Tozasertib (VX-680, MK-0457)

Catalog No.S1048

Tozasertib (VX-680, MK-0457) Chemical Structure

Molecular Weight(MW): 464.59

Tozasertib (VX-680, MK-0457) is a pan-Aurora inhibitor, mostly against Aurora A with Kiapp of 0.6 nM in a cell-free assay, less potent towards Aurora B/Aurora C and 100-fold more selective for Aurora A than 55 other kinases. Phase 2.

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Cited by 38 Publications

16 Customer Reviews

  • (G) Nocodazole-arrested HeLa cells were treated with VX-680 and MG132 and stained for CENP-E (Green), pT422 (Red) and DNA (Blue). (H) pT422 fluorescence intensity was normalized to the total CENP-E fluorescence. Plots show the mean of > 15 cells per condition from two independent experiments.

    Cell 2010 142, 444–455. Tozasertib (VX-680, MK-0457) purchased from Selleck.

    Senescence induction upon PKCι depletion combined with aurora kinase inhibition. ( a) MCF7 cells were transfected as above to deplete PKCι . Two days after transfection, cells were treated for the indicated time period with 400 n M VX-680. Medium with VX-680 was then removed and fresh medium was added. Cells were stained for SA-b -gal activity 5 days after the start of transfection.* indicates a P value <0.05. ( b) MCF7 cells were treated as above. Five days after transfection, cells were fixed and assessed for the presence of gH2AX foci by immunofluorescence microscopy. (c, d) MCF7 cells were treated with dimethyl sulfoxide (DMSO) control or 400 n M VX-680 for the indicated time periods. Total cell lysates were then analyzed by western blotting for levels of p21 and GAPDH (as loading control). A representative blot is shown in panel c. Quantitation of changes in p21 levels (normalized to vehicle-treated controls) is shown in panel d. The data shown are the means ±s.e. of three independent experiments.

    Oncogene 2012 31, 3584-96. Tozasertib (VX-680, MK-0457) purchased from Selleck.

  • Senescence induction upon PKCι depletion combined with aurora kinase inhibition in glioblastoma cells. (a, b) U87MG cells were transfected as above to deplete PKCι. Two days after transfection, cells were treated for 72 ( a)or24h (b) with 400 nM VX-680. Medium with VX-680 was then removed and fresh medium was added. Cells were stained for SA-b-gal activity 5 days after the start of transfection. * indicates a P value <0.05. (c) U87MG cells were treated as described in panel a above. Five days after transfection, cells were fixed and assessed for the presence of gH2AX foci by immunofluorescence microscopy. (d) U87MG cells were treated with the dimethyl sulfoxide (DMSO) control or 400 n M VX-680 for the indicated time periods. Total cell lysates were then analyzed by western blotting for levels of p21. The bar graph shows quantitation of p21 levels (normalized to vehicle-treated controls) from three independent experiments. A representative blot is also shown, with lanes aligned to correspond to the labels on the graph.

    Oncogene 2012 31, 3584-96. Tozasertib (VX-680, MK-0457) purchased from Selleck.

    MTT assay reveals a dose-dependent decrease in cell viability in mouse derived brainstem glioma cells treated with VX-680 ( P < 0.001) after 72 h of treatment. The error bars represent the standard deviation. Propidium iodide based cell sorting of mouse derived brainstem glioma cells after 72 h treatment with 5 μM reversine or 100 nM VX-680 respectively reveals increased cell populations with 4N and 8N DNA content as compared to vehicle control.

    Brain Pathol 2012 23, 244-53. Tozasertib (VX-680, MK-0457) purchased from Selleck.

  • Treatment of mouse derived brainstem glioma cells for 72 h with 5 μM reversine or 100 nM VX-680 increases cell size compared with vehicle-treated control and leads to irregular-shaped nuclei and micronuclei (F–H). Images F–H represent immunofluorescent staining for GFAP (green) with DAPI counter-stain (blue) and were taken at 400 ×magnification.

    Brain Pathol 2012 23, 244-53. Tozasertib (VX-680, MK-0457) purchased from Selleck.

     

    Aurora-A inhibitors severely impair neuronal migration. Migration of granular neurons after treatment of Aurora-A inhibitors was examined. a, Western blotting analysis of proteins or phosphorylated proteins. Aurora-A and NDEL1 displayed similar expression levels, whereas phosphorylated Aurora-A and NDEL1 proteins were decreased during treatment with Aurora-A inhibitors. Relative intensities of the bands of Western blotting are displayed at the bottom.

    J Neurosci 2012 32, 11050-11066. Tozasertib (VX-680, MK-0457) purchased from Selleck.

  • B, BLQ1 and UCSF02 cells were treated with increasing concentrations of VX-680 for 48 hours. The percentage of apoptotic cells was determined by fluorescence-activated cell sorting analysis. C, BLQ1 cells were treated with 1 μmol/L VX-680 and cell cycle distribution was determined by flow cytometry at time points of 24 and 48 hours.

    Mol Cancer Ther 2010 9, 1318–1327. Tozasertib (VX-680, MK-0457) purchased from Selleck.

    VX-680 eliminates Bcr/Abl kinase activities. BLQ1 (T315I mutation) and TXL2 (no mutation) cells were treated with the indicated concentrations of VX-680 with or without 100 nmol/L dasatinib for 24 hours. Western blot analysis was done on total lysates with the antibodies indicated to the left. Blots were stripped and reprobed with Bcr (N-20), Src, and GAPDH antibodies as loading controls.

    Mol Cancer Ther 2010 9, 1318–1327. Tozasertib (VX-680, MK-0457) purchased from Selleck.

  • Responses of human ALL cells to short-term VX-680 treatment. A, BLQ1 cells were treated with 1 μmol/L VX-680 for 3 days. After 3 days, the drug was removed from the medium and cells were cultured without VX-680. During this period (days 3-21) without drug, viability (top left), cell numbers (bottom left), and cell cycle distribution (right) of BLQ1 cells were assessed. B, BLQ1 and BLQ1-VX-Tx cells were cytospun onto glass slides and fixed, dried, and stained with Wright-Giemsa on day 21. All images are at ×63 magnification. C, BLQ1 and BLQ1-VX-Tx cells were treated with 1.5 μmol/L VX-680 or 5 nmol/L vincristine for 72 hours. Cell viability was measured by trypan blue exclusion. *, P < 0.05, vincristine-treated BLQ1 compared with vincristine-treated BLQ1-VX-Tx.

    Mol Cancer Ther 2010 9, 1318–1327. Tozasertib (VX-680, MK-0457) purchased from Selleck.

    VX-680 and dasatinib synergize to induce cytotoxic activity in wild-type Bcr/Abl-positive human ALL cells. A, TXL2 and UCSF02 cells were exposed to 1 μmol/L VX-680 with or without 100 nmol/L dasatinib for 24 to 72 hours as indicated, after which the percentage of viable cells was determined by trypan blue exclusion. B, TXL2 cells were treated with or without VX-680 and dasatinib for 48 hours in triplicate. **, P < 0.001, VX-680 and dasatinib cotreated TXL2 compared with VX-680-treated or dasatinib alone-treated TXL2 cells. Apoptotic cells were defined by flow cytometry as Annexin V and propidium iodide (PI) double-positive cells. C, TXL2 cells were exposed to VX-680 and/or dasatinib and cell cycle distribution was assessed by flow cytometry.

    Mol Cancer Ther 2010 9, 1318–1327. Tozasertib (VX-680, MK-0457) purchased from Selleck.

  • C, E: Expression of Aur-A and phosphorylated histone H3 in TPC-1 cells after VX-680 treatment. D, F: Expression of phosphorylated histone H3 in PTC tumor tissues after VX-680 treatment.

    Biochem Biophys Res Commun, 2016, 473(1):212-8. Tozasertib (VX-680, MK-0457) purchased from Selleck.

    Apoptosis induction in HB cells treated with a combination of VX-680. HUH6 (a) and HepT1 ( b ) were incubated with VX-680 (6 and 12.5 μM). Caspase-3 activation was detected with the NucView- 488 substrate 24 h later. Green fluorescent cells denote apoptotic cells.Scale bar represents 50 μm.

    Pediatr Surg Int 2012 28, 579-89. Tozasertib (VX-680, MK-0457) purchased from Selleck.

  • Morphological changes and histone H3 phosphorylation of HB cells treated with a combination of VX-680 and SAHA. HUH6 and HepT1 were incubated with VX-680 (6 μM) and SAHA (0.5 μM). Nuclei diameter (a) and cell diameter (b) were determined 72 h later by DAPI staining and microscopy. Data represent mean±SD of the diameters from 20 cells in each experiment. (* Two-way ANOVA, Bonferroni test, p \0.05). c Western blot analysis on HUH6 and HepT1 cells were carried out with an anti-phospho-Histone H3 (Ser 10) antibody (p-H3) 24 h after incubation with VX-680 (10 μM), SAHA (0.2 μM) or a combination of both. Controls were left untreated. Western blot analysis showed a decrease in p–H3 after treatment with VX-680 ( lane 2 ) relative to controls ( lane 1 ) and an increase when SAHA was added ( lane 3 ). For the combination of VX-680 and SAHA (lane 4 ) no p-H3 was detected.

    Pediatr Surg Int 2012 28, 579-89. Tozasertib (VX-680, MK-0457) purchased from Selleck.

    ENMD-2076 has benn tested it on two different neurobiastoma cell lines(SK-N-BE(2) and CHP-134),being calculated the IC50 by a WST-1(Roche) proliferation assay, as shown in the table below. Its in vitro activity is in the micromolar range and has a comparable effect on both lines.VX-680 was used as standard, and it proved more potent on CHP-134 cells.

    Dr. Antonino Maria Sparta ,University of Trento. Tozasertib (VX-680, MK-0457) purchased from Selleck.

  • SDS-PAGE of CHP-134 cells extracts after 24 h exposure to the indicated drug and concentration. N-myc levels were evaluated and compared to beta actin used as house-keeping protein. Aurora A blockade seems to diminish N-myc expression or stability.

    Dr. Antonino Maria Sparta ,University of Trento. Tozasertib (VX-680, MK-0457) purchased from Selleck.

    Western blot analysis of Histone and Aurora kinase. 0-10μM MK0457 was added.

    Dr. Zhang of Tianjin Medical University. Tozasertib (VX-680, MK-0457) purchased from Selleck.

Purity & Quality Control

Choose Selective Aurora Kinase Inhibitors

Biological Activity

Description Tozasertib (VX-680, MK-0457) is a pan-Aurora inhibitor, mostly against Aurora A with Kiapp of 0.6 nM in a cell-free assay, less potent towards Aurora B/Aurora C and 100-fold more selective for Aurora A than 55 other kinases. Phase 2.
Targets
Aurora A [1]
(Cell-free assay)
Aurora C [1]
(Cell-free assay)
Aurora B [1]
(Cell-free assay)
FLT3 [4]
(Cell-free assay)
Bcr-Abl [4]
(Cell-free assay)
0.6 nM(Ki app) 4.6 nM(Ki app) 18 nM(Ki app) 30 nM(Ki) 30 nM(Ki)
In vitro

Although its multi-kinase profile, VX-680 induces similar cytotoxicity with IC50 of approximately 300 nM and exhibits an AUR B-like inhibitory phenotype of G2/M arrest, endoreduplication and apoptosis in BaF3 cells transfected with ABL or FLT-3 (mutant and wild type) kinases. VX-680 prevents the CAL-62 proliferation in a time-dependent manner. VX-680 treatment for 14 days significantly decreases the number and size of colonies by approximately 70% in the 8305C and 90% in the CAL-62, 8505C and BHT-101. Treatment of the different ATC cells with VX-680 inhibits proliferation with the IC50 between 25 and 150  nM. The VX-680 significantly impairs the ability of the different cell lines to form colonies in soft agar. Analysis of caspase-3 activity indicates that VX-680 induces apoptosis in the different cell lines. CAL-62 cells exposed for 12  hours to VX-680 showed an accumulation of cells with ≥4N DNA content. Time-lapse analysis demonstrates that VX-680-treated CAL-62 cells exit metaphase without dividing. Moreover, histone H3 phosphorylation is abrogated following VX-680 treatment. [2] VX-680 has significant inhibitory activity against BCR-Abl bearing the T315I mutation in patient-derived samples. [3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
BE-13 M{XkdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2rsO2lEPTB;MD6wNFM{QCEQvF2= MXjTRW5IWkWU
RS4-11 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUm1PGsyUUN3ME2wMlAxPDB2IN88US=> M2HvNHNCVkeURWK=
MFH-ino MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHLiPZZKSzVyPUCuNFA6QSEQvF2= MXjTRW5IWkWU
NTERA-S-cl-D1 NV3LR|BCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mlr4TWM2OD1yLkCxOFM1KM7:TR?= M1LyZ3NCVkeURWK=
697 M1fROGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGGycZJKSzVyPUCuNFI1PzFizszN MWTTRW5IWkWU
NALM-6 MnTUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkW4TWM2OD1yLkCyOVUzKM7:TR?= M3LBcXNCVkeURWK=
ES8 NGf6XnpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWnaW49XUUN3ME2wMlA1PjF|IN88US=> MVTTRW5IWkWU
HUTU-80 M1n1O2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUDJR|UxRTBwMEWyPVkh|ryP Ml;PV2FPT1KHUh?=
MV-4-11 M3L5e2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1KzWmlEPTB;MD6wO|c5OiEQvF2= NEmzdFRUSU6JUlXS
MONO-MAC-6 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlTRTWM2OD1yLkC3PFc6KM7:TR?= NUjBPHp4W0GQR2LFVi=>
LC-2-ad MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHLHS25KSzVyPUCuNFg4QDlizszN M4Lye3NCVkeURWK=
BL-41 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXnMb2hEUUN3ME2wMlExPDR3IN88US=> NEPFS4xUSU6JUlXS
A4-Fuk Ml3kS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{jONWlEPTB;MD6xNVU3OyEQvF2= M{\q[HNCVkeURWK=
SW954 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXPJR|UxRTBwMUKyNlkh|ryP M{O1ZXNCVkeURWK=
BV-173 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHTuXIhKSzVyPUCuNVI3PDFizszN NIfxUHdUSU6JUlXS
TE-11 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M332cWlEPTB;MD6xOFk5OiEQvF2= NES4OYVUSU6JUlXS
SK-UT-1 MoHjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M37BfmlEPTB;MD6xOVk3PSEQvF2= M2D1e3NCVkeURWK=
SIG-M5 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1PzXWlEPTB;MD6xOlcxPyEQvF2= MnHIV2FPT1KHUh?=
OCUB-M NVzoOJdRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2TB[WlEPTB;MD6xOlk5OyEQvF2= MV7TRW5IWkWU
K052 NU\yZ444T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1LVSWlEPTB;MD6xPVQ5KM7:TR?= MYDTRW5IWkWU
VA-ES-BJ NVnScIJUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NITSOJhKSzVyPUCuNlAxQDZizszN MXfTRW5IWkWU
SW982 MmHYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmfUTWM2OD1yLkKxN|gh|ryP MWPTRW5IWkWU
LB647-SCLC NVW1Tm1YT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1ficmlEPTB;MD6yNVUzOyEQvF2= MkGzV2FPT1KHUh?=
PSN1 M4jMU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYjJR|UxRTBwMkKwNlYh|ryP MV7TRW5IWkWU
BB30-HNC NH;OXJpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnjuTWM2OD1yLkKyOVkyKM7:TR?= MYjTRW5IWkWU
ST486 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHqyPGFKSzVyPUCuNlMxQDdizszN MVnTRW5IWkWU
MOLT-4 M2DPWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGf3NHhKSzVyPUCuNlM{OzdizszN MVvTRW5IWkWU
EW-16 MlX5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXLHdFM6UUN3ME2wMlI{PzZ6IN88US=> MlPEV2FPT1KHUh?=
KS-1 NXiwfGtYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2DHRWlEPTB;MD6yN|c5PSEQvF2= NFjiPWxUSU6JUlXS
SR MnP2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYjjTYNtUUN3ME2wMlI1PTZ2IN88US=> MYXTRW5IWkWU
KM12 M3i2Zmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV7JR|UxRTBwMk[zOkDPxE1? NWTzSYo6W0GQR2LFVi=>
EM-2 MkLGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUTJcZVlUUN3ME2wMlI3PjRzIN88US=> MWnTRW5IWkWU
MEG-01 NE\UeYRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWPJR|UxRTBwMke4OFkh|ryP NGrr[VJUSU6JUlXS
NB13 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4\LeGlEPTB;MD6yO|k5PCEQvF2= NUHWNmFGW0GQR2LFVi=>
RKO NUfzXZJUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnfkTWM2OD1yLkOwPFE{KM7:TR?= MnLzV2FPT1KHUh?=
CESS M2P6c2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MU\JR|UxRTBwM{GzNlgh|ryP MnLvV2FPT1KHUh?=
EoL-1-cell NEnXZ5BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFu5N2xKSzVyPUCuN|M1PTlizszN NH\sWotUSU6JUlXS
DOHH-2 Mo\3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{DqZmlEPTB;MD6zN|c5OSEQvF2= Ml7wV2FPT1KHUh?=
A388 M4DMWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFvDUm1KSzVyPUCuN|QxQDZizszN MoS4V2FPT1KHUh?=
LAMA-84 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4LVTmlEPTB;MD6zOVE4QCEQvF2= MUfTRW5IWkWU
IMR-5 NWHxfY5uT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M33EUGlEPTB;MD6zOVU1KM7:TR?= Mnu1V2FPT1KHUh?=
KARPAS-422 Ml\3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIm4fXRKSzVyPUCuN|czPzJizszN M2Hh[3NCVkeURWK=
MRK-nu-1 M2Szcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1j1d2lEPTB;MD6zPFE{KM7:TR?= MmXDV2FPT1KHUh?=
BL-70 MlTES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkTGTWM2OD1yLkO4PVc1KM7:TR?= NXjKVXJIW0GQR2LFVi=>
LXF-289 NFPKUIxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGfMdWtKSzVyPUCuOFA1ODZizszN NGTSRYhUSU6JUlXS
RL95-2 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXS1TGtYUUN3ME2wMlQxPTZ5IN88US=> MkXzV2FPT1KHUh?=
QIMR-WIL NFX4T2pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVXJR|UxRTBwNEK2O|Yh|ryP MljrV2FPT1KHUh?=
K-562 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmHlTWM2OD1yLkSzOFczKM7:TR?= M{jhfXNCVkeURWK=
NCI-H510A M4rJeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWLzdmZkUUN3ME2wMlQ{QDJ|IN88US=> NHzkZXRUSU6JUlXS
NCI-H524 NWHRR4NlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHLLWGtKSzVyPUCuOVEyPDdizszN MWTTRW5IWkWU
KE-37 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV3JR|UxRTBwNUKxNFIh|ryP M13lXXNCVkeURWK=
KP-N-YS M2rGV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVf0fVQzUUN3ME2wMlU1Ozl{IN88US=> MYnTRW5IWkWU
LS-411N NYTVNGpFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXrJR|UxRTBwNUe3OVIh|ryP M12zS3NCVkeURWK=
CTV-1 NYfnfHdLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIS5TodKSzVyPUCuOVg4PzNizszN M3HGcXNCVkeURWK=
NCI-SNU-16 NVnmRXFmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWHRPJJwUUN3ME2wMlY{PTdzIN88US=> M2rve3NCVkeURWK=
HT-144 MnPoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlWzTWM2OD1yLk[zO|k5KM7:TR?= MXfTRW5IWkWU
NCI-H187 NGe3ZmZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX7DS4tVUUN3ME2wMlY1OTNizszN MlztV2FPT1KHUh?=
OCI-AML2 NVPpR|J6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVLJR|UxRTBwNkS0NFMh|ryP M1zYeXNCVkeURWK=
CCRF-CEM M4nTdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkX2TWM2OD1yLk[1N|Q3KM7:TR?= M4LVRnNCVkeURWK=
ONS-76 M{faNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MU\JR|UxRTBwNk[0OVgh|ryP NXHLPW9VW0GQR2LFVi=>
IST-SL2 NX[2eXBET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlzGTWM2OD1yLkexPVgzKM7:TR?= M2D6c3NCVkeURWK=
NB6 MoHrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mk\lTWM2OD1yLke3NlU1KM7:TR?= MmDaV2FPT1KHUh?=
SK-PN-DW MlLBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3TxV2lEPTB;MD63PVE1KM7:TR?= MnrYV2FPT1KHUh?=
HCC1599 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3PKSmlEPTB;MD64NFg4PCEQvF2= MWXTRW5IWkWU
MC116 MlflS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYK2RmF[UUN3ME2wMlg2ODFzIN88US=> M4foOHNCVkeURWK=
TE-15 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYXJR|UxRTBwOEWwPVgh|ryP NXj6THh1W0GQR2LFVi=>
HOP-62 NYj2PWVDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFe2bFNKSzVyPUCuPFY{OjlizszN NHTmRoJUSU6JUlXS
TGBC24TKB MmjyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{PaNWlEPTB;MD64OlM5PSEQvF2= MVrTRW5IWkWU
HCE-4 MoXKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmK2TWM2OD1yLki4NFY{KM7:TR?= MlLLV2FPT1KHUh?=
ALL-PO MoDQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NE\aPIhKSzVyPUCuPFgyPzVizszN M3z2W3NCVkeURWK=
KGN M4W3VWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1rp[GlEPTB;MD64PVk6PSEQvF2= M33hWXNCVkeURWK=
ML-2 NXfxdWQ5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn;RTWM2OD1yLkmwNlU6KM7:TR?= NV71TFBmW0GQR2LFVi=>
ES4 M1LGVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUnZXotwUUN3ME2wMlkyOTJ6IN88US=> NHntdWdUSU6JUlXS
SF126 NHnMXmFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkHOTWM2OD1yLkm0PFE6KM7:TR?= NWTIZ5I{W0GQR2LFVi=>
SK-N-DZ NGj0[I1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmjpTWM2OD1yLkm2NVg6KM7:TR?= MV;TRW5IWkWU
HCC1187 Mm\SS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4rwVWlEPTB;MT6wNFUxPSEQvF2= MnXRV2FPT1KHUh?=
DU-4475 NH:3SW1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkG2TWM2OD1zLkCxO|U3KM7:TR?= NXHDWlNZW0GQR2LFVi=>
NKM-1 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFLtUIlKSzVyPUGuNFI4PzVizszN MVrTRW5IWkWU
HL-60 M4ezR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV3QW3dpUUN3ME2xMlA3PTd2IN88US=> NXLXfGtEW0GQR2LFVi=>
SBC-1 NWXUVHRzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn;sTWM2OD1zLkGyOVQzKM7:TR?= M3vYeXNCVkeURWK=
TE-10 NGHDUllIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYSw[GdJUUN3ME2xMlEzQTR4IN88US=> M2XzV3NCVkeURWK=
ETK-1 M3zR[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{WySWlEPTB;MT6xN|YyOyEQvF2= MnPBV2FPT1KHUh?=
HAL-01 NGCzT25Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVjTbGFJUUN3ME2xMlE3PzB7IN88US=> MnHqV2FPT1KHUh?=
BB65-RCC NV3Q[2VHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIX1S4NKSzVyPUGuNVgxODVizszN M1H3WXNCVkeURWK=
EW-1 MkC2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2jFXmlEPTB;MT6xPFU3OiEQvF2= NIPNNHBUSU6JUlXS
SK-NEP-1 NVjQOW9KT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEHDNZBKSzVyPUGuNlEyOTFizszN NWP2VVY2W0GQR2LFVi=>
SK-LMS-1 MoHRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUfJR|UxRTFwMkKyNVIh|ryP MXnTRW5IWkWU
DEL MnfvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXzJR|UxRTFwMkW2OFMh|ryP MlrmV2FPT1KHUh?=
GT3TKB M4fodWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mm\ETWM2OD1zLkK4NFU4KM7:TR?= M4fo[XNCVkeURWK=
MOLT-16 NXHBboM5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGOzOWNKSzVyPUGuN|U1ODVizszN MXHTRW5IWkWU
CMK M2C3Omdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3:4OmlEPTB;MT60NlEyPyEQvF2= M2LQXHNCVkeURWK=
NB5 M3voc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{i1fWlEPTB;MT62OFIzQSEQvF2= M2PPUHNCVkeURWK=
NCI-H1963 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYfJR|UxRTFwN{C1PFMh|ryP NYjhS5luW0GQR2LFVi=>
KURAMOCHI NVrFcHd7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVLJR|UxRTFwN{i5NVEh|ryP M123Z3NCVkeURWK=
TE-8 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoqyTWM2OD1zLkiwN|Y5KM7:TR?= M1z2fHNCVkeURWK=
NCI-H1304 Mn:zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2PDfGlEPTB;MT64N|A4OyEQvF2= NWfyUJQ{W0GQR2LFVi=>
A101D M3X5[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFjXdHFKSzVyPUGuPFc{QTVizszN MUjTRW5IWkWU
SCLC-21H NG\sOGhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVzJR|UxRTFwOUewOVch|ryP NGrGb5pUSU6JUlXS
GB-1 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX2xe2FlUUN3ME2yMlAyPjR5IN88US=> MnrQV2FPT1KHUh?=
KARPAS-45 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX;0OJFwUUN3ME2yMlAzPjV2IN88US=> M4\rSXNCVkeURWK=
ATN-1 MmfkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{HpeGlEPTB;Mj6wNlg2QCEQvF2= MX7TRW5IWkWU
NCI-H720 NFvM[HpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFXOb3RKSzVyPUKuNFYzPDRizszN MmHNV2FPT1KHUh?=
RPMI-6666 M3;JNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFr2[lZKSzVyPUKuNVYzODdizszN NUHYWpRmW0GQR2LFVi=>
NB17 NEXWTIhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmnrTWM2OD1{LkK5Nlch|ryP M3fOTXNCVkeURWK=
IST-SL1 NXu1[3RST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYLJR|UxRTJwMkm3OlUh|ryP NVq1PZA{W0GQR2LFVi=>
SH-4 MlLKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2rvU2lEPTB;Mj6zNlQ3QSEQvF2= MnTZV2FPT1KHUh?=
K5 NVzCd21XT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYrhcWlIUUN3ME2yMlQxOzF7IN88US=> M2[0dnNCVkeURWK=
OVCAR-4 NVLFRpltT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NES4dWNKSzVyPUKuOFYyOyEQvF2= NFfreVVUSU6JUlXS
ACN MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFGye3RKSzVyPUKuOVAzOTNizszN NX\WTIJEW0GQR2LFVi=>
TGW MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnK4TWM2OD1{Lk[1PFMzKM7:TR?= M4TOfnNCVkeURWK=
NCI-H2107 NVPsOHcxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWHhbo9FUUN3ME2yMlg{PzFzIN88US=> MlmwV2FPT1KHUh?=
NCI-H82 NUPlWGt3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUjC[lFCUUN3ME2yMlg{QDN6IN88US=> MVjTRW5IWkWU
SK-N-FI MoHpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmjHTWM2OD1{Lki2PFY5KM7:TR?= M{TUVnNCVkeURWK=
LB1047-RCC NHPxVFZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX\PWWJGUUN3ME2yMlg5OTJ4IN88US=> Ml61V2FPT1KHUh?=
LU-134-A NWfleI4zT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV;KbXZrUUN3ME2yMlg6OjZizszN MXjTRW5IWkWU
NCI-H209 M3roU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH7YUHpKSzVyPUKuPVEzPTNizszN MYfTRW5IWkWU
NOMO-1 NXrCRpBFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUfJR|UxRTNwMEKyO|Qh|ryP NUXxOolyW0GQR2LFVi=>
RH-1 M2TiTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXTaPWc2UUN3ME2zMlE4OjlzIN88US=> MleyV2FPT1KHUh?=
LOUCY MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV;JR|UxRTNwMUi2PVMh|ryP MVvTRW5IWkWU
TE-9 NY[0SVI3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml7KTWM2OD1|LkK2O|M3KM7:TR?= MY\TRW5IWkWU
PF-382 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWPtUlUzUUN3ME2zMlM2Pzd6IN88US=> NYDtSGpqW0GQR2LFVi=>
RPMI-8402 M336eWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmjkTWM2OD1|LkW4OlA{KM7:TR?= MlnFV2FPT1KHUh?=
HEL NFXLO4VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlrvTWM2OD1|Lk[zNkDPxE1? M4XveHNCVkeURWK=
NOS-1 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX3JR|UxRTNwOES3OVQh|ryP MXvTRW5IWkWU
ES1 NUG2OWpIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NID2UYtKSzVyPUOuPVIzQTNizszN Mn71V2FPT1KHUh?=
NCI-H2171 NFPRbJlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NG\rXZZKSzVyPUOuPVI1OjNizszN NVfhSmliW0GQR2LFVi=>
NCI-H747 MoL2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3K0T2lEPTB;Mz65OFIzOSEQvF2= NGDXNmtUSU6JUlXS
MHH-NB-11 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVrvR3ppUUN3ME2zMlk2OzF{IN88US=> M3zMcHNCVkeURWK=
MZ1-PC NXLBWoM2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGPXOZhKSzVyPUOuPVkzPCEQvF2= M3H5OHNCVkeURWK=
MMAC-SF NInpT|VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWfJR|UxRTRwMEK0Olch|ryP MUjTRW5IWkWU
NMC-G1 M122OWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoD2TWM2OD12LkKyO|I{KM7:TR?= M{\PWXNCVkeURWK=
SW872 NED1VZVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYTzZ2U5UUN3ME20MlM1OzRizszN NFnmephUSU6JUlXS
TE-12 MoS5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYXGT2kyUUN3ME20MlU3Ozl2IN88US=> NEnYRXZUSU6JUlXS
LU-139 Mn:0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUjEd2F5UUN3ME20MlYyQDN3IN88US=> NWLCeWk{W0GQR2LFVi=>
HC-1 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEDNPXpKSzVyPUSuOlk1QTRizszN NYfNXFk4W0GQR2LFVi=>
COR-L279 NV;NbXBXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NG\iVpVKSzVyPUSuO|U5QTFizszN M2TCT3NCVkeURWK=
SF268 NVLX[25WT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFOy[25KSzVyPUSuO|k6OTZizszN M{LEdnNCVkeURWK=
MC-CAR NGf6SpRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVXJR|UxRTVwME[3OVch|ryP NFm5cotUSU6JUlXS
TK10 NV\pTpdkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml62TWM2OD13LkO1OFY6KM7:TR?= M13oW3NCVkeURWK=
TE-1 M2LT[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3qzTGlEPTB;NT60PVAxPCEQvF2= Mlq0V2FPT1KHUh?=
NCI-H2126 M4exVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVPOfJozUUN3ME21MlY1PTd2IN88US=> NFfPNI9USU6JUlXS
Daudi M{LxOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnLuTWM2OD13Lk[5NVIh|ryP NVvFOGpVW0GQR2LFVi=>
NCI-H1648 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX;tS4JmUUN3ME21MlgyPDV2IN88US=> MnO3V2FPT1KHUh?=
OS-RC-2 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWDJR|UxRTVwOUi1PVch|ryP MlW2V2FPT1KHUh?=
DJM-1 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2W0O2lEPTB;Nj6zOFY3PiEQvF2= M3r5dHNCVkeURWK=
LS-1034 Mmq5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnyxTWM2OD14Lke1OlYh|ryP NH3TeHVUSU6JUlXS
NCI-H1581 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWrzNHJLUUN3ME22Mlc5PDB3IN88US=> M2TwT3NCVkeURWK=
UACC-257 Ml\GS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2XFWWlEPTB;Nz6wOFUyOiEQvF2= MVPTRW5IWkWU
KM-H2 M3KzWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX\F[m1bUUN3ME23MlE5PDV5IN88US=> MmO1V2FPT1KHUh?=
NCI-H1436 M4LCO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2LqWGlEPTB;Nz62PVk{OiEQvF2= MYHTRW5IWkWU
IA-LM NWPXWmt4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmHvTWM2OD15Lki1PUDPxE1? MoLZV2FPT1KHUh?=
NCI-H526 NH6xdIJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEDvbHVKSzVyPUiuNlU3OzdizszN MUPTRW5IWkWU
GCIY MkLxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4D2dWlEPTB;OD6zOlk3PSEQvF2= M4HyUHNCVkeURWK=
CP67-MEL M1H2Wmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn3RTWM2OD16LkWzNlYh|ryP NVPSdXd7W0GQR2LFVi=>
KALS-1 NILVdnhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1e4OmlEPTB;OD64N|g2OSEQvF2= MkLtV2FPT1KHUh?=
NCI-H1770 NYOyVJpvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2HSdmlEPTB;OD65NFI3PSEQvF2= M17yeXNCVkeURWK=
8-MG-BA MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVnJR|UxRTlwM{K4OFQh|ryP NEjHd2VUSU6JUlXS
KY821 M3TXXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGDxSGxKSzVyPUmuO|c1QDRizszN NXvneHN[W0GQR2LFVi=>
SNB75 M2D1cGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NG\6NY5KSzVyPUGwMlA4PiEQvF2= M{CxOHNCVkeURWK=
NCCIT NWXLXWptT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1\RfGlEPTB;MUGuNFU5OiEQvF2= NWDZeGdpW0GQR2LFVi=>
SJSA-1 NXn6WIppT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn\GTWM2OD1zMT6yPFkyKM7:TR?= MVvTRW5IWkWU
LB373-MEL-D NGjtNmZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3PMemlEPTB;MUGuN|gzPyEQvF2= NE\OPWZUSU6JUlXS
TALL-1 NVnlZYwyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2rGUWlEPTB;MUGuOFA2QCEQvF2= NX\tZlc5W0GQR2LFVi=>
NB69 NHjFVHRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnfOTWM2OD1zMT63O|A2KM7:TR?= Ml7nV2FPT1KHUh?=
NCI-H1355 MkO1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mlf0TWM2OD1zMT65OFI3KM7:TR?= MlrKV2FPT1KHUh?=
DMS-153 NXPGWpQzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlvrTWM2OD1zMj6wOFI3KM7:TR?= MX\TRW5IWkWU
OPM-2 NHXnZ3RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1uz[GlEPTB;MUKuNVU6PiEQvF2= MnHLV2FPT1KHUh?=
NB1 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWHJR|UxRTF{LkK5JO69VQ>? NVXjXnFVW0GQR2LFVi=>
A3-KAW NWjs[pc1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4rqZ2lEPTB;MUKuN|I{PiEQvF2= M2HKZnNCVkeURWK=
NCI-H1882 Mk\wS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXfJR|UxRTF{LkSwOlYh|ryP NY\vV4dWW0GQR2LFVi=>
KG-1 Mk\kS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnPkTWM2OD1zMj62OVQ2KM7:TR?= MmnYV2FPT1KHUh?=
LC4-1 NHfVNYlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXrJR|UxRTF{Lke3NFYh|ryP MX3TRW5IWkWU
HCE-T NYXGUnVJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{jFRWlEPTB;MUOuNFA1QSEQvF2= NYXi[otlW0GQR2LFVi=>
NEC8 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnW2TWM2OD1zMz6xNFM5KM7:TR?= NVK3[pZ3W0GQR2LFVi=>
IST-MEL1 MmjXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHX4SXdKSzVyPUGzMlU4QDhizszN NIX5bZdUSU6JUlXS
EW-3 MknyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1\0XGlEPTB;MUOuO|QxOiEQvF2= NUTtU4gzW0GQR2LFVi=>
CTB-1 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1ToTWlEPTB;MUSuNFMzQSEQvF2= NYTscZo3W0GQR2LFVi=>
LS-123 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFTqZ5RKSzVyPUG0MlE2QDhizszN Mn61V2FPT1KHUh?=
NCI-H1417 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX\JR|UxRTF2LkOwOVIh|ryP MVfTRW5IWkWU
MZ7-mel MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX7JR|UxRTF2LkS0N|Mh|ryP M1TBeHNCVkeURWK=
JiyoyeP-2003 M17Ub2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mke2TWM2OD1zNT62N|I3KM7:TR?= MnrDV2FPT1KHUh?=
ES6 NGC4R4ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MU\JR|UxRTF4LkKzOlEh|ryP NYCzc|hKW0GQR2LFVi=>
HH MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWO3ZodNUUN3ME2xO{4yQTZ|IN88US=> MYfTRW5IWkWU
SF539 M2\oemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXP2VotDUUN3ME2xO{46QTJ{IN88US=> MVfTRW5IWkWU
Calu-6 MnPIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml;rTWM2OD1zOT6yN|kh|ryP MULTRW5IWkWU
SK-MM-2 M1qzT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX\5d4toUUN3ME2xPU42PTVizszN NHuzVWhUSU6JUlXS
IST-MES1 M2\Jdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX\JR|UxRTF7Lk[2OlMh|ryP MnHGV2FPT1KHUh?=
GI-ME-N MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGrBWZVKSzVyPUG5MlgzOjdizszN NVT4VJdMW0GQR2LFVi=>
CAL-148 MoHSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXzJR|UxRTJyLkm5N|Qh|ryP M13mVHNCVkeURWK=
EVSA-T MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2[4XGlEPTB;MkGuNVQ6QSEQvF2= MYPTRW5IWkWU
LP-1 MmHtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUH3cWtqUUN3ME2yNU4{PDN{IN88US=> Mmi2V2FPT1KHUh?=
BOKU M1LFXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MojPTWM2OD1{MT60OVM{KM7:TR?= M2raN3NCVkeURWK=
KLE NFvTRm5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlTCTWM2OD1{Mj6xPVA{KM7:TR?= MVjTRW5IWkWU
LB831-BLC NWrtV|hZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXfXe2tJUUN3ME2yOU4yPTJ4IN88US=> NFHi[pFUSU6JUlXS
NCI-H889 NEDqOWlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYHOdGpxUUN3ME2yOU4yQTNzIN88US=> M4LaUXNCVkeURWK=
REH M{PYfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVnJR|UxRTJ3LkS2O|Eh|ryP MYTTRW5IWkWU
KP-N-RT-BM-1 MnjzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVzpR2FuUUN3ME2yOU41PzV{IN88US=> Mn;kV2FPT1KHUh?=
MPP-89 MkPuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{TCTmlEPTB;MkWuOVMyPCEQvF2= MkLBV2FPT1KHUh?=
no-11 NEDsdYtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGjHNYFKSzVyPUK1Mlc1PyEQvF2= NXjKd|A5W0GQR2LFVi=>
NCI-H748 NUHaOnJuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWHvW4k1UUN3ME2yOU44PjJ5IN88US=> Mkn6V2FPT1KHUh?=
LB2518-MEL NYjxbXU4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYTJR|UxRTJ5LkG3O|Mh|ryP NYTsWm5[W0GQR2LFVi=>
TGBC1TKB MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGT2T45KSzVyPUK3MlU2QDVizszN NVf0eVM4W0GQR2LFVi=>
MHH-PREB-1 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUj4TmxuUUN3ME2yPE4xPzN2IN88US=> M1PkPXNCVkeURWK=
MZ2-MEL NWnoeVhpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3\3dWlEPTB;MkiuOlE1OyEQvF2= MYTTRW5IWkWU
U-266 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF74XIhKSzVyPUK4MlY{PjZizszN NEXUZllUSU6JUlXS
SNU-C1 M{nEb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NULqRll2UUN3ME2yPE46PDNizszN MXjTRW5IWkWU
SW962 MmjMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml7aTWM2OD1|MD6yO|Q4KM7:TR?= MYHTRW5IWkWU
Raji M3\6emdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVXJR|UxRTNyLkW1PVIh|ryP M{\2SnNCVkeURWK=
KNS-42 NV\PVnZST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVrjOFhjUUN3ME2zNE45QTV4IN88US=> MkK4V2FPT1KHUh?=
LB996-RCC MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYDJR|UxRTNzLkG3NFIh|ryP NFPLVpRUSU6JUlXS
CHP-126 NInJOZNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml;pTWM2OD1|MT6xPVg1KM7:TR?= NELqRZRUSU6JUlXS
RXF393 NYfLRopDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGexVZVKSzVyPUOyMlQ6PyEQvF2= MWLTRW5IWkWU
COLO-684 Mn7ES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXrJR|UxRTN{Lk[0N|gh|ryP MlXFV2FPT1KHUh?=
A704 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkHrTWM2OD1|Mz61OVM5KM7:TR?= NGG0WXVUSU6JUlXS
A253 NHXLd|FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWLWcGFrUUN3ME2zN{42QDV{IN88US=> MlvtV2FPT1KHUh?=
KNS-81-FD NVf0VoFJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mm\oTWM2OD1|ND61OFU3KM7:TR?= MYnTRW5IWkWU
TE-441-T M3:3VWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHfmWIVKSzVyPUO0MlY{PzFizszN MlywV2FPT1KHUh?=
HCC2157 NEjSWXFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWf3dod{UUN3ME2zOU41PjF7IN88US=> MWTTRW5IWkWU
ES3 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEP4S3BKSzVyPUO2MlY4PSEQvF2= MWPTRW5IWkWU
NCI-H1155 M3XPdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXOzTpFkUUN3ME2zO{45OTVizszN NYPXUpBGW0GQR2LFVi=>
SNU-C2B MlrzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEfpdpdKSzVyPUO4MlE3PTRizszN MUPTRW5IWkWU
JAR NVjONVk6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4HhN2lEPTB;M{iuNlQ1QSEQvF2= NFjGPFJUSU6JUlXS
GDM-1 MmW4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4DRNGlEPTB;M{iuPVEyPiEQvF2= M2O0O3NCVkeURWK=
KU812 NH;XenlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIP6SWZKSzVyPUSxMlUxPyEQvF2= NFrSUotUSU6JUlXS
BC-1 NGPUTJRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVT4dGtxUUN3ME20Nk43PzNzIN88US=> NFPyN|VUSU6JUlXS
GI-1 NEjqfFdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmDlTWM2OD12Mj65NVkzKM7:TR?= MXzTRW5IWkWU
NCI-H1694 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHruVFFKSzVyPUS0Mlk1PzJizszN MmPyV2FPT1KHUh?=
DG-75 NEmwWYZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NInRcYxKSzVyPUS1MlE2PzdizszN M4X5eXNCVkeURWK=
COR-L88 NXrDcXlpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnPkTWM2OD12NT6yO|c5KM7:TR?= M3T0WnNCVkeURWK=
LS-513 MmfpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXzKTJNZUUN3ME20OU46OTV4IN88US=> MWPTRW5IWkWU
HD-MY-Z NF3pOXBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3TwRmlEPTB;NE[uOFYyOiEQvF2= NGjjcINUSU6JUlXS
L-363 NIj5TlJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWrhWHI3UUN3ME20Ok45QDFizszN NUG1RnNwW0GQR2LFVi=>
TE-6 NE\KfVFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYTYbotGUUN3ME20PE41PDZizszN NHPmbWpUSU6JUlXS
NCI-H345 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoDaTWM2OD12OD60Olgh|ryP NWDE[49RW0GQR2LFVi=>
TE-5 Mon1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlXtTWM2OD12OT63NVE5KM7:TR?= MlHIV2FPT1KHUh?=

... Click to View More Cell Line Experimental Data

In vivo VX-680 gives rise to a marked decrease in tumor size in a human AML (HL-60) xenograft model. In mude mice treateed with VX-680 at 75 mg/kg, twice a day intraperitoneally (b.i.d. i.p.) for 13 days, mean tumor volumes are reduced by 98%. Tumor growth decrease is dose dependent and significant at a dose of 12.5 mg/kg b.i.d. VX-680 is well tolerated, with a small decrease in body weight observed only at the highest dose. VX-680 also triggers tumor regresson in pancreatic and colon xenograft models. VX-680 also displays potent antitumor activity when infused i.v. in mude rats bearing established HCT116 tumors. A higher dose of VX-680 (2 mg/kg/h) improves efficacy with a 56% decrease in mean tumor volume. [1]

Protocol

Kinase Assay:

[3]

+ Expand

Kinase inhibition assays:

The consumption of ATP is coupled via the pyruvate kinase/lactic dehydrogenase enzyme pair to the oxidation of NADH, which can be monitored through the decrease in absorption at 340 nm. Reactions contains 100 mM Tris (pH 8), 10 mM MgCl2, 2.2 mM ATP, 1 mM phosphoenolpyruvate, 0.6 mg/mL NADH, 75 units/mL pyruvate kinase, 105 units/mL lactate dehydrogenase, and 0.5 mM substrate peptide (sequence: EAIYAAPFAKKK). Reactions (75 μL) are started by adding sufficient kinase to bring the reactions to 30 nM kinase concentration and the decrease in absorbance is monitored over 30 minutes at 30°C in a microtiter plate spectrophotometer. Inhibitory constants are obtained through addition of 3.75 μL VX-680 in 100% DMSO or DMSO alone. Ki values are calculated as follows, K i = IC50 / (1 + [S]/Kd), where [S] = [ATP] = 2.2 mM, and Kd (of ATP to Abl) = 70 μM. These values are calculated assuming a Kd (ATP) of 70 μM for wild type and H396P Abl kinase domain.
Cell Research:

[2]

+ Expand
  • Cell lines: CAL-62 cells
  • Concentrations: 5-500 nM
  • Incubation Time: 4 days
  • Method:

    The CAL-62 cells are cultured in the absence (dimethyl sulfoxide, DMSO) or the presence of 500  nM VX-680 for different periods of time (1-5 days). The dose-dependent effects of VX-680 on cell proliferation are evaluated by treating the different ATC cells for 4 days with different concentrations of the Aurora inhibitor (5–500  nM). The cells are pulse labeled with 30  mM BrdU for 2  hours before the end of the incubation time. The BrdU incorporation is analyzed by means of a colorimetric immunoassay using the cell proliferation ELISA kit. The results from VX-680-treated cells are compared with those observed in control cells and expressed as a fold of variation versus control.


    (Only for Reference)
Animal Research:

[1]

+ Expand
  • Animal Models: Female athymic NCr-nu mice bearing HL-60 leukemia cells
  • Formulation: 50% PEG300 in 50 mM phosphate buffer
  • Dosages: 50 mg/kg, 75 mg/kg
  • Administration: Administered via i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 93 mg/mL (200.17 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
5% DMSO+30% PEG 300+2% Tween 80+ddH2O
For best results, use promptly after mixing.
15mg/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 464.59
Formula

C23H28N8OS

CAS No. 639089-54-6
Storage powder
in solvent
Synonyms N/A

Bio Calculators

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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)

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Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00500006 Terminated Chronic Myelogenous Leukemia|Leukemia Lymphoblastic Acute Philadelphia-Positive Merck Sharp & Dohme Corp. October 2007 Phase 1
NCT00500006 Terminated Chronic Myelogenous Leukemia|Leukemia Lymphoblastic Acute Philadelphia-Positive Merck Sharp & Dohme Corp. October 2007 Phase 1
NCT00405054 Terminated Leukemia Merck Sharp & Dohme Corp. December 2006 Phase 2
NCT00405054 Terminated Leukemia Merck Sharp & Dohme Corp. December 2006 Phase 2
NCT00290550 Terminated Carcinoma Non-Small-Cell Lung Merck Sharp & Dohme Corp. June 2006 Phase 2
NCT00290550 Terminated Carcinoma Non-Small-Cell Lung Merck Sharp & Dohme Corp. June 2006 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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Aurora Kinase Signaling Pathway Map

Aurora Kinase Inhibitors with Unique Features

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID