Panobinostat (LBH589)

目录号:S1030 别名: NVP-LBH589

Panobinostat (LBH589) Chemical Structure

Molecular Weight(MW): 349.43

Panobinostat (LBH589)是一种新型的,广谱HDAC抑制剂,无细胞试验中IC50为5 nM。Phase 3。

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客户购买Selleck的此次产品后发表的文献52篇:

客户使用该产品的12个实验数据:

  • (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.

产品安全说明书

HDAC抑制剂选择性比较

生物活性

产品描述 Panobinostat (LBH589)是一种新型的,广谱HDAC抑制剂,无细胞试验中IC50为5 nM。Phase 3。
靶点
HDAC (MOLT-4 cells) [1] HDAC (Reh cells) [1]
5 nM 20 nM
体外研究

LBH589诱导MOLT-4和Reh细胞凋亡,这种作用具有时间和剂量依赖性。而且,LBH589作用于MOLT-4细胞比作用于Reh细胞更有效。LBH589明显阻止MOLT-4 和Reh细胞的生长,处理48小时,具有剂量依赖性。与对照组细胞相比,用LBH589处理的细胞,在细胞周期的G2/M期的细胞数量增多2到3倍。LBH589与组蛋白H3K9和H4K8的乙酰化作用相关,LBH589也降低c-Myc的表达水平,具有剂量依赖性。LBH589也增强p21的表达水平。最低剂量的LBH589(10 nM)处理Reh细胞,最初增强c-Myc的表达水平,之后一直降低c-Myc的表达水平。此外,LBH589促进mRNA水平的促凋亡和DNA修复基因的大量增多。在GADD45G启动子作用下,LBH589诱导乙酰化的组蛋白H3 和H4水平的增多。[1]此外, LBH589抑制非小细胞肺癌细胞系生长,如人类H1299,L55和A549,IC50分别为5,11和30 nM;间皮瘤细胞生长,如人类OK-6和 Ok-5,IC50分别为5和7 nM;及小细胞肺癌细胞系生长,如人类RG-1和LD-T,IC50分别为4和5 nM。[2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HT29 NX3lUFJJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mnz3NE0yOCEQvF2= M1rHWVAuPCCm MnvCbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYn;0bEB1cW2nLTDhcoQh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ MUiyOlcxOjd6NB?=
HepG2 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGT5VHMxNTFyIN88US=> NIfmcGwxNTRiZB?= NGPydYxqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDic5RpKHSrbXWtJIFv\CCmb4PlMYRmeGWwZHXueEBu[W6wZYK= NWe5eXA{OjZ5MEK3PFQ>
HT29 MkPhSpVv[3Srb36gRZN{[Xl? NVPzWlZiPTEEoH7N M165VFI1NTd{IHi= NIjZNHZqdmS3Y3XkJIFkfGm4YYTpc44hd2ZiY3HzdIF{\SB|IHHmeIVzKDR6wrDoxsA> NH[zSVczPjdyMke4OC=>
HepG2 MonrSpVv[3Srb36gRZN{[Xl? MnzZOVDDqG6P M3i4OVI1NTd{IHi= NIrSXYpqdmS3Y3XkJIFkfGm4YYTpc44hd2ZiY3HzdIF{\SB|IHHmeIVzKDJ2wrDoxsA> NXHWZnRtOjZ5MEK3PFQ>
HCC827 M{DEfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVjiV3Y1PS95LkWvNVAhdk1? M{LpbFczyqCq NYHiPIZKTE2VTx?= NF\zR2pmdmijbnPld{B1cGViYX70bZBzd2yrZnXyZZRqfmViZX\m[YN1KG:oIHXycI91cW6rYh?= NGf2[|AzPjZ5NUS4OC=>
A549  M2GwU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXnlUGl[OTBxMUWvNlAhdk1? M2rUSVczyqCq NIC0d2hFVVOR NV3LTllD\W6qYX7j[ZMhfGinIHHueIlxem:uaX\ldoF1cX[nIHXm[oVkfCCxZjDldoxwfGmwaXK= NYH2V2U6OjZ4N{W0PFQ>
NCI-H460  M2fQNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYHMToZqOTBxMkCvN|Ahdk1? M1fWcVczyqCq MkPJSG1UVw>? M17UdIVvcGGwY3XzJJRp\SCjboTpdJJwdGmoZYLheIl3\SCnZn\lZ5Qhd2ZiZYLsc5Rqdmmk MkLuNlY3PzV2OES=
J89GFP NIr5eoNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MojnSG1UV8Li NYfLc5d[TUN3ME20PU45PSEEsTCxNk43PSCwTR?= MUmyOlU3OzV4OB?=
THP89GFP MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGO0[YlFVVORwrC= MmfPSWM2OD1zOT6zOEDDuSB4LkSzJI5O M3XrdVI3PTZ|NU[4
SK-NEP-1 MlGwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVuwMlAy6oDVMUCuNEDPxE1? MlPpNlQhcA>? M{nGd2ROW00EoB?= MY\JR|UxRTd4LkO0JI5O M3fLflI3OTd4MkG5
G401 NYL0VnZ5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn7kNE4xOeLCk{GwMlAh|ryP MYeyOEBp MWTEUXNQyqB? M1X0cmlEPTB;MUSzMlAzKG6P NVzJPJl4OjZzN{[yNVk>
SK-NEP-1 M33hTWNmdGxiVnnhZoltcXS7IFHzd4F6 NV7vboxSPTBibl2= NW\mU5FbOeLCk{Sg[C=> MlnhSG1UV8Li M1:1WJJm\HWlZYOgZ4VtdCC|dYL2bZZidCCrbjDhJJRqdWViZHXw[Y5l\W62IH3hco5meg>? MYOyOlE4PjJzOR?=
G401 NWrOUow{S2WubDDWbYFjcWyrdImgRZN{[Xl? MXi1NEBvVQ>? NGDmRpEy6oDVNDDk MWLEUXNQyqB? MVPy[YR2[2W|IHPlcIwhe3W{dnn2ZYwhcW5iYTD0bY1mKGSncHXu[IVvfCCvYX7u[ZI> Mo[0NlYyPzZ{MUm=
SK-NEP-1 NHT4dnhCeG:ydH;zbZMhSXO|YYm= NUHhOYl3PTBxMUCwJI5O NUnPR5BEOjRiaB?= MWfEUXNQyqB? MWjpcoR2[2W|IHPlcIwh[XCxcITvd4l{KGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NWq5ZWF{OjZzN{[yNVk>
G401 NXv6WXplSXCxcITvd4l{KEG|c3H5 NIjwXlc2OC9zMECgcm0> MVOyOEBp MnH5SG1UV8Li MkDmbY5lfWOnczDj[YxtKGGyb4D0c5NqeyCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? Mn31NlYyPzZ{MUm=
SK-NEP-1 NIriWFlHfW6ldHnvckBCe3OjeR?= NISwR2c2OC9zMECgcm0> MkHaNlQhcA>? MmnYSG1UV8Li NGP3cYp{cG:5czD0bIUhcW6mdXP0bY9vKG:oIFTORUBnemGpbXXueIF1cW:w MoDWNlYyPzZ{MUm=
G401 NILacpBHfW6ldHnvckBCe3OjeR?= NW\leG1[PTBxMUCwJI5O MUmyOEBp MnqySG1UV8Li NIDqZWp{cG:5czD0bIUhcW6mdXP0bY9vKG:oIFTORUBnemGpbXXueIF1cW:w NF;2RZEzPjF5NkKxPS=>
SK-NEP-1 MmDISpVv[3Srb36gRZN{[Xl? NYjtVItlPTBxMUCwJI5O MXKyOEBp M4PER2ROW00EoB?= M4TTd4lv\HWlZYOgZ4VtdCCleXPs[UBlcXOxcnTlduKh MXSyOlE4PjJzOR?=
G401 MWDGeY5kfGmxbjDBd5NigQ>? NEG0OXg2OC9zMECgcm0> M3\pSFI1KGh? NVXCNZBkTE2VT9Mg NYSxPZV{cW6mdXPld{Bk\WyuIHP5Z4xmKGSrc3;y[IVzyqB? MXGyOlE4PjJzOR?=
RPMI 8226 Mn;PR4VtdCCVdYL2bZZidCCDc4PhfS=> NUj3[lZNOi92L{[gcm0> MWS0PQKBkWh? MXfpcoR2[2W|IHGgd4lodmmoaXPhcpQh\GWlcnXhd4UhcW5idHjlJINmdGxiZ4Lve5Rp MX6yOlAxODJ7Mh?=
OPM2 M2\q[GNmdGxiU4Xyeol3[WxiQYPzZZk> NY\EfWRwOi92L{[gcm0> M1S2N|Q56oDLaB?= M4PMS4lv\HWlZYOgZUB{cWewaX\pZ4FvfCCmZXPy[YF{\SCrbjD0bIUh[2WubDDndo94fGh? M2Lm[lI3ODByMkmy
U266 Mm\IR4VtdCCVdYL2bZZidCCDc4PhfS=> MWWyM|QwPiCwTR?= NG[yeng1QOLCiXi= Mm\NbY5lfWOnczDhJJNq\26rZnnjZY51KGSnY4LlZZNmKGmwIITo[UBk\WyuIHfyc5d1cA>? M2rsO|I3ODByMkmy
H929 M3LNbGNmdGxiU4Xyeol3[WxiQYPzZZk> MmX4Nk81NzZibl2= NWrTc5pVPDkkgJno MWnpcoR2[2W|IHGgd4lodmmoaXPhcpQh\GWlcnXhd4UhcW5idHjlJINmdGxiZ4Lve5Rp MYOyOlAxODJ7Mh?=
RPMI 8226  NXrl[JAzSXCxcITvd4l{KEG|c3H5 MlTvOQKBkW6P NUnnOY5vOjRxNEigbC=> NGizbWFqdmS3Y3XzJINmdGxiYYDvdJRwe2m|IHnuJIEhfGmvZT3k[ZBmdmSnboSgcYFvdmW{ M4raXlI3ODByMkmy
HCC827 M2j3d2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoL0NVAhdk1? MmTPOFghcA>? MWfEUXNQ M1jGSoVvcGGwY3XzJINqe3CuYYTpckB{\W6|aYTpeol1gcLi M2HadlI2QTR2NkG3
NCI-H23 MlnTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{\R[lExKG6P MkjzOFghcA>? NWjIN45KTE2VTx?= MV3lcohidmOnczDjbZNxdGG2aX6gd4Vve2m2aY\peJnDqA>? MWGyOVk1PDZzNx?=
AML3 MVLGeY5kfGmxbjDBd5NigQ>? NFXF[YsxNTFizszN NHSzcoEzPMLiaB?= MnvEbY5lfWOnczDEUmEh\nKjZ33lcpRifGmxbtMgbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK= M1Py[FI2PjF{OUSx
ML-1 M4fjbWZ2dmO2aX;uJGF{e2G7 MW[wMVEh|ryP MXKyOOKhcA>? NWDEe4xYcW6mdXPld{BFVkFiZoLh[41mdnSjdHnvcuKhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> M4fWZVI2PjF{OUSx
RPMI-8226vr10  NYDpfnFMTnWwY4Tpc44hSXO|YYm= MV2wMVEh|ryP MXuyOOKhcA>? M2LveYlv\HWlZYOgSG5CKG[{YXft[Y51[XSrb39CpIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy MnflNlU3OTJ7NEG=
ML-1 MWHGeY5kfGmxbjDBd5NigQ>? NY\iSWVxOSEQvF2= NXqxWmJMOjUEoHi= NITqbHpqdmO{ZXHz[ZMh[2G|cHHz[U0{KGGldHn2bZR6KDRvZn;s[C=> M4LEVVI2PjF{OUSx
RPMI-8226vr10  NX\IfY0{TnWwY4Tpc44hSXO|YYm= NYnIeWZmOSEQvF2= MYOyOOKhcA>? MVLpcoNz\WG|ZYOgZ4F{eGG|ZT2zJIFkfGm4aYT5JFIvPS2ob3zk MVGyOVYyOjl2MR?=
SK-N-BE (2) NYe3WmhbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWfpZ2s5OjUkgJno M2nBdWlEPTB;MUC0MlDjiIoEsfMAjVcvQCCwTR?= MUWyOVMxQDlzNh?=
SK-N-BE (2), PAN  MK MoLkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVqyOQKBkWh? NHrWUGhKSzVyPUGwOE4x6oDLwsJihKk4Njhibl2= NYHmRWdVOjV|MEi5NVY>
SK-N-BE (2), MK  PAN NHr0T2pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M33udlI16oDLaB?= MXjJR|UxRTN6Mj6w5qCKyrIkgJm0N{4zKG6P M2Pl[FI2OzB6OUG2
SK-N-AS M4jPNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnzpNlTjiImq MXPJR|UxRTN5LkJihKnDueLCiUKuOEBvVQ>? NHPDU3kzPTNyOEmxOi=>
SK-N-DZ M2XRVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{DXelI16oDLaB?= NHX0[4tKSzVyPUG3MlHjiIoEsfMAjVAvPCCwTR?= MY[yOVMxQDlzNh?=
Caki-1 M4X4XGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4WyPFExNzJ3L{WwJI5O MlrFOFghcA>? Mnn1bY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZIhe3mwZYLnbZN1cWOjbHz5JJdqfGhicnn0c45ifmm{ NHe4Z3AzPTJ5OUG5NS=>
ACHN M{nyemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmD1NVAwOjVxNUCgcm0> NE\4R|A1QCCq MWTpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldkB{gW6ncnfpd5Rq[2GubImge4l1cCC{aYTvcoF3cXJ? NGHEPZUzPTJ5OUG5NS=>
769-P M2Ppb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1W4XVExNzJ3L{WwJI5O MoO5OFghcA>? M{XEZYlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\SCmZYDlcoRmdnRibXHucoVzKHO7bnXy[4l{fGmlYXzsfUB4cXSqIILpeI9v[X[rch?= NYTUZppFOjV{N{mxPVE>
786-O  NU\DXYZFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH7Tb5EyOC9{NT:1NEBvVQ>? NXjTTGJiPDhiaB?= NEOxeXZqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meiC|eX7ldodqe3SrY3HscJkhf2m2aDDybZRwdmG4aYK= NETa[XkzPTJ5OUG5NS=>
Caki-1 MoDaRZBweHSxc3nzJGF{e2G7 MVm1NEBvVQ>? MofROFghcA>? NHTD[ppqdmS3Y3XzJINmdGxiYYDvdJRwe2m|IHPvcYJqdmWmIILpeI9v[X[rch?= NEDBWmgzPTJ5OUG5NS=>
ACHN NGfJNXZCeG:ydH;zbZMhSXO|YYm= NVXLd5A1PTBibl2= M3f3SVQ5KGh? MnfUbY5lfWOnczDj[YxtKGGyb4D0c5NqeyClb33ibY5m\CC{aYTvcoF3cXJ? M3TBfFI2Ojd7MUmx
769-P NVXYe20zSXCxcITvd4l{KEG|c3H5 NWDNXVhEPTBibl2= NYrQfFdRPDhiaB?= NWrkVIhPcW6mdXPld{Bk\WyuIHHwc5B1d3OrczDjc41jcW6nZDDybZRwdmG4aYK= MWSyOVI4QTF7MR?=
786-O  M1HPc2Fxd3C2b4Ppd{BCe3OjeR?= Mkj1OVAhdk1? M3LBbVQ5KGh? M2jWfIlv\HWlZYOgZ4VtdCCjcH;weI9{cXNiY3;tZolv\WRicnn0c45ifmm{ NGPleG8zPTJ5OUG5NS=>
Caki-1 NGn0TWlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml[5NlUwPTBibl2= NF\KV|U1QCCq NI[yfoVFVVOR MX\pcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldkB{gW6ncnfpd5Rq[2GubImge4l1cCCkb4L0[ZpwdWmk NXTDN4Q6OjVzN{[zOVQ>
ACHN MnHtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX[yOU82OCCwTR?= M1r6blQ5KGh? NFTzOpFFVVOR NXHqVZY6cW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJic4nu[ZJocXO2aXPhcIx6KHerdHigZo9zfGW8b33pZi=> MWeyOVE4PjN3NB?=
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SK-N-BE NF\FTZBCeG:ydH;zbZMhSXO|YYm= MVOw5qCUPDBibl2= NG\m[mE1QCCq NF\QflVxd3SnboTsfUBqdmS3Y3XkJIFxd3C2b4Ppd{BqdiCjIHTvd4Uu\GWyZX7k[Y51KG[jc3jpc44> NUPKVFNNOjRyOUi3PVk>
SK-N-AS MlPaSpVv[3Srb36gRZN{[Xl? NIXa[4Mx6oDVOECgcm0> MVK0PEBp M3;HN4lv\HWlZYOgZUBld3OnLXTldIVv\GWwdDDjcIVifmGpZTDv[kBk[XOyYYPlJFMh[W6mIGDBVnA> M3[xZlI1ODl6N{m5
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L3.6pl MWPBdI9xfG:|aYOgRZN{[Xl? NIW5b4YzPS93MD:xNFAhdk1? MlvsOFghcA>? MXfEUXNQ NFWyPHRqdmS3Y3XzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NFe5fm4zOzl{Mki4Oi=>
CFPAC-1  MnPzRZBweHSxc3nzJGF{e2G7 NX\UcmFoOjVxNUCvNVAxKG6P MX[0PEBp NIHTW3VFVVOR MoD2bY5lfWOnczDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NXXqR3BvOjN7MkK4PFY>
HN22 NGnBdoRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml7ENE0zOCCwTR?= MV:yOE81QCCq MX;EUXNQ NXXoNIJkcW6qaXLpeJMh[2WubDD2bYFjcWyrdImgbY4h[m:2aDD0bY1mNSCjbnSg[I9{\S1iZHXw[Y5l\W62IH3hco5meg>? NEX2cpkzOzh5N{KzOS=>
HSC4  NGHEWZFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFrrRYQxNTJyIH7N NF\hWVIzPC92ODDo MoH4SG1UVw>? M3vYfolvcGmkaYTzJINmdGxidnnhZoltcXS7IHnuJIJwfGhidHnt[U0h[W6mIHTvd4UuKGSncHXu[IVvfCCvYX7u[ZI> MWqyN|g4PzJ|NR?=
HN22 NYGxRWdnSXCxcITvd4l{KEG|c3H5 MormNE0zOCCwTR?= Ml;sOFghcA>? NHz2W5JFVVOR Mn;3bY5lfWOnczDj[YxtKGGyb4D0c5Nqew>? M4LSO|I{QDd5MkO1
HSC4  NVvwbXI6SXCxcITvd4l{KEG|c3H5 MWOwMVIxKG6P NFjVV3Y1QCCq NH\iTIVFVVOR NV7md4RRcW6mdXPld{Bk\WyuIHHwc5B1d3Orcx?= M{L2[lI{QDd5MkO1
HN22 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGjoXmcxNTJyIH7N NUnwWlNZPDhiaB?= NY\ad5ROTE2VTx?= NIDHPYRqdmS3Y3XzJGcyKHCqYYPlJINmdGxiY4njcIUh[XK{ZYP0xsA> MmPMNlM5Pzd{M{W=
HSC4  MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoCyNE0zOCCwTR?= MXy0PEBp NWfTVox7TE2VTx?= Mo\VbY5lfWOnczDHNUBxcGG|ZTDj[YxtKGO7Y3zlJIFzemW|dNMg M{K2e|I{QDd5MkO1
HN22 NYixcIFxTnWwY4Tpc44hSXO|YYm= NVj3OXVMOC1{MDDuUS=> MWO0PEBp NXrh[3ExTE2VTx?= NVPhcWcxe3WycILld5NmeyCVcEGg[ZhxemW|c3nvcuKh MmX5NlM5Pzd{M{W=
HSC4  NIXVbnBHfW6ldHnvckBCe3OjeR?= M13aclAuOjBibl2= M{e0PFQ5KGh? M2n4eWROW09? NVzrSld4e3WycILld5NmeyCVcEGg[ZhxemW|c3nvcuKh M4nXXlI{QDd5MkO1
Cal62 M3n6V2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV20ZXNOUUN3ME2zN{DDuSB2IH7N MVWyN|gzPDB4NB?=
Hth7 M2XacGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml\ZTWM2OD1zNTFCtUAzKG6P MYKyN|gzPDB4NB?=
Hth83 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3XmPGlEPTB;M{SgxtEhPSCwTR?= NYS0bI5WOjN6MkSwOlQ>
C643 NIDXZ5ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWT4Upp7UUN3ME23NUDDuSBzMDDuUS=> M3PaflI{QDJ2ME[0
SW1736 NFq3elhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NE\Hd3ZKSzVyPUO1JOKyKDhibl2= MkL4NlM5OjRyNkS=
T241 M2rDZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXPvdJJKUUN3ME22OUDDuSB5IH7N NVf3OnJXOjN6MkSwOlQ>
T351 NH7XXVhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUXzU41VUUN3ME21NEDDuSBzMDDuUS=> NYLSco1lOjN6MkSwOlQ>
BHP2-7 NVX6bJprT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MofLTWM2OD1|NzFCtUA3KG6P NH74WJgzOzh{NEC2OC=>
T238 NWi2UnJsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFHOWItKSzVyPUGsOVAxKMLzIEKwNEBvVQ>? NH\TNmczOzh{NEC2OC=>
HCT8 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnjXO|IhcA>? Mki0SG1UVw>? M3fTXGlEPTB;MUKuPgKBkcLz4pEJNU46KG6P NYrDZ|lsOjN{OUmzPFg>
H630 NITOSmtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2HwPVczKGh? MnPlSG1UVw>? NGHEcGRKSzVyPUGyMlTjiIoEsfMAjVMvOSCwTR?= MV[yN|I6QTN6OB?=
cH630 5-FU-res NIfsOolIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MornO|IhcA>? NHfCOIRFVVOR NH7IR2xKSzVyPUG1MlXjiIoEsfMAjVEvOiCwTR?= NFzZc5EzOzJ7OUO4PC=>
HCT116 MoXDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYq3NkBp MlzWSG1UVw>? MUjJR|UxRTFyLkhihKnDueLCiUKuNkBvVQ>? NHiwbpUzOzJ7OUO4PC=>
HCT116 p53−/− NEL2VoNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoDuO|IhcA>? NUDTPW9[TE2VTx?= NYDve29qUUN3ME24MlbjiIoEsfMAjVEvPyCwTR?= MnSzNlMzQTl|OEi=
dHCT116 p21−/− M3\EUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MorkO|IhcA>? M2XW[2ROW09? NULHW4pRUUN3ME21MlnjiIoEsfMAjVEvOyCwTR?= NXq5WWI5OjN{OUmzPFg>
HT29 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUDpZ2o{PzJiaB?= NYTueoRVTE2VTx?= MVLJR|UxRTF4LkRihKnDueLCiUKuN{BvVQ>? M1;Vc|I{Ojl7M{i4
LoVo MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnLzO|IhcA>? NIrtN4VFVVOR M3XzXmlEPTB;NT6x5qCKyrIkgJmwMlYhdk1? MXyyN|I6QTN6OB?=
RKO MkPlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUe3NkBp M{TzNmROW09? NHy5dY1KSzVyPUeuPgKBkcLz4pEJNk4zKG6P NIXhWHczOzJ7OUO4PC=>
SW480 MkjtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV7PVWxRPzJiaB?= MYPEUXNQ NHLNRm9KSzVyPUG3MlXjiIoEsfMAjVAvQCCwTR?= MWSyN|I6QTN6OB?=
eSW620 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlnIO|IhcA>? NEO1e3lFVVOR NFflNHVKSzVyPUmuNgKBkcLz4pEJNk4yKG6P NX3PO5pKOjN{OUmzPFg>

... Click to View More Cell Line Experimental Data

体内研究 LBH589作用于患肺癌和间皮瘤动物模型,明显降低肿瘤生长,与对照组相比平均降低62%。LBH589作用于免疫活性鼠和严重联合免疫缺陷鼠效果差不多,说明LBH589抑制肿瘤生长与免疫学无关。LBH589按20 mg/kg剂量腹腔注射,每周持续5天,导致在实验最后肿瘤生长平均下降70%。与相应的对照组肿瘤相比,LBH589作用于H526衍生的肿瘤下降53%,作用于BK-T衍生的肿瘤下降81%, 作用于RG-1衍生的肿瘤下降76%,作用于H69衍生的肿瘤下降 70%。在相同条件和剂量的情况下,LBH589 作用于NSCLC和Meso衍生的移植瘤,导致SCLC衍生的肿瘤中有两种衰退,伴随着BK-T衍生的平均肿瘤尺寸从实验开始时的296 mm3降低到实验结束时的116 mm3,RG-1衍生的平均肿瘤尺寸从实验开始时的185mm3降低到实验结束时的86 mm3[2]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

细胞实验:[1]
+ 展开
  • Cell lines: MOLT-4细胞和Reh(前体B细胞)
  • Concentrations: 50 nM
  • Incubation Time: 48小时
  • Method: 没有处理的细胞和LBH589处理的细胞[人类急性成淋巴细胞性白血病MOLT-4(T 细胞)和Reh(前体-B细胞)]用膜联蛋白V和碘化丙啶染色,然后加入膜联蛋白V-FITC细胞凋亡检测试剂盒I。通过流式细胞仪测定细胞凋亡和不能存活细胞的百分比。用CyAn ADP Violet细胞计数器收集至少5×104个细胞。根据所有的膜联蛋白V-阳性和膜联蛋白V/PI-阳性细胞细胞计算凋亡百分比,根据所有的膜联蛋白V-阳性和PI-阳性及膜联蛋白V/PI-阳性细胞计算细胞活力丢失百分比。
    (Only for Reference)
动物实验:[2]
+ 展开
  • Animal Models: 携带10×106个M30细胞或5×106个A549细胞的SCID鼠
  • Formulation: 溶于水的5%葡萄糖
  • Dosages: 10 mg/kg, 20 mg/kg
  • Administration: 腹腔注射
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 69 mg/mL (197.46 mM)
Water Insoluble
Ethanol Insoluble
体内 从左到右依次将纯溶剂加入产品,现配现用(数据来自Selleck实验检测而非文献):
2% DMSO+48% PEG 300+2% Tween 80+ddH2O
5mg/mL

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

化学数据

分子量 349.43
化学式

C21H23N3O2

CAS号 404950-80-7
稳定性 powder
in solvent
别名 NVP-LBH589

计算器

摩尔浓度计算器

摩尔浓度计算器

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

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

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

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

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

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

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

临床试验信息

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

技术支持

在订购、运输、储存和使用我们的产品的任何阶段,您遇到的任何问题,均可以通过拨打我们的热线电话400-668-6834,或者技术支持邮箱tech@selleck.cn,直接联系到我们。我们会在24小时内尽快联系您。

操作手册

如果有其他问题,请给我们留言。

  • * 必填项

常见问题及建议解决方法

  • 问题 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.

HDAC Signaling Pathway Map

HDAC Inhibitors with Unique Features

相关HDAC产品

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID