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
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USD 120 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 M3;JZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVS3NkBp M4jMe2ROW09? M4XTWmlEPTB;MD6wNFkhyrFiMD6wNFA6KM7:TR?= MWWyOVY2QTd|MR?=
M-07e MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVS3NkBp NIfvWnRFVVOR MkfhTWM2OD1yLkC0NEDDuSByLkCxN{DPxE1? M3TtUVI2PjV7N{Ox
THP-1 NX65TW16T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml:4O|IhcA>? M1LXPGROW09? NXSwdoRSUUN3ME2wMlA2OSEEsTCwMlAyOyEQvF2= M2C2TlI2PjV7N{Ox
CMK NVL2c5pGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3H6Z|czKGh? MmHDSG1UVw>? MlTvTWM2OD1yLkC1N{DDuSByLkCwPUDPxE1? NGThZWQzPTZ3OUezNS=>
MV4-11 NXvKVm57T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mme2O|IhcA>? MYfEUXNQ MWXJR|UxRTBwMEW1JOKyKDBwMEK4JO69VQ>? M3ywSVI2PjV7N{Ox
AML-193 NVvmZpp3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFXXXo44OiCq MmG5SG1UVw>? M2rUUWlEPTB;MD60OlIhyrFiMD6wOlAh|ryP NV3wUFlCOjV4NUm3N|E>
HL-60 MnPCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXq3NkBp MVvEUXNQ M{PobGlEPTB;MD6wNFEhyrFiMD6wNFAzKM7:TR?= MUiyOVY2QTd|MR?=
ML-2 Ml3tS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnvEO|IhcA>? NUfsPXd{TE2VTx?= NV7PN4lDUUN3ME2wMlAxQSEEsTCwMlAxOiEQvF2= M{PuS|I2PjV7N{Ox
OCI/AML3 M2LXbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVW3NkBp MmfVSG1UVw>? MXzJR|UxRTBwMEGxJOKyKDBwMECyJO69VQ>? NHTQS2UzPTZ3OUezNS=>
HEL M3\ifWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MojCO|IhcA>? M1jrTmROW09? MWTJR|UxRTBwNUW5JOKyKDBwMEO4JO69VQ>? M1PLN|I2PjV7N{Ox
ME-1 NWrXOIVVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1\kTlczKGh? NFrkNItFVVOR NHHHeY5KSzVyPUCuOlg1KMLzIECuNVc6KM7:TR?= MXuyOVY2QTd|MR?=
THP-1 M1m1c2Fxd3C2b4Ppd{BCe3OjeR?= NG\qSFgyyqEQvF2= MWG3NkBp MX7EUXNQ M{j6dIlv\HWlZYOgZZBweHSxc3nz MVmyOVY2QTd|MR?=
M-07e NYrUbnp6TnWwY4Tpc44hSXO|YYm= MYKw5qCUOcLizszN NGDIcpo4OiCq MojLSG1UVw>? MkXDbY5lfWOnczDkc5dvemWpdXzheIlwdiCxZjDTeZJ3cX[rbh?= NUnDTFdzOjV4NUm3N|E>
THP-1 M1rUO2Z2dmO2aX;uJGF{e2G7 M{H6VFDjiJNzwrFOwG0> Mlv3O|IhcA>? M1XNdGROW09? NGjCOnVqdmS3Y3XzJIRwf26{ZXf1cIF1cW:wIH;mJHN2en[rdnnu MojlNlU3PTl5M{G=
CMK Mn\5SpVv[3Srb36gRZN{[Xl? MoWwNQKBmzIEoN88US=> MVq3NkBp NHzpUFFFVVOR NIjyZmZqdmS3Y3XzJIRwf26{ZXf1cIF1cW:wIH;mJHN2en[rdnnu NXXoUGZjOjV4NUm3N|E>
AML-193 MXLGeY5kfGmxbjDBd5NigQ>? NYXk[XB6OOLCk{JCpO69VQ>? M123V|czKGh? MWTEUXNQ NEfuZ2lqdmS3Y3XzJIRwf26{ZXf1cIF1cW:wIH;mJHN2en[rdnnu MYWyOVY2QTd|MR?=
Kasumi-1 M3TCc2Z2dmO2aX;uJGF{e2G7 Mne1NQKBmzIEoN88US=> NUfSbXNvPzJiaB?= NHPhcXZFVVOR NWXhOI05cW6mdXPld{Bld3ewcnXneYxifGmxbjDv[kBUfXK4aY\pci=> NHPIc3czPTZ3OUezNS=>
MV4-11 M4X6VmZ2dmO2aX;uJGF{e2G7 NV;BV2s3OOLCk{JCpO69VQ>? M1PHNlczKGh? Moq3SG1UVw>? Mn[xbY5lfWOnczDkc5dvemWpdXzheIlwdiCxZjDTeZJ3cX[rbh?= Moe5NlU3PTl5M{G=
MUG-Chor  NWHI[ZBuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M17ZOVAuPSEQvF2= M1PWT|I1NzR6IHi= MUHJR|UxRTdwMEZihKlvVSCob4KgOFhp MYGyOVY1ODF6NR?=
U-CH1  Mn;DS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIP3N3AxNTVizszN NILqWpozPC92ODDo NI\h[YlKSzVyPUmuNFPjiImwTTDmc5IhPDiq MnrYNlU3PDBzOEW=
KATOIII MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkHLNVAwOjBibl2= MkCzOFghcA>? MnewbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NW[1XXpsOjV4M{WwOVU>
AGS  MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3rkVlExNzJyIH7N M4q5VVQ5KGh? NYH2THpJcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MlrrNlU3OzVyNUW=
SACC-83 MlnQSpVv[3Srb36gRZN{[Xl? NVTB[FJIPSCwTR?= NHTRRmo1QCCq NF\lXZVl\WO{ZXHz[ZMhdnWlbHXhdkBmgHC{ZYPzbY9vKG:oIFjJSk0y|rF? M2P2SFI2PDh3NkO1
INA-6 NHvEUJlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3[ySFAuPTByIH7N MVe0PEBp NVHsdJZUcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NGfvU4szPTJ7Nkm3PC=>
U-266 NWrXVHQ3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXvvU2syOC13MECgcm0> M1TOfFQ5KGh? M2LUfolvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz M1H5W|I2Ojl4OUe4
MOLP-8 M3rLN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV2wMVUxOCCwTR?= MmXZOFghcA>? NXz5foZUcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MV2yOVI6Pjl5OB?=
HG-1 M17Kfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYKwMVUxOCCwTR?= MVe0PEBp MmjvbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MlL4NlUzQTZ7N{i=
NCI-H929 NH3oOZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MojFNE02ODBibl2= M2HRO|Q5KGh? M37VTYlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz M1raNFI2Ojl4OUe4
OPM-2 NE\6boFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mmn3NE02ODBibl2= NFXUUlE1QCCq NH;xTGxqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? MWeyOVI6Pjl5OB?=
L-363 NHPvc5dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M37WV|AuPTByIH7N MXm0PEBp MWDpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NEnLVGszPTJ7Nkm3PC=>
MOLP-2 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWGwMVUxOCCwTR?= MXK0PEBp NWr5NJdqcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? M4XoR|I2Ojl4OUe4
KMS-12-BM M3nVVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXTCT4xoOC13MECgcm0> NEXHZnM1QCCq MVXpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NYPFbWFoOjV{OU[5O|g>
SK-MM-2 MlnxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF:0bYcxNTVyMDDuUS=> MVe0PEBp MkezbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> M{THXlI2Ojl4OUe4
U-266 Ml;uRZBweHSxc3nzJGF{e2G7 MW[wMVUxKG6P MojKNlQhcA>? MV\pcoR2[2W|IHHwc5B1d3Orcx?= NFLE[HMzPTJ7Nkm3PC=>
INA-6  NWXIU3k6SXCxcITvd4l{KEG|c3H5 MnKxNE02OCCwTR?= NH:3S5UzPCCq NYfTPYNScW6mdXPld{BieG:ydH;zbZM> MoDqNlUzQTZ7N{i=
MCF7 MoCxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXG3NkBp M1;oVmlEPTB;MUOgxtEhPiCwTR?= NUXVVIUzOjV{MkCyNlU>
MCF7-TamR6 MnTzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1:xS|czKGh? MmHHTWM2OD16INMxJFYhdk1? NHOzdVgzPTJ{MEKyOS=>
MCF7-TamR7 MmjrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFzF[2I4OiCq M3z0VWlEPTB;ODFCtUA{KG6P MnW4NlUzOjB{MkW=
MCF7-TamR8 M{DQRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFXQeok4OiCq MWnJR|UxRTF3INMxJFYhdk1? NFK5VnQzPTJ{MEKyOS=>
MCF7-TamC3 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWfNTHI{PzJiaB?= MX3JR|UxRTZiwsGgN{BvVQ>? NEDHWHMzPTJ{MEKyOS=>
MCF7-TamC6 NXj4UWpST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWq5N4VmPzJiaB?= MYTJR|UxRTZiwsGgNE4yKG6P MmPGNlUzOjB{MkW=
MDA-MB-231 M3zxd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVG3NkBp NH;mXYdKSzVyPUWgxtEhOSCwTR?= M{S4dlI2OjJyMkK1
SK-BR-3 M4TLWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXnjfVVqPzJiaB?= MWDJR|UxRTdiwsGgNE4{KG6P MkK1NlUzOjB{MkW=
Eca109 M{PDcmZ2dmO2aX;uJGF{e2G7 MVOxMVUxKG6P MXO0PEBp MUHEUXNQ MVXzeZBxemW|c3XzJJN2en[rdnnuJIV5eHKnc4Ppc44hcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> MmPFNlUyOzl|OUW=
TE13 MYnGeY5kfGmxbjDBd5NigQ>? MUSxMVUxKG6P NV3UdIJyPDhiaB?= Mo\hSG1UVw>? MnzMd5VxeHKnc4Pld{B{fXK4aY\pckBmgHC{ZYPzbY9vKGmwIHGg[I9{\SCmZYDlcoRmdnRibXHucoVz MYSyOVE{QTN7NR?=
Eca109 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoC0NE0yODBibl2= NFnw[40zPC92ODDo MnXTSG1UVw>? M2C5PIRm[3KnYYPld{Bk\WyuII\pZYJqdGm2eTDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= MXWyOVE{QTN7NR?=
TE13 NX3POpZbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV3VWYQzOC1zMECgcm0> NXrIeXVmOjRxNEigbC=> NU\nZllqTE2VTx?= M2i2bYRm[3KnYYPld{Bk\WyuII\pZYJqdGm2eTDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= Ml7pNlUyOzl|OUW=
MT-3 NEHPRnlMcW6jc3WgRZN{[Xl? NXfCTZNCPzJiaB?= NV\x[ndpTE2VTx?= NGe4WFlKSzVyPUKuPFYhyrFiMD61OEBvVSCob4KgSHI1KGW6cILld5Nqd25? MX6yOFg3PjV6NR?=
MDA-MB-468 NF7kZYRMcW6jc3WgRZN{[Xl? MkSyO|IhcA>? NWnhPYJUTE2VTx?= Mn6yTWM2OD1yLkGxJOKyKDBwMEGgcm0h\m:{IFTSOEBmgHC{ZYPzbY9v M1HnSFI1QDZ4NUi1
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BFTC909 NEfQc|ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUmwMVExODBibl2= MW[0PEBpyqB? NG\sWGRFVVOR MnTNTWM2OD1{MDDuUUwhcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? Ml;rNlQzQTd4NES=
BFTC905 MUfBdI9xfG:|aYOgRZN{[Xl? NVqzUHAxOjBibl2= M3vNTVQ5KGh? MUjEUXNQ Mn\xbY5lfWOnczDhdI9xfG:|aYO= NV\BdY9pOjR{OUe2OFQ>
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A2780p M3rSfGZ2dmO2aX;uJGF{e2G7 NWj0dllYOC1zMECgcm0> M1:2cFI1KGh? NHfyflVFVVOR MYrpcoR2[2W|IGP1dpZqfmmwIHTve45z\We3bHH0bY9vyqB? NHf6[mszPDJ4Mki3OS=>
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SH-SY5Y NVrRfWFZSXCxcITvd4l{KEG|c3H5 NH7RclgyNzFyL{GwNEDDvU1? M2Cyb|czKGh? M1v2NGROW09? NGf6ZVdqdmS3Y3XzJIFxd3C2b4Ppd{BqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NVnxeWhJOjR{NUS1OlA>
HL-60 NX\SVVZZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIjI[|E4OsLiaB?= MYXEUXNQ MWPJR|UxRTBwMzDuUS=> M175O|I{PjF6OE[y
U937  NX3POopnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWi3NuKhcA>? NFjDco1FVVOR M1z1d2lEPTB;MD64JI5O M2rRNFI{PjF6OE[y
HL-60  M{fwWGZ2dmO2aX;uJGF{e2G7 MYixxsDPxE1? NHW2WoY3NzF{L{K0JIg> M1vG[2ROW09? MV7pcohq[mm2czD0bIUh\XiycnXzd4lwdiCxZjDzeZJ3cX[rbh?= M4jiNlI{PjF6OE[y
U937  Mo[0SpVv[3Srb36gRZN{[Xl? MmTpNeKh|ryP M2\UUVYwOTJxMkSgbC=> M4O2bWROW09? M{fKeolvcGmkaYTzJJRp\SCneIDy[ZN{cW:wIH;mJJN2en[rdnnu M2LV[|I{PjF6OE[y
HL-60 MUDBdI9xfG:|aYOgRZN{[Xl? NWTMZXJFOC5zL{Gg{txO NH34cpY5KGh? NXjhSVlzTE2VTx?= NWXMWZNOcW6mdXPld{BieG:ydH;zbZM> NHvxRVczOzZzOEi2Ni=>
Sk-NEP-1  NXv6WpRNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXexMVExODByIH7N NIrId|AzPCCq M1X1RWROW09? NXO0Olh6UUN3ME2xNFAhdk1? NHXSXmIzOzJ4N{[5PS=>
SK-NEP-1  M335d2Fxd3C2b4Ppd{BCe3OjeR?= M1TGdFUxNzFyMDDuUS=> NWfBUXZQOTJxMkSgbC=> MnfxSG1UVw>? NYHUPZU3cW6mdXPld{BieG:ydH;zbZM> Mnr0NlMzPjd4OUm=
TC-32 MlnKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnHiNE4yNTFyMECgcm0> MoXvSWM2OD1|LkCgcm0tKGmwaHnibZR{KGOnbHyg[5Jwf3SqIHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ MV:yNlk3OTd4Mx?=
TC-71 MkS5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1S4NlAvOS1zMECwJI5O NIn3fmlGSzVyPUWuO{BvVSxiaX7obYJqfHNiY3XscEBoem:5dHigbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK= NVLDcWg3OjJ7NkG3OlM>
SK-ES-1 Mmi0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MW[wMlEuOTByMDDuUS=> MknCSWM2OD1{Lkigcm0tKGmwaHnibZR{KGOnbHyg[5Jwf3SqIHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ MlTtNlI6PjF5NkO=
RD-ES NGCyUWpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX2wMlEuOTByMDDuUS=> M1\hR2VEPTB;Nj6yJI5ONCCrbnjpZol1eyClZXzsJIdzd3e2aDDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= NYrMZmFuOjJ7NkG3OlM>
HEK293 MkP4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVqwMlEuOTByMDDuUS=> NHnaPXFGSzVyPUKzMlAhdk1uIHnubIljcXS|IHPlcIwh\3Kxd4ToJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy MkfqNlI6PjF5NkO=
M059J M3:2e2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVSwMVUxKG6P MV60PEBp MmO3bY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MnHZNlI4PzBzMUC=
M059K MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIHDXXAxNTVyIH7N MkDDOFghcA>? MVzpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NWXmN3BNOjJ5N{CxNVA>
M059J NGfKSIdCeG:ydH;zbZMhSXO|YYm= MmL6N|Ahdk1? M1XtclI1KGh? NIPpRnVqdmS3Y3XzJIFxd3C2b4Ppdy=> MUKyNlc4ODFzMB?=
M059K Mn;5RZBweHSxc3nzJGF{e2G7 MWizNEBvVQ>? NX[wcIhIOjRiaB?= M{iw[4lv\HWlZYOgZZBweHSxc3nz NXPhdldPOjJ5N{CxNVA>
PANC-1 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIfDZpoxNjBzLUGwNFAhdk1? MVe0PEBp MVvJR|UxRTNwNkmgcm0> NFPudJYzOjd{M{i3NS=>
MIAPaCa-2 MnvaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV[wMlAyNTFyMECgcm0> NVPLe3pVPDhiaB?= NI\TWWJKSzVyPUK5MlM3KG6P MnHLNlI4OjN6N{G=
BxPC-3 M37nOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHTyfpYxNjBzLUGwNFAhdk1? NGPoXYs1QCCq MUTJR|UxRTNyLkK2JI5O NFTtUowzOjd{M{i3NS=>
PANC-1 NXnJR5pUTnWwY4Tpc44hSXO|YYm= MWmwMVExODBibl2= M1\5SlI1KGh? M{\6N4lv\HWlZYOg[I94dnKnZ4XsZZRqd25ib3[gXGlCWCCjbnSgd5Vzfmm4aX6g[ZhxemW|c3nvci=> M3LqS|IzPzJ|OEex
MIAPaCa-2 NVXiN491TnWwY4Tpc44hSXO|YYm= MnnvNE0yODByIH7N MmjtNlQhcA>? NYG5VlFDcW6mdXPld{Bld3ewcnXneYxifGmxbjDv[kBZUUGSIHHu[EB{fXK4aY\pckBmgHC{ZYPzbY9v M2PV[VIzPzJ|OEex
BxPC-3 M1KwVWZ2dmO2aX;uJGF{e2G7 MkXCNE0yODByIH7N NYLyS4g6OjRiaB?= M3jiTolv\HWlZYOg[I94dnKnZ4XsZZRqd25ib3[gXGlCWCCjbnSgd5Vzfmm4aX6g[ZhxemW|c3nvci=> NV:wOnV5OjJ5MkO4O|E>
RPMI-7951 NGjtZVhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NY\MTlE4T0l3ME2zMlIhdk1? NIXNSokzOTd|N{WwNi=>
SK-MEL-5 M2jMXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmC2S2k2OD12LkKgcm0> NUHFVndPOjF5M{e1NFI>
A375 M1yzb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXPHTVUxRTZwMzDuUS=> M3jJU|IyPzN5NUCy
SK-MEL-28 Mn;BS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGHCbnRIUTVyPUeuOkBvVQ>? MUWyNVc{PzVyMh?=
SK-MEL-2 MkfrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUG3eVRFT0l3ME2xNUBvVQ>? NUHIO4JkOjF5M{e1NFI>
DB M1:2cmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4r2S|Q5yqCq M4G1ZWdKPTB;Mz61JI5O NFznclYzOTJ|N{WwPC=>
Pfeiffer M{jq[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M13PZlQ5yqCq MWLHTVUxRTNwOTDuUS=> NELaW3UzOTJ|N{WwPC=>
SU-DHL-5 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXK4S5JkPDkEoHi= NG[4c3hIUTVyPUCuNlMhdk1? NIfP[G4zOTJ|N{WwPC=>
SU-DHL-8 NFe1UoNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mkj4OFjDqGh? M1\udmdKPTB;MT60JI5O NVfwTZpkOjF{M{e1NFg>
WSU-DLCL-2 MmTpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1\5UFQ5yqCq NIHxTphIUTVyPUGuOEBvVQ>? NX25NHdoOjF{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
+ 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'-GCGCGCTCGAGTCTAGACATGCGGATATATTC-3' and 5'-GCGCGAA-GCTTTGGCGGTTAATGGCGCGC-3'. The resulting PCR fragment is digested with XhoI/HindIII and ligated into the XhoI/HindIII cleavage site of the pGL3-Basic vector. The resulting plasmid is named pSUR-luc. DNA sequencing is done on all amplified sequences by a DNA sequencer. The activity of pSUR-luc is confirmed by luciferase assay with transiently transfected HeLa-S3 cells. Luciferase assay is done. The pGL3 control vector, which contains the SV40 promoter and enhancer sequences, is used. HeLa cells are stably transfected with pSUR-luc and pSV2bsr by Lipofect-AMINE 2000. After blasticidin selection at 10 μg/mL, a single colony is chosen based on appropriate luciferase signals and genetic stability over time and named HeLa-SURP-luc. CHO cells are stably transfected with pGL3-control and pSV2bsr. After blasticidin selection at 10 μg/mL, a single colony is chosen based on appropriate luciferase signals and genetic stability over time and named CHO-SV40-luc. Stocked cells from the HeLa-SURP-luc and CHO-SV40-luc clones are used for chemical screening and characterization of YM155. YM155 in DMSO are added to the cells, which had been seeded the previous day on 96-well plastic plates at 5 × 103 per well. Luciferase activity is measured 24 hours later. IC50 is calculated by logistic analysis.
Cell Research
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  • 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
+ 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)

  • Mass
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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
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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):
    C6=C5/X C6: LOG(C6):
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    C8=C7/X C8: LOG(C8):
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