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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In DMSO USD 112 In stock
USD 70 In stock
USD 120 In stock
USD 270 In stock
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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

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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 NUjMVYR1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVy3b|JbPzJiaB?= MVfEUXNQ NEXEVW9KSzVyPUCuNFA6KMLzIECuNFAxQSEQvF2= M2DLUFI2PjV7N{Ox
M-07e NXTido9kT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NG\WRlE4OiCq Mkj2SG1UVw>? Mk\KTWM2OD1yLkC0NEDDuSByLkCxN{DPxE1? NEHz[|QzPTZ3OUezNS=>
THP-1 MlroS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYK3RmhjPzJiaB?= MnjQSG1UVw>? MXfJR|UxRTBwMEWxJOKyKDBwMEGzJO69VQ>? NWLP[VBMOjV4NUm3N|E>
CMK MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH3RSG04OiCq MnfjSG1UVw>? MnnLTWM2OD1yLkC1N{DDuSByLkCwPUDPxE1? NFLWNVczPTZ3OUezNS=>
MV4-11 NE\ONXBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVzOdYtwPzJiaB?= NXLGRVBMTE2VTx?= NYjHcIhOUUN3ME2wMlA2PSEEsTCwMlAzQCEQvF2= MW[yOVY2QTd|MR?=
AML-193 NGfNVlhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWm3OmNyPzJiaB?= NE\5OWlFVVOR MkDoTWM2OD1yLkS2NkDDuSByLkC2NEDPxE1? NX2xRnp2OjV4NUm3N|E>
HL-60 MoHsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV[3NkBp MYfEUXNQ MXTJR|UxRTBwMECxJOKyKDBwMECwNkDPxE1? M3nRTFI2PjV7N{Ox
ML-2 MkTIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVK3NkBp MYXEUXNQ M2f4XmlEPTB;MD6wNFkhyrFiMD6wNFIh|ryP NInXXXUzPTZ3OUezNS=>
OCI/AML3 M{PWbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnfJO|IhcA>? NE\RV2ZFVVOR NUHh[plqUUN3ME2wMlAyOSEEsTCwMlAxOiEQvF2= NETHeJIzPTZ3OUezNS=>
HEL MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{XXOlczKGh? MoDwSG1UVw>? NU\UclRxUUN3ME2wMlU2QSEEsTCwMlA{QCEQvF2= Mn\UNlU3PTl5M{G=
ME-1 MmO2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVO3NkBp M2rSV2ROW09? NFPNV3RKSzVyPUCuOlg1KMLzIECuNVc6KM7:TR?= MUeyOVY2QTd|MR?=
THP-1 MmTyRZBweHSxc3nzJGF{e2G7 NFj2[IEyyqEQvF2= MUG3NkBp NVzZSWpoTE2VTx?= NHnxXoRqdmS3Y3XzJIFxd3C2b4Ppdy=> NYW0UFNtOjV4NUm3N|E>
M-07e M3zjd2Z2dmO2aX;uJGF{e2G7 NVzSRYNsOOLCk{JCpO69VQ>? NEH4UGI4OiCq MkToSG1UVw>? MUjpcoR2[2W|IHTve45z\We3bHH0bY9vKG:oIGP1dpZqfmmw NEPFN5EzPTZ3OUezNS=>
THP-1 NHi4bnRHfW6ldHnvckBCe3OjeR?= NXLod|l3OOLCk{JCpO69VQ>? M170T|czKGh? NWXhUWZOTE2VTx?= NWfF[mlpcW6mdXPld{Bld3ewcnXneYxifGmxbjDv[kBUfXK4aY\pci=> MkPCNlU3PTl5M{G=
CMK MVjGeY5kfGmxbjDBd5NigQ>? MnPDNQKBmzIEoN88US=> Ml\nO|IhcA>? MVXEUXNQ MmTVbY5lfWOnczDkc5dvemWpdXzheIlwdiCxZjDTeZJ3cX[rbh?= Mlj1NlU3PTl5M{G=
AML-193 NVLveIJOTnWwY4Tpc44hSXO|YYm= NG[0clIx6oDVMdMg{txO Mn;JO|IhcA>? MkLlSG1UVw>? M17WVolv\HWlZYOg[I94dnKnZ4XsZZRqd25ib3[gV5Vzfmm4aX6= NH7JUlIzPTZ3OUezNS=>
Kasumi-1 NHTDeFJHfW6ldHnvckBCe3OjeR?= MWiw5qCUOcLizszN NUfLSIVQPzJiaB?= Mn3ISG1UVw>? M1zLSIlv\HWlZYOg[I94dnKnZ4XsZZRqd25ib3[gV5Vzfmm4aX6= MX:yOVY2QTd|MR?=
MV4-11 NHXaVlRHfW6ldHnvckBCe3OjeR?= NV\hWmdWOOLCk{JCpO69VQ>? MnXFO|IhcA>? MVTEUXNQ NUfkb4I6cW6mdXPld{Bld3ewcnXneYxifGmxbjDv[kBUfXK4aY\pci=> Mnq3NlU3PTl5M{G=
MUG-Chor  MnfTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIDPNHUxNTVizszN MYmyOE81QCCq Mk\oTWM2OD15LkC15qCKdk1iZn;yJFQ5cA>? MlPTNlU3PDBzOEW=
U-CH1  NGLLT3NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXKwMVUh|ryP M4X3S|I1NzR6IHi= NYrOWmVJUUN3ME25MlA{6oDLbl2g[o9zKDR6aB?= MVuyOVY1ODF6NR?=
KATOIII NXvuSI44T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEPYc4YyOC9{MDDuUS=> M{C2RlQ5KGh? M3S5WYlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MlPQNlU3OzVyNUW=
AGS  NYDXRoVGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3vKNlExNzJyIH7N MXG0PEBp NFH0SXZqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? M1WwNFI2PjN3MEW1
SACC-83 NIfRPXVHfW6ldHnvckBCe3OjeR?= MkGyOUBvVQ>? MXq0PEBp Ml;H[IVkemWjc3XzJI52[2ynYYKg[ZhxemW|c3nvckBw\iCKSV[tNe6y Mn[4NlU1QDV4M{W=
INA-6 MmiyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1vBdlAuPTByIH7N MYC0PEBp Ml7obY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MYqyOVI6Pjl5OB?=
U-266 MlH4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYewMVUxOCCwTR?= NWjiXHZuPDhiaB?= NF7jXXJqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NF3ld|IzPTJ7Nkm3PC=>
MOLP-8 MonXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M37kTFAuPTByIH7N M{PWOVQ5KGh? NW\OfVBscW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NXzEc25nOjV{OU[5O|g>
HG-1 M4SxR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHOyNG4xNTVyMDDuUS=> NUO5OHM2PDhiaB?= MX\pcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NFnFc2gzPTJ7Nkm3PC=>
NCI-H929 Mk\4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4ftclAuPTByIH7N M4WySFQ5KGh? NHrUXINqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NFOxcIkzPTJ7Nkm3PC=>
OPM-2 M{fyXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX3Q[XA2OC13MECgcm0> M1;aWFQ5KGh? M1L4O4lvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NHn0XpIzPTJ7Nkm3PC=>
L-363 NVfOToQyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mni0NE02ODBibl2= NYXqcWVpPDhiaB?= NFi5U|FqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NVPBUItVOjV{OU[5O|g>
MOLP-2 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4DEN|AuPTByIH7N MYC0PEBp MnO4bY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NY\aS3h3OjV{OU[5O|g>
KMS-12-BM M1PSSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV:3dmZ[OC13MECgcm0> Mnz3OFghcA>? M2HIfYlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz M1jzUVI2Ojl4OUe4
SK-MM-2 M2G4Wmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWOwMVUxOCCwTR?= NVvtSpdzPDhiaB?= MVHpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> M3jvUlI2Ojl4OUe4
U-266 MYjBdI9xfG:|aYOgRZN{[Xl? NHjxPWgxNTVyIH7N M33VclI1KGh? M2KyWolv\HWlZYOgZZBweHSxc3nz MlrpNlUzQTZ7N{i=
INA-6  NUf0TGNvSXCxcITvd4l{KEG|c3H5 MnLqNE02OCCwTR?= NHjOfHQzPCCq M2n4RYlv\HWlZYOgZZBweHSxc3nz Ml7NNlUzQTZ7N{i=
MCF7 Mk\rS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoWwO|IhcA>? M4L0R2lEPTB;MUOgxtEhPiCwTR?= MnW3NlUzOjB{MkW=
MCF7-TamR6 NXjXUlB[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUK3NkBp MnGwTWM2OD16INMxJFYhdk1? M4HwfVI2OjJyMkK1
MCF7-TamR7 NGPOW29Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{nFZ|czKGh? Mm[2TWM2OD16INMxJFMhdk1? M1G5RlI2OjJyMkK1
MCF7-TamR8 NX3hc5U4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1O1cVczKGh? NXTRZZptUUN3ME2xOUDDuSB4IH7N M1[1dVI2OjJyMkK1
MCF7-TamC3 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3zEdlczKGh? NXfGcWluUUN3ME22JOKyKDNibl2= M3r3T|I2OjJyMkK1
MCF7-TamC6 M{XVS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGfMSos4OiCq NGHBUWxKSzVyPU[gxtEhOC5zIH7N Ml65NlUzOjB{MkW=
MDA-MB-231 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIXoVm84OiCq M1y3NmlEPTB;NTFCtUAyKG6P NHrsXGgzPTJ{MEKyOS=>
SK-BR-3 M3O1cmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkDpO|IhcA>? NULJdlY5UUN3ME23JOKyKDBwMzDuUS=> M3;lOlI2OjJyMkK1
Eca109 MWjGeY5kfGmxbjDBd5NigQ>? MoTCNU02OCCwTR?= M{HmbFQ5KGh? M3\qSWROW09? NHLwOG1{fXCycnXzd4V{KHO3co\peolvKGW6cILld5Nqd25iaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? Mo\2NlUyOzl|OUW=
TE13 M1:xR2Z2dmO2aX;uJGF{e2G7 Mn6zNU02OCCwTR?= NFXpd4I1QCCq MmOySG1UVw>? NFrzeHV{fXCycnXzd4V{KHO3co\peolvKGW6cILld5Nqd25iaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? NHvQU|kzPTF|OUO5OS=>
Eca109 NYH2e4JXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4LyNVAuOTByIH7N NWf6XI9QOjRxNEigbC=> NXjweFNzTE2VTx?= NGTDd29l\WO{ZXHz[ZMh[2WubDD2bYFjcWyrdImgbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK= MlrlNlUyOzl|OUW=
TE13 MlP1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGSxTZQxNTFyMDDuUS=> NF3ZR5QzPC92ODDo M4PydGROW09? NXHiXXpk\GWlcnXhd4V{KGOnbHygeoli[mmuaYT5JIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy MmnDNlUyOzl|OUW=
MT-3 M3TJWmtqdmG|ZTDBd5NigQ>? MVy3NkBp M1TsV2ROW09? M1\Pe2lEPTB;Mj64OkDDuSByLkW0JI5OKG[xcjDEVlQh\XiycnXzd4lwdg>? MkTENlQ5PjZ3OEW=
MDA-MB-468 MVvLbY5ie2ViQYPzZZk> M{\v[FczKGh? NXT1c|B2TE2VTx?= NWLyVFJMUUN3ME2wMlEyKMLzIECuNFEhdk1iZn;yJGRTPCCneIDy[ZN{cW:w M3HEZ|I1QDZ4NUi1
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SH-SY5Y MVnBdI9xfG:|aYOgRZN{[Xl? MVWxM|ExNzFyMDFCuW0> NFzXXm84OiCq MVfEUXNQ MYLpcoR2[2W|IHHwc5B1d3OrczDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= NVfv[lNjOjR{NUS1OlA>
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RD-ES MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWqwMlEuOTByMDDuUS=> MWnFR|UxRTZwMjDuUUwhcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NFfye|UzOjl4MUe2Ny=>
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M059J M3TVXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1H4d|AuPTBibl2= NYDyVo1QPDhiaB?= MW\pcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MUSyNlc4ODFzMB?=
M059K MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn:2NE02OCCwTR?= NX[x[FZ{PDhiaB?= M2LTeIlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NY\RU3hkOjJ5N{CxNVA>
M059J NUO1ephxSXCxcITvd4l{KEG|c3H5 MlTRN|Ahdk1? M1:wUlI1KGh? NEW2fGFqdmS3Y3XzJIFxd3C2b4Ppdy=> NHr3ToszOjd5MEGxNC=>
M059K MVvBdI9xfG:|aYOgRZN{[Xl? M3vG[|MxKG6P M4X3NVI1KGh? NYL1WWhscW6mdXPld{BieG:ydH;zbZM> MXOyNlc4ODFzMB?=
PANC-1 M1jlNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVfNb|FZOC5yMT2xNFAxKG6P NIDrb|A1QCCq M1XGeGlEPTB;Mz62PUBvVQ>? MmLPNlI4OjN6N{G=
MIAPaCa-2 NF;SZ3lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MljVNE4xOS1zMECwJI5O NYHpSG9qPDhiaB?= NHLHendKSzVyPUK5MlM3KG6P MXWyNlczOzh5MR?=
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MIAPaCa-2 NXvj[5FnTnWwY4Tpc44hSXO|YYm= M{XaVlAuOTByMDDuUS=> NVrwdG0{OjRiaB?= M{f0cYlv\HWlZYOg[I94dnKnZ4XsZZRqd25ib3[gXGlCWCCjbnSgd5Vzfmm4aX6g[ZhxemW|c3nvci=> NHvTTI8zOjd{M{i3NS=>
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RPMI-7951 M4\ubmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NInnXZhIUTVyPUOuNkBvVQ>? NEfoWnkzOTd|N{WwNi=>
SK-MEL-5 NIPmUGNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVjHTVUxRTRwMjDuUS=> NUf2cYJSOjF5M{e1NFI>
A375 NGTSTIJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Moi0S2k2OD14LkOgcm0> NXPEUJZYOjF5M{e1NFI>
SK-MEL-28 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1jKS2dKPTB;Nz62JI5O NF7TdZYzOTd|N{WwNi=>
SK-MEL-2 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3jGXmdKPTB;MUGgcm0> NY\OTlU1OjF5M{e1NFI>
DB M{Xadmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVG0POKhcA>? NVH2cZdJT0l3ME2zMlUhdk1? MV:yNVI{PzVyOB?=
Pfeiffer M1rqb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGrJT2U1QMLiaB?= M1S3cmdKPTB;Mz65JI5O MmraNlEzOzd3MEi=
SU-DHL-5 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXrsPJJOPDkEoHi= MWPHTVUxRTBwMkOgcm0> MX6yNVI{PzVyOB?=
SU-DHL-8 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVS0POKhcA>? MlTZS2k2OD1zLkSgcm0> NHHZZpozOTJ|N{WwPC=>
WSU-DLCL-2 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWLsUJBQPDkEoHi= M1rmU2dKPTB;MT60JI5O MnnSNlEzOzd3MEi=

... 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 Saline 30 mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* 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 )

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* 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:

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Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

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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.

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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