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

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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 NYXZRZcxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NU[zVnlzPzJiaB?= Ml3mSG1UVw>? M1uxZmlEPTB;MD6wNFkhyrFiMD6wNFA6KM7:TR?= M3LP[lI2PjV7N{Ox
M-07e NUnuWmo5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmLoO|IhcA>? MWLEUXNQ M3rZNWlEPTB;MD6wOFAhyrFiMD6wNVMh|ryP NUT4[mRsOjV4NUm3N|E>
THP-1 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4TNZVczKGh? MkfNSG1UVw>? MkK1TWM2OD1yLkC1NUDDuSByLkCxN{DPxE1? NX;MWI5zOjV4NUm3N|E>
CMK M3LzXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYS3NkBp Mm\rSG1UVw>? M4TkVWlEPTB;MD6wOVMhyrFiMD6wNFkh|ryP NUXQ[41UOjV4NUm3N|E>
MV4-11 MlToS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFjrPYY4OiCq NWDoUYg5TE2VTx?= Mn\ETWM2OD1yLkC1OUDDuSByLkCyPEDPxE1? NETLd2wzPTZ3OUezNS=>
AML-193 M2HsXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHXzTW04OiCq NV;WbXA6TE2VTx?= MnjVTWM2OD1yLkS2NkDDuSByLkC2NEDPxE1? NFHWNo0zPTZ3OUezNS=>
HL-60 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mkf0O|IhcA>? MX\EUXNQ MmTCTWM2OD1yLkCwNUDDuSByLkCwNFIh|ryP MmTONlU3PTl5M{G=
ML-2 M2fQ[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXvmfHNPPzJiaB?= M3jtWGROW09? Mn3BTWM2OD1yLkCwPUDDuSByLkCwNkDPxE1? MU[yOVY2QTd|MR?=
OCI/AML3 M4LHTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2C2OlczKGh? MlTrSG1UVw>? NHnMUIVKSzVyPUCuNFEyKMLzIECuNFAzKM7:TR?= MmCxNlU3PTl5M{G=
HEL NGqyNpFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnvWO|IhcA>? M33BNmROW09? Mln3TWM2OD1yLkW1PUDDuSByLkCzPEDPxE1? MWiyOVY2QTd|MR?=
ME-1 MoXNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn7JO|IhcA>? MoH0SG1UVw>? M2TFeGlEPTB;MD62PFQhyrFiMD6xO|kh|ryP MUeyOVY2QTd|MR?=
THP-1 NFSyPHpCeG:ydH;zbZMhSXO|YYm= NYrBO5hjOcLizszN NXLUVnliPzJiaB?= MX7EUXNQ MYXpcoR2[2W|IHHwc5B1d3Orcx?= MXGyOVY2QTd|MR?=
M-07e MnHsSpVv[3Srb36gRZN{[Xl? M2L0U|DjiJNzwrFOwG0> Ml\hO|IhcA>? M{DldGROW09? NF65O2ZqdmS3Y3XzJIRwf26{ZXf1cIF1cW:wIH;mJHN2en[rdnnu MlHNNlU3PTl5M{G=
THP-1 NHK5clZHfW6ldHnvckBCe3OjeR?= M3vycVDjiJNzwrFOwG0> NV3INppiPzJiaB?= NYLHWWd1TE2VTx?= NVr5boU{cW6mdXPld{Bld3ewcnXneYxifGmxbjDv[kBUfXK4aY\pci=> NV\1UIFwOjV4NUm3N|E>
CMK M1rJRmZ2dmO2aX;uJGF{e2G7 MXSw5qCUOcLizszN NHiwdI04OiCq MlfpSG1UVw>? MYTpcoR2[2W|IHTve45z\We3bHH0bY9vKG:oIGP1dpZqfmmw NX7tPHBJOjV4NUm3N|E>
AML-193 NW\CNFBSTnWwY4Tpc44hSXO|YYm= NFXWVmkx6oDVMdMg{txO MlTZO|IhcA>? MVHEUXNQ M1fQOolv\HWlZYOg[I94dnKnZ4XsZZRqd25ib3[gV5Vzfmm4aX6= MUKyOVY2QTd|MR?=
Kasumi-1 MXfGeY5kfGmxbjDBd5NigQ>? NYHUc49KOOLCk{JCpO69VQ>? M4Ps[lczKGh? MUjEUXNQ MnvXbY5lfWOnczDkc5dvemWpdXzheIlwdiCxZjDTeZJ3cX[rbh?= NF;TT3EzPTZ3OUezNS=>
MV4-11 NGnseXlHfW6ldHnvckBCe3OjeR?= NWL4XGxYOOLCk{JCpO69VQ>? M1jqNlczKGh? MVnEUXNQ M3fQ[4lv\HWlZYOg[I94dnKnZ4XsZZRqd25ib3[gV5Vzfmm4aX6= M4e0OFI2PjV7N{Ox
MUG-Chor  NVr3NXpzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFjLfJExNTVizszN MmDINlQwPDhiaB?= Mo\TTWM2OD15LkC15qCKdk1iZn;yJFQ5cA>? NWPRVoREOjV4NECxPFU>
U-CH1  MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2f0flAuPSEQvF2= MVKyOE81QCCq MWHJR|UxRTlwMERihKlvVSCob4KgOFhp MYeyOVY1ODF6NR?=
KATOIII MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml7DNVAwOjBibl2= NVOxdVNZPDhiaB?= MkXJbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> Mn3CNlU3OzVyNUW=
AGS  NFL5R4dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXixNE8zOCCwTR?= NGn0WZk1QCCq NHr5R3ZqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? MofuNlU3OzVyNUW=
SACC-83 NYTGVHl1TnWwY4Tpc44hSXO|YYm= NEGweHU2KG6P MWq0PEBp MWrk[YNz\WG|ZYOgcpVkdGWjcjDlfJBz\XO|aX;uJI9nKEiLRj2x{tE> NFnzRogzPTR6NU[zOS=>
INA-6 M3TRbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NG\4cmkxNTVyMDDuUS=> M1zUPFQ5KGh? M4W3[olvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MWCyOVI6Pjl5OB?=
U-266 NFnFUmVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYiwMVUxOCCwTR?= M2\NWlQ5KGh? M3rhXIlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NIm1cY0zPTJ7Nkm3PC=>
MOLP-8 NYLhU4V1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmPnNE02ODBibl2= MXG0PEBp M4LIZYlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NV\RZ2RzOjV{OU[5O|g>
HG-1 Mn\lS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{LuS|AuPTByIH7N MnHuOFghcA>? NHTkUWhqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NHXwbnMzPTJ7Nkm3PC=>
NCI-H929 NVnXOnl2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVuwMVUxOCCwTR?= NHHh[2Q1QCCq MkfzbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> M2TNO|I2Ojl4OUe4
OPM-2 M{WwNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mk\vNE02ODBibl2= MmLnOFghcA>? M{\KTIlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NWTkOYh4OjV{OU[5O|g>
L-363 NUfuOnVFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUOwMVUxOCCwTR?= MX20PEBp M2TXS4lvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NX;OW4FiOjV{OU[5O|g>
MOLP-2 M2TiRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlLPNE02ODBibl2= NWjaOmt4PDhiaB?= Mmr1bY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MXeyOVI6Pjl5OB?=
KMS-12-BM M3z2dGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV\tc3F{OC13MECgcm0> M1HBTlQ5KGh? NWOzbFZ2cW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NULyeJpkOjV{OU[5O|g>
SK-MM-2 NFPhbWJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnW2NE02ODBibl2= NH7PZlM1QCCq MUnpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NHPY[24zPTJ7Nkm3PC=>
U-266 Mn3URZBweHSxc3nzJGF{e2G7 NEDIdo4xNTVyIH7N NVTpXIpSOjRiaB?= M4S4bYlv\HWlZYOgZZBweHSxc3nz MUKyOVI6Pjl5OB?=
INA-6  MYHBdI9xfG:|aYOgRZN{[Xl? M1HsW|AuPTBibl2= M33mcVI1KGh? M3vYOIlv\HWlZYOgZZBweHSxc3nz Mn3WNlUzQTZ7N{i=
MCF7 Mnv5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MonBO|IhcA>? NVHpcHdbUUN3ME2xN{DDuSB4IH7N M4fLZlI2OjJyMkK1
MCF7-TamR6 M3HmWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWq3NkBp NF;HVZdKSzVyPUigxtEhPiCwTR?= MleyNlUzOjB{MkW=
MCF7-TamR7 M3e3emdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{PYdVczKGh? M2\YcGlEPTB;ODFCtUA{KG6P MWiyOVIzODJ{NR?=
MCF7-TamR8 MoHiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUi3NkBp NIXzflFKSzVyPUG1JOKyKDZibl2= M4n2[lI2OjJyMkK1
MCF7-TamC3 NEPKco5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnnoO|IhcA>? NUjIfVN7UUN3ME22JOKyKDNibl2= NXLlbYlMOjV{MkCyNlU>
MCF7-TamC6 M1joe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEmwfmM4OiCq MXTJR|UxRTZiwsGgNE4yKG6P MlLLNlUzOjB{MkW=
MDA-MB-231 NVTZcWFOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVi3NkBp NFu3dmpKSzVyPUWgxtEhOSCwTR?= NH3nTXMzPTJ{MEKyOS=>
SK-BR-3 Mmq3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHe5dnY4OiCq MV;JR|UxRTdiwsGgNE4{KG6P MW[yOVIzODJ{NR?=
Eca109 NWHZU2h2TnWwY4Tpc44hSXO|YYm= MWexMVUxKG6P M4TqN|Q5KGh? M1\XemROW09? MnKzd5VxeHKnc4Pld{B{fXK4aY\pckBmgHC{ZYPzbY9vKGmwIHGg[I9{\SCmZYDlcoRmdnRibXHucoVz M{i0bFI2OTN7M{m1
TE13 MXjGeY5kfGmxbjDBd5NigQ>? NV7qcXFxOS13MDDuUS=> NE\ITZo1QCCq M2rCXWROW09? MkTxd5VxeHKnc4Pld{B{fXK4aY\pckBmgHC{ZYPzbY9vKGmwIHGg[I9{\SCmZYDlcoRmdnRibXHucoVz NW[5cXhbOjVzM{mzPVU>
Eca109 Mn;4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3zYUlAuOTByIH7N NWPJfVdlOjRxNEigbC=> NX[4WW9bTE2VTx?= MlXW[IVkemWjc3XzJINmdGxidnnhZoltcXS7IHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ NV;3NpRPOjVzM{mzPVU>
TE13 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX\xVXJCOC1zMECgcm0> NGXXeZEzPC92ODDo MYLEUXNQ NXjtTGJl\GWlcnXhd4V{KGOnbHygeoli[mmuaYT5JIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy Ml7sNlUyOzl|OUW=
MT-3 NXTmR45MU2mwYYPlJGF{e2G7 NF;lenE4OiCq MVLEUXNQ NHTjTZVKSzVyPUKuPFYhyrFiMD61OEBvVSCob4KgSHI1KGW6cILld5Nqd25? NYnt[GhQOjR6Nk[1PFU>
MDA-MB-468 M3\BdGtqdmG|ZTDBd5NigQ>? NV7renBQPzJiaB?= MYfEUXNQ NGnTb3dKSzVyPUCuNVEhyrFiMD6wNUBvVSCob4KgSHI1KGW6cILld5Nqd25? MmnNNlQ5PjZ3OEW=
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ACC-2 NH3ufGZCeG:ydH;zbZMhSXO|YYm= M{H2cVAuOjBibl2= NIXlXIozPCCq NGC0S49qdmS3Y3XzJIFxd3C2b4Ppd{BqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MWGyOFM4ODl7NR?=
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A2780cis MnPQSpVv[3Srb36gRZN{[Xl? M2fn[VAuOTByIH7N MXGyOEBp M3;2cWROW09? MkHPbY5lfWOnczDTeZJ3cX[rbjDkc5dvemWpdXzheIlwdsLi NWrSWJREOjR{NkK4O|U>
A2780p Mo\5RZBweHSxc3nzJGF{e2G7 MYq1MVExOCCwTR?= NELlblMzPC92ODDo NU[xdJB1TE2VTx?= MYTpcoNz\WG|ZYOgZZBweHSxc3nzJIlvKGFiY3;uZ4VvfHKjdHnvck1l\XCnbnTlcpQhdWGwbnXy MUiyOFI3Ojh5NR?=
A2780cis M4H6O2Fxd3C2b4Ppd{BCe3OjeR?= NVz0UG9zPS1zMECgcm0> MUOyOE81QCCq NYWzdI1pTE2VTx?= NYT4VWNRcW6lcnXhd4V{KGGyb4D0c5NqeyCrbjDhJINwdmOnboTyZZRqd25vZHXw[Y5l\W62IH3hco5meg>? M1nIT|I1OjZ{OEe1
SH-SY5Y NIHzRmxCeG:ydH;zbZMhSXO|YYm= M2H3XlEwOTBxMUCwJOK2VQ>? MonnO|IhcA>? MoLGSG1UVw>? NHO2VpRqdmS3Y3XzJIFxd3C2b4Ppd{BqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> M3\TOlI1OjV2NU[w
HL-60 NYL3XJNbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVe3NuKhcA>? MojISG1UVw>? NW\k[WRtUUN3ME2wMlMhdk1? NX7zVIdpOjN4MUi4OlI>
U937  MlTjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVjXdHFvPzMEoHi= MoXNSG1UVw>? NHr3VZJKSzVyPUCuPEBvVQ>? MoHRNlM3OTh6NkK=
HL-60  M4TjfGZ2dmO2aX;uJGF{e2G7 MX:xxsDPxE1? M4rEPVYwOTJxMkSgbC=> M2nuT2ROW09? MYnpcohq[mm2czD0bIUh\XiycnXzd4lwdiCxZjDzeZJ3cX[rbh?= NXjqcJV2OjN4MUi4OlI>
U937  NXe5SVF{TnWwY4Tpc44hSXO|YYm= MVuxxsDPxE1? M3jKR|YwOTJxMkSgbC=> MWPEUXNQ NVjUToNVcW6qaXLpeJMhfGinIHX4dJJme3Orb36gc4Yhe3W{dnn2bY4> NXzVZ4ViOjN4MUi4OlI>
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Sk-NEP-1  NVLDOWhoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFflbnEyNTFyMECwJI5O M{n4e|I1KGh? Mln1SG1UVw>? MXLJR|UxRTFyMDDuUS=> MX:yN|I3PzZ7OR?=
SK-NEP-1  MVvBdI9xfG:|aYOgRZN{[Xl? NH70ZXo2OC9zMECgcm0> MkHRNVIwOjRiaB?= MkHUSG1UVw>? MnzIbY5lfWOnczDhdI9xfG:|aYO= MYmyN|I3PzZ7OR?=
TC-32 NF\OTnRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmTWNE4yNTFyMECgcm0> NHf1cJpGSzVyPUOuNEBvVSxiaX7obYJqfHNiY3XscEBoem:5dHigbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK= M1[yO|IzQTZzN{[z
TC-71 NWr2fW5rT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEDwRosxNjFvMUCwNEBvVQ>? MUTFR|UxRTVwNzDuUUwhcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MoL0NlI6PjF5NkO=
SK-ES-1 NXLncW86T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF\lbmQxNjFvMUCwNEBvVQ>? MU\FR|UxRTJwODDuUUwhcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MnfzNlI6PjF5NkO=
RD-ES M4TsXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYDFdldmOC5zLUGwNFAhdk1? NX;Tfm9OTUN3ME22MlIhdk1uIHnubIljcXS|IHPlcIwh\3Kxd4ToJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy M2PUS|IzQTZzN{[z
HEK293 M17PS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmSxNE4yNTFyMECgcm0> NVPNcXg{TUN3ME2yN{4xKG6PLDDpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MYCyNlk3OTd4Mx?=
M059J MkL1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MU[wMVUxKG6P MWq0PEBp MknNbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MWeyNlc4ODFzMB?=
M059K MlnSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGnXbo8xNTVyIH7N MYm0PEBp MmrzbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NIrDTmwzOjd5MEGxNC=>
M059J NVfOb2ZHSXCxcITvd4l{KEG|c3H5 MnnGN|Ahdk1? MkD0NlQhcA>? MVvpcoR2[2W|IHHwc5B1d3Orcx?= NVHTS2NtOjJ5N{CxNVA>
M059K NGq2b|lCeG:ydH;zbZMhSXO|YYm= MlX4N|Ahdk1? NYrLflZoOjRiaB?= M{ntUolv\HWlZYOgZZBweHSxc3nz MkDnNlI4PzBzMUC=
PANC-1 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnHWNE4xOS1zMECwJI5O M4fGWVQ5KGh? M4W5eGlEPTB;Mz62PUBvVQ>? NIW4[YQzOjd{M{i3NS=>
MIAPaCa-2 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2jydlAvODFvMUCwNEBvVQ>? NF7mRWQ1QCCq NVH3VWpQUUN3ME2yPU4{PiCwTR?= NXnLeVBxOjJ5MkO4O|E>
BxPC-3 NVXDRpAxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYq3PJpIOC5yMT2xNFAxKG6P M3jOWFQ5KGh? NFXHVopKSzVyPUOwMlI3KG6P M2rCNVIzPzJ|OEex
PANC-1 MkiySpVv[3Srb36gRZN{[Xl? MnPYNE0yODByIH7N Ml;6NlQhcA>? NIPsdZFqdmS3Y3XzJIRwf26{ZXf1cIF1cW:wIH;mJHhKSVBiYX7kJJN2en[rdnnuJIV5eHKnc4Ppc44> Mkm0NlI4OjN6N{G=
MIAPaCa-2 MUTGeY5kfGmxbjDBd5NigQ>? M1e0XlAuOTByMDDuUS=> MUWyOEBp NXniZnllcW6mdXPld{Bld3ewcnXneYxifGmxbjDv[kBZUUGSIHHu[EB{fXK4aY\pckBmgHC{ZYPzbY9v MnfQNlI4OjN6N{G=
BxPC-3 MmX6SpVv[3Srb36gRZN{[Xl? MnLqNE0yODByIH7N M{HmeFI1KGh? M1mzdYlv\HWlZYOg[I94dnKnZ4XsZZRqd25ib3[gXGlCWCCjbnSgd5Vzfmm4aX6g[ZhxemW|c3nvci=> MUOyNlczOzh5MR?=
RPMI-7951 Mn;OS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVHHTVUxRTNwMjDuUS=> NYPSdGJKOjF5M{e1NFI>
SK-MEL-5 NV30XnF[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVPNVGFxT0l3ME20MlIhdk1? NGrJOngzOTd|N{WwNi=>
A375 NFjEPVlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUnOWYgyT0l3ME22MlMhdk1? Mon3NlE4Ozd3MEK=
SK-MEL-28 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mo\PS2k2OD15Lk[gcm0> Mk\oNlE4Ozd3MEK=
SK-MEL-2 MmXWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MonES2k2OD1zMTDuUS=> M1nxU|IyPzN5NUCy
DB NVjsfYltT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnrnOFjDqGh? MVHHTVUxRTNwNTDuUS=> MnKwNlEzOzd3MEi=
Pfeiffer NF\vd5VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2G3PVQ5yqCq NY\2e3Z6T0l3ME2zMlkhdk1? MkPGNlEzOzd3MEi=
SU-DHL-5 NET4XZJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVW0POKhcA>? MljES2k2OD1yLkKzJI5O MWmyNVI{PzVyOB?=
SU-DHL-8 NFzqVGVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3zT[lQ5yqCq NGmyZmhIUTVyPUGuOEBvVQ>? MWGyNVI{PzVyOB?=
WSU-DLCL-2 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHrLUIk1QMLiaB?= NHTKPI5IUTVyPUGuOEBvVQ>? MWmyNVI{PzVyOB?=

... 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'-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:[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

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

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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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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

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Survivin Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID