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 36 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 M2TSemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEWx[4VKSzVyPUCuNFA{OzhizszN M3zEbnNCVkeURWK=
RS4-11 NX[yPFlRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2TTNGlEPTB;MD6wNFQxPCEQvF2= Mn3KV2FPT1KHUh?=
MFH-ino NGXuNG9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1r3dWlEPTB;MD6wNFk6KM7:TR?= MY\TRW5IWkWU
NTERA-S-cl-D1 MoeyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVHZXmpJUUN3ME2wMlAyPDN2IN88US=> MWHTRW5IWkWU
697 NUjHUYhTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn;RTWM2OD1yLkCyOFcyKM7:TR?= M4XMbHNCVkeURWK=
NALM-6 NYHZPJdTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn;UTWM2OD1yLkCyOVUzKM7:TR?= MVrTRW5IWkWU
ES8 MmL4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmTyTWM2OD1yLkC0OlE{KM7:TR?= MmPHV2FPT1KHUh?=
HUTU-80 MojLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVTJR|UxRTBwMEWyPVkh|ryP NIDRSWNUSU6JUlXS
MV-4-11 M{\jUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1TwOGlEPTB;MD6wO|c5OiEQvF2= MWDTRW5IWkWU
MONO-MAC-6 NV3aR5J6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NULH[INTUUN3ME2wMlA4QDd7IN88US=> NFfueoRUSU6JUlXS
LC-2-ad M1rMc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV7JR|UxRTBwMEi3PFkh|ryP NUfRXlIyW0GQR2LFVi=>
BL-41 NYTx[ZM{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYjJR|UxRTBwMUC0OFUh|ryP M1LkSHNCVkeURWK=
A4-Fuk MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVrJR|UxRTBwMUG1OlMh|ryP MXnTRW5IWkWU
SW954 MlTxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXTJR|UxRTBwMUKyNlkh|ryP M1vsSnNCVkeURWK=
BV-173 NYXteFVvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlL6TWM2OD1yLkGyOlQyKM7:TR?= M1TE[nNCVkeURWK=
TE-11 NFHGbHVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH3EfppKSzVyPUCuNVQ6QDJizszN Mkf1V2FPT1KHUh?=
SK-UT-1 NIDaeY9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mk\FTWM2OD1yLkG1PVY2KM7:TR?= NIT4UVVUSU6JUlXS
SIG-M5 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmfJTWM2OD1yLkG2O|A4KM7:TR?= MoHsV2FPT1KHUh?=
OCUB-M MlzVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmPRTWM2OD1yLkG2PVg{KM7:TR?= NEfTcVRUSU6JUlXS
K052 Ml3LS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml7rTWM2OD1yLkG5OFgh|ryP NELJZYNUSU6JUlXS
VA-ES-BJ NVrPWZlwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF7nTXlKSzVyPUCuNlAxQDZizszN MkSwV2FPT1KHUh?=
SW982 NHHBOW1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnvKTWM2OD1yLkKxN|gh|ryP NHfKTYpUSU6JUlXS
LB647-SCLC MkLwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFvEdnVKSzVyPUCuNlE2OjNizszN MmSwV2FPT1KHUh?=
PSN1 NIX4dHlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkHqTWM2OD1yLkKyNFI3KM7:TR?= MoizV2FPT1KHUh?=
BB30-HNC NWP1eVlYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmDsTWM2OD1yLkKyOVkyKM7:TR?= MW\TRW5IWkWU
ST486 NVzuZWZxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2H4WGlEPTB;MD6yN|A5PyEQvF2= M3TJRXNCVkeURWK=
MOLT-4 MljoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXnJR|UxRTBwMkOzN|ch|ryP MnnmV2FPT1KHUh?=
EW-16 NE\CSZpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2nvVGlEPTB;MD6yN|c3QCEQvF2= NVH1c4FUW0GQR2LFVi=>
KS-1 NIC4V|hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVnJR5h1UUN3ME2wMlI{Pzh3IN88US=> MontV2FPT1KHUh?=
SR MnnGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NELYZ3lKSzVyPUCuNlQ2PjRizszN NGHkempUSU6JUlXS
KM12 MlG4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGjiSW9KSzVyPUCuNlY{PiEQvF2= M3H0W3NCVkeURWK=
EM-2 NIqxWItIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHH3WXRKSzVyPUCuNlY3PDFizszN M3;ubnNCVkeURWK=
MEG-01 NUL6NXJTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2\Mb2lEPTB;MD6yO|g1QSEQvF2= M1nyenNCVkeURWK=
NB13 NVvSVm5RT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkLBTWM2OD1yLkK3PVg1KM7:TR?= NETXdYFUSU6JUlXS
RKO MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoLpTWM2OD1yLkOwPFE{KM7:TR?= MojzV2FPT1KHUh?=
CESS NYC1VlFMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlXvTWM2OD1yLkOxN|I5KM7:TR?= M1jJdnNCVkeURWK=
EoL-1-cell M{\uemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUXJR|UxRTBwM{O0OVkh|ryP NVj4flNYW0GQR2LFVi=>
DOHH-2 NIjENHdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MU\JR|UxRTBwM{O3PFEh|ryP M37wd3NCVkeURWK=
A388 MoTDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{LWeGlEPTB;MD6zOFA5PiEQvF2= MoPCV2FPT1KHUh?=
LAMA-84 Mn3TS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWfJR|UxRTBwM{WxO|gh|ryP M2nQNXNCVkeURWK=
IMR-5 M{H6N2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVHJR|UxRTBwM{W1OEDPxE1? NEHPfHdUSU6JUlXS
KARPAS-422 M4jyNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3TFS2lEPTB;MD6zO|I4OiEQvF2= MnSyV2FPT1KHUh?=
MRK-nu-1 MlrPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmryTWM2OD1yLkO4NVMh|ryP NEfiU4NUSU6JUlXS
BL-70 M{\QfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnjITWM2OD1yLkO4PVc1KM7:TR?= NX\4fZM3W0GQR2LFVi=>
LXF-289 M3KwOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYeyNXI4UUN3ME2wMlQxPDB4IN88US=> M4PvSXNCVkeURWK=
RL95-2 NYjnVYl3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIS5[WlKSzVyPUCuOFA2PjdizszN MWPTRW5IWkWU
QIMR-WIL MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIPSeYdKSzVyPUCuOFI3PzZizszN NF\Be21USU6JUlXS
K-562 NXfrOHkyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXfJR|UxRTBwNEO0O|Ih|ryP NVnSUmdCW0GQR2LFVi=>
NCI-H510A NUnJXZFoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHjCRmZKSzVyPUCuOFM5OjNizszN M125cHNCVkeURWK=
NCI-H524 M3T6TGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnzCTWM2OD1yLkWxNVQ4KM7:TR?= NHTnPZJUSU6JUlXS
KE-37 M2jkd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoHsTWM2OD1yLkWyNVAzKM7:TR?= M2rrbHNCVkeURWK=
KP-N-YS M2Pud2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWXJR|UxRTBwNUSzPVIh|ryP NY[yNZBKW0GQR2LFVi=>
LS-411N MnTBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NITRbYFKSzVyPUCuOVc4PTJizszN MUnTRW5IWkWU
CTV-1 NGflXWNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWi5bI17UUN3ME2wMlU5Pzd|IN88US=> M2jmRnNCVkeURWK=
NCI-SNU-16 M1PmfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVvBVWtXUUN3ME2wMlY{PTdzIN88US=> MnTmV2FPT1KHUh?=
HT-144 MljUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoO3TWM2OD1yLk[zO|k5KM7:TR?= MnW5V2FPT1KHUh?=
NCI-H187 NWHSO|I5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmXITWM2OD1yLk[0NVMh|ryP MXnTRW5IWkWU
OCI-AML2 MlfsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX6wfIpWUUN3ME2wMlY1PDB|IN88US=> M{Pn[HNCVkeURWK=
CCRF-CEM MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYPlTllZUUN3ME2wMlY2OzR4IN88US=> MlTQV2FPT1KHUh?=
ONS-76 NGjYUmVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{XBfGlEPTB;MD62OlQ2QCEQvF2= NGPmOHpUSU6JUlXS
IST-SL2 NHrxOlhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MonxTWM2OD1yLkexPVgzKM7:TR?= NIfQdXlUSU6JUlXS
NB6 MnzZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXy1ZVlEUUN3ME2wMlc4OjV2IN88US=> M2m2SHNCVkeURWK=
SK-PN-DW MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M334WWlEPTB;MD63PVE1KM7:TR?= NIj4e|VUSU6JUlXS
HCC1599 NIToPIxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3XKemlEPTB;MD64NFg4PCEQvF2= NGPKXWxUSU6JUlXS
MC116 M2fS[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MonmTWM2OD1yLki1NFEyKM7:TR?= NH3QTldUSU6JUlXS
TE-15 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1H5VGlEPTB;MD64OVA6QCEQvF2= MXLTRW5IWkWU
HOP-62 NVnwS|Y2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkiwTWM2OD1yLki2N|I6KM7:TR?= NVv5NFY{W0GQR2LFVi=>
TGBC24TKB Mn;qS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mnf5TWM2OD1yLki2N|g2KM7:TR?= NVnMW4k4W0GQR2LFVi=>
HCE-4 NGHKZVNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2PzS2lEPTB;MD64PFA3OyEQvF2= NVToNIhUW0GQR2LFVi=>
ALL-PO NYCzXW03T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYfJR|UxRTBwOEixO|Uh|ryP M{jNOHNCVkeURWK=
KGN M2C0fGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4LvemlEPTB;MD64PVk6PSEQvF2= NHHiZ4hUSU6JUlXS
ML-2 M{XhTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnrFTWM2OD1yLkmwNlU6KM7:TR?= M4\wfHNCVkeURWK=
ES4 M4nZNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVPJR|UxRTBwOUGxNlgh|ryP M2LxOXNCVkeURWK=
SF126 NUjETpduT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEjNbYhKSzVyPUCuPVQ5OTlizszN NX;YOI9DW0GQR2LFVi=>
SK-N-DZ NFTyWIhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFXwW4dKSzVyPUCuPVYyQDlizszN MnjnV2FPT1KHUh?=
HCC1187 NEjZfplIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NG\FT41KSzVyPUGuNFA2ODVizszN Mly5V2FPT1KHUh?=
DU-4475 NFryWYtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHjHW|BKSzVyPUGuNFE4PTZizszN NE\DUVdUSU6JUlXS
NKM-1 NEHNbo1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXzJR|UxRTFwMEK3O|Uh|ryP NHLSbplUSU6JUlXS
HL-60 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWq1RmlHUUN3ME2xMlA3PTd2IN88US=> NUnLdJl4W0GQR2LFVi=>
SBC-1 M1racmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVPwb2gzUUN3ME2xMlEzPTR{IN88US=> NUHVbXpwW0GQR2LFVi=>
TE-10 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4DzWWlEPTB;MT6xNlk1PiEQvF2= NGmxOINUSU6JUlXS
ETK-1 MlfyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1rUTGlEPTB;MT6xN|YyOyEQvF2= NX\tT4hvW0GQR2LFVi=>
HAL-01 Mn61S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MULJR|UxRTFwMU[3NFkh|ryP MnnmV2FPT1KHUh?=
BB65-RCC MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXrDVpUxUUN3ME2xMlE5ODB3IN88US=> M{fsV3NCVkeURWK=
EW-1 M1XU[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVzJR|UxRTFwMUi1OlIh|ryP NYLDdFM6W0GQR2LFVi=>
SK-NEP-1 M{HqcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVrrbIRNUUN3ME2xMlIyOTFzIN88US=> NGLSOoxUSU6JUlXS
SK-LMS-1 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlrpTWM2OD1zLkKyNlEzKM7:TR?= M3LydXNCVkeURWK=
DEL MnXoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MojYTWM2OD1zLkK1OlQ{KM7:TR?= MnizV2FPT1KHUh?=
GT3TKB NI\GfIRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYHJR|UxRTFwMkiwOVch|ryP MlfqV2FPT1KHUh?=
MOLT-16 NH\vRmFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVLIcJN7UUN3ME2xMlM2PDB3IN88US=> MULTRW5IWkWU
CMK NFzWOW1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGe2PVZKSzVyPUGuOFIyOTdizszN NHzv[ZpUSU6JUlXS
NB5 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{H6VWlEPTB;MT62OFIzQSEQvF2= MmftV2FPT1KHUh?=
NCI-H1963 MlrDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlLhTWM2OD1zLkewOVg{KM7:TR?= MXPTRW5IWkWU
KURAMOCHI NWDSU2dwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoKxTWM2OD1zLke4PVEyKM7:TR?= NV3j[2xiW0GQR2LFVi=>
TE-8 NEnCVVNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXLpd4g5UUN3ME2xMlgxOzZ6IN88US=> NVGyOGo2W0GQR2LFVi=>
NCI-H1304 M3e2Rmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1zZSWlEPTB;MT64N|A4OyEQvF2= Mly5V2FPT1KHUh?=
A101D Ml23S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmrUTWM2OD1zLki3N|k2KM7:TR?= MojHV2FPT1KHUh?=
SCLC-21H NF7p[|lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{XaUGlEPTB;MT65O|A2PyEQvF2= MV\TRW5IWkWU
GB-1 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml\HTWM2OD1{LkCxOlQ4KM7:TR?= MXTTRW5IWkWU
KARPAS-45 MmTpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkfrTWM2OD1{LkCyOlU1KM7:TR?= M3nUPXNCVkeURWK=
ATN-1 NVH5bnh1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXT5cXFqUUN3ME2yMlAzQDV6IN88US=> M{TBZ3NCVkeURWK=
NCI-H720 NYDiN4pET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUXyUnVUUUN3ME2yMlA3OjR2IN88US=> MVLTRW5IWkWU
RPMI-6666 MkfJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYLNcIY2UUN3ME2yMlE3OjB5IN88US=> MW\TRW5IWkWU
NB17 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2TLWmlEPTB;Mj6yPVI4KM7:TR?= NVvSNYlHW0GQR2LFVi=>
IST-SL1 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4HMUmlEPTB;Mj6yPVc3PSEQvF2= M1LFVnNCVkeURWK=
SH-4 NVzrUIRzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{nhO2lEPTB;Mj6zNlQ3QSEQvF2= NYTJSFNQW0GQR2LFVi=>
K5 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2fwXWlEPTB;Mj60NFMyQSEQvF2= NXnyN45JW0GQR2LFVi=>
OVCAR-4 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWTtXog1UUN3ME2yMlQ3OTNizszN Mlj4V2FPT1KHUh?=
ACN M1GxUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnvMTWM2OD1{LkWwNlE{KM7:TR?= MWrTRW5IWkWU
TGW NUDLS2h{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoKzTWM2OD1{Lk[1PFMzKM7:TR?= MVTTRW5IWkWU
NCI-H2107 Mln6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGC4OFFKSzVyPUKuPFM4OTFizszN MXjTRW5IWkWU
NCI-H82 NFrXRpRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4nBdGlEPTB;Mj64N|g{QCEQvF2= NGPFVVNUSU6JUlXS
SK-N-FI NWfPSXpoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{mzbmlEPTB;Mj64Olg3QCEQvF2= MUPTRW5IWkWU
LB1047-RCC NWHSUW9{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmXvTWM2OD1{Lki4NVI3KM7:TR?= MnfDV2FPT1KHUh?=
LU-134-A MkHxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVjJR|UxRTJwOEmyOkDPxE1? M4nXdHNCVkeURWK=
NCI-H209 NIr3OIpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXjJR|UxRTJwOUGyOVMh|ryP MWXTRW5IWkWU
NOMO-1 MlW3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGDQNXRKSzVyPUOuNFIzPzRizszN MYjTRW5IWkWU
RH-1 NUPpNG5nT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4D0UWlEPTB;Mz6xO|I6OSEQvF2= MXrTRW5IWkWU
LOUCY M1jWcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXi0bmpCUUN3ME2zMlE5Pjl|IN88US=> MlPmV2FPT1KHUh?=
TE-9 M{P2S2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlfCTWM2OD1|LkK2O|M3KM7:TR?= MlvWV2FPT1KHUh?=
PF-382 M2rZdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoS5TWM2OD1|LkO1O|c5KM7:TR?= MXXTRW5IWkWU
RPMI-8402 M{LqOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYj1TmtvUUN3ME2zMlU5PjB|IN88US=> M1X0TnNCVkeURWK=
HEL MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mke4TWM2OD1|Lk[zNkDPxE1? MoPYV2FPT1KHUh?=
NOS-1 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXrJR|UxRTNwOES3OVQh|ryP MVXTRW5IWkWU
ES1 NUfOT3lwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFzQ[W1KSzVyPUOuPVIzQTNizszN MXfTRW5IWkWU
NCI-H2171 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXm4dXhJUUN3ME2zMlkzPDJ|IN88US=> MmPFV2FPT1KHUh?=
NCI-H747 M3TldGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYrzNHZrUUN3ME2zMlk1OjJzIN88US=> M1nydnNCVkeURWK=
MHH-NB-11 NWq2cIRQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1;aOGlEPTB;Mz65OVMyOiEQvF2= MmW1V2FPT1KHUh?=
MZ1-PC NHf2eohIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NE\FSZNKSzVyPUOuPVkzPCEQvF2= M4PUcXNCVkeURWK=
MMAC-SF NI\WcXJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmLLTWM2OD12LkCyOFY4KM7:TR?= NWnzZVFyW0GQR2LFVi=>
NMC-G1 NV;l[25ZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYHJR|UxRTRwMkK3NlMh|ryP NHPXPI9USU6JUlXS
SW872 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFLtZ4RKSzVyPUSuN|Q{PCEQvF2= NX;5R3h1W0GQR2LFVi=>
TE-12 NXH0XVlzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4DoRmlEPTB;ND61OlM6PCEQvF2= MVnTRW5IWkWU
LU-139 Mk[xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVHJR|UxRTRwNkG4N|Uh|ryP MVvTRW5IWkWU
HC-1 NX3xe2hQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3W4emlEPTB;ND62PVQ6PCEQvF2= NUfzZ3NkW0GQR2LFVi=>
COR-L279 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX7JR|UxRTRwN{W4PVEh|ryP MW\TRW5IWkWU
SF268 NUP0dYFwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1LrO2lEPTB;ND63PVkyPiEQvF2= MkHCV2FPT1KHUh?=
MC-CAR NW\DT4h7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mlr5TWM2OD13LkC2O|U4KM7:TR?= MnrrV2FPT1KHUh?=
TK10 MnfmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVjJR|UxRTVwM{W0Olkh|ryP M{fGWHNCVkeURWK=
TE-1 NHLMVnhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1zRfmlEPTB;NT60PVAxPCEQvF2= MVXTRW5IWkWU
NCI-H2126 NYPVbGprT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1KzbGlEPTB;NT62OFU4PCEQvF2= MoDRV2FPT1KHUh?=
Daudi MlTJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{[5OmlEPTB;NT62PVEzKM7:TR?= MnXXV2FPT1KHUh?=
NCI-H1648 NXn5OGVLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{P3ZmlEPTB;NT64NVQ2PCEQvF2= MX7TRW5IWkWU
OS-RC-2 NFrIfJJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnnETWM2OD13Lkm4OVk4KM7:TR?= M{jSTXNCVkeURWK=
DJM-1 NGjpbYZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mm\zTWM2OD14LkO0OlY3KM7:TR?= NUWzO|hIW0GQR2LFVi=>
LS-1034 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnjuTWM2OD14Lke1OlYh|ryP NVjURoxmW0GQR2LFVi=>
NCI-H1581 NFHxdJpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYXJR|UxRTZwN{i0NFUh|ryP M4LBXnNCVkeURWK=
UACC-257 NUXqXWFET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkXxTWM2OD15LkC0OVEzKM7:TR?= NITTeYtUSU6JUlXS
KM-H2 NFn6SXhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHXFUG5KSzVyPUeuNVg1PTdizszN MnXEV2FPT1KHUh?=
NCI-H1436 NUXwZ4tuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUfJR|UxRTdwNkm5N|Ih|ryP M13TcHNCVkeURWK=
IA-LM NGrRW2ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWPJR|UxRTdwOEW5JO69VQ>? NGr4NVJUSU6JUlXS
NCI-H526 MmDJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV[5W4YxUUN3ME24MlI2PjN5IN88US=> NVm3[oM4W0GQR2LFVi=>
GCIY NHrJN5BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnP2TWM2OD16LkO2PVY2KM7:TR?= MkDnV2FPT1KHUh?=
CP67-MEL M4DWO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmLLTWM2OD16LkWzNlYh|ryP NH\LVnVUSU6JUlXS
KALS-1 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn;BTWM2OD16LkizPFUyKM7:TR?= NIrp[5NUSU6JUlXS
NCI-H1770 M3TH[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX\SZWlYUUN3ME24MlkxOjZ3IN88US=> NYe1XlU6W0GQR2LFVi=>
8-MG-BA NHXKb3dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3G0bWlEPTB;OT6zNlg1PCEQvF2= NFPZWIdUSU6JUlXS
KY821 NFL0SVFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2XISWlEPTB;OT63O|Q5PCEQvF2= NVixepc6W0GQR2LFVi=>
SNB75 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnrnTWM2OD1zMD6wO|Yh|ryP MnTFV2FPT1KHUh?=
NCCIT NFntVIVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml7uTWM2OD1zMT6wOVgzKM7:TR?= NYnCPZBxW0GQR2LFVi=>
SJSA-1 M4rvXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFXEXpdKSzVyPUGxMlI5QTFizszN NXHyfZFpW0GQR2LFVi=>
LB373-MEL-D NVHRdJR[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXXJR|UxRTFzLkO4Nlch|ryP NWTXR3p2W0GQR2LFVi=>
TALL-1 MlTDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIPl[25KSzVyPUGxMlQxPThizszN Mly0V2FPT1KHUh?=
NB69 M1HEZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkLyTWM2OD1zMT63O|A2KM7:TR?= MYjTRW5IWkWU
NCI-H1355 NHmwV2ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NE\nZZNKSzVyPUGxMlk1OjZizszN MkLYV2FPT1KHUh?=
DMS-153 NEPFSJRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX;CeVBLUUN3ME2xNk4xPDJ4IN88US=> NVPKNlNJW0GQR2LFVi=>
OPM-2 NXOyS|lGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3T3U2lEPTB;MUKuNVU6PiEQvF2= MnTMV2FPT1KHUh?=
NB1 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWPJSmtvUUN3ME2xNk4zQSEQvF2= M1ixTXNCVkeURWK=
A3-KAW Mnv0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3n4TmlEPTB;MUKuN|I{PiEQvF2= NFfidI1USU6JUlXS
NCI-H1882 NITzNZNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXvOV4JHUUN3ME2xNk41ODZ4IN88US=> MmTMV2FPT1KHUh?=
KG-1 NH30Z|ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYjJR|UxRTF{Lk[1OFUh|ryP M3PFcXNCVkeURWK=
LC4-1 NGG5WpJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3;v[WlEPTB;MUKuO|cxPiEQvF2= M{PUS3NCVkeURWK=
HCE-T M{jxPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFXGV5FKSzVyPUGzMlAxPDlizszN MYfTRW5IWkWU
NEC8 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUnnXFBqUUN3ME2xN{4yODN6IN88US=> MXfTRW5IWkWU
IST-MEL1 NH7ETFRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFTJNHdKSzVyPUGzMlU4QDhizszN Ml\XV2FPT1KHUh?=
EW-3 M3PXUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2rQcGlEPTB;MUOuO|QxOiEQvF2= MY\TRW5IWkWU
CTB-1 NGDHNnBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXXJR|UxRTF2LkCzNlkh|ryP MULTRW5IWkWU
LS-123 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnTwTWM2OD1zND6xOVg5KM7:TR?= M3;KXHNCVkeURWK=
NCI-H1417 NHny[IZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYmwUZZSUUN3ME2xOE4{ODV{IN88US=> M1y0RXNCVkeURWK=
MZ7-mel NVjGOYJZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXW0NmhKUUN3ME2xOE41PDN|IN88US=> MYnTRW5IWkWU
JiyoyeP-2003 MnK3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYny[pdjUUN3ME2xOU43OzJ4IN88US=> MlHzV2FPT1KHUh?=
ES6 M2PmcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M124U2lEPTB;MU[uNlM3OSEQvF2= NFXPR5BUSU6JUlXS
HH MlPpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4rUSGlEPTB;MUeuNVk3OyEQvF2= M3LDdXNCVkeURWK=
SF539 NYf4NYpDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUDpRZQ6UUN3ME2xO{46QTJ{IN88US=> MlrHV2FPT1KHUh?=
Calu-6 MoLsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVzue2QzUUN3ME2xPU4zOzlizszN NVTD[nNTW0GQR2LFVi=>
SK-MM-2 NUPwNoxWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoG5TWM2OD1zOT61OVUh|ryP NWSzdGh6W0GQR2LFVi=>
IST-MES1 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3\R[mlEPTB;MUmuOlY3OyEQvF2= NGrK[ZpUSU6JUlXS
GI-ME-N M{fkRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3[wR2lEPTB;MUmuPFIzPyEQvF2= NVPpd2t6W0GQR2LFVi=>
CAL-148 NHXFV4NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoPUTWM2OD1{MD65PVM1KM7:TR?= Mn6xV2FPT1KHUh?=
EVSA-T MoHaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2n2OWlEPTB;MkGuNVQ6QSEQvF2= NFTh[4ZUSU6JUlXS
LP-1 NIf5eGFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoHvTWM2OD1{MT6zOFMzKM7:TR?= MWfTRW5IWkWU
BOKU NYj5NnRsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1LTW2lEPTB;MkGuOFU{OyEQvF2= MUjTRW5IWkWU
KLE MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXz6XVZsUUN3ME2yNk4yQTB|IN88US=> MnvJV2FPT1KHUh?=
LB831-BLC M{HPRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4DhXmlEPTB;MkWuNVUzPiEQvF2= M{LlPXNCVkeURWK=
NCI-H889 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHnVR3RKSzVyPUK1MlE6OzFizszN MWjTRW5IWkWU
REH M3LIV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1fIZ2lEPTB;MkWuOFY4OSEQvF2= M2PBN3NCVkeURWK=
KP-N-RT-BM-1 NHzlbpVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF34NlVKSzVyPUK1MlQ4PTJizszN NXjqOXRuW0GQR2LFVi=>
MPP-89 NEOwZlVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUPJR|UxRTJ3LkWzNVQh|ryP NHS2NJdUSU6JUlXS
no-11 NEPzUpJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVjJR|UxRTJ3Lke0O{DPxE1? MY\TRW5IWkWU
NCI-H748 NHnheodIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGTQbZBKSzVyPUK1Mlc3OjdizszN MWXTRW5IWkWU
LB2518-MEL NHvoVWtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3OwT2lEPTB;MkeuNVc4OyEQvF2= NX7Hb|N3W0GQR2LFVi=>
TGBC1TKB MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{LwemlEPTB;MkeuOVU5PSEQvF2= MnOxV2FPT1KHUh?=
MHH-PREB-1 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVvYTpN6UUN3ME2yPE4xPzN2IN88US=> NFfuNJNUSU6JUlXS
MZ2-MEL NH;xO3BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIrZcHRKSzVyPUK4MlYyPDNizszN Ml71V2FPT1KHUh?=
U-266 MoLBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWHEdIxrUUN3ME2yPE43OzZ4IN88US=> M4XFVnNCVkeURWK=
SNU-C1 NFrNOnVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWHJR|UxRTJ6Lkm0N{DPxE1? Mn23V2FPT1KHUh?=
SW962 MorQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVOxZ3ZGUUN3ME2zNE4zPzR5IN88US=> MULTRW5IWkWU
Raji NGL5dmJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGfGUYxKSzVyPUOwMlU2QTJizszN MYrTRW5IWkWU
KNS-42 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmixTWM2OD1|MD64PVU3KM7:TR?= M4PR[3NCVkeURWK=
LB996-RCC Ml3GS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmfHTWM2OD1|MT6xO|AzKM7:TR?= M3nlXHNCVkeURWK=
CHP-126 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnXhTWM2OD1|MT6xPVg1KM7:TR?= NXPJbmZpW0GQR2LFVi=>
RXF393 NHryS4tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVzJR|UxRTN{LkS5O{DPxE1? MlfIV2FPT1KHUh?=
COLO-684 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mom2TWM2OD1|Mj62OFM5KM7:TR?= M{XkSHNCVkeURWK=
A704 Mn:4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVPJR|UxRTN|LkW1N|gh|ryP Ml70V2FPT1KHUh?=
A253 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH[0d4RKSzVyPUOzMlU5PTJizszN M1jiWXNCVkeURWK=
KNS-81-FD M4niWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MY\JR|UxRTN2LkW0OVYh|ryP MoDJV2FPT1KHUh?=
TE-441-T MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFHNOm5KSzVyPUO0MlY{PzFizszN NGHHdHNUSU6JUlXS
HCC2157 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3m0TGlEPTB;M{WuOFYyQSEQvF2= MliwV2FPT1KHUh?=
ES3 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4DmSWlEPTB;M{[uOlc2KM7:TR?= M1PLbnNCVkeURWK=
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JAR M3S5cmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3L3SWlEPTB;M{iuNlQ1QSEQvF2= NUHrcYhoW0GQR2LFVi=>
GDM-1 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYSxRlhQUUN3ME2zPE46OTF4IN88US=> MV3TRW5IWkWU
KU812 MlLrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnPmTWM2OD12MT61NFch|ryP MWDTRW5IWkWU
BC-1 M2GyNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEnwWVdKSzVyPUSyMlY4OzFizszN Ml:3V2FPT1KHUh?=
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DG-75 NHnIcY5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIHBcpdKSzVyPUS1MlE2PzdizszN NYn6cWJ4W0GQR2LFVi=>
COR-L88 MoHkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH65Z5RKSzVyPUS1MlI4PzhizszN MVjTRW5IWkWU
LS-513 NXXFXHRIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGfzVm5KSzVyPUS1MlkyPTZizszN MmOzV2FPT1KHUh?=
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L-363 NFLTVmhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGrTVIRKSzVyPUS2Mlg5OSEQvF2= NUnRWmVuW0GQR2LFVi=>
TE-6 NF7mRXJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoL2TWM2OD12OD60OFYh|ryP MVPTRW5IWkWU
NCI-H345 NHfDO4ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFHPbIlKSzVyPUS4MlQ3QCEQvF2= NXXnRWcyW0GQR2LFVi=>
TE-5 MoG5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV3JR|UxRTR7LkexNVgh|ryP MofmV2FPT1KHUh?=

... 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

Molarity Calculator

Molarity Calculator

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

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

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

Dilution Calculator

Dilution Calculator

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

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

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

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Molecular Weight Calculator

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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
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
NCT00111683 Completed Chronic Myelogenous Leukemia in Blast Crisis|Lymphocytic Leukemia B Cell Acute|Myelodysplastic Syndromes|Myelogenous Leukemia Chronic Merck Sharp & Dohme Corp. June 2005 Phase 1
NCT02532868 Terminated Cancer Merck Sharp & Dohme Corp. May 2005 Phase 1
NCT00099346 Terminated Colorectal Cancer|Advanced Solid Tumors Merck Sharp & Dohme Corp. January 2005 Phase 1

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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Aurora Kinase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID