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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客户使用Selleck该产品发表文献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 NVPKRXh1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX\uRlk6OC1zMDFOwG0> NILZO|QxNTRiZB?= MnnkbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYn;0bEB1cW2nLTDhcoQh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ NITVTpgzPjdyMke4OC=>
HepG2 MlvTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1PTVlAuOTBizszN NH65[m0xNTRiZB?= MXTpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCkb4ToJJRqdWVvIHHu[EBld3OnLXTldIVv\GWwdDDtZY5v\XJ? M3K1RVI3PzB{N{i0
HT29 NITXW2VHfW6ldHnvckBCe3OjeR?= M3zDcFUxyqCwTR?= NVPmRYR[OjRvN{KgbC=> MlfrbY5lfWOnZDDhZ5RqfmG2aX;uJI9nKGOjc4Dhd4UhOyCjZoTldkA1QMLiaNMg NYPtZ4V6OjZ5MEK3PFQ>
HepG2 NFXHUpJHfW6ldHnvckBCe3OjeR?= M1zocFUxyqCwTR?= M2Lk[FI1NTd{IHi= NHG5dJJqdmS3Y3XkJIFkfGm4YYTpc44hd2ZiY3HzdIF{\SB|IHHmeIVzKDJ2wrDoxsA> NH36WHMzPjdyMke4OC=>
HCC827 NVe4V|dPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVS1M|cvPS9zMDDuUS=> M4nzelczyqCq NXuxTZdVTE2VTx?= NH;hcWhmdmijbnPld{B1cGViYX70bZBzd2yrZnXyZZRqfmViZX\m[YN1KG:oIHXycI91cW6rYh?= MlXDNlY3PzV2OES=
A549  NInaSVNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlXjNVAwOTVxMkCgcm0> NUnzfmI3PzMEoHi= MoPBSG1UVw>? NHrGS3JmdmijbnPld{B1cGViYX70bZBzd2yrZnXyZZRqfmViZX\m[YN1KG:oIHXycI91cW6rYh?= MlzmNlY3PzV2OES=
NCI-H460  M{mxXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXnBTpJzOTBxMkCvN|Ahdk1? NHf2T3o4OsLiaB?= NHzMWmlFVVOR NE\Mc|BmdmijbnPld{B1cGViYX70bZBzd2yrZnXyZZRqfmViZX\m[YN1KG:oIHXycI91cW6rYh?= MmCzNlY3PzV2OES=
J89GFP MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUTEUXNQyqB? MUjFR|UxRTR7Lki1JOKyKDF{Lk[1JI5O NHvjZY4zPjV4M{W2PC=>
THP89GFP M3rPUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHnZ[o5FVVORwrC= NIO2eZhGSzVyPUG5MlM1KMLzIE[uOFMhdk1? NGf0c2wzPjV4M{W2PC=>
SK-NEP-1 NEPrXVZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWWwMlAy6oDVMUCuNEDPxE1? NET3epYzPCCq MWPEUXNQyqB? MUDJR|UxRTd4LkO0JI5O NHK0bHQzPjF5NkKxPS=>
G401 NGKwcZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWmwMlAy6oDVMUCuNEDPxE1? MlH2NlQhcA>? MWLEUXNQyqB? NHrVSlZKSzVyPUG0N{4xOiCwTR?= MYCyOlE4PjJzOR?=
SK-NEP-1 NYnHOopFS2WubDDWbYFjcWyrdImgRZN{[Xl? MUC1NEBvVQ>? NVvPUoQxOeLCk{Sg[C=> MoDvSG1UV8Li MXXy[YR2[2W|IHPlcIwhe3W{dnn2ZYwhcW5iYTD0bY1mKGSncHXu[IVvfCCvYX7u[ZI> Ml\PNlYyPzZ{MUm=
G401 NEj0SlZE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M3TDOlUxKG6P NEe5WXcy6oDVNDDk MVfEUXNQyqB? MVny[YR2[2W|IHPlcIwhe3W{dnn2ZYwhcW5iYTD0bY1mKGSncHXu[IVvfCCvYX7u[ZI> MnPxNlYyPzZ{MUm=
SK-NEP-1 M4\ne2Fxd3C2b4Ppd{BCe3OjeR?= NEfaRpE2OC9zMECgcm0> MWCyOEBp MWjEUXNQyqB? MkfNbY5lfWOnczDj[YxtKGGyb4D0c5NqeyCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? MkfCNlYyPzZ{MUm=
G401 Ml6wRZBweHSxc3nzJGF{e2G7 MVe1NE8yODBibl2= NVy1b4wyOjRiaB?= MnnJSG1UV8Li M2TUSolv\HWlZYOgZ4VtdCCjcH;weI9{cXNiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NV:0[HA1OjZzN{[yNVk>
SK-NEP-1 MXXGeY5kfGmxbjDBd5NigQ>? NH3xZ5M2OC9zMECgcm0> NH3VN5QzPCCq NX\mNm5ITE2VT9Mg NU\hcnJve2ixd4OgeIhmKGmwZIXjeIlwdiCxZjDEUmEh\nKjZ33lcpRifGmxbh?= NFTybZMzPjF5NkKxPS=>
G401 NXqwSVM{TnWwY4Tpc44hSXO|YYm= MlnhOVAwOTByIH7N MlfiNlQhcA>? Mk\TSG1UV8Li Mmi5d4hwf3NidHjlJIlv\HWldHnvckBw\iCGTlGg[pJi\22nboTheIlwdg>? NGjhNIwzPjF5NkKxPS=>
SK-NEP-1 NW\zdnRPTnWwY4Tpc44hSXO|YYm= NEm0e5I2OC9zMECgcm0> MWSyOEBp MoXZSG1UV8Li M1z4Solv\HWlZYOgZ4VtdCCleXPs[UBlcXOxcnTlduKh MU[yOlE4PjJzOR?=
G401 M{f4bmZ2dmO2aX;uJGF{e2G7 MWm1NE8yODBibl2= M4\wbFI1KGh? M2LoXGROW00EoB?= M1H5Rolv\HWlZYOgZ4VtdCCleXPs[UBlcXOxcnTlduKh M{jvelI3OTd4MkG5
RPMI 8226 M3XPNWNmdGxiU4Xyeol3[WxiQYPzZZk> MV[yM|QwPiCwTR?= MlzuOFjjiImq M4LJWYlv\HWlZYOgZUB{cWewaX\pZ4FvfCCmZXPy[YF{\SCrbjD0bIUh[2WubDDndo94fGh? M2nTS|I3ODByMkmy
OPM2 NYLuTpR{S2WubDDTeZJ3cX[jbDDBd5NigQ>? MXiyM|QwPiCwTR?= M2DET|Q56oDLaB?= NIXB[nlqdmS3Y3XzJIEhe2mpbnnmbYNidnRiZHXjdoVie2ViaX6geIhmKGOnbHyg[5Jwf3Sq MoLxNlYxODB{OUK=
U266 MWDD[YxtKFO3co\peoFtKEG|c3H5 MXeyM|QwPiCwTR?= MW[0PQKBkWh? MmXPbY5lfWOnczDhJJNq\26rZnnjZY51KGSnY4LlZZNmKGmwIITo[UBk\WyuIHfyc5d1cA>? NUP5Nm9qOjZyMECyPVI>
H929 NX7QdYMyS2WubDDTeZJ3cX[jbDDBd5NigQ>? M2\lS|IwPC94IH7N NVeyXI1QPDkkgJno MoiybY5lfWOnczDhJJNq\26rZnnjZY51KGSnY4LlZZNmKGmwIITo[UBk\WyuIHfyc5d1cA>? MUKyOlAxODJ7Mh?=
RPMI 8226  NEO3OoFCeG:ydH;zbZMhSXO|YYm= MX:05qCKdk1? NIDIcoozPC92ODDo MUnpcoR2[2W|IHPlcIwh[XCxcITvd4l{KGmwIHGgeIlu\S2mZYDlcoRmdnRibXHucoVz NF:zfGUzPjByMEK5Ni=>
HCC827 M{TN[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFTJeYcyOCCwTR?= Mo\iOFghcA>? M2LUdmROW09? MnPJ[Y5p[W6lZYOgZ4l{eGyjdHnuJJNmdnOrdHn2bZR6yqB? NUXiTVZHOjV7NES2NVc>
NCI-H23 MkC3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1G5XlExKG6P MV60PEBp MkLRSG1UVw>? NFjoVZBmdmijbnPld{BkcXOybHH0bY4he2Wwc3n0bZZqfHoEoB?= NIjLPZIzPTl2NE[xOy=>
AML3 MnW5SpVv[3Srb36gRZN{[Xl? M2ntZVAuOSEQvF2= NWD0NVd2OjUEoHi= NW[1S3V6cW6mdXPld{BFVkFiZoLh[41mdnSjdHnvcuKhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NVfSNZpPOjV4MUK5OFE>
ML-1 NXHEfGE5TnWwY4Tpc44hSXO|YYm= MkDhNE0yKM7:TR?= MUSyOOKhcA>? NYfFelBEcW6mdXPld{BFVkFiZoLh[41mdnSjdHnvcuKhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NX;XRW5MOjV4MUK5OFE>
RPMI-8226vr10  NH3nPJVHfW6ldHnvckBCe3OjeR?= M3j6VFAuOSEQvF2= MmjDNlTDqGh? NGHrdYJqdmS3Y3XzJGRPSSCocnHncYVvfGG2aX;uxsBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> Mn7rNlU3OTJ7NEG=
ML-1 NIH5WIhHfW6ldHnvckBCe3OjeR?= MUCxJO69VQ>? Mm\CNlTDqGh? MlzCbY5kemWjc3XzJINie3Cjc3WtN{Bi[3Srdnn0fUA1NW[xbHS= M13sc|I2PjF{OUSx
RPMI-8226vr10  M4rCTGZ2dmO2aX;uJGF{e2G7 NWDv[FdIOSEQvF2= NUnmb2hkOjUEoHi= NXfPR2JScW6lcnXhd4V{KGOjc4Dhd4UuOyCjY4Tpeol1gSB{LkWt[o9t\A>? M4Xxe|I2PjF{OUSx
SK-N-BE (2) NFXtcZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3LLbFI16oDLaB?= M1TQUmlEPTB;MUC0MlDjiIoEsfMAjVcvQCCwTR?= MVWyOVMxQDlzNh?=
SK-N-BE (2), PAN  MK NHfVVVhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUOyOQKBkWh? MVHJR|UxRTFyND6w5qCKyrIkgJm3Mlghdk1? NYrRXmNUOjV|MEi5NVY>
SK-N-BE (2), MK  PAN MmPyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlTaNlTjiImq NUXPeGs1UUN3ME2zPFIvOOLCidMx5qCKPDNwMjDuUS=> MVGyOVMxQDlzNh?=
SK-N-AS MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEHNNGQzPOLCiXi= MWjJR|UxRTN5LkJihKnDueLCiUKuOEBvVQ>? MkXwNlU{ODh7MU[=
SK-N-DZ MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFTMSXkzPOLCiXi= M4HxSmlEPTB;MUeuNgKBkcLz4pEJNE41KG6P NFjN[|MzPTNyOEmxOi=>
Caki-1 M2n3OGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH;JT|IyOC9{NT:1NEBvVQ>? MoriOFghcA>? NYXibnk2cW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJic4nu[ZJocXO2aXPhcIx6KHerdHigdol1d26jdnny NXnPZlBHOjV{N{mxPVE>
ACHN NIW5ZXNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHT6XFMyOC9{NT:1NEBvVQ>? MYS0PEBp NVjpdIZLcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJic4nu[ZJocXO2aXPhcIx6KHerdHigdol1d26jdnny Mk\mNlUzPzlzOUG=
769-P NHXxSW1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH;BV|QyOC9{NT:1NEBvVQ>? MXG0PEBp M1HBbIlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\SCmZYDlcoRmdnRibXHucoVzKHO7bnXy[4l{fGmlYXzsfUB4cXSqIILpeI9v[X[rch?= M2e0TVI2Ojd7MUmx
786-O  NInWbGVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4HRXVExNzJ3L{WwJI5O M1PQd|Q5KGh? NHjhcFBqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meiC|eX7ldodqe3SrY3HscJkhf2m2aDDybZRwdmG4aYK= MXuyOVI4QTF7MR?=
Caki-1 MkK3RZBweHSxc3nzJGF{e2G7 MmDqOVAhdk1? NUWwV25tPDhiaB?= M1K1b4lv\HWlZYOgZ4VtdCCjcH;weI9{cXNiY3;tZolv\WRicnn0c45ifmm{ NELZfGQzPTJ5OUG5NS=>
ACHN MkL4RZBweHSxc3nzJGF{e2G7 NHrKd5U2OCCwTR?= NV3NUGE3PDhiaB?= M3fGUYlv\HWlZYOgZ4VtdCCjcH;weI9{cXNiY3;tZolv\WRicnn0c45ifmm{ MWGyOVI4QTF7MR?=
769-P NWfWXZJnSXCxcITvd4l{KEG|c3H5 M4TtelUxKG6P M4jJS|Q5KGh? M2nOeIlv\HWlZYOgZ4VtdCCjcH;weI9{cXNiY3;tZolv\WRicnn0c45ifmm{ M4fsRVI2Ojd7MUmx
786-O  M{TiPWFxd3C2b4Ppd{BCe3OjeR?= NVmyV2xuPTBibl2= NULDV496PDhiaB?= MXLpcoR2[2W|IHPlcIwh[XCxcITvd4l{KGOxbXLpcoVlKHKrdH;uZZZqeg>? M4H5[|I2Ojd7MUmx
Caki-1 NVnqU3d2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX2yOU82OCCwTR?= MVu0PEBp MkfqSG1UVw>? MYfpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldkB{gW6ncnfpd5Rq[2GubImge4l1cCCkb4L0[ZpwdWmk NVzOVGUxOjVzN{[zOVQ>
ACHN NIfCeHlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4TFWVI2NzVyIH7N MlXJOFghcA>? NWnIbWtETE2VTx?= M2LTUYlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\SCmZYDlcoRmdnRibXHucoVzKHO7bnXy[4l{fGmlYXzsfUB4cXSqIHLvdpRmgm:vaXK= NEiwOZczPTF5NkO1OC=>
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PC3-AR M1zPPGFxd3C2b4Ppd{BCe3OjeR?= NFXXepExNTFyMDDuUS=> NVv0dHJ1OjRxNEigbC=> MkfDbY5lfWOnczDhdI9xfG:|aYOgbY4h[m:2aDD0bY1mNSCjbnSg[I9{\S2mZYDlcoRmdnRibXHucoVz NFTNT48zPDF4M{KzNC=>
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SK-N-BE NGXRZVBCeG:ydH;zbZMhSXO|YYm= M3fuSVDjiJN2MDDuUS=> NFrqeGc1QCCq Mnz6dI91\W62bImgbY5lfWOnZDDhdI9xfG:|aYOgbY4h[SCmb4PlMYRmeGWwZHXueEBn[XOqaX;u NFzTRVczPDB7OEe5PS=>
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HepG2 MkK3RZBweHSxc3nzJGF{e2G7 M33TRVUxKG6P M1nCO|Q5KGh? M2OzSWROW09? MV\pcoR2[2W|IHPlcIwh[XCxcITvd4l{KHOrZ37p[olk[W62bImgbY4h[SClYYPwZZNmNWSncHXu[IVvfCCvYX7u[ZIh[nliY3zlZZZi\2Vib3[gZ4F{eGG|ZYOgN{whQCCjbnSgPS=> NFT1d24zPDB7M{m1Oi=>
SMMC-7721 NXr5[pRkSXCxcITvd4l{KEG|c3H5 MnK0OVAhdk1? NGXPSVk1QCCq M4nYOGROW09? NYK2PXhUcW6mdXPld{Bk\WyuIHHwc5B1d3OrczDzbYdvcW[rY3HueIx6KGmwIHGgZ4F{eGG|ZT3k[ZBmdmSnboSgcYFvdmW{IHL5JINt\WG4YXflJI9nKGOjc4Dhd4V{KDNuIEigZY5lKDl? MVuyOFA6Ozl3Nh?=
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HepG2 MofTSpVv[3Srb36gRZN{[Xl? M2L2[lUxNzFyMDDuUS=> NUX4[FlkOjRiaB?= NXjycI5oTE2VTx?= MV\k[YNz\WG|ZYOgeIhmKGyndnXsd{Bw\iCyLWPURXQ{KGGwZDDwMWFsfMLi NFvNcJozPDB7M{m1Oi=>
SMMC-7721 NHvVUlNHfW6ldHnvckBCe3OjeR?= Mmf1OVAwOTByIH7N NV;XWGZSOjRiaB?= NVLwSplITE2VTx?= MkXj[IVkemWjc3XzJJRp\SCuZY\lcJMhd2ZicD3TWGFVOyCjbnSgdE1Cc3UEoB?= MUGyOFA6Ozl3Nh?=
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FaDu M4Tk[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFTSXooyODEkgJXuUS=> M1jKcFgwOTBxMUKgbC=> MoHD[Il{eGyjeXXkJIEhe2mpbnnmbYNidnRiYX7kJJBzd2yxbnfl[EBIOi:PIHHydoV{fCCjdDC4JIFv\CBzMvMAiYgheG:|dDDy[Yxm[XOn NXP1bHNPOjRyMk[0PFI>
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RWPE-1  NVLicYlOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NU\2eFBuOC1{MDFOwG0> M320elI1NzR6L{eyJIg> MUfpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCkb4ToJJRqdWVvIHHu[EBld3OnLXTldIVv\GWwdDDtZY5v\XJ? M17JOFI{QTlzMkG2
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CFPAC-1  M4jSZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVexZ4dxOjVxNUCvNVAxKG6P MWO0PEBp MV3EUXNQ MWry[YR2[2W|IHPlcIwh\3Kxd4ToJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy MVmyN|kzOjh6Nh?=
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L3.6pl MU\BdI9xfG:|aYOgRZN{[Xl? MYiyOU82OC9zMECgcm0> NFT4PVM1QCCq NXLSVIlZTE2VTx?= NXLhbldbcW6mdXPld{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? MkXsNlM6OjJ6OE[=
CFPAC-1  MlLhRZBweHSxc3nzJGF{e2G7 MorDNlUwPTBxMUCwJI5O NYLSUZhHPDhiaB?= MXLEUXNQ NIDpOIFqdmS3Y3XzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz M2PFc|I{QTJ{OEi2
HN22 NF[2[G9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVWwMVIxKG6P NFLkXnIzPC92ODDo MUfEUXNQ NInpW5RqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDpckBjd3SqIITpcYUuKGGwZDDkc5NmNSCmZYDlcoRmdnRibXHucoVz MlP4NlM5Pzd{M{W=
HSC4  NIi5S2pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIq4XGkxNTJyIH7N Ml6xNlQwPDhiaB?= MojISG1UVw>? M{[y[olvcGmkaYTzJINmdGxidnnhZoltcXS7IHnuJIJwfGhidHnt[U0h[W6mIHTvd4UuKGSncHXu[IVvfCCvYX7u[ZI> M3zpTVI{QDd5MkO1
HN22 MkTORZBweHSxc3nzJGF{e2G7 MXiwMVIxKG6P NHrYV5Q1QCCq MY\EUXNQ Mk\xbY5lfWOnczDj[YxtKGGyb4D0c5Nqew>? NIroXogzOzh5N{KzOS=>
HSC4  MUfBdI9xfG:|aYOgRZN{[Xl? MoSxNE0zOCCwTR?= M2PMPVQ5KGh? M3XHR2ROW09? MYLpcoR2[2W|IHPlcIwh[XCxcITvd4l{ MkO2NlM5Pzd{M{W=
HN22 NEPMbnpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUThRoxJOC1{MDDuUS=> M3L1[VQ5KGh? MkDMSG1UVw>? NV\wT5NFcW6mdXPld{BIOSCyaHHz[UBk\WyuIHP5Z4xmKGG{cnXzeOKh NHr2SnYzOzh5N{KzOS=>
HSC4  MoPFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXmwMVIxKG6P NEX0TIg1QCCq M4LZXGROW09? MUfpcoR2[2W|IFexJJBp[XOnIHPlcIwh[3mlbHWgZZJz\XO2wrC= M{GzdVI{QDd5MkO1
HN22 NU\QU2x5TnWwY4Tpc44hSXO|YYm= M4DY[|AuOjBibl2= MVK0PEBp M3yxSGROW09? MVjzeZBxemW|c3XzJHNxOSCneIDy[ZN{cW:wwrC= NWHQV41bOjN6N{eyN|U>
HSC4  NYKzb5RQTnWwY4Tpc44hSXO|YYm= NX3rTG55OC1{MDDuUS=> MXy0PEBp NVTnOJNMTE2VTx?= NF3BXXB{fXCycnXzd4V{KFOyMTDlfJBz\XO|aX;uxsA> NYj1R3Y4OjN6N{eyN|U>
Cal62 M4nafWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnzDTWM2OD1|MzFCtUA1KG6P M4\nPVI{QDJ2ME[0
Hth7 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnmwTWM2OD1zNTFCtUAzKG6P M2fxSlI{QDJ2ME[0
Hth83 MnK3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml3CTWM2OD1|NDFCtUA2KG6P MoGyNlM5OjRyNkS=
C643 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWCwSpBLUUN3ME23NUDDuSBzMDDuUS=> NFzqe2wzOzh{NEC2OC=>
SW1736 MmTjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVjJR|UxRTN3INMxJFghdk1? M{TrTVI{QDJ2ME[0
T241 M3fFTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUTJR|UxRTZ3INMxJFchdk1? NW\3Uo5lOjN6MkSwOlQ>
T351 MmL2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4nRfWlEPTB;NUCgxtEhOTBibl2= M2W4RVI{QDJ2ME[0
BHP2-7 NV;5SWQ2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHO2Z3NKSzVyPUO3JOKyKDZibl2= NUXHXHFbOjN6MkSwOlQ>
T238 NF7MeXRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWHJR|UxRTFuNUCwJOKyKDJyMDDuUS=> NY\XXoJDOjN6MkSwOlQ>
HCT8 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWW3NkBp NFTvdJNFVVOR NF62NndKSzVyPUGyMlnjiIoEsfMAjVEvQSCwTR?= NWDzT5VVOjN{OUmzPFg>
H630 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NE\aXG04OiCq MXfEUXNQ M3rtOmlEPTB;MUKuOQKBkcLz4pEJN{4yKG6P MVeyN|I6QTN6OB?=
cH630 5-FU-res MoLqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnPPO|IhcA>? M{LVOWROW09? MULJR|UxRTF3LkZihKnDueLCiUGuNkBvVQ>? M2nVTVI{Ojl7M{i4
HCT116 M1\6Wmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWDGVmZnPzJiaB?= M4P4SWROW09? M4TFR2lEPTB;MUCuO-KBkcLz4pEJNk4zKG6P MWSyN|I6QTN6OB?=
HCT116 p53−/− Mn;JS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1LJXFczKGh? MXLEUXNQ NVj2V4xzUUN3ME24MlbjiIoEsfMAjVEvPyCwTR?= MXOyN|I6QTN6OB?=
dHCT116 p21−/− MofYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3TRWlczKGh? M2SxVGROW09? MXXJR|UxRTVwOfMAjeKy6oDLMT6zJI5O MYOyN|I6QTN6OB?=
HT29 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWi3NkBp NVj2VXNpTE2VTx?= NUXJVVlsUUN3ME2xOk4{6oDLwsJihKkzNjNibl2= NFe5cIMzOzJ7OUO4PC=>
LoVo MmS4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2Lqd|czKGh? NIPRdJhFVVOR NETZPFhKSzVyPUWuNgKBkcLz4pEJNE43KG6P M2D6WFI{Ojl7M{i4
RKO NHPpfWtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXntcmFvPzJiaB?= M1vIdWROW09? MXfJR|UxRTdwOfMAjeKy6oDLMj6yJI5O M2DvXFI{Ojl7M{i4
SW480 M2rLSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF7WUY04OiCq MWnEUXNQ NWn0NlNFUUN3ME2xO{426oDLwsJihKkxNjhibl2= NUnrcodYOjN{OUmzPFg>
eSW620 MmXHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1vWU|czKGh? MWXEUXNQ NVu5ZW4xUUN3ME25MlHjiIoEsfMAjVIvOSCwTR?= NYDaWpkyOjN{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
NCT03878524 Not yet recruiting Breast Cancer|Prostate Cancer|Pancreatic Cancer|Acute Myelogenous Leukemia OHSU Knight Cancer Institute|Oregon Health and Science University|Prospect Creek Foundation March 14 2019 Phase 1
NCT03632317 Recruiting Glioma|Diffuse Intrinsic Pontine Glioma University of Michigan Rogel Cancer Center March 2019 Phase 2
NCT03878524 Not yet recruiting Breast Cancer|Prostate Cancer|Pancreatic Cancer|Acute Myelogenous Leukemia OHSU Knight Cancer Institute|Oregon Health and Science University|Prospect Creek Foundation March 14 2019 Phase 1
NCT03632317 Recruiting Glioma|Diffuse Intrinsic Pontine Glioma University of Michigan Rogel Cancer Center March 2019 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
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

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