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

文献中の使用例(48)

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.

  • 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.

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 NWCwW2dCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWqwMVExKM7:TR?= MnXCNE01KGR? NV\Z[ZFncW6qaXLpeJMh[2WubDDndo94fGhiaX6gZo91cCC2aX3lMUBidmRiZH;z[U1l\XCnbnTlcpQhdWGwbnXy M3uyUFI3PzB{N{i0
HepG2 NWHFVJloT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkLFNE0yOCEQvF2= MV:wMVQh\A>? MVjpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCkb4ToJJRqdWVvIHHu[EBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MkT3NlY4ODJ5OES=
HT29 MULGeY5kfGmxbjDBd5NigQ>? M3i5UVUxyqCwTR?= M1LTXlI1NTd{IHi= MkLhbY5lfWOnZDDhZ5RqfmG2aX;uJI9nKGOjc4Dhd4UhOyCjZoTldkA1QMLiaNMg M4joTlI3PzB{N{i0
HepG2 MmnKSpVv[3Srb36gRZN{[Xl? NHz0d5E2OMLibl2= MVyyOE04OiCq MVrpcoR2[2WmIHHjeIl3[XSrb36gc4Yh[2G|cHHz[UA{KGGodHXyJFI1yqCqwrC= MVyyOlcxOjd6NB?=
HCC827 M4\2dmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH\ZRmQ2NzdwNT:xNEBvVQ>? NVrER3ZCPzMEoHi= NHLTPGdFVVOR Mnnp[Y5p[W6lZYOgeIhmKGGwdHnwdo9tcW[ncnH0bZZmKGWoZnXjeEBw\iCncnzveIlvcWJ? M3X3bFI3Pjd3NEi0
A549  M3nqRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnHFNVAwOTVxMkCgcm0> MVi3NuKhcA>? M4XWdGROW09? MV;lcohidmOnczD0bIUh[W62aYDyc4xq\mW{YYTpeoUh\W[oZXP0JI9nKGW{bH;0bY5q[g>? MXKyOlY4PTR6NB?=
NCI-H460  NWDZNo9CT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFP1WYIyOC9{MD:zNEBvVQ>? NUXl[ZNFPzMEoHi= NEjBdoZFVVOR NU\1PJBF\W6qYX7j[ZMhfGinIHHueIlxem:uaX\ldoF1cX[nIHXm[oVkfCCxZjDldoxwfGmwaXK= Mnz2NlY3PzV2OES=
J89GFP NFjzR|NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWjrPGcxTE2VT9Mg MlfySWM2OD12OT64OUDDuSBzMj62OUBvVQ>? M2PZSlI3PTZ|NU[4
THP89GFP MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MontSG1UV8Li NFnvRXBGSzVyPUG5MlM1KMLzIE[uOFMhdk1? MYiyOlU3OzV4OB?=
SK-NEP-1 M2rIUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NY[3fmM3OC5yMfMAl|ExNjBizszN MkjsNlQhcA>? MlfISG1UV8Li NX3weWFJUUN3ME23Ok4{PCCwTR?= NUSxNZF4OjZzN{[yNVk>
G401 NF;UfmZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkPxNE4xOeLCk{GwMlAh|ryP MnL3NlQhcA>? Mn3VSG1UV8Li MlvjTWM2OD1zNEOuNFIhdk1? NXrUcGtEOjZzN{[yNVk>
SK-NEP-1 NV\k[Y06S2WubDDWbYFjcWyrdImgRZN{[Xl? Mo\MOVAhdk1? NEHJepAy6oDVNDDk MmPOSG1UV8Li M2rwcZJm\HWlZYOgZ4VtdCC|dYL2bZZidCCrbjDhJJRqdWViZHXw[Y5l\W62IH3hco5meg>? NH;iZ|QzPjF5NkKxPS=>
G401 NI\YUHhE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NGfYPG42OCCwTR?= M{HLSVHjiJN2IHS= NGqxclZFVVORwrC= M{fkXZJm\HWlZYOgZ4VtdCC|dYL2bZZidCCrbjDhJJRqdWViZHXw[Y5l\W62IH3hco5meg>? NHu4XYYzPjF5NkKxPS=>
SK-NEP-1 MmGzRZBweHSxc3nzJGF{e2G7 Mn3rOVAwOTByIH7N NHrySlAzPCCq NIn2enJFVVORwrC= NGLESVJqdmS3Y3XzJINmdGxiYYDvdJRwe2m|IHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ NIfqfmUzPjF5NkKxPS=>
G401 M4jZbWFxd3C2b4Ppd{BCe3OjeR?= MXy1NE8yODBibl2= NEnxN3UzPCCq NIDPO3RFVVORwrC= MX;pcoR2[2W|IHPlcIwh[XCxcITvd4l{KGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NXXhXowyOjZzN{[yNVk>
SK-NEP-1 MnrpSpVv[3Srb36gRZN{[Xl? MWe1NE8yODBibl2= NYnHWHZIOjRiaB?= M4TTN2ROW00EoB?= MkPwd4hwf3NidHjlJIlv\HWldHnvckBw\iCGTlGg[pJi\22nboTheIlwdg>? NFzHeXAzPjF5NkKxPS=>
G401 MXjGeY5kfGmxbjDBd5NigQ>? Mn7qOVAwOTByIH7N NVPLZnFsOjRiaB?= MYnEUXNQyqB? M2izOpNpd3e|IITo[UBqdmS3Y4Tpc44hd2ZiRF7BJIZz[WevZX70ZZRqd25? MnW0NlYyPzZ{MUm=
SK-NEP-1 NVvTRY9yTnWwY4Tpc44hSXO|YYm= MVK1NE8yODBibl2= Mk\xNlQhcA>? M4jJXWROW00EoB?= NVLZTFFGcW6mdXPld{Bk\WyuIHP5Z4xmKGSrc3;y[IVzyqB? MonINlYyPzZ{MUm=
G401 NYD6dW5FTnWwY4Tpc44hSXO|YYm= M2jacVUxNzFyMDDuUS=> MWKyOEBp MnP0SG1UV8Li MYjpcoR2[2W|IHPlcIwh[3mlbHWg[Il{d3KmZYNCpC=> M{XYNFI3OTd4MkG5
RPMI 8226 NEXRXmVE\WyuIGP1dpZqfmGuIFHzd4F6 NWrJd5FsOi92L{[gcm0> M4nOW|Q56oDLaB?= Moq3bY5lfWOnczDhJJNq\26rZnnjZY51KGSnY4LlZZNmKGmwIITo[UBk\WyuIHfyc5d1cA>? MXyyOlAxODJ7Mh?=
OPM2 M4r3bmNmdGxiU4Xyeol3[WxiQYPzZZk> NH\tZ24zNzRxNjDuUS=> MlzqOFjjiImq MWTpcoR2[2W|IHGgd4lodmmoaXPhcpQh\GWlcnXhd4UhcW5idHjlJINmdGxiZ4Lve5Rp Mn2xNlYxODB{OUK=
U266 M{XXWGNmdGxiU4Xyeol3[WxiQYPzZZk> NVvIdGptOi92L{[gcm0> MVu0PQKBkWh? MWPpcoR2[2W|IHGgd4lodmmoaXPhcpQh\GWlcnXhd4UhcW5idHjlJINmdGxiZ4Lve5Rp MXKyOlAxODJ7Mh?=
H929 MY\D[YxtKFO3co\peoFtKEG|c3H5 NX3vNI9mOi92L{[gcm0> MmnzOFjjiImq NEfRO2JqdmS3Y3XzJIEhe2mpbnnmbYNidnRiZHXjdoVie2ViaX6geIhmKGOnbHyg[5Jwf3Sq MUiyOlAxODJ7Mh?=
RPMI 8226  NHm2XVVCeG:ydH;zbZMhSXO|YYm= NUTj[2hTPOLCiX7N M2mwN|I1NzR6IHi= M4XyXolv\HWlZYOgZ4VtdCCjcH;weI9{cXNiaX6gZUB1cW2nLXTldIVv\GWwdDDtZY5v\XJ? MX[yOlAxODJ7Mh?=
HCC827 NHXTPYpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYOxNEBvVQ>? M{PJVlQ5KGh? NHfteWZFVVOR MX;lcohidmOnczDjbZNxdGG2aX6gd4Vve2m2aY\peJnDqA>? M3PqU|I2QTR2NkG3
NCI-H23 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3HTelExKG6P NIL4U2k1QCCq NVXDeoZ{TE2VTx?= M{\uV4VvcGGwY3XzJINqe3CuYYTpckB{\W6|aYTpeol1gcLi NYnhZYxNOjV7NES2NVc>
AML3 NHnpWIdHfW6ldHnvckBCe3OjeR?= MXKwMVEh|ryP NYLGOI8yOjUEoHi= M3GyRolv\HWlZYOgSG5CKG[{YXft[Y51[XSrb39CpIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy M13WbFI2PjF{OUSx
ML-1 NV7uc5ZRTnWwY4Tpc44hSXO|YYm= MVWwMVEh|ryP NIG3SpAzPMLiaB?= MnLTbY5lfWOnczDEUmEh\nKjZ33lcpRifGmxbtMgbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK= NYDSSXh5OjV4MUK5OFE>
RPMI-8226vr10  NGG4R5JHfW6ldHnvckBCe3OjeR?= NE\pcoQxNTFizszN M{fWdlI1yqCq MYnpcoR2[2W|IFTORUBnemGpbXXueIF1cW:wwrDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= M3voRlI2PjF{OUSx
ML-1 M3LNVWZ2dmO2aX;uJGF{e2G7 MoPCNUDPxE1? MW[yOOKhcA>? MUTpcoNz\WG|ZYOgZ4F{eGG|ZT2zJIFkfGm4aYT5JFQu\m:uZB?= MoDqNlU3OTJ7NEG=
RPMI-8226vr10  MXfGeY5kfGmxbjDBd5NigQ>? MXmxJO69VQ>? M2TXWlI1yqCq Ml;ZbY5kemWjc3XzJINie3Cjc3WtN{Bi[3Srdnn0fUAzNjVvZn;s[C=> M3PYbFI2PjF{OUSx
SK-N-BE (2) MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHrGXpAzPOLCiXi= M37PO2lEPTB;MUC0MlDjiIoEsfMAjVcvQCCwTR?= M37P[FI2OzB6OUG2
SK-N-BE (2), PAN  MK NVXxb4pIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NW[1W5F7OjUkgJno NYf6bHhRUUN3ME2xNFQvOOLCidMx5qCKPy56IH7N M2C5NFI2OzB6OUG2
SK-N-BE (2), MK  PAN MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXqyOQKBkWh? NYXpUJZPUUN3ME2zPFIvOOLCidMx5qCKPDNwMjDuUS=> MWiyOVMxQDlzNh?=
SK-N-AS MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFfnXIwzPOLCiXi= M3nTOGlEPTB;M{euNgKBkcLz4pEJNk41KG6P M1q0dVI2OzB6OUG2
SK-N-DZ M4f2SGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4\qVlI16oDLaB?= NVHoZ|BiUUN3ME2xO{4y6oDLwsJihKkxNjRibl2= NGjuZnAzPTNyOEmxOi=>
Caki-1 MnzrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3nUfFExNzJ3L{WwJI5O NWPReFJ3PDhiaB?= NHHi[mRqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meiC|eX7ldodqe3SrY3HscJkhf2m2aDDybZRwdmG4aYK= MkDwNlUzPzlzOUG=
ACHN MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWXt[ox[OTBxMkWvOVAhdk1? NEnMbI01QCCq MmL1bY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZIhe3mwZYLnbZN1cWOjbHz5JJdqfGhicnn0c45ifmm{ M4n5[lI2Ojd7MUmx
769-P NUjlcYM{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEHRNpEyOC9{NT:1NEBvVQ>? MXy0PEBp NX\Je5JScW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJic4nu[ZJocXO2aXPhcIx6KHerdHigdol1d26jdnny MVKyOVI4QTF7MR?=
786-O  MknPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFjOWpcyOC9{NT:1NEBvVQ>? NHjTPWM1QCCq NHPwcIRqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meiC|eX7ldodqe3SrY3HscJkhf2m2aDDybZRwdmG4aYK= MXOyOVI4QTF7MR?=
Caki-1 NIT6eIdCeG:ydH;zbZMhSXO|YYm= NYH5R5F2PTBibl2= Ml;1OFghcA>? MYfpcoR2[2W|IHPlcIwh[XCxcITvd4l{KGOxbXLpcoVlKHKrdH;uZZZqeg>? M2\lV|I2Ojd7MUmx
ACHN NHPHbFRCeG:ydH;zbZMhSXO|YYm= NEXYb4g2OCCwTR?= M{nvTVQ5KGh? NHfBWXpqdmS3Y3XzJINmdGxiYYDvdJRwe2m|IHPvcYJqdmWmIILpeI9v[X[rch?= NXLiTXBCOjV{N{mxPVE>
769-P NVvwUWh4SXCxcITvd4l{KEG|c3H5 NF7JTVc2OCCwTR?= M2W5fFQ5KGh? M1[yWYlv\HWlZYOgZ4VtdCCjcH;weI9{cXNiY3;tZolv\WRicnn0c45ifmm{ NEDkU5IzPTJ5OUG5NS=>
786-O  NV;KVlZzSXCxcITvd4l{KEG|c3H5 MmnrOVAhdk1? M3W0dlQ5KGh? M4GzUIlv\HWlZYOgZ4VtdCCjcH;weI9{cXNiY3;tZolv\WRicnn0c45ifmm{ NIXib|QzPTJ5OUG5NS=>
Caki-1 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWmyOU82OCCwTR?= MYq0PEBp Mo\QSG1UVw>? M{XPS4lvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\SCmZYDlcoRmdnRibXHucoVzKHO7bnXy[4l{fGmlYXzsfUB4cXSqIHLvdpRmgm:vaXK= NWn5NWdzOjVzN{[zOVQ>
ACHN M4XoOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEflNnYzPS93MDDuUS=> NGLrTIU1QCCq MWXEUXNQ NGruOnVqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meiC|eX7ldodqe3SrY3HscJkhf2m2aDDic5J1\XqxbXni NUToWZB3OjVzN{[zOVQ>
769-P M2jYOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4\xeFI2NzVyIH7N M2nxc|Q5KGh? M3v6dmROW09? M3LVeYlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\SCmZYDlcoRmdnRibXHucoVzKHO7bnXy[4l{fGmlYXzsfUB4cXSqIHLvdpRmgm:vaXK= M4OxNlI2OTd4M{W0
Caki-1 NEm4cJFEd2yxbomgSo9zdWG2aX;uJGF{e2G7 NVvzSolxPTBibl2= MXO3MVE1KGR? MXPEUXNQ MkDPd5VxeHKnc4Pl[EBkd2yxbomg[o9zdWG2aX;uJJNq\26rZnnjZY51dHliY3;tZolv\WRid3n0bEB4cXSqIHLvdpRmgm:vaXKgxsA> MmDVNlUyPzZ|NUS=
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OCI-AML3  NH64bnlCeG:ydH;zbZMhSXO|YYm= M{LGUFDjiJN2MDDuUeKh M2rZNlQ5KGh? MUTpcoR2[2W|IHHwc5B1d3OrczDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= NWrDUYZ2OjR{NES0Nlk>
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PC3-AR NUDmOpM4SXCxcITvd4l{KEG|c3H5 M1O3dVAuOTByIH7N MUKyOE81QCCq NGXxcIFqdmS3Y3XzJIFxd3C2b4Ppd{BqdiCkb4ToJJRqdWVvIHHu[EBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NFLVTVgzPDF4M{KzNC=>
PC3 NGPZW|lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYGwMVExOCCwTR?= NWm2TI9DOjRxNEigbC=> NXP0TYxicW6mdXPld{Bi[2O3bYXsZZRqd25ib3[gd5VjTzFicH;weYxifGmxbh?= M2LoOFI1OTZ|MkOw
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PC3-AR MnPISpVv[3Srb36gRZN{[Xl? NFXpe5gxNTFyMDDuUS=> NV3sb4UxOjRiaB?= MmDXd5VxeHKnc4Pld{BmgHC{ZYPzbY9vKG:oIHHjeIl3[XSnZDDBWG0tKEGtdDDhcoQhTXKtMT:yJJBzd3SnaX6= NWXUbHNvOjRzNkOyN|A>
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SK-N-BE Mn3ZRZBweHSxc3nzJGF{e2G7 NWHxeIdHOOLCk{SwJI5O MXq0PEBp M{HX[ZBwfGWwdHz5JIlv\HWlZXSgZZBweHSxc3nzJIlvKGFiZH;z[U1l\XCnbnTlcpQh\mG|aHnvci=> MXGyOFA6QDd7OR?=
SK-N-AS Mn6ySpVv[3Srb36gRZN{[Xl? NFvNT3Ax6oDVOECgcm0> MUC0PEBp NECxXY1qdmS3Y3XzJIEh\G:|ZT3k[ZBmdmSnboSgZ4xm[X[jZ3Wgc4Yh[2G|cHHz[UA{KGGwZDDQRXJR MXGyOFA6QDd7OR?=
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SK-N-SH NFj4TXlHfW6ldHnvckBCe3OjeR?= MmPENQKBmzRyIH7N NHLSU5I1QCCq NH[5O4JqdmS3Y3XzJIEh\G:|ZT3k[ZBmdmSnboSgZ4xm[X[jZ3Wgc4Yh[2G|cHHz[UA{KGGwZDDQRXJR MlvnNlQxQTh5OUm=
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SMMC-7721 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWjSbmltOS1zMECwJI5O NX;1dI94OjRxNEivO|IhcA>? M3PMW2ROW09? NYfDOFBWcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZo91cCC2aX3lMUBidmRiZH;z[U1l\XCnbnTlcpQhdWGwbnXy M1;oeVI1ODl|OUW2
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SMMC-7721 M1LRVGZ2dmO2aX;uJGF{e2G7 MXW1NE8yODBibl2= MmDJNlQhcA>? M2fqT2ROW09? M2K0NoRwf26{ZXf1cIF1\XNiQnPsMZhNKGW6cILld5Nqd25? NE\QXnIzPDB7M{m1Oi=>
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PC-3  MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYTXNVZGOC1zMDFOwG0> NIm0W|czPC92OD:3NkBp MlXjbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYn;0bEB1cW2nLTDhcoQh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ NXzpVY9jOjN7OUGyNVY>
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RWPE-1  MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{T1[FAuOjBizszN NIT3flUzPC92OD:3NkBp M2LLO4lvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHLveIghfGmvZT2gZY5lKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= M{PycVI{QTlzMkG2
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CFPAC-1  M{nFbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml;uNlUwPTBxMUCwJI5O MVO0PEBp MVrEUXNQ NUf4T5VsemWmdXPld{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NG\kWpozOzl{Mki4Oi=>
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HSC4  MWXBdI9xfG:|aYOgRZN{[Xl? M{LiTlAuOjBibl2= NHLxO401QCCq MXPEUXNQ M4f5R4lv\HWlZYOgZ4VtdCCjcH;weI9{cXN? MljCNlM5Pzd{M{W=
HN22 MkmwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlrvNE0zOCCwTR?= Mm\mOFghcA>? NVnqUWNVTE2VTx?= MnHxbY5lfWOnczDHNUBxcGG|ZTDj[YxtKGO7Y3zlJIFzemW|dNMg NWXnO241OjN6N{eyN|U>
HSC4  NYLr[G5nT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXHNVpJ{OC1{MDDuUS=> NWTIZplLPDhiaB?= NYm0XpN4TE2VTx?= NX;LXmsxcW6mdXPld{BIOSCyaHHz[UBk\WyuIHP5Z4xmKGG{cnXzeOKh M4\HR|I{QDd5MkO1
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HSC4  MYLGeY5kfGmxbjDBd5NigQ>? M2KzdlAuOjBibl2= MnLvOFghcA>? MXrEUXNQ M{D5bpN2eHC{ZYPz[ZMhW3BzIHX4dJJme3Orb39CpC=> MWSyN|g4PzJ|NR?=
Cal62 NWrZcFR2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3q4NWlEPTB;M{OgxtEhPCCwTR?= MWeyN|gzPDB4NB?=
Hth7 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWC0XZFpUUN3ME2xOUDDuSB{IH7N MXqyN|gzPDB4NB?=
Hth83 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGDQbZZKSzVyPUO0JOKyKDVibl2= NFLjPZMzOzh{NEC2OC=>
C643 M3fiSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWn3PXpjUUN3ME23NUDDuSBzMDDuUS=> NUfEeHhJOjN6MkSwOlQ>
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T241 Mof2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2LuZ2lEPTB;NkWgxtEhPyCwTR?= NX\lbWxyOjN6MkSwOlQ>
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BHP2-7 NEX6dYtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFT2b2ZKSzVyPUO3JOKyKDZibl2= MojUNlM5OjRyNkS=
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dHCT116 p21−/− NV20S2F4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NULURXRNPzJiaB?= NXzaUFRRTE2VTx?= M2HpOWlEPTB;NT655qCKyrIkgJmxMlMhdk1? MVeyN|I6QTN6OB?=
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SW480 NW\JVIJwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlTLO|IhcA>? NU\DfoptTE2VTx?= MXzJR|UxRTF5LkZihKnDueLCiUCuPEBvVQ>? MU[yN|I6QTN6OB?=
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多くの細胞株試験データを見る場合、クリックしてください

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:
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

解決のために必要とされるマス、ボリュームまたは濃度を計算してください。

マス (g) = 濃度 (mol/L) x ボリューム (L) x 分子量 (g/mol)

モル濃度計算器方程式

  • マス
    濃度
    ボリューム
    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

貯蔵液を準備することを要求される希釈剤を計算してください. セレック希釈計算器は、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 ( 輸入 輸出 )

  • 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

マス 濃度 ボリューム 分子量

臨床試験

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

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