo NVi5dY9qcW6mdXPld{BieG:ydH;zbZMhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MlezNlQyPjN{M{C=
PC3-AR NF\JcJFCeG:ydH;zbZMhSXO|YYm= MnPSNE0yODBibl2= MUmyOE81QCCq M17SRolv\HWlZYOgZZBweHSxc3nzJIlvKGKxdHigeIlu\S1iYX7kJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NU\xOFhLOjRzNkOyN|A>
PC3 NIL5dllIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2m1[FAuOTByIH7N M{nFNlI1NzR6IHi= M1qzT4lv\HWlZYOgZYNkfW23bHH0bY9vKG:oIIP1ZmcyKHCxcIXsZZRqd25? MUOyOFE3OzJ|MB?=
PC3-AR MkHkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2jhZlAuOTByIH7N M2XXdlI1NzR6IHi= NXPUcJZTcW6mdXPld{Bk\WyuIHP5Z4xmKGG{cnXzeEBqdiC2aHWgS|JOKHCqYYPl NWfNcVl1OjRzNkOyN|A>
PC3 MVfGeY5kfGmxbjDBd5NigQ>? MoPyNE0yODBibl2= M2X1T|I1KGh? MXTzeZBxemW|c3XzJIV5eHKnc4Ppc44hd2ZiYXP0bZZifGWmIFHUUUwhSWu2IHHu[EBGemtzL{KgdJJwfGWrbh?= M1GwSFI1OTZ|MkOw
PC3-AR MlHtSpVv[3Srb36gRZN{[Xl? Ml23NE0yODBibl2= MonUNlQhcA>? NH7Ddnp{fXCycnXzd4V{KGW6cILld5Nqd25ib3[gZYN1cX[jdHXkJGFVVSxiQXv0JIFv\CCHcnuxM|IheHKxdHXpci=> M4S2dVI1OTZ|MkOw
OS-RC-2 MV7D[YxtKF[rYXLpcIl1gSCDc4PhfS=> NHLqcFUxNTFyMECgcm0> Mnr0NlQwPDhxN{KgbC=> NX3H[GI5TE2VTx?= MV;k[YNz\WG|ZYOgZ4VtdCC4aXHibYxqfHliaX6gZo91cCC2aX3lMUBidmRiZH;z[U1l\XCnbnTlcpQhdWGwbnXy Ml3zNlQyPDR5M{e=
OS-RC-2 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXK1NEBvVQ>? MonSOFghcA>? M17rNWROW09? NVTLZ3BmcW6mdXPld{BIOi:PIHHydoV{fA>? NHzYO24zPDF2NEezOy=>
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SK-N-DZ NEm3eWdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF\MRlEx6oDVOECgcm0> M{HxOFQ5KGh? Mo\tTWM2OD1{MT65JI5O NWLJd25TOjRyOUi3PVk>
SK-N-SH MlfqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWKw5qCUQDBibl2= M4jydFQ5KGh? NFrEVYZKSzVyPUeyMlMhdk1? NXnMToU5OjRyOUi3PVk>
SK-N-BE MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2\5W|DjiJN6MDDuUS=> MkP1OFghcA>? M1HhV2lEPTB;N{WuOEBvVQ>? NHLhbZczPDB7OEe5PS=>
SK-N-AS MoLwRZBweHSxc3nzJGF{e2G7 MkPPNQKBmzhyIH7N MnT2OFghcA>? NGf2UIhxd3SnboTsfUBqdmS3Y3XkJIFxd3C2b4Ppd{BqdiCjIHTvd4Uu\GWyZX7k[Y51KG[jc3jpc44> MWeyOFA6QDd7OR?=
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SK-N-SH M3LJe2Fxd3C2b4Ppd{BCe3OjeR?= NHThXG4x6oDVNECgcm0> MmHEOFghcA>? M1rFPJBwfGWwdHz5JIlv\HWlZXSgZZBweHSxc3nzJIlvKGFiZH;z[U1l\XCnbnTlcpQh\mG|aHnvci=> M2rxZlI1ODl6N{m5
SK-N-BE NFfXeYtCeG:ydH;zbZMhSXO|YYm= MWKw5qCUPDBibl2= NI\Kb3o1QCCq NWrSTVFteG:2ZX70cJkhcW6mdXPl[EBieG:ydH;zbZMhcW5iYTDkc5NmNWSncHXu[IVvfCCoYYPobY9v NY\VU45UOjRyOUi3PVk>
SK-N-AS Mn7TSpVv[3Srb36gRZN{[Xl? NX65Tm1JOOLCk{iwJI5O NX7t[2hoPDhiaB?= NECyTYVqdmS3Y3XzJIEh\G:|ZT3k[ZBmdmSnboSgZ4xm[X[jZ3Wgc4Yh[2G|cHHz[UA{KGGwZDDQRXJR MkPWNlQxQTh5OUm=
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SK-N-BE NGW0NWRHfW6ldHnvckBCe3OjeR?= M4Tvc|DjiJN2MDDuUS=> MlPsOFghcA>? M1zFdolv\HWlZYOgZUBld3OnLXTldIVv\GWwdDDjcIVifmGpZTDv[kBk[XOyYYPlJFMh[W6mIGDBVnA> NW\pdG1GOjRyOUi3PVk>
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HepG2 MnzuRZBweHSxc3nzJGF{e2G7 NXTFNYFLPTBibl2= M362WlQ5KGh? NWHBXIVNTE2VTx?= MVvpcoR2[2W|IHPlcIwh[XCxcITvd4l{KHOrZ37p[olk[W62bImgbY4h[SClYYPwZZNmNWSncHXu[IVvfCCvYX7u[ZIh[nliY3zlZZZi\2Vib3[gZ4F{eGG|ZYOgN{whQCCjbnSgPS=> NHPkXngzPDB7M{m1Oi=>
SMMC-7721 MX\BdI9xfG:|aYOgRZN{[Xl? M2nNbVUxKG6P NGHHNXk1QCCq MW\EUXNQ NV[4OXF{cW6mdXPld{Bk\WyuIHHwc5B1d3OrczDzbYdvcW[rY3HueIx6KGmwIHGgZ4F{eGG|ZT3k[ZBmdmSnboSgcYFvdmW{IHL5JINt\WG4YXflJI9nKGOjc4Dhd4V{KDNuIEigZY5lKDl? MY[yOFA6Ozl3Nh?=
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HepG2 MWfGeY5kfGmxbjDBd5NigQ>? NHvJWW02OC9zMECgcm0> M2HEe|I1KGh? MojJSG1UVw>? NVjvXHU6\GWlcnXhd4V{KHSqZTDs[ZZmdHNib3[gdE1UXEGWMzDhcoQheC2Da4VCpC=> NXnRdWVkOjRyOUO5OVY>
SMMC-7721 Ml[2SpVv[3Srb36gRZN{[Xl? MmX0OVAwOTByIH7N NEHwdFEzPCCq MoXJSG1UVw>? M3vTNIRm[3KnYYPld{B1cGVibHX2[Yx{KG:oIICtV3RCXDNiYX7kJJAuSWu2wrC= MYiyOFA6Ozl3Nh?=
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HepG2 NISyNYZHfW6ldHnvckBCe3OjeR?= M4nyc|UxNzFyMDDuUS=> MlPENlQhcA>? NVv3WYRtTE2VTx?= NWn3Vppz\G:5boLl[5Vt[XSnczDCZ4wugExiZYjwdoV{e2mxbh?= M2XmUVI1ODl|OUW2
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FaDu NE\HdotIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWH2TopROTBy4pEFcm0> MnT6PE8yOC9zMjDo MX\kbZNxdGG7ZXSgZUB{cWewaX\pZ4FvfCCjbnSgdJJwdG:wZ3XkJGczN01iYYLy[ZN1KGG2IEigZY5lKDF{4pEFbEBxd3O2IILlcIVie2V? MV2yOFAzPjR6Mh?=
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PC-3  NILyXY1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFLvUHgxNTFyIN88US=> NVf1UGZ3OjRxNEivO|IhcA>? NHXmRZdqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDic5RpKHSrbXWtJIFv\CCmb4PlMYRmeGWwZHXueEBu[W6wZYK= NGPVe2szOzl7MUKxOi=>
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RWPE-1  NG\6dFRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4\3PFAuOjBizszN NEfP[IYzPC92OD:3NkBp MVLpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCkb4ToJJRqdWVvIHHu[EBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NYfpNGFjOjN7OUGyNVY>
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CFPAC-1  MlHsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX2yOU82OC9zMECgcm0> MYG0PEBp M2HmOGROW09? MlvGdoVlfWOnczDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MoC1NlM6OjJ6OE[=
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CFPAC-1  NXO5[VV4SXCxcITvd4l{KEG|c3H5 MWqyOU82OC9zMECgcm0> NYXnc2pjPDhiaB?= M{KweWROW09? NHvES2FqdmS3Y3XzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz M{H1Z|I{QTJ{OEi2
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HSC4  NVLxS|hrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYLoS5RwOC1{MDDuUS=> NYHHV4tbOjRxNEigbC=> NVjCV2pQTE2VTx?= MknLbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliaX6gZo91cCC2aX3lMUBidmRiZH;z[U0h\GWyZX7k[Y51KG2jbn7ldi=> NF;jdlczOzh5N{KzOS=>
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HSC4  NW\1N5ZFSXCxcITvd4l{KEG|c3H5 MmPRNE0zOCCwTR?= NYTJblNmPDhiaB?= M1fhXmROW09? M125U4lv\HWlZYOgZ4VtdCCjcH;weI9{cXN? M4DWfVI{QDd5MkO1
HN22 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3TjVlAuOjBibl2= MWC0PEBp NHHqVllFVVOR NWHWRpV6cW6mdXPld{BIOSCyaHHz[UBk\WyuIHP5Z4xmKGG{cnXzeOKh NVq3WlFmOjN6N{eyN|U>
HSC4  NX7kSWJLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkDINE0zOCCwTR?= M{P6flQ5KGh? MknYSG1UVw>? MlHabY5lfWOnczDHNUBxcGG|ZTDj[YxtKGO7Y3zlJIFzemW|dNMg Mn;RNlM5Pzd{M{W=
HN22 MlnBSpVv[3Srb36gRZN{[Xl? NVr4dIw5OC1{MDDuUS=> M2TQSlQ5KGh? NFvC[phFVVOR NU[0XopIe3WycILld5NmeyCVcEGg[ZhxemW|c3nvcuKh NXrqWWNROjN6N{eyN|U>
HSC4  NUnlcpRYTnWwY4Tpc44hSXO|YYm= NEHXS4IxNTJyIH7N MoDxOFghcA>? NIHvWFVFVVOR NFO1PY1{fXCycnXzd4V{KFOyMTDlfJBz\XO|aX;uxsA> NH3CTlQzOzh5N{KzOS=>
Cal62 M{nyPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX7nNmt6UUN3ME2zN{DDuSB2IH7N M3fJVlI{QDJ2ME[0
Hth7 MmLwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYLJR|UxRTF3INMxJFIhdk1? Mkm4NlM5OjRyNkS=
Hth83 M{PWWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFqwOWNKSzVyPUO0JOKyKDVibl2= NW\zSYlHOjN6MkSwOlQ>
C643 M3jEWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2TTVGlEPTB;N{GgxtEhOTBibl2= MkjXNlM5OjRyNkS=
SW1736 MojFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmfRTWM2OD1|NTFCtUA5KG6P NGq4bWszOzh{NEC2OC=>
T241 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3r3VmlEPTB;NkWgxtEhPyCwTR?= MnX6NlM5OjRyNkS=
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T238 NVu5fFI3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVPJR|UxRTFuNUCwJOKyKDJyMDDuUS=> MmPCNlM5OjRyNkS=
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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