Belinostat (PXD101)

製品コードS1085 別名:NSC726630, PX-105684

Belinostat (PXD101)化学構造

分子量(MW):318.35

Belinostat (PXD101) is a novel HDAC inhibitor with IC50 of 27 nM in a cell-free assay, with activity demonstrated in cisplatin-resistant tumors.

サイズ 価格(税別)  
JPY 26560.00
JPY 19920.00
JPY 61420.00
JPY 94620.00
JPY 161020.00

カスタマーフィードバック(8)

  • A375DR and parental cells were seeded 50,000 cells per well in 6-well plates and treated with 1 mMvorinostat (Vor), 0.5 mMbelinostat (Bel), 5 nMpanobinostat (Pan), and/or combination of 5 nM trametinib and 0.125 mM dabrafenib.

    Cell, 2018, 173(6):1413-1425. Belinostat (PXD101) purchased from Selleck.

    (C) Cell lysates were harvested from lung SCC cells after treatment with increasing doses of belinostat (0.1, 0.2, 0.3, 1, 3 lM). Immunoblotting was performed to evaluate the changes in phosphorylated protein levels of the targets identified in 1D (ERK1/2, p38, B-Raf, MEK1/2) as well as PARP. b-Actin shown as loading control.

    Mol Oncol, 2017, 11(8):965-980. Belinostat (PXD101) purchased from Selleck.

  • (B) Western blotting for cyclin D1. Cells were treated for 48 h with 5 μM belinostat and/or 25 or 50 μM ritonavir. Actin was used for the loading control. Representative blots are shown.

    Oncol Res, 2016, 24(5):327-335. Belinostat (PXD101) purchased from Selleck.

    Inhibition of LSD1 activity by HDAC inhibitors. a MDA-MB-231 and MDA-MB-468 cells were exposed to indicated HDAC inhibitors for 24 h.

    Breast Cancer Res Treat 2012 131, 777-789. Belinostat (PXD101) 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 2010 131(3), 777-789. Belinostat (PXD101) 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-β-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. Belinostat (PXD101) 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 -β-actin antibody.

     

     

    PLoS One 2011 6, e17138. Belinostat (PXD101) purchased from Selleck.

    MDA-MB-231 Breast cancer cells were pretreated with Acetyl-H3 and H3, and then treated with the indicated concentrations of  PXD101.

    Dr. Zhang of Tianjin Medical University. Belinostat (PXD101) 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 Belinostat (PXD101) is a novel HDAC inhibitor with IC50 of 27 nM in a cell-free assay, with activity demonstrated in cisplatin-resistant tumors.
特性 Lead compound of Topotarget.
ターゲット
HDAC [1]
(Cell-free assay)
27 nM
体外試験

Belinostat inhibits the growth of tumor cells (A2780, HCT116, HT29, WIL, CALU-3, MCF7, PC3 and HS852) with IC50 from 0.2-0.66 μM. PD101 shows low activity in A2780/cp70 and 2780AD cells, which are cisplatin and doxorubicin-resistant derivatives of A2780 cells. Belinostat could induce apoptosis through PARP cleavage and acetylation of histones H3/H4. [1] Belinostat inhibits bladder cancer cell growth, especially in 5637 cells, which shows accumulation of G0-G1 phase, decrease in S phase and increase in G2-M phase. [2] The growth inhibitory activity of belinostat on cell lines is not strongly influenced by the multidrug-resistant phenotype, whereas the activity of docetaxel is clearly affected. Belinostat could enhance the growth inhibitory activity of docetaxel or carboplatin in OVCAR-3 and A2780 cells. Belinostat also shows enhanced tubulin acetylation in ovarian cancer cell lines. [3] A recent study shows that Belinostat activates protein kinase A in a TGF-β signaling-dependent mechanism and decreases survivin mRNA. [4]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
NB4 M{npdGNmdGxiVnnhZoltcXS7IFHzd4F6 M3rIR|AvOi9{wrFOwG0> NXvjVY9zOjRxNEivO|IhcA>? MX;k[YNz\WG|ZYOgZ4VtdCC4aXHibYxqfHliaX6gZo91cCC2aX3lJIFv\CCmb4PlJIRmeGWwZHXueEBu[W6wZYK= M2TrWFI2QDZ2N{Oy
HL-60  MlvCR4VtdCCYaXHibYxqfHliQYPzZZk> MoXLNE4zNzMEoN88US=> MWSyOE81QC95MjDo M2LVeoRm[3KnYYPld{Bk\WyuII\pZYJqdGm2eTDpckBjd3SqIITpcYUh[W6mIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> NFPlfI8zPTh4NEezNi=>
NB4 NFrDVnZHfW6ldHnvckBCe3OjeR?= NEfMRWEzyqEQvF2= MoflNlQwPDhiaB?= NHrkbotjdG:la4OgZ4VtdCCleXPs[UBqdiCVIIDoZZNm NYDnPZd1OjV6NkS3N|I>
HL-60  NGjzfpFHfW6ldHnvckBCe3OjeR?= Ml2zNuKh|ryP MofJNlQwPDhiaB?= MofrZoxw[2u|IHPlcIwh[3mlbHWgbY4hWyCyaHHz[S=> NVn6dHUyOjV6NkS3N|I>
NB4 M1LD[2Z2dmO2aX;uJGF{e2G7 NXLOfGk6OC5{wrFOwG0> MYCyOE81QC95MjDo NGj2NXlmdmijbnPld{BTSS2rbnT1Z4VlKGe{YX71cI9kgXSrYzDkbYZn\XKnboTpZZRqd25? MkTKNlU5PjR5M{K=
HL-60  MX;GeY5kfGmxbjDBd5NigQ>? NXn1eJBXOC5{wrFOwG0> MWCyOE81QC95MjDo M1zn[IVvcGGwY3XzJHJCNWmwZIXj[YQh\3KjboXsc4N6fGmlIHTp[oZmemWwdHnheIlwdg>? NHu1cGwzPTh4NEezNi=>
PANC-1 NV3aV49PTnWwY4Tpc44hSXO|YYm= NXHWSJlqOTEEoN88US=> MYmyM|QwPiCq NWP1cHczTE2VTx?= NFmz[ZZqdmS3Y3XzJGFOWEtiYXP0bZZifGmxbh?= MViyN|c1OzF7OB?=
PANC-1 Mlf2R4VtdCCYaXHibYxqfHliQYPzZZk> NXXIdos3OS9zMNMg{txO NF\wUXE1QCCq MX\EUXNQ NFXQToxl\WO{ZXHz[ZMh[2WubDD2bYFjcWyrdImgbY4h[SCmb4PlJIRmeGWwZHXueEBu[W6wZYK= MWOyN|c1OzF7OB?=
PANC-1 Mk[0SpVv[3Srb36gRZN{[Xl? M{HndlExyqEQvF2= M1XB[lIwPCCq MV7EUXNQ NUCwZ4xucW6lcnXhd4V{KGmwdILhZ4VtdHWuYYKgVm9UKGyndnXs MoSxNlM4PDNzOUi=
H1666 M{fLXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1;sVVczyqCq NET3XopFVVOR NUjnZppkUUN3ME6xNEDPxE1? NGnVRlQzOzVzNUe1Ni=>
H460 MoPYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1X3TVczyqCq MV3EUXNQ MULJR|UxRTBwOE[g{txO NYrBRXdGOjN3MUW3OVI>
H1299 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M37lWlczyqCq M3:0d2ROW09? MX7JR|UxRTFwMjFOwG0> MnfnNlM2OTV5NUK=
H520 M3izT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV:3NuKhcA>? M1vDZmROW09? MnmwTWM2OD1yLke1JO69VQ>? MUiyN|UyPTd3Mh?=
H1975 MkDDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NInj[VQ4OsLiaB?= NX7PbZBDTE2VTx?= MliyTWM2OD1yLk[4JO69VQ>? NEj6T4IzOzVzNUe1Ni=>
H1650 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NG\JUXo4OsLiaB?= NHnr[2RFVVOR MkXjTWM2OD1yLki4JO69VQ>? MmCyNlM2OTV5NUK=
H820 NWXBSVVtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2TlRlczyqCq NGLPSmRFVVOR MWjJR|UxRTBwNDFOwG0> NXjOZXJtOjN3MUW3OVI>
PC9 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXK3NuKhcA>? NWH5O4dDTE2VTx?= NHLMb|JKSzVyPUCuNlkh|ryP MVOyN|UyPTd3Mh?=
HCC2279 NHj3dGJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGXyR5Y4OsLiaB?= M3TWUWROW09? NEPXbGpKSzVyPUCuOEDPxE1? NGi4XY4zOzVzNUe1Ni=>
HCC827 NWTTZWJJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIfPUZo4OsLiaB?= M371WGROW09? NYG3ZnBDUUN3ME2wMlI6KM7:TR?= NV\YWox7OjN3MUW3OVI>
HCC2935 NEH4fZpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{f0e|czyqCq Mkj1SG1UVw>? NUjKXXBkUUN3ME2wMlk4KM7:TR?= MnzmNlM2OTV5NUK=
HCC4006 NFzZ[XJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGruNIc4OsLiaB?= MoLySG1UVw>? M{KyN2lEPTB;MD60OkDPxE1? MmThNlM2OTV5NUK=
H460 NVLV[mxHTnWwY4Tpc44hSXO|YYm= M2\mXlUxOMLibl2= Mn3ZNlTDqGh? NWXIVHd2TE2VTx?= M17XOYRm[3KnYYPld{BGT0[UIHX4dJJme3Orb36= NGPCZ5kzOzVzNUe1Ni=>
H1650 Mn\JSpVv[3Srb36gRZN{[Xl? NWPZUGFxPTBywrDuUS=> NHfSTHMzPMLiaB?= M2\YfWROW09? M2n2fYRm[3KnYYPld{BGT0[UIHX4dJJme3Orb36= M13GNVI{PTF3N{Wy
PC9 NXvIfoNETnWwY4Tpc44hSXO|YYm= MojNOVAxyqCwTR?= NHLGTlEzPMLiaB?= M3KwPGROW09? M4\xdoRm[3KnYYPld{BGT0[UIHX4dJJme3Orb36= M1z2R|I{PTF3N{Wy
H460 NVvkNXZ5TnWwY4Tpc44hSXO|YYm= NV7ZNVZ{OC53L{GvNkDPxE1? MluyOEBp NYXRPJMyTE2VTx?= MYHpcohq[mm2czD0bIUhdGW4ZXzzJI9nKEGtdDCodE1Cc3RrIHHu[EBGT0[U M{CxWlI{PTF3N{Wy
H1650 NX36NmJFTnWwY4Tpc44hSXO|YYm= NYjEZXVKOC53L{GvNkDPxE1? MnOzOEBp NFOyT4dFVVOR NFn5TmRqdmirYnn0d{B1cGVibHX2[Yx{KG:oIFHreEApeC2Da4SpJIFv\CCHR1\S MVKyN|UyPTd3Mh?=
PC9 NWPLcplzTnWwY4Tpc44hSXO|YYm= NFm0TooxNjVxMT:yJO69VQ>? NWnNfo9uPCCq MVvEUXNQ NFjOb4pqdmirYnn0d{B1cGVibHX2[Yx{KG:oIFHreEApeC2Da4SpJIFv\CCHR1\S M2rOTFI{PTF3N{Wy
AsPc1 NHTneVdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4HDSFQ5KGh? MUnFR|UxRTBwMzFOwG0> NGXEboczOzR5NU[5OS=>
Panc0327 NX3uN5lbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmjZOFghcA>? NV\MS5hRTUN3ME2wMlUh|ryP NHfmNZozOzR5NU[5OS=>
MiaPaCa2 MmPQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mmj3OFghcA>? MlXNSWM2OD1yLkeg{txO MnvqNlM1PzV4OUW=
BxPc3 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NULvWVRTPDhiaB?= MojsSWM2OD1zLkCg{txO MUCyN|Q4PTZ7NR?=
Panc0403 NGC3eWJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4P3ZVQ5KGh? NXXHOnlCTUN3ME2xMlEh|ryP MYeyN|Q4PTZ7NR?=
Panc1005 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{fLc|Q5KGh? MYnFR|UxRTFwMTFOwG0> M{HHeVI{PDd3Nkm1
PL45 NFXmNIlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVnOXJd4PDhiaB?= Mk\1SWM2OD1{MD64JO69VQ>? MVmyN|Q4PTZ7NR?=
Panc0203 M1;1SGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{DKTVQ5KGh? NWSxSIltTUN3ME2yNk4zKM7:TR?= M4\2UVI{PDd3Nkm1
Panc0327 MoCxRZBweHSxc3nzJGF{e2G7 NF23SlUyKM7:TR?= M3LPeVI1KGh? MV7pcoR2[2W|IHHwc5B1d3Orcx?= MYOyN|Q4PTZ7NR?=
Panc1005 M2e5WmFxd3C2b4Ppd{BCe3OjeR?= NGLoSJQyKM7:TR?= MYCyOEBp M3PsZolv\HWlZYOgZZBweHSxc3nz NVLlWpZ6OjN2N{W2PVU>
Panc0403 M4TzNGFxd3C2b4Ppd{BCe3OjeR?= Ml\RNUDPxE1? NYPofnZJOjRiaB?= NFfxO5ZqdmS3Y3XzJIFxd3C2b4Ppdy=> MVOyN|Q4PTZ7NR?=
AsPc1 NIjxW2VHfW6ldHnvckBCe3OjeR?= MXSxM|ExKM7:TR?= M4PJSFI1KGh? NHzOU29qdmS3Y3XzJEBoem:5dHigZZJz\XO2ZXSgbY4hTzJxTR?= NETFV2ozOzR5NU[5OS=>
MiaPaCa2 NV7GWZZETnWwY4Tpc44hSXO|YYm= NH21cHUyNzFyIN88US=> MWiyOEBp MV;pcoR2[2W|IDDndo94fGhiYYLy[ZN1\WRiaX6gS|IwVQ>? MWeyN|Q4PTZ7NR?=
T3M4 M3r3SWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{nhdFAuQDByIH7N MV20PEBp NYr1PXNRcW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9vKGmwIHGg[I9{\SCmZYDlcoRmdnRibXHucoVz M3jtZVIzPjhzNkm4
AsPC-1 M{nPUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHXVS4MxNThyMDDuUS=> M2O3cFQ5KGh? NFKyT3dqdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44hcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> NXrjdnVoOjJ4OEG2PVg>
Panc-1  NWX3SWt2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFzONmsxNThyMDDuUS=> M17xTVQ5KGh? NV:2N2t6cW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9vKGmwIHGg[I9{\SCmZYDlcoRmdnRibXHucoVz Mn36NlI3QDF4OUi=
T3M4 MX3BdI9xfG:|aYOgRZN{[Xl? MXGxNFAwPTByL{GwNFAhdk1? NY\LZ3RTPDhiaB?= M1TiV4lv\HWlZYOg[I9{\SCmZYDlcoRmdnRiYYDvdJRwe2m| NH;kToEzOjZ6MU[5PC=>
AsPC-1 MYjBdI9xfG:|aYOgRZN{[Xl? M170SVExOC93MECvNVAxOCCwTR?= NFvGc5A1QCCq MUfpcoR2[2W|IHTvd4Uh\GWyZX7k[Y51KGGyb4D0c5Nqew>? MUCyNlY5OTZ7OB?=
Panc-1  MnrqRZBweHSxc3nzJGF{e2G7 MVuxNFAwPTByL{GwNFAhdk1? MmfuOFghcA>? M4DzTYlv\HWlZYOg[I9{\SCmZYDlcoRmdnRiYYDvdJRwe2m| MnzxNlI3QDF4OUi=
HBL-2 MlrtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NE\zeHozPCCq MX3JR|UxRTBwNDFOwG0> Ml\mNlAxPjhyOEC=
Jeko-1 NFHGd5BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnrTNlQhcA>? M4rXd2lEPTB;MD6yJO69VQ>? MmnzNlAxPjhyOEC=
Granta-519 NUe0UoRGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn6yNlQhcA>? M2SyfmlEPTB;NU[uN{DPxE1? M3PUflIxODZ6MEiw
HCT116 M1i4Umdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXnYSIoyPDhiaB?= M3HUOmVEPTB;MD6yPEDPxE1? MmrlNVcyOjR3OUS=
HCT116 NXXqOIJWTnWwY4Tpc44hSXO|YYm= NE\rVpkxNjoEoN88UeKh Ml;tNlQhcA>? NIT1dIFld3ewLYLl[5Vt[XS|IGTTJJBzd3SnaX6gcIV3\Wy|IHHmeIVzKDcEoHigbY5kfWKjdHnvci=> NEnXXZkyPzF{NEW5OC=>

他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい

体内試験 Belinostat indicates significant tumor growth delay in A2780 and A2780/cp70 xenograft at a dose of 10mg/kg with no effects on the body weight. [1] Belinostat also induces p21WAF1, HDAC core and cell communication genes in mouse bladder tumors. [2] Belinostat monotherapy induces dose-proportional antitumor effects with TGI of 47% at a dose of 100mg/kg in A2780 xenograft. The combination of Belinostat (100 mg/kg) with carboplatin (40 mg/kg) could delay tumor growth from 18.6 days to 22.5 days. [3] Combining with bortezomib, Belinostat results in great tumor inhibition and gastrointestinal toxicity in mice with bortezomib-resistant UMSCC-11A xenograft. [5]

お薦めの試験操作(参考用のみ)

キナーゼ試験:[1]
+ 展開

Histone Deacetylase Activity:

Subconfluent cultures are harvested and washed twice in ice cold PBS and pelleted by centrifugation at 200 × g for 5 min. The cell pellet is resuspended in two volumes of lysis buffer [60 mM Tris buffer (pH 7.4) containing 30% glycerol and 450 mM NaCl] and lysed by three freeze (dry ice) thaw (30 °C water bath) cycles. Cell debris is removed by centrifugation at 1.2 × 104 g for 5 min, and the supernatant is stored at −80 °C. Histone H4 peptide (sequence SGRGKGGKGLGKGGAKRHRK corresponding to the 20 NH2-terminal residues) is acetylated by a recombinant protein containing the hypoxanthine-aminopterin-thymidine domain of p300, using [3H]acetyl CoA as a source of acetate. H4 peptide (100 μg) is mixed with hypoxanthine-aminopterin-thymidine buffer (50 mM Tris HCl pH 8.0, 5% glycerol, 50 mM KCl, and 0.1 mM EDTA), 1 mM DTT, 1 mM 4-(2-aminoethyl) benzenesulfonylfluoride, 1 × complete protease inhibitors, 50 μL of purified p300, and 1.85 m [3H]acetyl CoA (4.50Ci/mmol) in a final volume of 300 μL and incubated at 30 °C for 45 min. The p300 protein is removed by incubation with 20 μL of 50% Ni-agaroase beads for 1 hour at 4 °C and centrifugation. The supernatant is applied to a 2 mL Sephadex G15 column, and the flow through is collected. One milliliter of distilled H2O is gently applied, and three drop fractions are collected; this is repeated until 4–5 mL of distilled H2O has been added, and ∼40 fractions are collected. Three microliters of each fraction are diluted in 2 mL of scintillation fluid and counted in a scintillation counter to identify the fractions containing the labeled peptide. These fractions are pooled, and 1 μL of the combined sample is measured to assess the radioactivity in every peptide batch (3-7×103 cpm/μL). For activity assays, the reaction is carried out in a total volume of 150 μL of buffer [60 mM Tris (pH 7.4) containing 30% glycerol] containing 2 μL of cell extract and, where used, 2 μL of belinostat. The reaction is started by the addition of 2 μL of [3H] labeled substrate (acetylated histone H4 peptide corresponding to the 20 NH2-terminal residues). Samples are incubated at 37 °C for 45 min, and the reaction stopped by the addition of HCl and acetic acid (0.72 and 0.12 M final concentrations, respectively). Released [3H]acetate is extracted into 750 μL of ethyl acetate, and samples are centrifuged at 1.2× 104 g for 5 min. The upper phase (600 μL) is transferred to 3 mL of scintillation fluid and counted.
細胞試験: [1]
+ 展開
  • 細胞株: A2780, A2780/cp70, 2780AD, HCT116, HT29, WIL, CALU-3, MCF7, PC3 and HS852
  • 濃度: 0.016 - 10 μM
  • 反応時間: 24 hours
  • 実験の流れ: Tumor cell lines are seeded in 5 mL of medium at a density of 8 × 104 cells/25 cm2 flask and incubated for 48 hours. Cells are exposed to Belinostat (0.016 to 10 μM) for 24 hours. The medium is removed, and 1 mL of trypsin/EDTA is added to each flask. Once the cells have detached, 1 mL of medium is added, the cells are resuspended, and those from the control untreated flask are counted. Cells are diluted and plated into 6-cm Petri dishes (three per flask) at a density of 0.5-2× 103 cells/dish depending on the cell line. Cells from the drug-treated flasks are diluted and plated as for the control flasks. Dishes are incubated for 10–15 days at 37 °C. Cells are washed with PBS, fixed in methanol, and stained with crystal violet, and colonies that contained ≥50 cells counted. Sensitivity is expressed as the IC50 defined as the concentration of belinostat required to reduce the number of colonies to 50% of that of the control untreated cells.
    (参考用のみ)
動物試験:[1]
+ 展開
  • 動物モデル: A2780, A2780/cp70 and HCT116 cells are injected s.c. into the right flank of CD1 nu/nu mice.
  • 製剤: Dissolved in DMSO and then diluted in water to give a final concentration of DMSO of 10%
  • 投薬量: ≤40 mg/kg
  • 投与方法: Administered via i.p.
    (参考用のみ)

溶解度 (25°C)

体外 DMSO 64 mg/mL (201.03 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(文献ではなく、Selleckの実験によるデータ):
2% DMSO+30% PEG 300+ddH2O
混合させたのち直ちに使用することを推奨します。
10mg/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 318.35
化学式

C15H14N2O4S

CAS No. 414864-00-9
保管
in solvent
別名 NSC726630, PX-105684

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モル濃度計算器

モル濃度計算器

求めたい質量、体積または濃度を計算してください。

質量 (g) = 濃度 (mol/L) x 体積 (L) x 分子量 (g/mol)

モル濃度計算器方程式

  • 質量
    濃度
    体積
    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

貯蔵液を準備するために必要な希釈率を計算してください。Selleck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 ( 入力 出力 )

  • 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

質量 濃度 体積 分子量

臨床試験

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03772925 Not yet recruiting Recurrent Acute Myeloid Leukemia|Recurrent Myelodysplastic Syndrome|Refractory Acute Myeloid Leukemia|Refractory Myelodysplastic Syndrome National Cancer Institute (NCI) May 31 2019 Phase 1
NCT03772925 Not yet recruiting Recurrent Acute Myeloid Leukemia|Recurrent Myelodysplastic Syndrome|Refractory Acute Myeloid Leukemia|Refractory Myelodysplastic Syndrome National Cancer Institute (NCI) May 31 2019 Phase 1
NCT03432741 Recruiting Breast Adenocarcinoma|Recurrent Breast Carcinoma|Recurrent Hodgkin Lymphoma|Recurrent Mycosis Fungoides|Recurrent Non-Hodgkin Lymphoma|Recurrent Primary Cutaneous T-Cell Non-Hodgkin Lymphoma|Refractory Hodgkin Lymphoma|Refractory Mycosis Fungoides|Refractory Nodal Marginal Zone Lymphoma|Refractory Non-Hodgkin Lymphoma|Refractory Primary Cutaneous T-Cell Non-Hodgkin Lymphoma|Stage IV Breast Cancer AJCC v6 and v7 Mayo Clinic|National Cancer Institute (NCI) March 27 2018 Phase 1
NCT03432741 Recruiting Breast Adenocarcinoma|Recurrent Breast Carcinoma|Recurrent Hodgkin Lymphoma|Recurrent Mycosis Fungoides|Recurrent Non-Hodgkin Lymphoma|Recurrent Primary Cutaneous T-Cell Non-Hodgkin Lymphoma|Refractory Hodgkin Lymphoma|Refractory Mycosis Fungoides|Refractory Nodal Marginal Zone Lymphoma|Refractory Non-Hodgkin Lymphoma|Refractory Primary Cutaneous T-Cell Non-Hodgkin Lymphoma|Stage IV Breast Cancer AJCC v6 and v7 Mayo Clinic|National Cancer Institute (NCI) March 27 2018 Phase 1
NCT02737046 Recruiting Adult T-cell Leukemia-Lymphoma|ATLL University of Miami December 12 2016 Phase 2
NCT02737046 Recruiting Adult T-cell Leukemia-Lymphoma|ATLL University of Miami December 12 2016 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:

    Could you please give some suggestions for the use of Belinostat in vivo (i.p. injection)?

  • 回答:

    For I.P. injection, S1085 Belinostat (PXD101) can be dissolved in 2% DMSO+30% PEG 300+ddH2O at 10 mg/ml clearly. When preparing the solution, please dissolve the compound in DMSO clearly first. Then add PEG, after they mixed well, then dilute with water. Hope this information is useful to you.

HDACシグナル伝達経路

HDAC Inhibitors with Unique Features

相関HDAC製品

Tags: Belinostat (PXD101)を買う | Belinostat (PXD101) ic50 | Belinostat (PXD101)供給者 | Belinostat (PXD101)を購入する | Belinostat (PXD101)費用 | Belinostat (PXD101)生産者 | オーダーBelinostat (PXD101) | Belinostat (PXD101)化学構造 | Belinostat (PXD101)分子量 | Belinostat (PXD101)代理店
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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