YM155 (Sepantronium Bromide)

Catalog No.S1130

YM155 (Sepantronium Bromide) Chemical Structure

Molecular Weight(MW): 443.29

YM155 (Sepantronium Bromide) is a potent survivin suppressant by inhibiting Survivin promoter activity with IC50 of 0.54 nM in HeLa-SURP-luc and CHO-SV40-luc cells; does not significantly inhibit SV40 promoter activity, but is observed to slightly inhibit the interaction of Survivin with XIAP. Phase 2.

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Cited by 41 Publications

12 Customer Reviews

  • Dose response of ALL cell lines to YM155. Asynchronous populations of cells were treated with increasing doses of YM155 for 72 h. Then, viability was measured by MTS and normalized to no drug control. S.e.m. bars are inserted. Dotted line represents 50% viability.

    Leukemia 2012 26, 623-632. YM155 (Sepantronium Bromide) purchased from Selleck.

    Treatment of SUPB15 cells with imatinib or YM155. Top panel shows cells treated with siRNA in the presence of 500 nM imatinib. Cells were treated with siRNA, and then subsequently incubated in 500 nM imatinib for 96 h. Bottom panel shows the partial rescue of SUPB15 cells treated with 100 nM YM155 for 96 h. S.e.m. bars are inserted into each graph.

    Leukemia 2012 26, 623-632. YM155 (Sepantronium Bromide) purchased from Selleck.

  • Inhibition of survivin expression restricts VZV repl ication and sprea d in vitro . ( A ) HEL F were infected w ith VZV-GFP in the presence of YM155 or DMSO, and infectious virus yields were determined at 48 hpi by titration on melanoma cells. ( B) VZV-GFP-infected HELF were treated with DMSO or YM155; plaques were detected by staining with anti-VZV IgG at 48 hpi. Plaque sizes were determined using ImageJ; the graph shows the mean size ?S EM o f 30 plaques . (C )Expression of VZV proteins was assessed in VZV-infected HELF lysat e s (24 hp i) treated with YM155 or DMSO.

    Proc Natl Acad Sci U S A 2012 109, 600-5. YM155 (Sepantronium Bromide) purchased from Selleck.

    MM cell lines UM9 (left panel) or U266 (right panel) were cultured in presence or absence of accessory cells prior to incubation with CTLs alone, YM155 alone or the combination. Survival of UM9 and U266 MM cells was assessed by CS-BLI. Results show % lysis of MM cells after 24 hour incubation and are depicted for three doses.

    Clin Cancer Res 2013 19, 5591-601. YM155 (Sepantronium Bromide) purchased from Selleck.

  • Survivin inhibitor increased apoptosis in burn serum-stimulated cardiomyocytes. a YM155 increased apoptosis in burn serumstimulated cardiomyocytes in a concentration-dependent manner. Neonatal rat cardiomyocytes were treated with YM155 (3-300 nM at the indicated) for 2 h prior to stimulation burn serum for 12 h. The extent of DNA fragmentation was quantified using the Cell Death Detection ELISA. versus 0 nM YM155 plus stimulation with burn serum. b YM155 (100 nM) pretreatment increased the apoptosis production at 2 or 12 h after burn serum stimulation. c Representative blots of survivin and cleaved caspase-3 in YM155 (100 nM) pretreated cardiomyocytes at 2 and 12 h after burn serum stimulation. d Bar graphs show the relative proteins.

    Basic Res Cardiol 2011 106, 1207-1220. YM155 (Sepantronium Bromide) purchased from Selleck.

    Induction of cardiomyocytes apoptosis by survivin inhibitor in vivo. After YM155 was administered (5 mg/kg/day) for 5 days, the rats were exposed to a 40% TBSA burn (burn injury) or 25C water (sham) and killed 6 h after burn injury. The frozen sections of the ventricular tissues or whole cell lysates were prepared. Apoptotic staining was performed using the TUNEL method and immunostained using a-sarcomeric actin. The survivin and cleaved caspase-3 levels were measured by Western blot analysis. a Representative blots of survivin and cleaved caspase-3. b The statistical analysis of the relative proteins .c Figures are representative of two independent TUNEL experiments. Green fluorescence represents apoptotic cells, whereas red stain indicates staining for a-sarcomeric actin specific for cardiac myocytes. d Bar graph summarizes the counted apoptotic cells.

     

     

    Basic Res Cardiol 2011 106, 1207-1220. YM155 (Sepantronium Bromide) purchased from Selleck.

  • YM-155 sensitizes ABT-263-induced apoptosis in HCC cells. A. LH86 and B. Huh7 cells were untreated or treated with ABT-263(1 μM), YM-155(1 μM) or combination of ABT-263(1 μM) and YM-155(1 μM) for up to 6 h. Then apoptotic cells were assessed as in Figure 2A and2B (representative apoptotic cells were marked with white arrows). C. LH86 and D. Huh7 cells were untreated or treated with ABT-263(1 μM), YM-155(1 μM) or combination of ABT-263(1 μM) and YM-155(1 μM) for 6 h. Cells with apoptotic nuclei were counted to determine cell death ratio (*p<0.05, **p<0.05). E. LH86 cells and F. Huh7 cells were treated as indicated and cell lysates were prepared and subjected to Western blotting.Apoptosis was evaluated through caspase 3 activation. b-actin was used as an equal protein loading control. G. LH86 cells grown in six-well plate were untreated (control) or treated with different conditions as indicated for 48 h. After rinsed with fresh culture medium for 3 times, cells were cultured for another two weeks. Cell colony formation assays were performed with crystal violet staining. H. colony number were counted to show combination treatment with ABT-263 and YM-155 resulted in reduction of clonogenesis (#p<0.05).

    PLoS One 2011 6, e21980. YM155 (Sepantronium Bromide) purchased from Selleck.

    Survivin down-regulation sensitizes ABT-263-induced apoptosis in HCC cells. A. LH86 cells were treated as indicated and cell lysates were prepared for Western blotting. Pro-apoptotic proteins: Bax, Bad, and Bak and anti-apoptotic proteins Bcl-xL and Mcl-1 were assessed with specific antibodies respectively. b-actin was detected and served as an equal protein loading control. B. LH86 cells were untreated or treated with ABT-263 (1 μM), YM-155 (1 μM) or combination of ABT-263 (1 μM) and YM155 (1 μM) for up to 6 h as indicated. Then cells were harvested and cell lysates were prepared for Western blotting. Anti-survivin and anti-Bcl-xL polyclonal antibodies were used to assess protein levels for survivin and Bcl-xL respectively. b-actin was used as an equal protein loading control. The band intensities of survivin, Bcl-xL, and b-actin was qualified with Image J software. C. LH86 cells were transiently transfected with synthesized random siRNA (control) or survivin specific siRNA duplexes, and 48 h posttransfection, cells were subjected to Western blotting analysis with anti-survivin polyclonal antibody. β-actin was used as an equal protein loading control. D. LH86 cells were transfected with synthesized random control siRNA or survivin specific siRNA, and 48 h post-transfection, cells were untreated or treated with ABT-263 (1 μM) for 24 h and then subjected to Hoechst staining to show apoptotic cells with condensed nuclei (representative apoptotic cells were marked with white arrows). E. LH86 cells were treated as in Figure 4D and apoptosis was measured as in Figure 2A. Statistical analysis was performed for apoptosis ratio by counting the number of cells with apoptotic nuclei (*p<0.05). F. LH86 cells treated as in Figure 4D were harvested and cell lysates were prepared and subjected to Western blotting. Apoptosis was determined through caspase 3 activation. β-actin was used as an equal protein loading control.

    PLoS One 2011 6, e21980. YM155 (Sepantronium Bromide) purchased from Selleck.

  • Effects of YM155 on cell viability (A) and cell cycle (B), and on experiment of survivin mRNA (C) and protein (D) in the MiaPaCa-2 human pancreatic cancer cell line.

    Anticancer Res 2012 32, 1681-8. YM155 (Sepantronium Bromide) purchased from Selleck.

     

    IPF fibroblasts from 8 different patients were cultured to 60% confluence in DMEM supplemented with 10% fetal bovine serum and growth-arrested for 24 hours in serum-free DMEM prior to treatment for 16 hours with/without the Fas-activating antibody CH11 (FasL; 250 ng/ml) in the presence/absence of the survivin inhibitors CAY10625 (5 µM) or YM155 (10.0 µM), or with the survivin inhibitors alone. (a) Apoptosis was assessed using ELISA-based detection of histone associated DNA fragments. To allow relative comparisons of apoptosis across experiments, the data for each cell line is expressed as the percentage of the assay positive control that was included on each ELISA plate. The scatter plot shows the distribution of responses in individual cell lines along with the mean ± standard error for each treatment group. p = 0.038 overall (ANOVA). p = 0.027 for FasL compared to FasL/CAY10625, and p = 0.046 for FasL compared to FasL/YM155; (b) The correlation of apoptosis between IPF fibroblasts treated with FasL/CAY10625 and FasL/YM155. Each point represents a different IPF cell line. The Spearman correlation (r) = 0.95.
     

    Adv Biosci Biotechnol 2012 3, 657-664. YM155 (Sepantronium Bromide) purchased from Selleck.

  • Total RNA from livers of these mice were isolated from tissues using TRIZOL (Invitrogen). cDNA synthesis was performed with the M-MLV RTase cDNA Synthesis Kit (Promega). qRT-PCR reactions were performed using SYBR Green (Takara) on ABI 7500 Fast system. Expression levels of Survivin gene were measured by qRT-PCR in livers injected with 0.9% Nacl (91#,92#) or YM155 48 hours after DEN treatment.

    Lihua Min of Chinese Academy of Sciences. YM155 (Sepantronium Bromide) purchased from Selleck.

    Western blot analysis of Survivin. U-251 and PC-3 cell line was treated with 0-100nM YM-155.

     

     

    Dr. Chunrong Yu of RoswelI Park Cancer Institute. YM155 (Sepantronium Bromide) purchased from Selleck.

Purity & Quality Control

Choose Selective Survivin Inhibitors

Biological Activity

Description YM155 (Sepantronium Bromide) is a potent survivin suppressant by inhibiting Survivin promoter activity with IC50 of 0.54 nM in HeLa-SURP-luc and CHO-SV40-luc cells; does not significantly inhibit SV40 promoter activity, but is observed to slightly inhibit the interaction of Survivin with XIAP. Phase 2.
Targets
Survivin [1]
(HeLa-SURP-luc, CHO-SV40-luc cells)
0.54 nM
In vitro

YM155 is not sensitive to survivn gene promoter-driven luciferase reporter activity even at 30 μM. YM155 significantly inhibits endogenous survivin expression in PC-3 and PPC-1 human HRPC cells with deficient p53 through transcriptional inhibition of the survivin gene promoter. On the contrary YM155 shows no sufficient effect on protein expression of c-IAP2, XIAP, Bcl-2, Bcl-xL, Bad, α-actin, and β-tubulin at 100 nM. YM155 indicates great apoptosis in human cancer cell lines including PC-3 and PPC-1 with a concomitant increase in caspase-3 activity. YM155 potently inhibits human cancer cell lines (mutated or truncated p53) including PC-3, PPC-1, DU145, TSU-Pr1, 22Rv1, SK-MEL-5 and A375 with IC50 from 2.3 to 11 nM, respectively. [1] YM155 increases the sensitivity of NSCLC cells to γ-radiation. The combination of YM155 and γ-radiation increases both the number of apoptotic cells and the activity of caspase-3. YM155 delays the repair of radiation-induced double-strand breaks in nuclear DNA. [2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Kasumi-1 NF3EeGFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWK3NkBp NFLY[oJFVVOR NFXveGNKSzVyPUCuNFA6KMLzIECuNFAxQSEQvF2= Mnv4NlU3PTl5M{G=
M-07e NYfuWGZ[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlS2O|IhcA>? MULEUXNQ NF;TOZlKSzVyPUCuNFQxKMLzIECuNFE{KM7:TR?= Mni1NlU3PTl5M{G=
THP-1 NGjWOmdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NY\1VHBCPzJiaB?= MnPMSG1UVw>? MVnJR|UxRTBwMEWxJOKyKDBwMEGzJO69VQ>? NUf2VYJ2OjV4NUm3N|E>
CMK Mn\oS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnzCO|IhcA>? MXnEUXNQ MnPFTWM2OD1yLkC1N{DDuSByLkCwPUDPxE1? MmrXNlU3PTl5M{G=
MV4-11 NIPuNWpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1vJelczKGh? M2fwVmROW09? MVzJR|UxRTBwMEW1JOKyKDBwMEK4JO69VQ>? NX3iXYl1OjV4NUm3N|E>
AML-193 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVW3NkBp M2i1ZWROW09? NX7hUHdQUUN3ME2wMlQ3OiEEsTCwMlA3OCEQvF2= MkX6NlU3PTl5M{G=
HL-60 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVPwW2Q5PzJiaB?= M4PNO2ROW09? NGfYWIRKSzVyPUCuNFAyKMLzIECuNFAxOiEQvF2= MmW5NlU3PTl5M{G=
ML-2 M2i1dWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2rzPFczKGh? M{fnTmROW09? NW\0cJpSUUN3ME2wMlAxQSEEsTCwMlAxOiEQvF2= NHXtTnozPTZ3OUezNS=>
OCI/AML3 NWnvSnNrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFfyfIo4OiCq NUXpS41bTE2VTx?= NX\Me5R6UUN3ME2wMlAyOSEEsTCwMlAxOiEQvF2= M1rWWVI2PjV7N{Ox
HEL NXzXW4RST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mne3O|IhcA>? NFrOfYFFVVOR M4i2[mlEPTB;MD61OVkhyrFiMD6wN|gh|ryP NEjKOXUzPTZ3OUezNS=>
ME-1 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH;KeIE4OiCq MlXHSG1UVw>? MUTJR|UxRTBwNki0JOKyKDBwMUe5JO69VQ>? NVTZXmNbOjV4NUm3N|E>
THP-1 MVPBdI9xfG:|aYOgRZN{[Xl? M2[yVFHDqM7:TR?= NFW1Vo44OiCq MnLWSG1UVw>? M2H1Rolv\HWlZYOgZZBweHSxc3nz NVvHd5VqOjV4NUm3N|E>
M-07e NGDuU5VHfW6ldHnvckBCe3OjeR?= NFLQcIgx6oDVMdMg{txO MYe3NkBp NH7QfoRFVVOR M2HtNIlv\HWlZYOg[I94dnKnZ4XsZZRqd25ib3[gV5Vzfmm4aX6= NIjQbIczPTZ3OUezNS=>
THP-1 M1PNOGZ2dmO2aX;uJGF{e2G7 M{GzfFDjiJNzwrFOwG0> NWrSUWpuPzJiaB?= MVXEUXNQ MX\pcoR2[2W|IHTve45z\We3bHH0bY9vKG:oIGP1dpZqfmmw M2rEVFI2PjV7N{Ox
CMK NH;H[GdHfW6ldHnvckBCe3OjeR?= NEO3fYcx6oDVMdMg{txO NHfxTlM4OiCq M4faeWROW09? NYPYblFkcW6mdXPld{Bld3ewcnXneYxifGmxbjDv[kBUfXK4aY\pci=> NInMT4YzPTZ3OUezNS=>
AML-193 MXrGeY5kfGmxbjDBd5NigQ>? MYGw5qCUOcLizszN MUK3NkBp NECwOWJFVVOR MnjNbY5lfWOnczDkc5dvemWpdXzheIlwdiCxZjDTeZJ3cX[rbh?= MWmyOVY2QTd|MR?=
Kasumi-1 NFzLc5ZHfW6ldHnvckBCe3OjeR?= NWTCOGJQOOLCk{JCpO69VQ>? NX[1O45WPzJiaB?= MkjoSG1UVw>? MWHpcoR2[2W|IHTve45z\We3bHH0bY9vKG:oIGP1dpZqfmmw M1;EfFI2PjV7N{Ox
MV4-11 Mn;SSpVv[3Srb36gRZN{[Xl? MVmw5qCUOcLizszN MX[3NkBp NH\IdmFFVVOR M1f3TIlv\HWlZYOg[I94dnKnZ4XsZZRqd25ib3[gV5Vzfmm4aX6= MYSyOVY2QTd|MR?=
MUG-Chor  M{DSbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVGwMVUh|ryP M120blI1NzR6IHi= NFX4S|JKSzVyPUeuNFXjiImwTTDmc5IhPDiq MWCyOVY1ODF6NR?=
U-CH1  MlnDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoHHNE02KM7:TR?= NUjQWWZ7OjRxNEigbC=> Ml;TTWM2OD17LkCz5qCKdk1iZn;yJFQ5cA>? M4C3U|I2PjRyMUi1
KATOIII MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmPtNVAwOjBibl2= MmK3OFghcA>? M2K5S4lvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz Mo\BNlU3OzVyNUW=
AGS  M{izUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3PpTlExNzJyIH7N MWO0PEBp NELrN|FqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? MWeyOVY{PTB3NR?=
SACC-83 NVnKZnVUTnWwY4Tpc44hSXO|YYm= NHvIZ4Y2KG6P M{HWcVQ5KGh? MofL[IVkemWjc3XzJI52[2ynYYKg[ZhxemW|c3nvckBw\iCKSV[tNe6y M4rYVFI2PDh3NkO1
INA-6 MmjpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH3tXlQxNTVyMDDuUS=> NGTMV|M1QCCq MUfpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NF7RXIgzPTJ7Nkm3PC=>
U-266 NFfWeWlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlH1NE02ODBibl2= MkPnOFghcA>? M{DiVolvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NIHmeW4zPTJ7Nkm3PC=>
MOLP-8 MnHZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXewMVUxOCCwTR?= Mn21OFghcA>? M2[yfIlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NH\tV2YzPTJ7Nkm3PC=>
HG-1 NU[xTVNDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml:3NE02ODBibl2= Mn:1OFghcA>? NYm2[Y5ocW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NYO5R|l7OjV{OU[5O|g>
NCI-H929 M1jaTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGL1[2gxNTVyMDDuUS=> NFz0UJc1QCCq MoTTbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MViyOVI6Pjl5OB?=
OPM-2 M2noZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHTBN5YxNTVyMDDuUS=> NGPMTo81QCCq NVfHVVRHcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NHXnbIEzPTJ7Nkm3PC=>
L-363 Mly5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2K1OVAuPTByIH7N MYC0PEBp NFrXVo9qdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NVvucI9yOjV{OU[5O|g>
MOLP-2 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXfNUmdxOC13MECgcm0> NVLGfWIzPDhiaB?= M13aN4lvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz M2HaelI2Ojl4OUe4
KMS-12-BM MkDPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4DTPVAuPTByIH7N NUPwUXlzPDhiaB?= MWfpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MkTLNlUzQTZ7N{i=
SK-MM-2 M2Loemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M37vVVAuPTByIH7N M1j5dFQ5KGh? NUjjOWhicW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MViyOVI6Pjl5OB?=
U-266 NHvmWFBCeG:ydH;zbZMhSXO|YYm= NF3ze4MxNTVyIH7N Mnr0NlQhcA>? M3vqeIlv\HWlZYOgZZBweHSxc3nz NGPOWm0zPTJ7Nkm3PC=>
INA-6  NEPUPJdCeG:ydH;zbZMhSXO|YYm= MVSwMVUxKG6P NXGxdFc4OjRiaB?= NX7hU3R7cW6mdXPld{BieG:ydH;zbZM> MYeyOVI6Pjl5OB?=
MCF7 NHXkcIdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmnUO|IhcA>? M1TCU2lEPTB;MUOgxtEhPiCwTR?= M{S3WVI2OjJyMkK1
MCF7-TamR6 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MW[3NkBp M{DzSWlEPTB;ODFCtUA3KG6P NUfZOo51OjV{MkCyNlU>
MCF7-TamR7 NITYWZNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3;YR|czKGh? M{nOVWlEPTB;ODFCtUA{KG6P NV\Bb2NqOjV{MkCyNlU>
MCF7-TamR8 M{m0V2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlftO|IhcA>? M3jnbWlEPTB;MUWgxtEhPiCwTR?= NHXh[pozPTJ{MEKyOS=>
MCF7-TamC3 M123Z2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkC5O|IhcA>? NVTRT3BMUUN3ME22JOKyKDNibl2= NWK1[I5sOjV{MkCyNlU>
MCF7-TamC6 MnLUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1nz[FczKGh? NF\5VXdKSzVyPU[gxtEhOC5zIH7N MYiyOVIzODJ{NR?=
MDA-MB-231 NFrwdZVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX6wbIRRPzJiaB?= NYW3Sm5jUUN3ME21JOKyKDFibl2= NUnTeVhwOjV{MkCyNlU>
SK-BR-3 MnW5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIDTO3g4OiCq NIXKXJBKSzVyPUegxtEhOC5|IH7N M{PVeFI2OjJyMkK1
Eca109 NXPiN45NTnWwY4Tpc44hSXO|YYm= NV;P[4o3OS13MDDuUS=> NIjOPW81QCCq M2Lzc2ROW09? Ml;Rd5VxeHKnc4Pld{B{fXK4aY\pckBmgHC{ZYPzbY9vKGmwIHGg[I9{\SCmZYDlcoRmdnRibXHucoVz MmO2NlUyOzl|OUW=
TE13 NFS3eHRHfW6ldHnvckBCe3OjeR?= MUWxMVUxKG6P M2\GS|Q5KGh? M2TnU2ROW09? MkTyd5VxeHKnc4Pld{B{fXK4aY\pckBmgHC{ZYPzbY9vKGmwIHGg[I9{\SCmZYDlcoRmdnRibXHucoVz M2HTNVI2OTN7M{m1
Eca109 NF;ocFlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYf5WVRlOC1zMECgcm0> M{fEb|I1NzR6IHi= M{fGbWROW09? NXvzZ3d5\GWlcnXhd4V{KGOnbHygeoli[mmuaYT5JIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy MVuyOVE{QTN7NR?=
TE13 NIHuOVJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1;DblAuOTByIH7N Ml;pNlQwPDhiaB?= NVTofW1XTE2VTx?= NGD5dXBl\WO{ZXHz[ZMh[2WubDD2bYFjcWyrdImgbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK= MYSyOVE{QTN7NR?=
MT-3 M3K3cmtqdmG|ZTDBd5NigQ>? NXXu[JgzPzJiaB?= MV3EUXNQ NVXXfWdxUUN3ME2yMlg3KMLzIECuOVQhdk1iZn;yJGRTPCCneIDy[ZN{cW:w MlfHNlQ5PjZ3OEW=
MDA-MB-468 M3;mVGtqdmG|ZTDBd5NigQ>? MoL0O|IhcA>? M3nPcmROW09? NG\3WFNKSzVyPUCuNVEhyrFiMD6wNUBvVSCob4KgSHI1KGW6cILld5Nqd25? MWSyOFg3PjV6NR?=
SUM-159 MoizT4lv[XOnIFHzd4F6 NEizcpY4OiCq NXrnNHdiTE2VTx?= MkL5TWM2OD1zLkeyJOKyKDBwM{Ogcm0h\m:{IFTSOEBmgHC{ZYPzbY9v NYLBTHVzOjR6Nk[1PFU>
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M059J MYfBdI9xfG:|aYOgRZN{[Xl? NIrjW2Q{OCCwTR?= MXSyOEBp MXzpcoR2[2W|IHHwc5B1d3Orcx?= MlHVNlI4PzBzMUC=
M059K NEj6SnRCeG:ydH;zbZMhSXO|YYm= MnXvN|Ahdk1? NGixT2wzPCCq NGK2cFlqdmS3Y3XzJIFxd3C2b4Ppdy=> MYeyNlc4ODFzMB?=
PANC-1 NITBbnlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3PwflAvODFvMUCwNEBvVQ>? MVu0PEBp MoP2TWM2OD1|Lk[5JI5O NVLWd|NoOjJ5MkO4O|E>
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MIAPaCa-2 MXLGeY5kfGmxbjDBd5NigQ>? MXewMVExODBibl2= M3zSfVI1KGh? NVX0T3U4cW6mdXPld{Bld3ewcnXneYxifGmxbjDv[kBZUUGSIHHu[EB{fXK4aY\pckBmgHC{ZYPzbY9v NHzoU5MzOjd{M{i3NS=>
BxPC-3 MkHMSpVv[3Srb36gRZN{[Xl? NI\YTVkxNTFyMECgcm0> M3\uO|I1KGh? NY\vNot3cW6mdXPld{Bld3ewcnXneYxifGmxbjDv[kBZUUGSIHHu[EB{fXK4aY\pckBmgHC{ZYPzbY9v MX:yNlczOzh5MR?=
RPMI-7951 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXHFd|JyT0l3ME2zMlIhdk1? M13DfVIyPzN5NUCy
SK-MEL-5 NWLVUJV7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH\3[pRIUTVyPUSuNkBvVQ>? M{H6PFIyPzN5NUCy
A375 NVO0fnJHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFrkcVBIUTVyPU[uN{BvVQ>? MoDBNlE4Ozd3MEK=
SK-MEL-28 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWXHTVUxRTdwNjDuUS=> NVH3TW9tOjF5M{e1NFI>
SK-MEL-2 NUHDfo9DT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MW\HTVUxRTFzIH7N Mo\HNlE4Ozd3MEK=
DB M{nDU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXW0POKhcA>? NGDCdVNIUTVyPUOuOUBvVQ>? MkfYNlEzOzd3MEi=
Pfeiffer NGPucpRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlHjOFjDqGh? MlvkS2k2OD1|Lkmgcm0> NET1TIQzOTJ|N{WwPC=>
SU-DHL-5 NXWybpZiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH3tTXk1QMLiaB?= NHn0c|NIUTVyPUCuNlMhdk1? Mn;FNlEzOzd3MEi=
SU-DHL-8 NHiyd3JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mk\WOFjDqGh? M2LRT2dKPTB;MT60JI5O NXuwXoI5OjF{M{e1NFg>
WSU-DLCL-2 MmPSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUO0POKhcA>? M2G3bWdKPTB;MT60JI5O NV6yOpZDOjF{M{e1NFg>

... Click to View More Cell Line Experimental Data

In vivo YM155 completely inhibits the tumor growth of PC-3 s.c. xenografted prostate tumors at doses of 3 and 10 mg/kg, without body weight loss and blood cell count decrease. Pharmacokinetic analysis shows that YM155 is highly distributed to tumor tissue. Moreover, YM155 shows 80% TGI at a dose of 5 mg/kg in PC-3 orthotopic xenografts. [1] The combination therapy with YM155 and γ-radiation shows great antitumor activity against H460 or Calu6 xenografts in nude mice. [2]

Protocol

Kinase Assay:

[1]

+ Expand

Promoter-luciferase reporter assay:

A 2,767-bp sequence of human survivin gene promoter is isolated from human genomic DNA by PCR using Pyrobest polymerase and the following primers: 5
Cell Research:

[1]

+ Expand
  • Cell lines: Hormone refractory prostate cancer cell lines (PC-3, PPC-1, DU145, TSU-Pr1 and 22Rv1) and malignant melanoma cell lines (SK-MEL-5 and A375)
  • Concentrations: ~ 100 nM
  • Incubation Time: 48 hours
  • Method:

    Cells are seeded in 96-well plates at a density of 5-40 × 103. YM155 is dissolved in DMSO and added to cells for 48 hours. Then the cell count is determined by sulforhodamine B assay.


    (Only for Reference)
Animal Research:

[1]

+ Expand
  • Animal Models: PC-3 s.c. (orthotopic) xenografts in male nude mice (BALB/c nu/nu)
  • Formulation: Dissolved and diluted in saline immediately before administration
  • Dosages: 5 mg/kg
  • Administration: Subcutaneous injection as a 3-day continuous infusion per week for 3 weeks by an implanted micro-osmotic pump
    (Only for Reference)

Solubility (25°C)

In vitro Water 89 mg/mL (200.77 mM)
DMSO 55 mg/mL (124.07 mM)
Ethanol 6 mg/mL (13.53 mM)
In vivo Add solvents individually and in order:
Saline
30 mg/mL

* 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 443.29
Formula

C20H19BrN4O3

CAS No. 781661-94-7
Storage powder
in solvent
Synonyms N/A

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
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    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • 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):
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Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

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To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01100931 Completed NSCLC|Solid Tumors National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) February 2010 Phase 1|Phase 2
NCT01038804 Completed Breast Cancer Astellas Pharma Inc December 2009 Phase 2
NCT01023386 Completed Cancer Astellas Pharma Inc November 2009 Phase 1
NCT01009775 Completed Melanoma Astellas Pharma Inc November 2009 Phase 2
NCT01007292 Completed Non-Hodgkins Lymphoma Astellas Pharma Inc November 2009 Phase 2
NCT00498914 Terminated Lymphoma, Large-Cell, Diffuse|Lymphoma, B-Cell Refractory Astellas Pharma Inc June 2007 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

If you have any other enquiries, please leave a message.

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Survivin Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID