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 35 Publications

15 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.

  • 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 NEDlUJdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX3FRpp{UUN3ME2wMlAxOzN6IN88US=> M2T2NXNCVkeURWK=
RS4-11 NEixc4NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NInzNFFKSzVyPUCuNFA1ODRizszN NILZTG9USU6JUlXS
MFH-ino NUO0b2RTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnH5TWM2OD1yLkCwPVkh|ryP M1PjS3NCVkeURWK=
NTERA-S-cl-D1 MnvXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2HrRWlEPTB;MD6wNVQ{PCEQvF2= NYrjTIw1W0GQR2LFVi=>
697 NIjLUItIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYT5WIg5UUN3ME2wMlAzPDdzIN88US=> Mmn2V2FPT1KHUh?=
NALM-6 MoK5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1O0SmlEPTB;MD6wNlU2OiEQvF2= M2TZc3NCVkeURWK=
ES8 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnPCTWM2OD1yLkC0OlE{KM7:TR?= NXrOcGRyW0GQR2LFVi=>
HUTU-80 Ml;ES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4nDWmlEPTB;MD6wOVI6QSEQvF2= NF;KOopUSU6JUlXS
MV-4-11 M2PSXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIHpdmJKSzVyPUCuNFc4QDJizszN NUXLWG1TW0GQR2LFVi=>
MONO-MAC-6 M3\UZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHPnUIpKSzVyPUCuNFc5PzlizszN NILCNJVUSU6JUlXS
LC-2-ad NF3WXJVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoH5TWM2OD1yLkC4O|g6KM7:TR?= NIHCVVFUSU6JUlXS
BL-41 NIHNdpNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4L3SGlEPTB;MD6xNFQ1PSEQvF2= NIXlcWJUSU6JUlXS
A4-Fuk MnHkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{C5OGlEPTB;MD6xNVU3OyEQvF2= MoDaV2FPT1KHUh?=
SW954 NF3vT41Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2WwbGlEPTB;MD6xNlIzQSEQvF2= MYLTRW5IWkWU
BV-173 NVK4OW9ET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXHJR|UxRTBwMUK2OFEh|ryP NH3GNotUSU6JUlXS
TE-11 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIf5e4tKSzVyPUCuNVQ6QDJizszN NV7jU2dbW0GQR2LFVi=>
SK-UT-1 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVnJR|UxRTBwMUW5OlUh|ryP NGjRRpVUSU6JUlXS
SIG-M5 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWLtOnNVUUN3ME2wMlE3PzB5IN88US=> NXniTm1HW0GQR2LFVi=>
OCUB-M MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4fJU2lEPTB;MD6xOlk5OyEQvF2= M3PlSnNCVkeURWK=
K052 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEjZOGtKSzVyPUCuNVk1QCEQvF2= MYfTRW5IWkWU
VA-ES-BJ NGnDcIFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVXkbXlDUUN3ME2wMlIxODh4IN88US=> MmPNV2FPT1KHUh?=
SW982 Ml\5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIrLN4RKSzVyPUCuNlE{QCEQvF2= MmTuV2FPT1KHUh?=
LB647-SCLC M3nZVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoHoTWM2OD1yLkKxOVI{KM7:TR?= MXjTRW5IWkWU
PSN1 Mne1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYizb|RMUUN3ME2wMlIzODJ4IN88US=> NV\CT4dQW0GQR2LFVi=>
BB30-HNC MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUnJR|UxRTBwMkK1PVEh|ryP MmTXV2FPT1KHUh?=
ST486 NWLrdmhST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXXJR|UxRTBwMkOwPFch|ryP M3i0UnNCVkeURWK=
MOLT-4 MmDxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1jQXmlEPTB;MD6yN|M{PyEQvF2= MmjHV2FPT1KHUh?=
EW-16 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NG\1WYZKSzVyPUCuNlM4PjhizszN M{HXZXNCVkeURWK=
KS-1 NGnWeXhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1;zfWlEPTB;MD6yN|c5PSEQvF2= NGrKboVUSU6JUlXS
SR MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{HPNGlEPTB;MD6yOFU3PCEQvF2= MWTTRW5IWkWU
KM12 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlfKTWM2OD1yLkK2N|Yh|ryP MVfTRW5IWkWU
EM-2 MonKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXrJR|UxRTBwMk[2OFEh|ryP Mle1V2FPT1KHUh?=
MEG-01 MkPxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWjJR|UxRTBwMke4OFkh|ryP NIT2e2pUSU6JUlXS
NB13 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NILyNoVKSzVyPUCuNlc6QDRizszN MV;TRW5IWkWU
RKO MmLkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnrVTWM2OD1yLkOwPFE{KM7:TR?= NH\6RY9USU6JUlXS
CESS NXLWPFhMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIfybZNKSzVyPUCuN|E{OjhizszN MXfTRW5IWkWU
EoL-1-cell NYPjR4pET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXH6UFdXUUN3ME2wMlM{PDV7IN88US=> NXi4OVA5W0GQR2LFVi=>
DOHH-2 NFL3OVRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4q3TWlEPTB;MD6zN|c5OSEQvF2= MUPTRW5IWkWU
A388 NF3rd|hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NELPSVdKSzVyPUCuN|QxQDZizszN NGLWRoZUSU6JUlXS
LAMA-84 NH3wXnlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MU\JR|UxRTBwM{WxO|gh|ryP NVu4Z2U1W0GQR2LFVi=>
IMR-5 NYT2OlVkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{HndGlEPTB;MD6zOVU1KM7:TR?= MnXuV2FPT1KHUh?=
KARPAS-422 NYGzRVc{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4PxcWlEPTB;MD6zO|I4OiEQvF2= M4LnSnNCVkeURWK=
MRK-nu-1 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mnr3TWM2OD1yLkO4NVMh|ryP MoTnV2FPT1KHUh?=
BL-70 MoDNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlfFTWM2OD1yLkO4PVc1KM7:TR?= M17VWHNCVkeURWK=
LXF-289 M2C3UWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYfjeXhOUUN3ME2wMlQxPDB4IN88US=> NX7SSlJlW0GQR2LFVi=>
RL95-2 MmDIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFjiSopKSzVyPUCuOFA2PjdizszN NX6yUIZxW0GQR2LFVi=>
QIMR-WIL NIPF[GxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIWweY5KSzVyPUCuOFI3PzZizszN MXrTRW5IWkWU
K-562 MkfWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUnJR|UxRTBwNEO0O|Ih|ryP MnnyV2FPT1KHUh?=
NCI-H510A MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mmj6TWM2OD1yLkSzPFI{KM7:TR?= NGXzSItUSU6JUlXS
NCI-H524 MlTNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWnzcG5QUUN3ME2wMlUyOTR5IN88US=> MkP1V2FPT1KHUh?=
KE-37 NYPwZ29vT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXrJR|UxRTBwNUKxNFIh|ryP NEf1ZmdUSU6JUlXS
KP-N-YS NVnNN2huT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGD6b25KSzVyPUCuOVQ{QTJizszN NVLpTppIW0GQR2LFVi=>
LS-411N NEDyN2hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1;oPWlEPTB;MD61O|c2OiEQvF2= NHTTb|hUSU6JUlXS
CTV-1 NWXGN|VLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1;CVGlEPTB;MD61PFc4OyEQvF2= NX;UeZU1W0GQR2LFVi=>
NCI-SNU-16 M3zDVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX70cXpIUUN3ME2wMlY{PTdzIN88US=> MlTmV2FPT1KHUh?=
HT-144 Ml7nS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGPYOolKSzVyPUCuOlM4QThizszN MlHZV2FPT1KHUh?=
NCI-H187 NV[5bJNyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M13QN2lEPTB;MD62OFE{KM7:TR?= M17senNCVkeURWK=
OCI-AML2 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXP4RWdUUUN3ME2wMlY1PDB|IN88US=> M2\wcXNCVkeURWK=
CCRF-CEM M2HvdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXfYVGpWUUN3ME2wMlY2OzR4IN88US=> NWT6c5JpW0GQR2LFVi=>
ONS-76 M4La[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWnUWW5UUUN3ME2wMlY3PDV6IN88US=> NH3EfJFUSU6JUlXS
IST-SL2 NGP4[VZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXvJR|UxRTBwN{G5PFIh|ryP MmjnV2FPT1KHUh?=
NB6 NUT4O|dET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mk[1TWM2OD1yLke3NlU1KM7:TR?= MXLTRW5IWkWU
SK-PN-DW NViwfFhRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUPJR|UxRTBwN{mxOEDPxE1? NHXPUIJUSU6JUlXS
HCC1599 NW\6UY9jT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF3m[VlKSzVyPUCuPFA5PzRizszN MmO0V2FPT1KHUh?=
MC116 M1jMOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXK4WGhUUUN3ME2wMlg2ODFzIN88US=> NGOxS2FUSU6JUlXS
TE-15 M2jXZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmjXTWM2OD1yLki1NFk5KM7:TR?= NFzzUYVUSU6JUlXS
HOP-62 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml;STWM2OD1yLki2N|I6KM7:TR?= M1HSOXNCVkeURWK=
TGBC24TKB MnW1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmDlTWM2OD1yLki2N|g2KM7:TR?= MWrTRW5IWkWU
HCE-4 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVLQ[nBLUUN3ME2wMlg5ODZ|IN88US=> NHfpbG5USU6JUlXS
ALL-PO NHjK[2lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUPJR|UxRTBwOEixO|Uh|ryP MYLTRW5IWkWU
KGN M1e3U2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXnJR|UxRTBwOEm5PVUh|ryP NF;ZcG5USU6JUlXS
ML-2 NUTWUJhTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIXpeGFKSzVyPUCuPVAzPTlizszN MUjTRW5IWkWU
ES4 NVXKW2tQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHrpXpFKSzVyPUCuPVEyOjhizszN MnPkV2FPT1KHUh?=
SF126 NFr1NWxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVPhNpJDUUN3ME2wMlk1QDF7IN88US=> MkHkV2FPT1KHUh?=
SK-N-DZ M4LJXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUHMSW81UUN3ME2wMlk3OTh7IN88US=> M1zPZXNCVkeURWK=
HCC1187 NIXZdItIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3z6NmlEPTB;MT6wNFUxPSEQvF2= NFLGWVZUSU6JUlXS
DU-4475 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXfrdVJZUUN3ME2xMlAyPzV4IN88US=> NH3GPVRUSU6JUlXS
NKM-1 M1PW[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUX0TolOUUN3ME2xMlAzPzd3IN88US=> NFW5SYlUSU6JUlXS
HL-60 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUfJR|UxRTFwME[1O|Qh|ryP NXP5VFdJW0GQR2LFVi=>
SBC-1 MkPtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHjSXGJKSzVyPUGuNVI2PDJizszN NUXjd45tW0GQR2LFVi=>
TE-10 NV7EZZF4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV7JR|UxRTFwMUK5OFYh|ryP NVX1ZldIW0GQR2LFVi=>
ETK-1 MoPmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmqzTWM2OD1zLkGzOlE{KM7:TR?= Mo[1V2FPT1KHUh?=
HAL-01 M3P5d2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M13oR2lEPTB;MT6xOlcxQSEQvF2= M37hXnNCVkeURWK=
BB65-RCC NUGwV5JJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmDKTWM2OD1zLkG4NFA2KM7:TR?= NXXL[phEW0GQR2LFVi=>
EW-1 M3jiWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYTJR|UxRTFwMUi1OlIh|ryP M{n3[HNCVkeURWK=
SK-NEP-1 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NE\P[XRKSzVyPUGuNlEyOTFizszN NYDFcHpKW0GQR2LFVi=>
SK-LMS-1 NW\hd|lsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnGyTWM2OD1zLkKyNlEzKM7:TR?= MnPGV2FPT1KHUh?=
DEL MnzYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlTQTWM2OD1zLkK1OlQ{KM7:TR?= M3fGW3NCVkeURWK=
GT3TKB NUPnU2I{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUjld4R1UUN3ME2xMlI5ODV5IN88US=> M3rDdHNCVkeURWK=
MOLT-16 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1LabWlEPTB;MT6zOVQxPSEQvF2= MUDTRW5IWkWU
CMK M1[1Z2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmS1TWM2OD1zLkSyNVE4KM7:TR?= NW\nUJhYW0GQR2LFVi=>
NB5 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3S3XmlEPTB;MT62OFIzQSEQvF2= NHrSVYJUSU6JUlXS
NCI-H1963 NVHzb4VJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWDGZ2djUUN3ME2xMlcxPTh|IN88US=> MkXjV2FPT1KHUh?=
KURAMOCHI NYi4Znk4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NW[1WpRzUUN3ME2xMlc5QTFzIN88US=> NVTmdXpCW0GQR2LFVi=>
TE-8 MlHzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF3scJFKSzVyPUGuPFA{PjhizszN NV;HNnFSW0GQR2LFVi=>
NCI-H1304 NVLLbI1GT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mo\1TWM2OD1zLkizNFc{KM7:TR?= M3raNHNCVkeURWK=
A101D M33NdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NY\SbFlbUUN3ME2xMlg4Ozl3IN88US=> MmPnV2FPT1KHUh?=
SCLC-21H NIGxRYJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYfJR|UxRTFwOUewOVch|ryP MnO2V2FPT1KHUh?=
GB-1 M2\nZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2T0OGlEPTB;Mj6wNVY1PyEQvF2= MXPTRW5IWkWU
KARPAS-45 NF;N[5NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVTzdIpSUUN3ME2yMlAzPjV2IN88US=> M3ntcnNCVkeURWK=
ATN-1 M2jRNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVTJR|UxRTJwMEK4OVgh|ryP M3jVWnNCVkeURWK=
NCI-H720 MnviS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mk\TTWM2OD1{LkC2NlQ1KM7:TR?= NVi5S4Y5W0GQR2LFVi=>
RPMI-6666 NWfrZXZYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHvnbWRKSzVyPUKuNVYzODdizszN MWLTRW5IWkWU
NB17 Mlj0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoLITWM2OD1{LkK5Nlch|ryP M2LYbnNCVkeURWK=
IST-SL1 MnTzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXnIS|g3UUN3ME2yMlI6PzZ3IN88US=> MV;TRW5IWkWU
SH-4 M2Sydmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3LM[mlEPTB;Mj6zNlQ3QSEQvF2= NXnI[HlXW0GQR2LFVi=>
K5 M1XpPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnnNTWM2OD1{LkSwN|E6KM7:TR?= MWLTRW5IWkWU
OVCAR-4 NGnQbFBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEjscItKSzVyPUKuOFYyOyEQvF2= NWW5[4JlW0GQR2LFVi=>
ACN NHL0PWtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYDY[pBLUUN3ME2yMlUxOjF|IN88US=> MoT1V2FPT1KHUh?=
TGW MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1fxZmlEPTB;Mj62OVg{OiEQvF2= MUTTRW5IWkWU
NCI-H2107 M3zXT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYO0SWV{UUN3ME2yMlg{PzFzIN88US=> NXrwNFdGW0GQR2LFVi=>
NCI-H82 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MofBTWM2OD1{LkizPFM5KM7:TR?= M2X6XnNCVkeURWK=
SK-N-FI NVjUT|YzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2\aN2lEPTB;Mj64Olg3QCEQvF2= MVfTRW5IWkWU
LB1047-RCC M{S5e2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXrJR|UxRTJwOEixNlYh|ryP MYPTRW5IWkWU
LU-134-A NUf0O5VzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIH2RmVKSzVyPUKuPFkzPiEQvF2= MUfTRW5IWkWU
NCI-H209 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MorqTWM2OD1{LkmxNlU{KM7:TR?= MXPTRW5IWkWU
NOMO-1 M3PlO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV;JR|UxRTNwMEKyO|Qh|ryP MlfwV2FPT1KHUh?=
RH-1 MlXSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWLJR|UxRTNwMUeyPVEh|ryP NXfsRVNlW0GQR2LFVi=>
LOUCY M1v5NGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1ns[GlEPTB;Mz6xPFY6OyEQvF2= NXPmdI5RW0GQR2LFVi=>
TE-9 NFf2NIJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MonkTWM2OD1|LkK2O|M3KM7:TR?= NWD5OZpXW0GQR2LFVi=>
PF-382 MkjFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mk\pTWM2OD1|LkO1O|c5KM7:TR?= MmrYV2FPT1KHUh?=
RPMI-8402 MlvaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M36z[mlEPTB;Mz61PFYxOyEQvF2= M2fuVnNCVkeURWK=
HEL M3XycGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFvobG9KSzVyPUOuOlMzKM7:TR?= M3\seXNCVkeURWK=
NOS-1 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVW3Wog2UUN3ME2zMlg1PzV2IN88US=> M{\TS3NCVkeURWK=
ES1 NUjUVJNzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUXJR|UxRTNwOUKyPVMh|ryP MULTRW5IWkWU
NCI-H2171 NYnv[md{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXHJR|UxRTNwOUK0NlMh|ryP M4TuTnNCVkeURWK=
NCI-H747 M3ribGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWDjS2QxUUN3ME2zMlk1OjJzIN88US=> NXTpTZBLW0GQR2LFVi=>
MHH-NB-11 NGXUTpNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1HESGlEPTB;Mz65OVMyOiEQvF2= NHT3UFNUSU6JUlXS
MZ1-PC M3uyU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXjJR|UxRTNwOUmyOEDPxE1? NXTTSHZnW0GQR2LFVi=>
MMAC-SF NYTSWVJIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2POc2lEPTB;ND6wNlQ3PyEQvF2= NHTiRmNUSU6JUlXS
NMC-G1 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnT5TWM2OD12LkKyO|I{KM7:TR?= M1L6dXNCVkeURWK=
SW872 NXu2OZBtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn3DTWM2OD12LkO0N|Qh|ryP MkXPV2FPT1KHUh?=
TE-12 NHXZS25Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVzoTZNkUUN3ME20MlU3Ozl2IN88US=> MVTTRW5IWkWU
LU-139 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{jDU2lEPTB;ND62NVg{PSEQvF2= MVLTRW5IWkWU
HC-1 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1[xcWlEPTB;ND62PVQ6PCEQvF2= NHq4cINUSU6JUlXS
COR-L279 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHS3bGxKSzVyPUSuO|U5QTFizszN NFvzVmJUSU6JUlXS
SF268 M1zFTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVLJR|UxRTRwN{m5NVYh|ryP NV2zZ|JWW0GQR2LFVi=>
MC-CAR Mk\nS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYXJR|UxRTVwME[3OVch|ryP NHLsdHZUSU6JUlXS
TK10 M4rB[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHO4OndKSzVyPUWuN|U1PjlizszN NU[3[5R2W0GQR2LFVi=>
TE-1 MlPZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmDJTWM2OD13LkS5NFA1KM7:TR?= NVjZXGFKW0GQR2LFVi=>
NCI-H2126 NF34R5RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUXJR|UxRTVwNkS1O|Qh|ryP M2TrRXNCVkeURWK=
Daudi NXzQe5FVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1vFUWlEPTB;NT62PVEzKM7:TR?= NVHVfJN7W0GQR2LFVi=>
NCI-H1648 Mm\US5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlT6TWM2OD13LkixOFU1KM7:TR?= NITvUGRUSU6JUlXS
OS-RC-2 NXz0dm1ZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M33zN2lEPTB;NT65PFU6PyEQvF2= MVzTRW5IWkWU
DJM-1 MonIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NY\JRoptUUN3ME22MlM1PjZ4IN88US=> MUnTRW5IWkWU
LS-1034 NELsWWpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH32bVRKSzVyPU[uO|U3PiEQvF2= M3LCdHNCVkeURWK=
NCI-H1581 NEHpbXdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIjId49KSzVyPU[uO|g1ODVizszN NVLoZYpFW0GQR2LFVi=>
UACC-257 MnXNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXHkeGZwUUN3ME23MlA1PTF{IN88US=> NFO1bXZUSU6JUlXS
KM-H2 NFTMNm1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3zxTWlEPTB;Nz6xPFQ2PyEQvF2= NYfwSZU1W0GQR2LFVi=>
NCI-H1436 MoHFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWjO[lFPUUN3ME23MlY6QTN{IN88US=> MUDTRW5IWkWU
IA-LM MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHXIe2NKSzVyPUeuPFU6KM7:TR?= MYHTRW5IWkWU
NCI-H526 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYjJR|UxRThwMkW2N|ch|ryP NW[yVm5FW0GQR2LFVi=>
GCIY NF:4[lNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUjiXpV7UUN3ME24MlM3QTZ3IN88US=> Ml3iV2FPT1KHUh?=
CP67-MEL MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{PZSmlEPTB;OD61N|I3KM7:TR?= M2i3VHNCVkeURWK=
KALS-1 M1PFUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVvJR|UxRThwOEO4OVEh|ryP NGCxTYlUSU6JUlXS
NCI-H1770 MmnqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYLJR|UxRThwOUCyOlUh|ryP MXXTRW5IWkWU
8-MG-BA NIm5co5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYTJR|UxRTlwM{K4OFQh|ryP MX7TRW5IWkWU
KY821 MkD5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF7sW4NKSzVyPUmuO|c1QDRizszN MV\TRW5IWkWU
SNB75 NILPbFZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWXJR|UxRTFyLkC3OkDPxE1? M4L6[HNCVkeURWK=
NCCIT NEW1WIlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXK5dJY3UUN3ME2xNU4xPTh{IN88US=> MnzCV2FPT1KHUh?=
SJSA-1 NH[zPJNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3TG[GlEPTB;MUGuNlg6OSEQvF2= MonWV2FPT1KHUh?=
LB373-MEL-D NHXIfZVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlTQTWM2OD1zMT6zPFI4KM7:TR?= NHv1XmhUSU6JUlXS
TALL-1 M4LPSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1\oSmlEPTB;MUGuOFA2QCEQvF2= NGDVd5ZUSU6JUlXS
NB69 NETJ[3NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml7UTWM2OD1zMT63O|A2KM7:TR?= M4nV[HNCVkeURWK=
NCI-H1355 NVjKdG5pT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUPEVmJGUUN3ME2xNU46PDJ4IN88US=> NXu2TGZTW0GQR2LFVi=>
DMS-153 NHrKXFVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1L2XWlEPTB;MUKuNFQzPiEQvF2= NYrIS5NxW0GQR2LFVi=>
OPM-2 M4rvcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlTmTWM2OD1zMj6xOVk3KM7:TR?= MlryV2FPT1KHUh?=
NB1 NF;pTnlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVfOfGxvUUN3ME2xNk4zQSEQvF2= MUDTRW5IWkWU
A3-KAW Ml\yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2WyPGlEPTB;MUKuN|I{PiEQvF2= NIjlbFhUSU6JUlXS
NCI-H1882 MmXDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX;5SIxDUUN3ME2xNk41ODZ4IN88US=> MY\TRW5IWkWU
KG-1 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHXXZ|RKSzVyPUGyMlY2PDVizszN NWnt[oNjW0GQR2LFVi=>
LC4-1 M3LUb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml22TWM2OD1zMj63O|A3KM7:TR?= MXHTRW5IWkWU
HCE-T Mn;iS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXLJR|UxRTF|LkCwOFkh|ryP NVXvbW94W0GQR2LFVi=>
NEC8 MlrsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGC2fXRKSzVyPUGzMlExOzhizszN MoPHV2FPT1KHUh?=
IST-MEL1 NXvBbI9sT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHG5NIhKSzVyPUGzMlU4QDhizszN M3z5UXNCVkeURWK=
EW-3 MmjES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFXYUpFKSzVyPUGzMlc1ODJizszN MUjTRW5IWkWU
CTB-1 MmfCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2TtUmlEPTB;MUSuNFMzQSEQvF2= NHHnS2hUSU6JUlXS
LS-123 M4SyPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3\XeWlEPTB;MUSuNVU5QCEQvF2= NHK0cWdUSU6JUlXS
NCI-H1417 NXjhdHZ1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWfJR|UxRTF2LkOwOVIh|ryP NHi2e|BUSU6JUlXS
MZ7-mel MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mlv0TWM2OD1zND60OFM{KM7:TR?= M1PqbHNCVkeURWK=
JiyoyeP-2003 M{PEN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmrTTWM2OD1zNT62N|I3KM7:TR?= MlrEV2FPT1KHUh?=
ES6 MoHXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{DLVWlEPTB;MU[uNlM3OSEQvF2= M{ixOXNCVkeURWK=
HH NGPiUnRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NED4flhKSzVyPUG3MlE6PjNizszN Ml64V2FPT1KHUh?=
SF539 M2O1Z2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFHpb4dKSzVyPUG3Mlk6OjJizszN NFjnUldUSU6JUlXS
Calu-6 NH23ZlhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXHJR|UxRTF7LkKzPUDPxE1? NXrWWIQ5W0GQR2LFVi=>
SK-MM-2 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV3JR|UxRTF7LkW1OUDPxE1? MlX5V2FPT1KHUh?=
IST-MES1 NWLJeoRZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX7JR|UxRTF7Lk[2OlMh|ryP M{XiPXNCVkeURWK=
GI-ME-N MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGXH[4FKSzVyPUG5MlgzOjdizszN M3SxOHNCVkeURWK=
CAL-148 NIr0NXhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmTSTWM2OD1{MD65PVM1KM7:TR?= M2TRXHNCVkeURWK=
EVSA-T NECxVIFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NE\xXYJKSzVyPUKxMlE1QTlizszN M1vlXXNCVkeURWK=
LP-1 M4XkNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHjNcm9KSzVyPUKxMlM1OzJizszN MnWyV2FPT1KHUh?=
BOKU M3;NWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV74OVB2UUN3ME2yNU41PTN|IN88US=> M1LkOHNCVkeURWK=
KLE MmfOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXzMempSUUN3ME2yNk4yQTB|IN88US=> MnPRV2FPT1KHUh?=
LB831-BLC NGX2d|dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV;JR|UxRTJ3LkG1NlYh|ryP M3\mVnNCVkeURWK=
NCI-H889 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnzxTWM2OD1{NT6xPVMyKM7:TR?= NUnkPWc6W0GQR2LFVi=>
REH MkLHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXH5Roc1UUN3ME2yOU41PjdzIN88US=> MmPMV2FPT1KHUh?=
KP-N-RT-BM-1 M{Xxbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlTYTWM2OD1{NT60O|UzKM7:TR?= MX;TRW5IWkWU
MPP-89 M3nld2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFGwTVdKSzVyPUK1MlU{OTRizszN MmfUV2FPT1KHUh?=
no-11 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH31dXZKSzVyPUK1Mlc1PyEQvF2= M1j4cnNCVkeURWK=
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LB2518-MEL MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlvlTWM2OD1{Nz6xO|c{KM7:TR?= M1zUb3NCVkeURWK=
TGBC1TKB MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWnJR|UxRTJ5LkW1PFUh|ryP MXnTRW5IWkWU
MHH-PREB-1 MlfwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1y5V2lEPTB;MkiuNFc{PCEQvF2= MUnTRW5IWkWU
MZ2-MEL MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1zQRmlEPTB;MkiuOlE1OyEQvF2= NUfoRZhZW0GQR2LFVi=>
U-266 NXfrfG9ET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoHNTWM2OD1{OD62N|Y3KM7:TR?= NWXrSm8xW0GQR2LFVi=>
SNU-C1 NH7xT4JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUHJR|UxRTJ6Lkm0N{DPxE1? MVzTRW5IWkWU
SW962 MojvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX7JR|UxRTNyLkK3OFch|ryP MmDjV2FPT1KHUh?=
Raji NEXqdINIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmLnTWM2OD1|MD61OVkzKM7:TR?= NHjXcIdUSU6JUlXS
KNS-42 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUja[GZ7UUN3ME2zNE45QTV4IN88US=> NYDCeGRRW0GQR2LFVi=>
LB996-RCC MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYrJR|UxRTNzLkG3NFIh|ryP NIWwbYtUSU6JUlXS
CHP-126 NHnJdFZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYTJR|UxRTNzLkG5PFQh|ryP NY\IWWhDW0GQR2LFVi=>
RXF393 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3zPNGlEPTB;M{KuOFk4KM7:TR?= NY\VeYh1W0GQR2LFVi=>
COLO-684 MlK0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{HaZ2lEPTB;M{KuOlQ{QCEQvF2= MVfTRW5IWkWU
A704 NHjRVXlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFTUSG5KSzVyPUOzMlU2OzhizszN Mn2xV2FPT1KHUh?=
A253 MkTLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWHyU|FFUUN3ME2zN{42QDV{IN88US=> MWXTRW5IWkWU
KNS-81-FD MlTIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV3JR|UxRTN2LkW0OVYh|ryP MWnTRW5IWkWU
TE-441-T NHnYZWdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYLJR|UxRTN2Lk[zO|Eh|ryP MWjTRW5IWkWU
HCC2157 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mmr3TWM2OD1|NT60OlE6KM7:TR?= MXvTRW5IWkWU
ES3 NFj5Z45Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHTKbWxKSzVyPUO2MlY4PSEQvF2= MmnqV2FPT1KHUh?=
NCI-H1155 M2fSTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NW\Hem9xUUN3ME2zO{45OTVizszN NHTqVnBUSU6JUlXS
SNU-C2B NH;TXpRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVnMO49IUUN3ME2zPE4yPjV2IN88US=> MlfjV2FPT1KHUh?=
JAR M4LDOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWDJR|UxRTN6LkK0OFkh|ryP NEHYcIJUSU6JUlXS
GDM-1 NYmz[XlbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXzJR|UxRTN6LkmxNVYh|ryP MVPTRW5IWkWU
KU812 M{\HU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NELKR|lKSzVyPUSxMlUxPyEQvF2= NHTiSXFUSU6JUlXS
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GI-1 MojCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1;uSWlEPTB;NEKuPVE6OiEQvF2= NYHDSHI5W0GQR2LFVi=>
NCI-H1694 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoDBTWM2OD12ND65OFczKM7:TR?= NVLTXGJPW0GQR2LFVi=>
DG-75 MlPwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIfuSHZKSzVyPUS1MlE2PzdizszN MUnTRW5IWkWU
COR-L88 MnPXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVKydlFIUUN3ME20OU4zPzd6IN88US=> MVXTRW5IWkWU
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L-363 NFTLSIZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWfJR|UxRTR4Lki4NUDPxE1? M4jC[nNCVkeURWK=
TE-6 M1fuWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVL3[5oxUUN3ME20PE41PDZizszN MnHZV2FPT1KHUh?=
NCI-H345 MmDqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFXNflNKSzVyPUS4MlQ3QCEQvF2= MYPTRW5IWkWU
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... 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 <1 mg/mL
Ethanol <1 mg/mL
In vivo 30% PEG400+0.5% Tween80+5% propylene glycol 30 mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 464.59
Formula

C23H28N8OS

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

Bio Calculators

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

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

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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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID