Panobinostat (LBH589)

Catalog No.S1030 Synonyms: NVP-LBH589

Panobinostat (LBH589) Chemical Structure

Molecular Weight(MW): 349.43

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

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Cited by 47 Publications

11 Customer Reviews

  • 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.

    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.

    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.

  • 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.

    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.

  • 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.

Purity & Quality Control

Choose Selective HDAC Inhibitors

Biological Activity

Description Panobinostat (LBH589) is a novel broad-spectrum HDAC inhibitor with IC50 of 5 nM in a cell-free assay. Phase 3.
Targets
HDAC (MOLT-4 cells) [1] HDAC (Reh cells) [1]
5 nM 20 nM
In vitro

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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HT29 MlXHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGLDUm0xNTFyIN88US=> M{XpVlAuPCCm NHjFRpJqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDic5RpKHSrbXWtJIFv\CCmb4PlMYRmeGWwZHXueEBu[W6wZYK= MWWyOlcxOjd6NB?=
HepG2 MkXSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXGwMVExKM7:TR?= NIHmdpMxNTRiZB?= NH\j[I5qdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDic5RpKHSrbXWtJIFv\CCmb4PlMYRmeGWwZHXueEBu[W6wZYK= MXKyOlcxOjd6NB?=
HT29 NGfzS2FHfW6ldHnvckBCe3OjeR?= MnjrOVDDqG6P MojxNlQuPzJiaB?= M1vO[Ylv\HWlZXSgZYN1cX[jdHnvckBw\iClYYPwZZNmKDNiYX\0[ZIhPDkEoHlCpC=> NF6wZ4ozPjdyMke4OC=>
HepG2 M1XiZWZ2dmO2aX;uJGF{e2G7 NFvGWFU2OMLibl2= Mmf1NlQuPzJiaB?= MmXobY5lfWOnZDDhZ5RqfmG2aX;uJI9nKGOjc4Dhd4UhOyCjZoTldkAzPMLiaNMg M{XFblI3PzB{N{i0
HCC827 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NY\BdGM1PS95LkWvNVAhdk1? MV23NuKhcA>? MUfEUXNQ NH\HUlRmdmijbnPld{B1cGViYX70bZBzd2yrZnXyZZRqfmViZX\m[YN1KG:oIHXycI91cW6rYh?= NHn4WGczPjZ5NUS4OC=>
A549  NEH3W4FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{ToVFExNzF3L{KwJI5O M1iyUlczyqCq MmnLSG1UVw>? M3vTU4VvcGGwY3XzJJRp\SCjboTpdJJwdGmoZYLheIl3\SCnZn\lZ5Qhd2ZiZYLsc5Rqdmmk MYSyOlY4PTR6NB?=
NCI-H460  NV62R|ZRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnzlNVAwOjBxM{Cgcm0> M2HRR|czyqCq Mnm1SG1UVw>? M{n4U4VvcGGwY3XzJJRp\SCjboTpdJJwdGmoZYLheIl3\SCnZn\lZ5Qhd2ZiZYLsc5Rqdmmk NWnnPJVzOjZ4N{W0PFQ>
J89GFP NXjSPHh5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml[wSG1UV8Li M{iyTWVEPTB;NEmuPFUhyrFiMUKuOlUhdk1? NWLkfmZjOjZ3NkO1Olg>
THP89GFP NYDwbmtKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkPhSG1UV8Li MkHDSWM2OD1zOT6zOEDDuSB4LkSzJI5O NFn3OFYzPjV4M{W2PC=>
SK-NEP-1 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1rqOlAvODIkgKOxNE4xKM7:TR?= MmHnNlQhcA>? NVi4TZl[TE2VT9Mg Ml7OTWM2OD15Nj6zOEBvVQ>? NUHId4c3OjZzN{[yNVk>
G401 M1jjSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWjIbXpbOC5yMfMAl|ExNjBizszN NFrzbo8zPCCq NUDNe5RHTE2VT9Mg MVfJR|UxRTF2Mz6wNkBvVQ>? MXGyOlE4PjJzOR?=
SK-NEP-1 MYfD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NG\jeJU2OCCwTR?= MYqx5qCUPCCm M{jxTmROW00EoB?= NYXUUJpVemWmdXPld{Bk\WyuIIP1dpZqfmGuIHnuJIEhfGmvZTDk[ZBmdmSnboSgcYFvdmW{ MWqyOlE4PjJzOR?=
G401 M3TVW2NmdGxiVnnhZoltcXS7IFHzd4F6 M{TqdFUxKG6P MYGx5qCUPCCm MWHEUXNQyqB? MnjXdoVlfWOnczDj[YxtKHO3co\peoFtKGmwIHGgeIlu\SCmZYDlcoRmdnRibXHucoVz MX2yOlE4PjJzOR?=
SK-NEP-1 NU\PSmpkSXCxcITvd4l{KEG|c3H5 MkDuOVAwOTByIH7N M{T1R|I1KGh? MmHQSG1UV8Li NYnrZZh[cW6mdXPld{Bk\WyuIHHwc5B1d3OrczDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= NIPhboszPjF5NkKxPS=>
G401 M{HTXmFxd3C2b4Ppd{BCe3OjeR?= M1L0VVUxNzFyMDDuUS=> MnPUNlQhcA>? MWLEUXNQyqB? MV3pcoR2[2W|IHPlcIwh[XCxcITvd4l{KGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MoCyNlYyPzZ{MUm=
SK-NEP-1 Mne0SpVv[3Srb36gRZN{[Xl? MUW1NE8yODBibl2= MkXuNlQhcA>? NVe5UYRGTE2VT9Mg NH\jOYZ{cG:5czD0bIUhcW6mdXP0bY9vKG:oIFTORUBnemGpbXXueIF1cW:w MVGyOlE4PjJzOR?=
G401 NWLwU|J[TnWwY4Tpc44hSXO|YYm= NEHyem42OC9zMECgcm0> MWCyOEBp M{LxWmROW00EoB?= NYHEdJVGe2ixd4OgeIhmKGmwZIXjeIlwdiCxZjDEUmEh\nKjZ33lcpRifGmxbh?= NVvmTVBQOjZzN{[yNVk>
SK-NEP-1 NInx[4lHfW6ldHnvckBCe3OjeR?= NYL4bno5PTBxMUCwJI5O MX[yOEBp M13SXGROW00EoB?= NFK4WlZqdmS3Y3XzJINmdGxiY4njcIUh\Gm|b4Lk[ZLDqA>? MkD2NlYyPzZ{MUm=
G401 NYrLNYRDTnWwY4Tpc44hSXO|YYm= M1TBXVUxNzFyMDDuUS=> NFzCR2czPCCq NX:0eYhJTE2VT9Mg NEfBSYtqdmS3Y3XzJINmdGxiY4njcIUh\Gm|b4Lk[ZLDqA>? NX7qfowyOjZzN{[yNVk>
RPMI 8226 NWHJVpJqS2WubDDTeZJ3cX[jbDDBd5NigQ>? MVyyM|QwPiCwTR?= NHXMZoI1QOLCiXi= NYLxO5p4cW6mdXPld{BiKHOrZ37p[olk[W62IHTlZ5Jm[XOnIHnuJJRp\SClZXzsJIdzd3e2aB?= NW[4R2NoOjZyMECyPVI>
OPM2 NXrEVYhPS2WubDDTeZJ3cX[jbDDBd5NigQ>? NHnmNnczNzRxNjDuUS=> NVPONI5KPDkkgJno MW\pcoR2[2W|IHGgd4lodmmoaXPhcpQh\GWlcnXhd4UhcW5idHjlJINmdGxiZ4Lve5Rp NGjTdFIzPjByMEK5Ni=>
U266 M2jaNmNmdGxiU4Xyeol3[WxiQYPzZZk> NICwOYMzNzRxNjDuUS=> NWjIXZVJPDkkgJno Mn32bY5lfWOnczDhJJNq\26rZnnjZY51KGSnY4LlZZNmKGmwIITo[UBk\WyuIHfyc5d1cA>? MWWyOlAxODJ7Mh?=
H929 M1vwVmNmdGxiU4Xyeol3[WxiQYPzZZk> NFLNZZUzNzRxNjDuUS=> MYe0PQKBkWh? M{Hybolv\HWlZYOgZUB{cWewaX\pZ4FvfCCmZXPy[YF{\SCrbjD0bIUh[2WubDDndo94fGh? NXzXS4h7OjZyMECyPVI>
RPMI 8226  NYHSdY5ESXCxcITvd4l{KEG|c3H5 NVLuV4J3POLCiX7N NIrWUJYzPC92ODDo NHzKSYRqdmS3Y3XzJINmdGxiYYDvdJRwe2m|IHnuJIEhfGmvZT3k[ZBmdmSnboSgcYFvdmW{ NGfQbI0zPjByMEK5Ni=>
HCC827 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlXXNVAhdk1? MkfzOFghcA>? M1fw[mROW09? NHfBRpVmdmijbnPld{BkcXOybHH0bY4he2Wwc3n0bZZqfHoEoB?= NUHOU3VbOjV7NES2NVc>
NCI-H23 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXWxNEBvVQ>? NWjPbXZ4PDhiaB?= Mkn1SG1UVw>? Mmjr[Y5p[W6lZYOgZ4l{eGyjdHnuJJNmdnOrdHn2bZR6yqB? NW[5[3lCOjV7NES2NVc>
AML3 MoSySpVv[3Srb36gRZN{[Xl? M1GwT|AuOSEQvF2= MUGyOOKhcA>? M3j4Solv\HWlZYOgSG5CKG[{YXft[Y51[XSrb39CpIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy MU[yOVYyOjl2MR?=
ML-1 MorzSpVv[3Srb36gRZN{[Xl? NXXEd4lxOC1zIN88US=> NFnhWJMzPMLiaB?= M{LsdYlv\HWlZYOgSG5CKG[{YXft[Y51[XSrb39CpIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy NGPOd2QzPTZzMkm0NS=>
RPMI-8226vr10  MlnzSpVv[3Srb36gRZN{[Xl? M1njNVAuOSEQvF2= MkPrNlTDqGh? MWnpcoR2[2W|IFTORUBnemGpbXXueIF1cW:wwrDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= NYjzdZVCOjV4MUK5OFE>
ML-1 NEX2PYZHfW6ldHnvckBCe3OjeR?= NFrXXnQyKM7:TR?= NF7HOmszPMLiaB?= MWDpcoNz\WG|ZYOgZ4F{eGG|ZT2zJIFkfGm4aYT5JFQu\m:uZB?= MVuyOVYyOjl2MR?=
RPMI-8226vr10  NFLacndHfW6ldHnvckBCe3OjeR?= NUXL[nZXOSEQvF2= NWj5cXFkOjUEoHi= NVf6RmxqcW6lcnXhd4V{KGOjc4Dhd4UuOyCjY4Tpeol1gSB{LkWt[o9t\A>? MUKyOVYyOjl2MR?=
SK-N-BE (2) M1XvfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWOyOQKBkWh? NW\oOXhbUUN3ME2xNFQvOOLCidMx5qCKPy56IH7N MnTNNlU{ODh7MU[=
SK-N-BE (2), PAN  MK MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3zIbFI16oDLaB?= MlfaTWM2OD1zMESuNQKBkcLz4pEJO{45KG6P MUeyOVMxQDlzNh?=
SK-N-BE (2), MK  PAN MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHnaTYYzPOLCiXi= M3XsXmlEPTB;M{iyMlDjiIoEsfMAjVQ{NjJibl2= MWiyOVMxQDlzNh?=
SK-N-AS MofhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmfDNlTjiImq MlnsTWM2OD1|Nz6x5qCKyrIkgJmyMlQhdk1? M1O3d|I2OzB6OUG2
SK-N-DZ NH6wSGxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mm\4NlTjiImq M4XsV2lEPTB;MUeuNgKBkcLz4pEJNE41KG6P NVHjTVJxOjV|MEi5NVY>
Caki-1 M13PW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NG\iZZMyOC9{NT:1NEBvVQ>? NEXMZlg1QCCq MXTpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldkB{gW6ncnfpd5Rq[2GubImge4l1cCC{aYTvcoF3cXJ? MY[yOVI4QTF7MR?=
ACHN M33TRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX[xNE8zPS93MDDuUS=> NILIOms1QCCq NUP5dZZqcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJic4nu[ZJocXO2aXPhcIx6KHerdHigdol1d26jdnny M1vKXlI2Ojd7MUmx
769-P MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUnGZpJQOTBxMkWvOVAhdk1? NEK5T2Y1QCCq M2SyOYlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\SCmZYDlcoRmdnRibXHucoVzKHO7bnXy[4l{fGmlYXzsfUB4cXSqIILpeI9v[X[rch?= MX6yOVI4QTF7MR?=
786-O  NHP3XmRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV3xd|E5OTBxMkWvOVAhdk1? M3LVdVQ5KGh? MmDIbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZIhe3mwZYLnbZN1cWOjbHz5JJdqfGhicnn0c45ifmm{ NHr2bmEzPTJ5OUG5NS=>
Caki-1 MXHBdI9xfG:|aYOgRZN{[Xl? M2TvcFUxKG6P NYKxRXpSPDhiaB?= M1z0dIlv\HWlZYOgZ4VtdCCjcH;weI9{cXNiY3;tZolv\WRicnn0c45ifmm{ M3PRPFI2Ojd7MUmx
ACHN NIrTenVCeG:ydH;zbZMhSXO|YYm= M1HoXlUxKG6P NV;SSZJoPDhiaB?= MnjxbY5lfWOnczDj[YxtKGGyb4D0c5NqeyClb33ibY5m\CC{aYTvcoF3cXJ? MmfHNlUzPzlzOUG=
769-P MmXNRZBweHSxc3nzJGF{e2G7 NHT0Uno2OCCwTR?= M2Hme|Q5KGh? MnHrbY5lfWOnczDj[YxtKGGyb4D0c5NqeyClb33ibY5m\CC{aYTvcoF3cXJ? MX2yOVI4QTF7MR?=
786-O  MVPBdI9xfG:|aYOgRZN{[Xl? MoX4OVAhdk1? MXe0PEBp MUnpcoR2[2W|IHPlcIwh[XCxcITvd4l{KGOxbXLpcoVlKHKrdH;uZZZqeg>? M4DiflI2Ojd7MUmx
Caki-1 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX;zc4NoOjVxNUCgcm0> MWC0PEBp NIf4[VZFVVOR M2XNc4lvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\SCmZYDlcoRmdnRibXHucoVzKHO7bnXy[4l{fGmlYXzsfUB4cXSqIHLvdpRmgm:vaXK= NELodGMzPTF5NkO1OC=>
ACHN M1\oT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkTrNlUwPTBibl2= MUm0PEBp MmXzSG1UVw>? MVzpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldkB{gW6ncnfpd5Rq[2GubImge4l1cCCkb4L0[ZpwdWmk NWnjRoRTOjVzN{[zOVQ>
769-P M3Xk[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWmyOU82OCCwTR?= Ml;COFghcA>? NIHjbFNFVVOR M{O0b4lvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\SCmZYDlcoRmdnRibXHucoVzKHO7bnXy[4l{fGmlYXzsfUB4cXSqIHLvdpRmgm:vaXK= Mo\xNlUyPzZ|NUS=
Caki-1 NVzLWllmS2:ub375JGZwem2jdHnvckBCe3OjeR?= M33udlUxKG6P NV7ObGhNPy1zNDDk NGS0Z4ZFVVOR NHPiXXV{fXCycnXzd4VlKGOxbH;ufUBnd3KvYYTpc44he2mpbnnmbYNidnSueTDjc41jcW6nZDD3bZRpKHerdHigZo9zfGW8b33pZkDDqA>? M{TNO|I2OTd4M{W0
ACHN NELTflFEd2yxbomgSo9zdWG2aX;uJGF{e2G7 MlexOVAhdk1? M1\N[|cuOTRiZB?= M360bmROW09? NV7Zd|h{e3WycILld5Nm\CClb3zvcpkh\m:{bXH0bY9vKHOrZ37p[olk[W62bImgZ49u[mmwZXSge4l1cCC5aYToJIJwenSnen;tbYIhyqB? NH;KSpAzPTF5NkO1OC=>
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Caki-1 MWDBdI9xfG:|aYOgRZN{[Xl? MX21NEBvVQ>? NIDBSJA1QCCq Mn;XSG1UVw>? M3\Pbolv\HWlZYOgZ4VtdCCjcH;weI9{cXN? NEXuVIwzPTF5NkO1OC=>
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SK-N-AS M3rpN2Z2dmO2aX;uJGF{e2G7 MlzhNQKBmzhyIH7N M1nkWlQ5KGh? NGrX[4pqdmS3Y3XzJIEh\G:|ZT3k[ZBmdmSnboSgZ4xm[X[jZ3Wgc4Yh[2G|cHHz[UA{KGGwZDDQRXJR NEjDNYQzPDB7OEe5PS=>
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HepG2 MV3BdI9xfG:|aYOgRZN{[Xl? NHPKNng2OCCwTR?= MnLBOFghcA>? NX\Zfpo6TE2VTx?= MWrpcoR2[2W|IHPlcIwh[XCxcITvd4l{KHOrZ37p[olk[W62bImgbY4h[SClYYPwZZNmNWSncHXu[IVvfCCvYX7u[ZIh[nliY3zlZZZi\2Vib3[gZ4F{eGG|ZYOgN{whQCCjbnSgPS=> MYOyOFA6Ozl3Nh?=
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HSC4  M3jsc2Fxd3C2b4Ppd{BCe3OjeR?= MYKwMVIxKG6P MXm0PEBp NF3FVGRFVVOR NI\U[lNqdmS3Y3XzJINmdGxiYYDvdJRwe2m| NV7VWZZuOjN6N{eyN|U>
HN22 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mmj0NE0zOCCwTR?= MknVOFghcA>? NEXsOm9FVVOR MVfpcoR2[2W|IFexJJBp[XOnIHPlcIwh[3mlbHWgZZJz\XO2wrC= M3XseVI{QDd5MkO1
HSC4  MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoX3NE0zOCCwTR?= MXS0PEBp NFPMVIpFVVOR NYrwPXZrcW6mdXPld{BIOSCyaHHz[UBk\WyuIHP5Z4xmKGG{cnXzeOKh NYfOXnRqOjN6N{eyN|U>
HN22 MYfGeY5kfGmxbjDBd5NigQ>? NITa[oMxNTJyIH7N NV\i[HlvPDhiaB?= MmfUSG1UVw>? M2\5UZN2eHC{ZYPz[ZMhW3BzIHX4dJJme3Orb39CpC=> MVWyN|g4PzJ|NR?=
HSC4  MnfhSpVv[3Srb36gRZN{[Xl? NF3jeI8xNTJyIH7N NITte5Y1QCCq NGjYRWhFVVOR M1OxOJN2eHC{ZYPz[ZMhW3BzIHX4dJJme3Orb39CpC=> M1zq[FI{QDd5MkO1
Cal62 NFG1[5pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUDJR|UxRTN|INMxJFQhdk1? NXjGbVNiOjN6MkSwOlQ>
Hth7 MlfFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV;0XY9uUUN3ME2xOUDDuSB{IH7N MmnONlM5OjRyNkS=
Hth83 M2nDUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2rQcGlEPTB;M{SgxtEhPSCwTR?= MXmyN|gzPDB4NB?=
C643 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVm1coVGUUN3ME23NUDDuSBzMDDuUS=> MX6yN|gzPDB4NB?=
SW1736 M2n5O2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2fyNGlEPTB;M{WgxtEhQCCwTR?= MYeyN|gzPDB4NB?=
T241 M2e4dGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlvwTWM2OD14NTFCtUA4KG6P NFzGVIwzOzh{NEC2OC=>
T351 M2TBZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV30c|VVUUN3ME21NEDDuSBzMDDuUS=> NUn6TpkzOjN6MkSwOlQ>
BHP2-7 NHTPeFhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWrJR|UxRTN5INMxJFYhdk1? MnOwNlM5OjRyNkS=
T238 NV3kW3pYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoTwTWM2OD1zLEWwNEDDuSB{MECgcm0> NFXzR|gzOzh{NEC2OC=>
HCT8 M2XmPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIP6SGY4OiCq MnK5SG1UVw>? MmDaTWM2OD1zMj655qCKyrIkgJmxMlkhdk1? NFXVNo8zOzJ7OUO4PC=>
H630 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVLKeGloPzJiaB?= NUjzZ3ZSTE2VTx?= NX7ROI1QUUN3ME2xNk416oDLwsJihKk{NjFibl2= MViyN|I6QTN6OB?=
cH630 5-FU-res M1u3Zmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1HV[lczKGh? NGj1[5hFVVOR NYrNPFhkUUN3ME2xOU426oDLwsJihKkyNjJibl2= NUDWUGI4OjN{OUmzPFg>
HCT116 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYnpfoRxPzJiaB?= M2nJSmROW09? MVfJR|UxRTFyLkhihKnDueLCiUKuNkBvVQ>? MViyN|I6QTN6OB?=
HCT116 p53−/− NYnMdHJsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUWwOpdpPzJiaB?= NGfV[YVFVVOR MYrJR|UxRThwNvMAjeKy6oDLMT63JI5O M4jq[FI{Ojl7M{i4
dHCT116 p21−/− NWH1PWs1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3n3eVczKGh? MVTEUXNQ NF\ke2dKSzVyPUWuPgKBkcLz4pEJNU4{KG6P Ml3NNlMzQTl|OEi=
HT29 Mo\GS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoHiO|IhcA>? MlPJSG1UVw>? MlnPTWM2OD1zNj6z5qCKyrIkgJmyMlMhdk1? M3LhZlI{Ojl7M{i4
LoVo MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnjNO|IhcA>? MoXvSG1UVw>? NX\sNZRJUUN3ME21MlHjiIoEsfMAjVAvPiCwTR?= MWKyN|I6QTN6OB?=
RKO NUTr[GdMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXfpeWlzPzJiaB?= MWXEUXNQ NIHsNoFKSzVyPUeuPgKBkcLz4pEJNk4zKG6P M{Hsb|I{Ojl7M{i4
SW480 MljLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4O2S|czKGh? MVnEUXNQ MU\JR|UxRTF5LkZihKnDueLCiUCuPEBvVQ>? NIPNbW4zOzJ7OUO4PC=>
eSW620 Mmf1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mlr5O|IhcA>? NXvmNJRvTE2VTx?= NF\iToNKSzVyPUmuNgKBkcLz4pEJNk4yKG6P NVv1OGFkOjN{OUmzPFg>

... Click to View More Cell Line Experimental Data

In vivo 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]

Protocol

Cell Research:[1]
+ Expand
  • Cell lines: MOLT-4 cell lines and Reh (pre-B cells)
  • Concentrations: 50 nM
  • Incubation Time: 48 hours
  • Method: 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.
    (Only for Reference)
Animal Research:[2]
+ Expand
  • Animal Models: 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
  • Formulation: Dextrose 5% in water
  • Dosages: 10 mg/kg, 20 mg/kg
  • Administration: Administered via i.p. injection
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 69 mg/mL (197.46 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
In vivo 2% DMSO+48% PEG 300+2% Tween 80+ddH2O 5mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* 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 349.43
Formula

C21H23N3O2

CAS No. 404950-80-7
Storage powder
Synonyms NVP-LBH589

Bio Calculators

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02802163 Not yet recruiting Multiple Myeloma H. Lee Moffitt Cancer Center and Research Institute|Novartis|Amgen April 30, 2017 Phase 1|Phase 2
NCT02654990 Recruiting Multiple Myeloma Novartis Pharmaceuticals|Novartis April 27, 2016 Phase 2
NCT02890069 Recruiting Colorectal Cancer|Non-small Cell Lung Carcinoma (Adenocarcinoma)|Triple Negative Breast Cancer Novartis Pharmaceuticals|Novartis October 26, 2016 Phase 1
NCT01802879 Active, not recruiting Hematologic Neoplasms Novartis Pharmaceuticals|Novartis June 24, 2013 Phase 2
NCT00532675 Active, not recruiting Multiple Myeloma Novartis Pharmaceuticals|Novartis April 22, 2008 Phase 1
NCT02961816 Not yet recruiting Lymphoma M.D. Anderson Cancer Center February 2017 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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID