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 44 Publications

8 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.

    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.

Purity & Quality Control

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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 NXLRZYZQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUGwMVExKM7:TR?= M1Ls[VAuPCCm MWjpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCkb4ToJJRqdWVvIHHu[EBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MnL1NlY4ODJ5OES=
HepG2 MoXtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnfkNE0yOCEQvF2= NIDJSGgxNTRiZB?= MoTVbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYn;0bEB1cW2nLTDhcoQh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ MlX2NlY4ODJ5OES=
HT29 M13CfGZ2dmO2aX;uJGF{e2G7 MmTQOVDDqG6P M2HZcVI1NTd{IHi= MlLlbY5lfWOnZDDhZ5RqfmG2aX;uJI9nKGOjc4Dhd4UhOyCjZoTldkA1QMLiaNMg MkHaNlY4ODJ5OES=
HepG2 NF7POFVHfW6ldHnvckBCe3OjeR?= MWi1NOKhdk1? M3TTcFI1NTd{IHi= MkfFbY5lfWOnZDDhZ5RqfmG2aX;uJI9nKGOjc4Dhd4UhOyCjZoTldkAzPMLiaNMg MY[yOlcxOjd6NB?=
HCC827 MoXFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXOwOo86PS95LkWvNVAhdk1? NF\wXpg4OsLiaB?= NIL6NWRFVVOR NHPofHBmdmijbnPld{B1cGViYX70bZBzd2yrZnXyZZRqfmViZX\m[YN1KG:oIHXycI91cW6rYh?= MY[yOlY4PTR6NB?=
A549  NUK4Zmd{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVGxNE8yPS9{MDDuUS=> NIjyc|Q4OsLiaB?= NF;WUW1FVVOR NW\qZoc5\W6qYX7j[ZMhfGinIHHueIlxem:uaX\ldoF1cX[nIHXm[oVkfCCxZjDldoxwfGmwaXK= M4HW[|I3Pjd3NEi0
NCI-H460  NHGzWJZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX[zbHB3OTBxMkCvN|Ahdk1? M4LxdVczyqCq MX\EUXNQ M2nBO4VvcGGwY3XzJJRp\SCjboTpdJJwdGmoZYLheIl3\SCnZn\lZ5Qhd2ZiZYLsc5Rqdmmk MXSyOlY4PTR6NB?=
J89GFP Mn7OS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXrEUXNQyqB? M2K2TWVEPTB;NEmuPFUhyrFiMUKuOlUhdk1? Ml62NlY2PjN3Nki=
THP89GFP M2iyXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXLEUXNQyqB? NWe5dW93TUN3ME2xPU4{PCEEsTC2MlQ{KG6P MmL2NlY2PjN3Nki=
SK-NEP-1 NF32RY9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYfOWWptOC5yMfMAl|ExNjBizszN NFjmUYMzPCCq MkfoSG1UV8Li MWrJR|UxRTd4LkO0JI5O M1;4blI3OTd4MkG5
G401 M3r2ZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYXjU3c2OC5yMfMAl|ExNjBizszN MWSyOEBp M3HPXmROW00EoB?= MXzJR|UxRTF2Mz6wNkBvVQ>? MXKyOlE4PjJzOR?=
SK-NEP-1 M2PreWNmdGxiVnnhZoltcXS7IFHzd4F6 MXO1NEBvVQ>? NXfjXXVyOeLCk{Sg[C=> Mlj2SG1UV8Li MlW4doVlfWOnczDj[YxtKHO3co\peoFtKGmwIHGgeIlu\SCmZYDlcoRmdnRibXHucoVz MVeyOlE4PjJzOR?=
G401 M1j4cGNmdGxiVnnhZoltcXS7IFHzd4F6 NUOwc3hjPTBibl2= NFHMXY0y6oDVNDDk NHTKdHJFVVORwrC= MmDGdoVlfWOnczDj[YxtKHO3co\peoFtKGmwIHGgeIlu\SCmZYDlcoRmdnRibXHucoVz MkTZNlYyPzZ{MUm=
SK-NEP-1 NXTxbYxGSXCxcITvd4l{KEG|c3H5 M{[1WlUxNzFyMDDuUS=> MV[yOEBp MWjEUXNQyqB? NYfIO5hzcW6mdXPld{Bk\WyuIHHwc5B1d3OrczDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= M1XjSFI3OTd4MkG5
G401 M2rESGFxd3C2b4Ppd{BCe3OjeR?= NF71d5o2OC9zMECgcm0> MVOyOEBp NW[wZ|ZmTE2VT9Mg MoPjbY5lfWOnczDj[YxtKGGyb4D0c5NqeyCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? MWmyOlE4PjJzOR?=
SK-NEP-1 M3\qV2Z2dmO2aX;uJGF{e2G7 NFzGN3A2OC9zMECgcm0> MoDvNlQhcA>? MkjVSG1UV8Li M3ywTpNpd3e|IITo[UBqdmS3Y4Tpc44hd2ZiRF7BJIZz[WevZX70ZZRqd25? MXKyOlE4PjJzOR?=
G401 NV;I[WZkTnWwY4Tpc44hSXO|YYm= NVGxN3J3PTBxMUCwJI5O MkfxNlQhcA>? MkfoSG1UV8Li NIHNdJl{cG:5czD0bIUhcW6mdXP0bY9vKG:oIFTORUBnemGpbXXueIF1cW:w MVOyOlE4PjJzOR?=
SK-NEP-1 NVLHcGw1TnWwY4Tpc44hSXO|YYm= Mlz0OVAwOTByIH7N MnS1NlQhcA>? NUPUV3NCTE2VT9Mg MVzpcoR2[2W|IHPlcIwh[3mlbHWg[Il{d3KmZYNCpC=> NH\4NoIzPjF5NkKxPS=>
G401 NETxUohHfW6ldHnvckBCe3OjeR?= MXK1NE8yODBibl2= Mmi2NlQhcA>? NInKfVRFVVORwrC= NXPVOlZKcW6mdXPld{Bk\WyuIHP5Z4xmKGSrc3;y[IVzyqB? MUeyOlE4PjJzOR?=
RPMI 8226 MoK0R4VtdCCVdYL2bZZidCCDc4PhfS=> MVeyM|QwPiCwTR?= NVfteYdwPDkkgJno NUDvNnVzcW6mdXPld{BiKHOrZ37p[olk[W62IHTlZ5Jm[XOnIHnuJJRp\SClZXzsJIdzd3e2aB?= MYGyOlAxODJ7Mh?=
OPM2 MYDD[YxtKFO3co\peoFtKEG|c3H5 NVOzb3kxOi92L{[gcm0> NV20NJdMPDkkgJno MoX3bY5lfWOnczDhJJNq\26rZnnjZY51KGSnY4LlZZNmKGmwIITo[UBk\WyuIHfyc5d1cA>? MnvTNlYxODB{OUK=
U266 Mo\pR4VtdCCVdYL2bZZidCCDc4PhfS=> NVvKTG0yOi92L{[gcm0> MnLoOFjjiImq NVvWZmpucW6mdXPld{BiKHOrZ37p[olk[W62IHTlZ5Jm[XOnIHnuJJRp\SClZXzsJIdzd3e2aB?= M37sdVI3ODByMkmy
H929 MVLD[YxtKFO3co\peoFtKEG|c3H5 M3rFVlIwPC94IH7N NIHINmE1QOLCiXi= MVfpcoR2[2W|IHGgd4lodmmoaXPhcpQh\GWlcnXhd4UhcW5idHjlJINmdGxiZ4Lve5Rp MXuyOlAxODJ7Mh?=
RPMI 8226  M3;DfWFxd3C2b4Ppd{BCe3OjeR?= Ml7vOQKBkW6P Mmn5NlQwPDhiaB?= NU\zcmJKcW6mdXPld{Bk\WyuIHHwc5B1d3OrczDpckBiKHSrbXWt[IVx\W6mZX70JI1idm6nch?= NVnzRVJ5OjZyMECyPVI>
HCC827 M1rMWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIfvfoMyOCCwTR?= M3;6fFQ5KGh? MkK3SG1UVw>? MYXlcohidmOnczDjbZNxdGG2aX6gd4Vve2m2aY\peJnDqA>? NIjpfJkzPTl2NE[xOy=>
NCI-H23 M1vkVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHXNbGUyOCCwTR?= MmT2OFghcA>? MWTEUXNQ NFP2bGdmdmijbnPld{BkcXOybHH0bY4he2Wwc3n0bZZqfHoEoB?= MUKyOVk1PDZzNx?=
AML3 Mnr4SpVv[3Srb36gRZN{[Xl? MlyzNE0yKM7:TR?= MXuyOOKhcA>? M3Hoe4lv\HWlZYOgSG5CKG[{YXft[Y51[XSrb39CpIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy M4XRPVI2PjF{OUSx
ML-1 NGDFNoZHfW6ldHnvckBCe3OjeR?= NFTOV28xNTFizszN M2\3RVI1yqCq NWryOIZWcW6mdXPld{BFVkFiZoLh[41mdnSjdHnvcuKhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NU\DSVVoOjV4MUK5OFE>
RPMI-8226vr10  MVPGeY5kfGmxbjDBd5NigQ>? MonUNE0yKM7:TR?= NYizRZZlOjUEoHi= NV63WZp2cW6mdXPld{BFVkFiZoLh[41mdnSjdHnvcuKhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NGHGSlAzPTZzMkm0NS=>
ML-1 NInxPZJHfW6ldHnvckBCe3OjeR?= M3LkS|Eh|ryP MUmyOOKhcA>? NHHtenBqdmO{ZXHz[ZMh[2G|cHHz[U0{KGGldHn2bZR6KDRvZn;s[C=> MYiyOVYyOjl2MR?=
RPMI-8226vr10  MkLRSpVv[3Srb36gRZN{[Xl? MlHGNUDPxE1? M3rHNVI1yqCq MVvpcoNz\WG|ZYOgZ4F{eGG|ZT2zJIFkfGm4aYT5JFIvPS2ob3zk Mn;XNlU3OTJ7NEG=
SK-N-BE (2) MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFnCfJEzPOLCiXi= M1[yT2lEPTB;MUC0MlDjiIoEsfMAjVcvQCCwTR?= NXzCbJZoOjV|MEi5NVY>
SK-N-BE (2), PAN  MK MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWiyOQKBkWh? M1fWdWlEPTB;MUC0MlDjiIoEsfMAjVcvQCCwTR?= NWqyfGZnOjV|MEi5NVY>
SK-N-BE (2), MK  PAN NW\vW5dGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mlv0NlTjiImq MWXJR|UxRTN6Mj6w5qCKyrIkgJm0N{4zKG6P M4qwTlI2OzB6OUG2
SK-N-AS M3Hibmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3nqNFI16oDLaB?= MVTJR|UxRTN5LkJihKnDueLCiUKuOEBvVQ>? MlLLNlU{ODh7MU[=
SK-N-DZ NIXtVHZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV\5e2ZvOjUkgJno NWPlS5I2UUN3ME2xO{4y6oDLwsJihKkxNjRibl2= Mn\xNlU{ODh7MU[=
Caki-1 NFnxdGNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4XQfVExNzJ3L{WwJI5O Mnn2OFghcA>? NIjldoxqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meiC|eX7ldodqe3SrY3HscJkhf2m2aDDybZRwdmG4aYK= M1zHVFI2Ojd7MUmx
ACHN M4e3[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHzUfpYyOC9{NT:1NEBvVQ>? NVPpclV3PDhiaB?= MWfpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldkB{gW6ncnfpd5Rq[2GubImge4l1cCC{aYTvcoF3cXJ? NV7hSoZVOjV{N{mxPVE>
769-P NV\OVHpOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEjqc|cyOC9{NT:1NEBvVQ>? NWnnVFdZPDhiaB?= M1[zUolvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\SCmZYDlcoRmdnRibXHucoVzKHO7bnXy[4l{fGmlYXzsfUB4cXSqIILpeI9v[X[rch?= M2jMTlI2Ojd7MUmx
786-O  NVHyOGpvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M33UXFExNzJ3L{WwJI5O NHPYUZI1QCCq NWr0VpllcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJic4nu[ZJocXO2aXPhcIx6KHerdHigdol1d26jdnny MW[yOVI4QTF7MR?=
Caki-1 MWHBdI9xfG:|aYOgRZN{[Xl? MUi1NEBvVQ>? MkDoOFghcA>? MWrpcoR2[2W|IHPlcIwh[XCxcITvd4l{KGOxbXLpcoVlKHKrdH;uZZZqeg>? NIm3cWYzPTJ5OUG5NS=>
ACHN NWD6[lQ4SXCxcITvd4l{KEG|c3H5 M1;HNlUxKG6P NFfZNWM1QCCq MkPzbY5lfWOnczDj[YxtKGGyb4D0c5NqeyClb33ibY5m\CC{aYTvcoF3cXJ? MUOyOVI4QTF7MR?=
769-P M2PsVGFxd3C2b4Ppd{BCe3OjeR?= Ml3XOVAhdk1? NXHMV25IPDhiaB?= Mm\NbY5lfWOnczDj[YxtKGGyb4D0c5NqeyClb33ibY5m\CC{aYTvcoF3cXJ? NYrDTVB[OjV{N{mxPVE>
786-O  NV65TnhISXCxcITvd4l{KEG|c3H5 M4DDTFUxKG6P MVS0PEBp M2C4Uolv\HWlZYOgZ4VtdCCjcH;weI9{cXNiY3;tZolv\WRicnn0c45ifmm{ MUOyOVI4QTF7MR?=
Caki-1 NV2zfpV{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mnf0NlUwPTBibl2= NVrPTXpJPDhiaB?= MnTHSG1UVw>? MV;pcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldkB{gW6ncnfpd5Rq[2GubImge4l1cCCkb4L0[ZpwdWmk MlLvNlUyPzZ|NUS=
ACHN Mlr0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NY\kXGpNOjVxNUCgcm0> M3q4UFQ5KGh? Ml7xSG1UVw>? NXrKNmFJcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJic4nu[ZJocXO2aXPhcIx6KHerdHigZo9zfGW8b33pZi=> NG\SbY0zPTF5NkO1OC=>
769-P MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVKyOU82OCCwTR?= MnzSOFghcA>? MnX0SG1UVw>? M1\wUYlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\SCmZYDlcoRmdnRibXHucoVzKHO7bnXy[4l{fGmlYXzsfUB4cXSqIHLvdpRmgm:vaXK= NHrmbVQzPTF5NkO1OC=>
Caki-1 MmjLR49td267IF\vdo1ifGmxbjDBd5NigQ>? M1;WOFUxKG6P M2W4dlcuOTRiZB?= MUXEUXNQ NIHMZ5R{fXCycnXzd4VlKGOxbH;ufUBnd3KvYYTpc44he2mpbnnmbYNidnSueTDjc41jcW6nZDD3bZRpKHerdHigZo9zfGW8b33pZkDDqA>? MVqyOVE4PjN3NB?=
ACHN M3HjfWNwdG:weTDGc5Ju[XSrb36gRZN{[Xl? NFHKepc2OCCwTR?= MVm3MVE1KGR? NXG0b2JsTE2VTx?= M2XDV5N2eHC{ZYPz[YQh[2:ub375JIZwem2jdHnvckB{cWewaX\pZ4FvfGy7IHPvcYJqdmWmIIfpeIghf2m2aDDic5J1\XqxbXniJOKh MmL1NlUyPzZ|NUS=
769-P NHWzfGFEd2yxbomgSo9zdWG2aX;uJGF{e2G7 Mke5OVAhdk1? M{DOd|cuOTRiZB?= NVLndol{TE2VTx?= M3fRTJN2eHC{ZYPz[YQh[2:ub375JIZwem2jdHnvckB{cWewaX\pZ4FvfGy7IHPvcYJqdmWmIIfpeIghf2m2aDDic5J1\XqxbXniJOKh NGm2SVYzPTF5NkO1OC=>
Caki-1 MUXBdI9xfG:|aYOgRZN{[Xl? M3vS[FUxKG6P NX2yV21{PDhiaB?= M1OwUmROW09? MUHpcoR2[2W|IHPlcIwh[XCxcITvd4l{ NV3UcYtMOjVzN{[zOVQ>
ACHN NWTlUnZ6SXCxcITvd4l{KEG|c3H5 NWfK[I9iPTBibl2= MV20PEBp MnnoSG1UVw>? MlzCbY5lfWOnczDj[YxtKGGyb4D0c5Nqew>? MoC3NlUyPzZ|NUS=
769-P M1riWWFxd3C2b4Ppd{BCe3OjeR?= MYG1NEBvVQ>? MX60PEBp M37YWmROW09? MUDpcoR2[2W|IHPlcIwh[XCxcITvd4l{ M1LieVI2OTd4M{W0
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Hth7 NEfD[WZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlTCTWM2OD1zNTFCtUAzKG6P M4\sOFI{QDJ2ME[0
Hth83 NIj1XY5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEjHbYFKSzVyPUO0JOKyKDVibl2= MnXwNlM5OjRyNkS=
C643 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4LJfWlEPTB;N{GgxtEhOTBibl2= NWnhe3FYOjN6MkSwOlQ>
SW1736 NHTMXmpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX71enY2UUN3ME2zOUDDuSB6IH7N Mk\vNlM5OjRyNkS=
T241 NHvjenRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYHrNnlkUUN3ME22OUDDuSB5IH7N M4SxeFI{QDJ2ME[0
T351 MoLJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYXJR|UxRTVyINMxJFExKG6P NIXKT2MzOzh{NEC2OC=>
BHP2-7 M2\TOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXvZc5pEUUN3ME2zO{DDuSB4IH7N MWqyN|gzPDB4NB?=
T238 MoDBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVrYbol4UUN3ME2xMFUxOCEEsTCyNFAhdk1? MXWyN|gzPDB4NB?=
HCT8 MkTpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV7F[3Z5PzJiaB?= NGP0[5dFVVOR MonpTWM2OD1zMj655qCKyrIkgJmxMlkhdk1? M1jRXVI{Ojl7M{i4
H630 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{D1U|czKGh? MXjEUXNQ NUDuZW1YUUN3ME2xNk416oDLwsJihKk{NjFibl2= NXruPIRKOjN{OUmzPFg>
cH630 5-FU-res MoDzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2LLO|czKGh? M{nC[mROW09? MoXDTWM2OD1zNT615qCKyrIkgJmxMlIhdk1? NVHWUINvOjN{OUmzPFg>
HCT116 NHfVUYFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NW\tc5ZGPzJiaB?= Mlz1SG1UVw>? M37QS2lEPTB;MUCuO-KBkcLz4pEJNk4zKG6P MnPNNlMzQTl|OEi=
HCT116 p53−/− M17tfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH6zcnE4OiCq M3XHUWROW09? NUXlZ|AyUUN3ME24MlbjiIoEsfMAjVEvPyCwTR?= NXX0bmdNOjN{OUmzPFg>
dHCT116 p21−/− NFnyVopIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1fiflczKGh? NEW3eGhFVVOR Mn:5TWM2OD13LkpihKnDueLCiUGuN{BvVQ>? M16xWVI{Ojl7M{i4
HT29 MoexS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4PndFczKGh? NYXjbJN7TE2VTx?= MkfLTWM2OD1zNj6z5qCKyrIkgJmyMlMhdk1? MUiyN|I6QTN6OB?=
LoVo NVzOfXl[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIO5O3A4OiCq M2DMNGROW09? MlXRTWM2OD13LkJihKnDueLCiUCuOkBvVQ>? NVfTNYhZOjN{OUmzPFg>
RKO MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFvSV3A4OiCq NVLaWpRkTE2VTx?= MUjJR|UxRTdwOfMAjeKy6oDLMj6yJI5O MmfGNlMzQTl|OEi=
SW480 NIO3NIhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVO2OVdWPzJiaB?= NILyPG1FVVOR MWPJR|UxRTF5LkZihKnDueLCiUCuPEBvVQ>? MUeyN|I6QTN6OB?=
eSW620 NEfYXlZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYfFbnlKPzJiaB?= MWTEUXNQ NE\4OpdKSzVyPUmuNgKBkcLz4pEJNk4yKG6P MYKyN|I6QTN6OB?=

... 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

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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