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.

     

    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.

  • 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.

  • 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 NUPoNIhrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2T1SmlEPTB;MD6wNFM{QCEQvF2= Mn3TV2FPT1KHUh?=
RS4-11 NFmxbHVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnPkTWM2OD1yLkCwOFA1KM7:TR?= NXT2SXc6W0GQR2LFVi=>
MFH-ino NUX6SZNpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX;JR|UxRTBwMEC5PUDPxE1? M3\3enNCVkeURWK=
NTERA-S-cl-D1 NI[zN4tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWTWeVdwUUN3ME2wMlAyPDN2IN88US=> M4HWbHNCVkeURWK=
697 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NI[3S5lKSzVyPUCuNFI1PzFizszN M4Oye3NCVkeURWK=
NALM-6 Mny3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH3zbGxKSzVyPUCuNFI2PTJizszN MWnTRW5IWkWU
ES8 MljDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHvSOphKSzVyPUCuNFQ3OTNizszN MoXyV2FPT1KHUh?=
HUTU-80 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{n2S2lEPTB;MD6wOVI6QSEQvF2= NYK3eJpkW0GQR2LFVi=>
MV-4-11 NHH5eXhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlTvTWM2OD1yLkC3O|gzKM7:TR?= NXHTenpUW0GQR2LFVi=>
MONO-MAC-6 Mlr4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmHFTWM2OD1yLkC3PFc6KM7:TR?= NIjRO|dUSU6JUlXS
LC-2-ad NYDnfFFZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUHZfZhrUUN3ME2wMlA5Pzh7IN88US=> NEK3O|dUSU6JUlXS
BL-41 M2fSbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUexV3VFUUN3ME2wMlExPDR3IN88US=> MVjTRW5IWkWU
A4-Fuk M37LTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoS4TWM2OD1yLkGxOVY{KM7:TR?= MYrTRW5IWkWU
SW954 NHH3[HpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYe5OohjUUN3ME2wMlEzOjJ7IN88US=> MUHTRW5IWkWU
BV-173 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHfDSYhKSzVyPUCuNVI3PDFizszN NFPFWGtUSU6JUlXS
TE-11 M{[3TWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXzJR|UxRTBwMUS5PFIh|ryP MofiV2FPT1KHUh?=
SK-UT-1 Mn\aS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYXJR|UxRTBwMUW5OlUh|ryP NXWxPWpIW0GQR2LFVi=>
SIG-M5 M{nF[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUj2UW1[UUN3ME2wMlE3PzB5IN88US=> NF:wNJBUSU6JUlXS
OCUB-M NGfYSVRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlHHTWM2OD1yLkG2PVg{KM7:TR?= M3P3V3NCVkeURWK=
K052 NHLTOZpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWfFRoppUUN3ME2wMlE6PDhizszN MlnQV2FPT1KHUh?=
VA-ES-BJ MlLoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVXJR|UxRTBwMkCwPFYh|ryP MWfTRW5IWkWU
SW982 NXzmN4V5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlXITWM2OD1yLkKxN|gh|ryP NV7qc5pHW0GQR2LFVi=>
LB647-SCLC NX3DeGx{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3jkSWlEPTB;MD6yNVUzOyEQvF2= M{HKS3NCVkeURWK=
PSN1 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlfaTWM2OD1yLkKyNFI3KM7:TR?= M3W1cXNCVkeURWK=
BB30-HNC NUXuRVlVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWfHe5VyUUN3ME2wMlIzPTlzIN88US=> MWPTRW5IWkWU
ST486 NVPse3ZST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH3RZWJKSzVyPUCuNlMxQDdizszN MUXTRW5IWkWU
MOLT-4 MnT3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHrkcpRKSzVyPUCuNlM{OzdizszN M1XxVXNCVkeURWK=
EW-16 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWToWo06UUN3ME2wMlI{PzZ6IN88US=> MYDTRW5IWkWU
KS-1 MnjjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmTNTWM2OD1yLkKzO|g2KM7:TR?= NXnvVm1lW0GQR2LFVi=>
SR MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoHOTWM2OD1yLkK0OVY1KM7:TR?= NXnvNlZEW0GQR2LFVi=>
KM12 NEixc2pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mk\HTWM2OD1yLkK2N|Yh|ryP MmLuV2FPT1KHUh?=
EM-2 M3SzeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFW2VI9KSzVyPUCuNlY3PDFizszN MXTTRW5IWkWU
MEG-01 MoHqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGjIXnVKSzVyPUCuNlc5PDlizszN MVnTRW5IWkWU
NB13 NFW4e21Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXHnPZQ2UUN3ME2wMlI4QTh2IN88US=> NIfKPJVUSU6JUlXS
RKO NFfK[GJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUnJR|UxRTBwM{C4NVMh|ryP MWXTRW5IWkWU
CESS NFzSTpdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3WyVmlEPTB;MD6zNVMzQCEQvF2= MYjTRW5IWkWU
EoL-1-cell M2\2Tmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkHRTWM2OD1yLkOzOFU6KM7:TR?= M33obXNCVkeURWK=
DOHH-2 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mlz4TWM2OD1yLkOzO|gyKM7:TR?= M3rMdHNCVkeURWK=
A388 MonsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH[5VGxKSzVyPUCuN|QxQDZizszN MXXTRW5IWkWU
LAMA-84 NWPrcJp3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NU[2RWdxUUN3ME2wMlM2OTd6IN88US=> MlvxV2FPT1KHUh?=
IMR-5 NFXWPJlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1nIS2lEPTB;MD6zOVU1KM7:TR?= MUjTRW5IWkWU
KARPAS-422 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGq4U|JKSzVyPUCuN|czPzJizszN MVLTRW5IWkWU
MRK-nu-1 NU\sWlU1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmDOTWM2OD1yLkO4NVMh|ryP MkPiV2FPT1KHUh?=
BL-70 M2f4fWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX7HWmprUUN3ME2wMlM5QTd2IN88US=> NIXGNHdUSU6JUlXS
LXF-289 NGT5SoRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGHDZoxKSzVyPUCuOFA1ODZizszN MmTBV2FPT1KHUh?=
RL95-2 NYDuPVM1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXnncnVHUUN3ME2wMlQxPTZ5IN88US=> NX\OO5M3W0GQR2LFVi=>
QIMR-WIL MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUWwZnhKUUN3ME2wMlQzPjd4IN88US=> NI\EWGZUSU6JUlXS
K-562 NGHwVWtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MW\JR|UxRTBwNEO0O|Ih|ryP NXTvcGlMW0GQR2LFVi=>
NCI-H510A NYjMWVdVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2XkcWlEPTB;MD60N|gzOyEQvF2= MVzTRW5IWkWU
NCI-H524 NXTvSmRmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3e5[GlEPTB;MD61NVE1PyEQvF2= M{L4T3NCVkeURWK=
KE-37 M3u2NWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVnJR|UxRTBwNUKxNFIh|ryP NXPyXYZmW0GQR2LFVi=>
KP-N-YS MoDES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlzXTWM2OD1yLkW0N|kzKM7:TR?= MUPTRW5IWkWU
LS-411N NWm3bok6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlLGTWM2OD1yLkW3O|UzKM7:TR?= MUjTRW5IWkWU
CTV-1 NHfRUXNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoTTTWM2OD1yLkW4O|c{KM7:TR?= MnqxV2FPT1KHUh?=
NCI-SNU-16 MnfPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUXJR|UxRTBwNkO1O|Eh|ryP MYDTRW5IWkWU
HT-144 MoTaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWPJR|UxRTBwNkO3PVgh|ryP M1fKTHNCVkeURWK=
NCI-H187 M4LmPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXnJR|UxRTBwNkSxN{DPxE1? MUjTRW5IWkWU
OCI-AML2 NGXqXVhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVnZ[Gh2UUN3ME2wMlY1PDB|IN88US=> NYXVXnBGW0GQR2LFVi=>
CCRF-CEM M3qxfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2HFU2lEPTB;MD62OVM1PiEQvF2= NVPqR4ZQW0GQR2LFVi=>
ONS-76 NXTOVFdtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVPJR|UxRTBwNk[0OVgh|ryP M17qOHNCVkeURWK=
IST-SL2 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFq3SY5KSzVyPUCuO|E6QDJizszN MoTuV2FPT1KHUh?=
NB6 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4XBeWlEPTB;MD63O|I2PCEQvF2= NYD3fVUyW0GQR2LFVi=>
SK-PN-DW NULJT4dCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2\LfGlEPTB;MD63PVE1KM7:TR?= MWrTRW5IWkWU
HCC1599 MoL4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2rXcmlEPTB;MD64NFg4PCEQvF2= MnKzV2FPT1KHUh?=
MC116 NWDTWVRYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEe2XmJKSzVyPUCuPFUxOTFizszN NHzSXWhUSU6JUlXS
TE-15 NIfXO4NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWrrbm5UUUN3ME2wMlg2ODl6IN88US=> NIWwSpVUSU6JUlXS
HOP-62 Mo\6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWPJR|UxRTBwOE[zNlkh|ryP NUGxTI85W0GQR2LFVi=>
TGBC24TKB NWrt[Wd2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEDmZXBKSzVyPUCuPFY{QDVizszN NGmy[ZBUSU6JUlXS
HCE-4 NFPsT2VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH7QS5BKSzVyPUCuPFgxPjNizszN MoXHV2FPT1KHUh?=
ALL-PO MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYnJR|UxRTBwOEixO|Uh|ryP M1TQOnNCVkeURWK=
KGN NYDw[XNST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEfNcYtKSzVyPUCuPFk6QTVizszN MX\TRW5IWkWU
ML-2 NX7qWVRtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXXJR|UxRTBwOUCyOVkh|ryP M3PFSHNCVkeURWK=
ES4 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlKyTWM2OD1yLkmxNVI5KM7:TR?= M{XaVXNCVkeURWK=
SF126 M1\DVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MknyTWM2OD1yLkm0PFE6KM7:TR?= Mn\3V2FPT1KHUh?=
SK-N-DZ NVXFemVXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXzQ[Ic2UUN3ME2wMlk3OTh7IN88US=> MYHTRW5IWkWU
HCC1187 M3:1NWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGLJ[VlKSzVyPUGuNFA2ODVizszN NGXUNJlUSU6JUlXS
DU-4475 NHXLZVFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmXCTWM2OD1zLkCxO|U3KM7:TR?= MV;TRW5IWkWU
NKM-1 NFvwPVNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmTqTWM2OD1zLkCyO|c2KM7:TR?= MYTTRW5IWkWU
HL-60 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NU\6VmhWUUN3ME2xMlA3PTd2IN88US=> NX\K[G9GW0GQR2LFVi=>
SBC-1 NF\ZcWZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mmi1TWM2OD1zLkGyOVQzKM7:TR?= NG\w[nJUSU6JUlXS
TE-10 MlL0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUPJR|UxRTFwMUK5OFYh|ryP NF;KTY5USU6JUlXS
ETK-1 Ml3YS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1zm[2lEPTB;MT6xN|YyOyEQvF2= MUjTRW5IWkWU
HAL-01 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn;oTWM2OD1zLkG2O|A6KM7:TR?= NGLzSWtUSU6JUlXS
BB65-RCC MoHhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnyzTWM2OD1zLkG4NFA2KM7:TR?= M4LVNHNCVkeURWK=
EW-1 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkThTWM2OD1zLkG4OVYzKM7:TR?= M{\UV3NCVkeURWK=
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SK-LMS-1 MkmwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1GxXmlEPTB;MT6yNlIyOiEQvF2= M{jxdXNCVkeURWK=
DEL NUWyOI9lT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXvJR|UxRTFwMkW2OFMh|ryP MVfTRW5IWkWU
GT3TKB MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{Dlb2lEPTB;MT6yPFA2PyEQvF2= NGrHVG9USU6JUlXS
MOLT-16 M4TyXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVTJR|UxRTFwM{W0NFUh|ryP NW\5VZIyW0GQR2LFVi=>
CMK Mn;pS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmnOTWM2OD1zLkSyNVE4KM7:TR?= NV;QdFY1W0GQR2LFVi=>
NB5 M4nYZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnXYTWM2OD1zLk[0NlI6KM7:TR?= NIniV2ZUSU6JUlXS
NCI-H1963 M1e2N2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUe5NI1tUUN3ME2xMlcxPTh|IN88US=> M1\rT3NCVkeURWK=
KURAMOCHI M2H1Nmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYLJR|UxRTFwN{i5NVEh|ryP Ml7OV2FPT1KHUh?=
TE-8 NVfx[WxTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFP6VFZKSzVyPUGuPFA{PjhizszN MmLoV2FPT1KHUh?=
NCI-H1304 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnvhTWM2OD1zLkizNFc{KM7:TR?= MWjTRW5IWkWU
A101D NHzkdFZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlPGTWM2OD1zLki3N|k2KM7:TR?= M{D0fnNCVkeURWK=
SCLC-21H NFroUFZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnznTWM2OD1zLkm3NFU4KM7:TR?= M1:5[nNCVkeURWK=
GB-1 NUXsfml7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{DxWWlEPTB;Mj6wNVY1PyEQvF2= MVjTRW5IWkWU
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ATN-1 NIrJboRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXrJR|UxRTJwMEK4OVgh|ryP NHu2flhUSU6JUlXS
NCI-H720 M13sU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIfBWGlKSzVyPUKuNFYzPDRizszN MXPTRW5IWkWU
RPMI-6666 NYL2SI9DT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXvJR|UxRTJwMU[yNFch|ryP NULEPJFnW0GQR2LFVi=>
NB17 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3fHVmlEPTB;Mj6yPVI4KM7:TR?= MWfTRW5IWkWU
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OVCAR-4 NH\ze3ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHy1[IpKSzVyPUKuOFYyOyEQvF2= NHnnW4JUSU6JUlXS
ACN M4jpZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUTJR|UxRTJwNUCyNVMh|ryP M{fBcXNCVkeURWK=
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NCI-H2107 NW\wNY02T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUPJR|UxRTJwOEO3NVEh|ryP NGPBTGlUSU6JUlXS
NCI-H82 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MknZTWM2OD1{LkizPFM5KM7:TR?= NHjORW5USU6JUlXS
SK-N-FI MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVLJRodHUUN3ME2yMlg3QDZ6IN88US=> NYXOcW84W0GQR2LFVi=>
LB1047-RCC Mnr6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVy4ZnpmUUN3ME2yMlg5OTJ4IN88US=> MVzTRW5IWkWU
LU-134-A M{jSeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIHBeFBKSzVyPUKuPFkzPiEQvF2= MlLoV2FPT1KHUh?=
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NOMO-1 NVvs[HhFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3nScGlEPTB;Mz6wNlI4PCEQvF2= NGPBZVdUSU6JUlXS
RH-1 MnL1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYDUNVJxUUN3ME2zMlE4OjlzIN88US=> NVXsRlFRW0GQR2LFVi=>
LOUCY Ml76S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHK0fJlKSzVyPUOuNVg3QTNizszN NVXvZ3pMW0GQR2LFVi=>
TE-9 MonNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGfjXXlKSzVyPUOuNlY4OzZizszN NHLQSlVUSU6JUlXS
PF-382 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1PFXWlEPTB;Mz6zOVc4QCEQvF2= NUn0eJhZW0GQR2LFVi=>
RPMI-8402 MlTNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWrYW3ZmUUN3ME2zMlU5PjB|IN88US=> MljiV2FPT1KHUh?=
HEL NVn3PFNbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFLNWmtKSzVyPUOuOlMzKM7:TR?= MX;TRW5IWkWU
NOS-1 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHrqboFKSzVyPUOuPFQ4PTRizszN MWjTRW5IWkWU
ES1 M{m2Vmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWPJR|UxRTNwOUKyPVMh|ryP NV7OXHUyW0GQR2LFVi=>
NCI-H2171 M3XtSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV3JR|UxRTNwOUK0NlMh|ryP NVH5VGNzW0GQR2LFVi=>
NCI-H747 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWHRSFJkUUN3ME2zMlk1OjJzIN88US=> NFz4S25USU6JUlXS
MHH-NB-11 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4nST2lEPTB;Mz65OVMyOiEQvF2= M3P2R3NCVkeURWK=
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MMAC-SF NUXtUYFbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUD3OFNNUUN3ME20MlAzPDZ5IN88US=> NYXWSFIzW0GQR2LFVi=>
NMC-G1 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXv4R|ZCUUN3ME20MlIzPzJ|IN88US=> M3\ObXNCVkeURWK=
SW872 NFfIN|hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkTGTWM2OD12LkO0N|Qh|ryP MofKV2FPT1KHUh?=
TE-12 MkjlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUXJR|UxRTRwNU[zPVQh|ryP NFvpeZhUSU6JUlXS
LU-139 NXzGU2dZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NW\6U5NRUUN3ME20MlYyQDN3IN88US=> M1vDXHNCVkeURWK=
HC-1 M4TufGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4fyNmlEPTB;ND62PVQ6PCEQvF2= NFH5VYFUSU6JUlXS
COR-L279 M3v1NWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3Xi[GlEPTB;ND63OVg6OSEQvF2= MX;TRW5IWkWU
SF268 Mn3sS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkKxTWM2OD12Lke5PVE3KM7:TR?= MUDTRW5IWkWU
MC-CAR M17rSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUPJR|UxRTVwME[3OVch|ryP M3\iOnNCVkeURWK=
TK10 NFT5VFZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NES2bpNKSzVyPUWuN|U1PjlizszN MVzTRW5IWkWU
TE-1 NYXmfZJ[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2fzOmlEPTB;NT60PVAxPCEQvF2= NGT3fHpUSU6JUlXS
NCI-H2126 MmKxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIDuR3VKSzVyPUWuOlQ2PzRizszN NXvRXG5kW0GQR2LFVi=>
Daudi MmjnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NW\oWXFjUUN3ME21MlY6OTJizszN MUjTRW5IWkWU
NCI-H1648 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4nkV2lEPTB;NT64NVQ2PCEQvF2= Mny3V2FPT1KHUh?=
OS-RC-2 MkXxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVvPTpFlUUN3ME21Mlk5PTl5IN88US=> M1PFUXNCVkeURWK=
DJM-1 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnjJTWM2OD14LkO0OlY3KM7:TR?= NVT5NFVoW0GQR2LFVi=>
LS-1034 M2eyd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1L4NmlEPTB;Nj63OVY3KM7:TR?= MojpV2FPT1KHUh?=
NCI-H1581 M{Kx[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUDJR|UxRTZwN{i0NFUh|ryP MkXuV2FPT1KHUh?=
UACC-257 NIHPXpBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MljXTWM2OD15LkC0OVEzKM7:TR?= M1XZXHNCVkeURWK=
KM-H2 NF3WUHJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX:2XHp3UUN3ME23MlE5PDV5IN88US=> MULTRW5IWkWU
NCI-H1436 NEfzRppIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXTXcZVRUUN3ME23MlY6QTN{IN88US=> NIjBNXFUSU6JUlXS
IA-LM MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NY\TfVBNUUN3ME23Mlg2QSEQvF2= MVLTRW5IWkWU
NCI-H526 NGfoZ5RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWO3XmZFUUN3ME24MlI2PjN5IN88US=> M2TYd3NCVkeURWK=
GCIY M1riTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3PBSmlEPTB;OD6zOlk3PSEQvF2= MkjRV2FPT1KHUh?=
CP67-MEL NXLaRYhkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVzJR|UxRThwNUOyOkDPxE1? M17DWnNCVkeURWK=
KALS-1 NEW2UllIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkjyTWM2OD16LkizPFUyKM7:TR?= M4\JSHNCVkeURWK=
NCI-H1770 NEjrdJdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGrqNWtKSzVyPUiuPVAzPjVizszN MnXLV2FPT1KHUh?=
8-MG-BA NIHUbnNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX\JR|UxRTlwM{K4OFQh|ryP MkDxV2FPT1KHUh?=
KY821 NIPjcoxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mnf3TWM2OD17Lke3OFg1KM7:TR?= MX;TRW5IWkWU
SNB75 NWruUIdzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3fEPWlEPTB;MUCuNFc3KM7:TR?= NXPrc5hGW0GQR2LFVi=>
NCCIT MoX4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX:wOXZlUUN3ME2xNU4xPTh{IN88US=> M4fHNHNCVkeURWK=
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LB373-MEL-D NYe5RVRbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkTVTWM2OD1zMT6zPFI4KM7:TR?= MYnTRW5IWkWU
TALL-1 NFnaXnNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4nFTmlEPTB;MUGuOFA2QCEQvF2= MVTTRW5IWkWU
NB69 MmX1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEGyOI1KSzVyPUGxMlc4ODVizszN MUfTRW5IWkWU
NCI-H1355 NXTFXFFvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVTJR|UxRTFzLkm0NlYh|ryP MXrTRW5IWkWU
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OPM-2 MlXDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NITHbo5KSzVyPUGyMlE2QTZizszN MmTqV2FPT1KHUh?=
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A3-KAW Mlz3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX62fFhWUUN3ME2xNk4{OjN4IN88US=> MlXlV2FPT1KHUh?=
NCI-H1882 M1LuWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{G3[mlEPTB;MUKuOFA3PiEQvF2= M{LsTnNCVkeURWK=
KG-1 MlLHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWLJR|UxRTF{Lk[1OFUh|ryP NYTiclh4W0GQR2LFVi=>
LC4-1 NF7ZZ4JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYnJR|UxRTF{Lke3NFYh|ryP MYrTRW5IWkWU
HCE-T NY\PbmtUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXr0T5JwUUN3ME2xN{4xODR7IN88US=> MWDTRW5IWkWU
NEC8 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3vobGlEPTB;MUOuNVA{QCEQvF2= MWHTRW5IWkWU
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EW-3 MoL5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX;5clFVUUN3ME2xN{44PDB{IN88US=> M2PmS3NCVkeURWK=
CTB-1 NI\V[YZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3rLbWlEPTB;MUSuNFMzQSEQvF2= NH;BUYJUSU6JUlXS
LS-123 M{L2dmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUTkdHBUUUN3ME2xOE4yPTh6IN88US=> MV7TRW5IWkWU
NCI-H1417 NU\Jdmc5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M363TWlEPTB;MUSuN|A2OiEQvF2= NH[xOWRUSU6JUlXS
MZ7-mel M2XBNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWPmXYF5UUN3ME2xOE41PDN|IN88US=> NF23fY9USU6JUlXS
JiyoyeP-2003 M1vXcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVjJR|UxRTF3Lk[zNlYh|ryP MVHTRW5IWkWU
ES6 NEe2dmlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHHYN5dKSzVyPUG2MlI{PjFizszN NGnMW5FUSU6JUlXS
HH Ml;iS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mk\aTWM2OD1zNz6xPVY{KM7:TR?= NWjGSG5FW0GQR2LFVi=>
SF539 M{XIeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGTDbIVKSzVyPUG3Mlk6OjJizszN MXrTRW5IWkWU
Calu-6 NFTNN25Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV3JR|UxRTF7LkKzPUDPxE1? NYrFdIdMW0GQR2LFVi=>
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GI-ME-N MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1y0d2lEPTB;MUmuPFIzPyEQvF2= MmrIV2FPT1KHUh?=
CAL-148 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MluxTWM2OD1{MD65PVM1KM7:TR?= M4jneXNCVkeURWK=
EVSA-T NYTHVpBkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3zOeWlEPTB;MkGuNVQ6QSEQvF2= M2\BbHNCVkeURWK=
LP-1 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4HEdWlEPTB;MkGuN|Q{OiEQvF2= NV\YS4JuW0GQR2LFVi=>
BOKU NFPrOVdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV3aToFjUUN3ME2yNU41PTN|IN88US=> MXjTRW5IWkWU
KLE MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M13mfGlEPTB;MkKuNVkxOyEQvF2= MnjNV2FPT1KHUh?=
LB831-BLC M3LYRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXrJSoRuUUN3ME2yOU4yPTJ4IN88US=> Mn;HV2FPT1KHUh?=
NCI-H889 NWXOdldTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUTFVnU6UUN3ME2yOU4yQTNzIN88US=> NWX2eld3W0GQR2LFVi=>
REH NXKye2NnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIfwVppKSzVyPUK1MlQ3PzFizszN MmDmV2FPT1KHUh?=
KP-N-RT-BM-1 MofzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M13FXWlEPTB;MkWuOFc2OiEQvF2= NGnYTmFUSU6JUlXS
MPP-89 Mn;mS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmPxTWM2OD1{NT61N|E1KM7:TR?= MVfTRW5IWkWU
no-11 M{jMfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEX3bXJKSzVyPUK1Mlc1PyEQvF2= MWrTRW5IWkWU
NCI-H748 NFPOVWFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkCxTWM2OD1{NT63OlI4KM7:TR?= MoTtV2FPT1KHUh?=
LB2518-MEL MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVjJR|UxRTJ5LkG3O|Mh|ryP NV62NW1{W0GQR2LFVi=>
TGBC1TKB MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1rl[GlEPTB;MkeuOVU5PSEQvF2= MlK5V2FPT1KHUh?=
MHH-PREB-1 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVnJR|UxRTJ6LkC3N|Qh|ryP MoG2V2FPT1KHUh?=
MZ2-MEL MkHqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnLzTWM2OD1{OD62NVQ{KM7:TR?= NFnGVGlUSU6JUlXS
U-266 Mo\IS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NY\EUZB2UUN3ME2yPE43OzZ4IN88US=> NEjjdIhUSU6JUlXS
SNU-C1 MmLSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3W5bWlEPTB;MkiuPVQ{KM7:TR?= NG\IOnJUSU6JUlXS
SW962 M17QbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2XBTWlEPTB;M{CuNlc1PyEQvF2= NFXzPWxUSU6JUlXS
Raji NXq2XXl6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUS2WW5{UUN3ME2zNE42PTl{IN88US=> NEjQOZFUSU6JUlXS
KNS-42 NEXid5lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2\mc2lEPTB;M{CuPFk2PiEQvF2= MVnTRW5IWkWU
LB996-RCC NInsdFNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXnRSld7UUN3ME2zNU4yPzB{IN88US=> NHjaUnFUSU6JUlXS
CHP-126 NFLZZlRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn3WTWM2OD1|MT6xPVg1KM7:TR?= M2jFbXNCVkeURWK=
RXF393 M4r1N2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MW\JR|UxRTN{LkS5O{DPxE1? MkW2V2FPT1KHUh?=
COLO-684 M{facGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHfNUFdKSzVyPUOyMlY1OzhizszN MkT3V2FPT1KHUh?=
A704 NYH2b2NST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXPJR|UxRTN|LkW1N|gh|ryP NUH2T5NXW0GQR2LFVi=>
A253 NVfvRZFUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmT4TWM2OD1|Mz61PFUzKM7:TR?= MYrTRW5IWkWU
KNS-81-FD M4TFXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnHETWM2OD1|ND61OFU3KM7:TR?= M{\lNHNCVkeURWK=
TE-441-T NWLl[5BCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWfkXm5ZUUN3ME2zOE43OzdzIN88US=> MYnTRW5IWkWU
HCC2157 Mo[3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX[we2tJUUN3ME2zOU41PjF7IN88US=> NIezclBUSU6JUlXS
ES3 MnmwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoXzTWM2OD1|Nj62O|Uh|ryP NFrPVGxUSU6JUlXS
NCI-H1155 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF62e5VKSzVyPUO3MlgyPSEQvF2= M2LxcXNCVkeURWK=
SNU-C2B MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1TEemlEPTB;M{iuNVY2PCEQvF2= NWrSVmU1W0GQR2LFVi=>
JAR MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn3mTWM2OD1|OD6yOFQ6KM7:TR?= NYrkOFA2W0GQR2LFVi=>
GDM-1 MonGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIi4cI1KSzVyPUO4MlkyOTZizszN MUnTRW5IWkWU
KU812 MlPSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFfX[oNKSzVyPUSxMlUxPyEQvF2= Mor2V2FPT1KHUh?=
BC-1 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmfUTWM2OD12Mj62O|MyKM7:TR?= M334W3NCVkeURWK=
GI-1 M4X4VGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4rXemlEPTB;NEKuPVE6OiEQvF2= M4XybnNCVkeURWK=
NCI-H1694 MkLCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVjJR|UxRTR2Lkm0O|Ih|ryP MWnTRW5IWkWU
DG-75 M{HtSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MorQTWM2OD12NT6xOVc4KM7:TR?= NV3ZbmJvW0GQR2LFVi=>
COR-L88 NYrWe5ZuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYjnR25RUUN3ME20OU4zPzd6IN88US=> M{e2NXNCVkeURWK=
LS-513 M3XC[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYPJR|UxRTR3LkmxOVYh|ryP MlXZV2FPT1KHUh?=
HD-MY-Z M1nzZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUXJR|UxRTR4LkS2NVIh|ryP MYPTRW5IWkWU
L-363 NEm1dGNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVTJR|UxRTR4Lki4NUDPxE1? MXjTRW5IWkWU
TE-6 M1zydmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3jTTGlEPTB;NEiuOFQ3KM7:TR?= NYXGS45mW0GQR2LFVi=>
NCI-H345 Mn;TS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVPMbHA1UUN3ME20PE41PjhizszN M2fIfHNCVkeURWK=
TE-5 NXWwS2FGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1HF[mlEPTB;NEmuO|EyQCEQvF2= NFjPc4JUSU6JUlXS

... 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:
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
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:

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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).

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Dilution Calculator

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

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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

If you have any other enquiries, please leave a message.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID