VX-680 (Tozasertib, MK-0457)

Catalog No.S1048

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

Molecular Weight(MW): 464.59

VX-680 (Tozasertib, 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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In DMSO USD 134 In stock
USD 147 In stock
USD 370 In stock
USD 470 In stock

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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. VX-680 (Tozasertib, 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. VX-680 (Tozasertib, 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. VX-680 (Tozasertib, 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. VX-680 (Tozasertib, 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. VX-680 (Tozasertib, 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. VX-680 (Tozasertib, 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. VX-680 (Tozasertib, 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. VX-680 (Tozasertib, 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. VX-680 (Tozasertib, 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. VX-680 (Tozasertib, 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. VX-680 (Tozasertib, 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. VX-680 (Tozasertib, 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. VX-680 (Tozasertib, 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. VX-680 (Tozasertib, MK-0457) purchased from Selleck.

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

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

Purity & Quality Control

Choose Selective Aurora Kinase Inhibitors

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

Biological Activity

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

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

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
BE-13 M{S5VGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXfwRW1ZUUN3ME2wMlAxOzN6IN88US=> M1XrNnNCVkeURWK=
RS4-11 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnHYTWM2OD1yLkCwOFA1KM7:TR?= M37WPXNCVkeURWK=
MFH-ino M{PPfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFTLU2xKSzVyPUCuNFA6QSEQvF2= NYnFOJZoW0GQR2LFVi=>
NTERA-S-cl-D1 MkjzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkfGTWM2OD1yLkCxOFM1KM7:TR?= M1nFVHNCVkeURWK=
697 MmDGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFLL[XhKSzVyPUCuNFI1PzFizszN NUOwdWlqW0GQR2LFVi=>
NALM-6 NH3xUo9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYHJR|UxRTBwMEK1OVIh|ryP M3fuTXNCVkeURWK=
ES8 NXfHSYRvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3viO2lEPTB;MD6wOFYyOyEQvF2= M{nie3NCVkeURWK=
HUTU-80 NXr1bJdvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWPEZ5lyUUN3ME2wMlA2Ojl7IN88US=> NHjLb2FUSU6JUlXS
MV-4-11 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWD3fotsUUN3ME2wMlA4Pzh{IN88US=> NVfub4hJW0GQR2LFVi=>
MONO-MAC-6 NX\sS2JvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{X2XmlEPTB;MD6wO|g4QSEQvF2= MWfTRW5IWkWU
LC-2-ad Mn\3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV\2fo5CUUN3ME2wMlA5Pzh7IN88US=> NWPhc5dlW0GQR2LFVi=>
BL-41 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoLCTWM2OD1yLkGwOFQ2KM7:TR?= M3joWXNCVkeURWK=
A4-Fuk NUnYb|VvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NY[4bmJjUUN3ME2wMlEyPTZ|IN88US=> NV;uc|luW0GQR2LFVi=>
SW954 M1PxbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1PFS2lEPTB;MD6xNlIzQSEQvF2= NVHD[HZEW0GQR2LFVi=>
BV-173 NWjySJc1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{fLOWlEPTB;MD6xNlY1OSEQvF2= NHmzc3pUSU6JUlXS
TE-11 M4XyfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHvkeVNKSzVyPUCuNVQ6QDJizszN MV;TRW5IWkWU
SK-UT-1 NXThdYxmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYXJR|UxRTBwMUW5OlUh|ryP MkTmV2FPT1KHUh?=
SIG-M5 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV3nRYc4UUN3ME2wMlE3PzB5IN88US=> MVLTRW5IWkWU
OCUB-M Ml30S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3rDZ2lEPTB;MD6xOlk5OyEQvF2= MmnxV2FPT1KHUh?=
K052 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlXNTWM2OD1yLkG5OFgh|ryP MV\TRW5IWkWU
VA-ES-BJ MmH5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2i0WGlEPTB;MD6yNFA5PiEQvF2= MYXTRW5IWkWU
SW982 NYHoUJJZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NY\K[VkxUUN3ME2wMlIyOzhizszN Ml7DV2FPT1KHUh?=
LB647-SCLC NG\4XVhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MofETWM2OD1yLkKxOVI{KM7:TR?= MkGxV2FPT1KHUh?=
PSN1 MnzVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYLJR|UxRTBwMkKwNlYh|ryP MYTTRW5IWkWU
BB30-HNC M3zqcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NES2bJFKSzVyPUCuNlI2QTFizszN NWrnPIhoW0GQR2LFVi=>
ST486 M2L6Smdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3XXSmlEPTB;MD6yN|A5PyEQvF2= NF\UWVFUSU6JUlXS
MOLT-4 Mo[xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHXwSnpKSzVyPUCuNlM{OzdizszN M{PQZ3NCVkeURWK=
EW-16 M2TESWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmjqTWM2OD1yLkKzO|Y5KM7:TR?= NHnvTFVUSU6JUlXS
KS-1 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{DXUmlEPTB;MD6yN|c5PSEQvF2= NH3WS3NUSU6JUlXS
SR M1fWb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{TxPWlEPTB;MD6yOFU3PCEQvF2= NVjEV4tSW0GQR2LFVi=>
KM12 M4X1emdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2TzfGlEPTB;MD6yOlM3KM7:TR?= MlPtV2FPT1KHUh?=
EM-2 MmTOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVTJR|UxRTBwMk[2OFEh|ryP M2j3XHNCVkeURWK=
MEG-01 NUC2[5JUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVLNdmdFUUN3ME2wMlI4QDR7IN88US=> NXT1fGVRW0GQR2LFVi=>
NB13 NVTaTnlbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWjsdnJjUUN3ME2wMlI4QTh2IN88US=> NFXkU5hUSU6JUlXS
RKO MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3HPfWlEPTB;MD6zNFgyOyEQvF2= MVHTRW5IWkWU
CESS M2HrUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIHxTolKSzVyPUCuN|E{OjhizszN MlX4V2FPT1KHUh?=
EoL-1-cell M{nuNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NU\mPYRqUUN3ME2wMlM{PDV7IN88US=> M2jpVnNCVkeURWK=
DOHH-2 M3Wx[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1rBOmlEPTB;MD6zN|c5OSEQvF2= MmH5V2FPT1KHUh?=
A388 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWW0b3F7UUN3ME2wMlM1ODh4IN88US=> NGrHfW5USU6JUlXS
LAMA-84 NHnRRY9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml;jTWM2OD1yLkO1NVc5KM7:TR?= NXfFbW5zW0GQR2LFVi=>
IMR-5 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEHZdpVKSzVyPUCuN|U2PCEQvF2= M1PZZXNCVkeURWK=
KARPAS-422 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1jFZWlEPTB;MD6zO|I4OiEQvF2= NGT1ZYJUSU6JUlXS
MRK-nu-1 NHTPTIFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1v4SmlEPTB;MD6zPFE{KM7:TR?= Mkf1V2FPT1KHUh?=
BL-70 M{jONWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NICy[W5KSzVyPUCuN|g6PzRizszN NXjhS|dTW0GQR2LFVi=>
LXF-289 NI[5UY9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH\LPYxKSzVyPUCuOFA1ODZizszN MWrTRW5IWkWU
RL95-2 NEm4[ZpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4i3e2lEPTB;MD60NFU3PyEQvF2= NYfMbZRRW0GQR2LFVi=>
QIMR-WIL NFi1cnZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWGxPW1MUUN3ME2wMlQzPjd4IN88US=> MknkV2FPT1KHUh?=
K-562 M{\6fWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYTJR|UxRTBwNEO0O|Ih|ryP NWr0U3p7W0GQR2LFVi=>
NCI-H510A MlqyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXHq[3pQUUN3ME2wMlQ{QDJ|IN88US=> M36wSHNCVkeURWK=
NCI-H524 MmHNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX7JR|UxRTBwNUGxOFch|ryP M1Tne3NCVkeURWK=
KE-37 NHja[XFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MojRTWM2OD1yLkWyNVAzKM7:TR?= MonhV2FPT1KHUh?=
KP-N-YS Mn;DS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF22N3pKSzVyPUCuOVQ{QTJizszN NVPPb4pNW0GQR2LFVi=>
LS-411N M{jsTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGPKNmJKSzVyPUCuOVc4PTJizszN M2f1d3NCVkeURWK=
CTV-1 NIXq[W5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV:1PFI2UUN3ME2wMlU5Pzd|IN88US=> MnH6V2FPT1KHUh?=
NCI-SNU-16 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV7QN2NoUUN3ME2wMlY{PTdzIN88US=> NYT5WmE3W0GQR2LFVi=>
HT-144 Mnv0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NY\adZlTUUN3ME2wMlY{Pzl6IN88US=> M3jL[3NCVkeURWK=
NCI-H187 MlfkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV\JR|UxRTBwNkSxN{DPxE1? NGjo[2RUSU6JUlXS
OCI-AML2 MnLzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFmzeY5KSzVyPUCuOlQ1ODNizszN M1zWdXNCVkeURWK=
CCRF-CEM NIrYXoNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NES2eXpKSzVyPUCuOlU{PDZizszN M325O3NCVkeURWK=
ONS-76 MmLlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWDDUo9GUUN3ME2wMlY3PDV6IN88US=> M4jGZXNCVkeURWK=
IST-SL2 NGTmeYRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXPJR|UxRTBwN{G5PFIh|ryP NUDt[3VlW0GQR2LFVi=>
NB6 NFntdm1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M33nRWlEPTB;MD63O|I2PCEQvF2= MUnTRW5IWkWU
SK-PN-DW NHr5NFZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnfuTWM2OD1yLke5NVQh|ryP M1;xWnNCVkeURWK=
HCC1599 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlrBTWM2OD1yLkiwPFc1KM7:TR?= MXTTRW5IWkWU
MC116 M1ruXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3e5V2lEPTB;MD64OVAyOSEQvF2= NETjU4NUSU6JUlXS
TE-15 NGnzWZRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnLFTWM2OD1yLki1NFk5KM7:TR?= NIPJXHJUSU6JUlXS
HOP-62 M{jQcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mk\RTWM2OD1yLki2N|I6KM7:TR?= NXrUWnIxW0GQR2LFVi=>
TGBC24TKB MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVLJR|UxRTBwOE[zPFUh|ryP NVuyTGFmW0GQR2LFVi=>
HCE-4 NGq3b5FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mo\VTWM2OD1yLki4NFY{KM7:TR?= NX3yTXB5W0GQR2LFVi=>
ALL-PO NHjpdmJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXn0b5hNUUN3ME2wMlg5OTd3IN88US=> NF;LfFNUSU6JUlXS
KGN Mny4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWTJR|UxRTBwOEm5PVUh|ryP NEXaeZlUSU6JUlXS
ML-2 NF\vWoxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmXZTWM2OD1yLkmwNlU6KM7:TR?= M1ywWHNCVkeURWK=
ES4 MofBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1\kPGlEPTB;MD65NVEzQCEQvF2= NGLQdW5USU6JUlXS
SF126 M1TpNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmTRTWM2OD1yLkm0PFE6KM7:TR?= MoLzV2FPT1KHUh?=
SK-N-DZ NXXkNm9uT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIjWS4dKSzVyPUCuPVYyQDlizszN Mnz5V2FPT1KHUh?=
HCC1187 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1rBdmlEPTB;MT6wNFUxPSEQvF2= MV7TRW5IWkWU
DU-4475 M1\y[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWPJR|UxRTFwMEG3OVYh|ryP NVnrbVdLW0GQR2LFVi=>
NKM-1 Ml\aS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2jke2lEPTB;MT6wNlc4PSEQvF2= MoDHV2FPT1KHUh?=
HL-60 M1Lnbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mk\JTWM2OD1zLkC2OVc1KM7:TR?= M{n1V3NCVkeURWK=
SBC-1 M170OGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3i3b2lEPTB;MT6xNlU1OiEQvF2= NGHhTm1USU6JUlXS
TE-10 MkLnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFP1Z|dKSzVyPUGuNVI6PDZizszN M{i3SHNCVkeURWK=
ETK-1 NYPwS4lqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn\2TWM2OD1zLkGzOlE{KM7:TR?= NG\tdpVUSU6JUlXS
HAL-01 MoS1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXLJR|UxRTFwMU[3NFkh|ryP M{LmVXNCVkeURWK=
BB65-RCC MoH3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUDWWm93UUN3ME2xMlE5ODB3IN88US=> M{jaWHNCVkeURWK=
EW-1 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGTpRm1KSzVyPUGuNVg2PjJizszN MnHiV2FPT1KHUh?=
SK-NEP-1 M2L5WGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIrB[Y5KSzVyPUGuNlEyOTFizszN M{LkXHNCVkeURWK=
SK-LMS-1 NEDOXldIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkjyTWM2OD1zLkKyNlEzKM7:TR?= NWnlO2NUW0GQR2LFVi=>
DEL MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX64XlhYUUN3ME2xMlI2PjR|IN88US=> MXTTRW5IWkWU
GT3TKB M1nsb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3TJXGlEPTB;MT6yPFA2PyEQvF2= NGi3WppUSU6JUlXS
MOLT-16 NWHtc5M{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYq5WmY{UUN3ME2xMlM2PDB3IN88US=> NXPHOW04W0GQR2LFVi=>
CMK NFLoSmxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIfYd|ZKSzVyPUGuOFIyOTdizszN NEnSb3VUSU6JUlXS
NB5 NHP3R21Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NG\3cnJKSzVyPUGuOlQzOjlizszN MYfTRW5IWkWU
NCI-H1963 NVLNZ21CT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFzTcmdKSzVyPUGuO|A2QDNizszN MnjOV2FPT1KHUh?=
KURAMOCHI MnK0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWjJR|UxRTFwN{i5NVEh|ryP NIm4R5JUSU6JUlXS
TE-8 NUfQTXlFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWHwSVZzUUN3ME2xMlgxOzZ6IN88US=> MXPTRW5IWkWU
NCI-H1304 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MofPTWM2OD1zLkizNFc{KM7:TR?= MmO3V2FPT1KHUh?=
A101D NFrXXYFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn;5TWM2OD1zLki3N|k2KM7:TR?= NWPQSHAzW0GQR2LFVi=>
SCLC-21H MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3LUVGlEPTB;MT65O|A2PyEQvF2= MYHTRW5IWkWU
GB-1 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX;UTnVIUUN3ME2yMlAyPjR5IN88US=> MlnzV2FPT1KHUh?=
KARPAS-45 NUjZPIc3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M13NNWlEPTB;Mj6wNlY2PCEQvF2= M3myPHNCVkeURWK=
ATN-1 MmjJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVnJR|UxRTJwMEK4OVgh|ryP NWrzS3F{W0GQR2LFVi=>
NCI-H720 NGDZc|lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MULJR|UxRTJwME[yOFQh|ryP MYnTRW5IWkWU
RPMI-6666 NUnM[ZdRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHHnc|VKSzVyPUKuNVYzODdizszN NY[4SVd7W0GQR2LFVi=>
NB17 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF7VUWdKSzVyPUKuNlkzPyEQvF2= MmLhV2FPT1KHUh?=
IST-SL1 M{XieWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFO4THdKSzVyPUKuNlk4PjVizszN M4rxPXNCVkeURWK=
SH-4 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVTKdWhCUUN3ME2yMlMzPDZ7IN88US=> NWqzRmhNW0GQR2LFVi=>
K5 MlrxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkfFTWM2OD1{LkSwN|E6KM7:TR?= NYXtN5pEW0GQR2LFVi=>
OVCAR-4 NIX4VW9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1jIdGlEPTB;Mj60OlE{KM7:TR?= M2q4NXNCVkeURWK=
ACN MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NULTTlVMUUN3ME2yMlUxOjF|IN88US=> MV\TRW5IWkWU
TGW M3j5e2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV3JR|UxRTJwNkW4N|Ih|ryP NFe2ZlBUSU6JUlXS
NCI-H2107 M1vaemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF7Zd|JKSzVyPUKuPFM4OTFizszN NGCxWFlUSU6JUlXS
NCI-H82 NXe1c2FHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEnmZXZKSzVyPUKuPFM5OzhizszN MVXTRW5IWkWU
SK-N-FI MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGj6NZNKSzVyPUKuPFY5PjhizszN MWHTRW5IWkWU
LB1047-RCC MnTkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXXJR|UxRTJwOEixNlYh|ryP MnzrV2FPT1KHUh?=
LU-134-A MkDLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXPJR|UxRTJwOEmyOkDPxE1? M4rJPXNCVkeURWK=
NCI-H209 NH3rWZRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH7KdZJKSzVyPUKuPVEzPTNizszN NH\G[pFUSU6JUlXS
NOMO-1 NYfte2VQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{ixO2lEPTB;Mz6wNlI4PCEQvF2= M3nEVXNCVkeURWK=
RH-1 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVXJR|UxRTNwMUeyPVEh|ryP MoLMV2FPT1KHUh?=
LOUCY MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVLJR|UxRTNwMUi2PVMh|ryP NFXyeZBUSU6JUlXS
TE-9 M4j5PWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3i0R2lEPTB;Mz6yOlc{PiEQvF2= NGL6UY9USU6JUlXS
PF-382 NFrkVYZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVHw[GlqUUN3ME2zMlM2Pzd6IN88US=> MmXGV2FPT1KHUh?=
RPMI-8402 NF7DPXNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnL4TWM2OD1|LkW4OlA{KM7:TR?= MXrTRW5IWkWU
HEL NHm1UZRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGracHJKSzVyPUOuOlMzKM7:TR?= MnXsV2FPT1KHUh?=
NOS-1 NUnZb5pkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXHJR|UxRTNwOES3OVQh|ryP M{jZSnNCVkeURWK=
ES1 Mo\xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFzySpZKSzVyPUOuPVIzQTNizszN MWPTRW5IWkWU
NCI-H2171 NHr6NlVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MojFTWM2OD1|LkmyOFI{KM7:TR?= MWTTRW5IWkWU
NCI-H747 NVPS[lZqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGP3PG5KSzVyPUOuPVQzOjFizszN MUnTRW5IWkWU
MHH-NB-11 M{XU[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2foemlEPTB;Mz65OVMyOiEQvF2= M2LDfXNCVkeURWK=
MZ1-PC M1P6OGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYnhboxsUUN3ME2zMlk6OjRizszN MUPTRW5IWkWU
MMAC-SF M1[xSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnnGTWM2OD12LkCyOFY4KM7:TR?= MnPIV2FPT1KHUh?=
NMC-G1 M2\jdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWXJR|UxRTRwMkK3NlMh|ryP M1rQeXNCVkeURWK=
SW872 NIPa[2RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIS4eZNKSzVyPUSuN|Q{PCEQvF2= M{Xu[HNCVkeURWK=
TE-12 NIXXfJhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoD4TWM2OD12LkW2N|k1KM7:TR?= NXnxW2RqW0GQR2LFVi=>
LU-139 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX7iT|lWUUN3ME20MlYyQDN3IN88US=> NGTxfHlUSU6JUlXS
HC-1 NEW0dFhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlPDTWM2OD12Lk[5OFk1KM7:TR?= NI\HVoJUSU6JUlXS
COR-L279 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYrJR|UxRTRwN{W4PVEh|ryP MnfQV2FPT1KHUh?=
SF268 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGTwTFdKSzVyPUSuO|k6OTZizszN NFH4e4dUSU6JUlXS
MC-CAR MkX5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYTJR|UxRTVwME[3OVch|ryP NFfqWXhUSU6JUlXS
TK10 NX6ycnU4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYDONnBOUUN3ME21MlM2PDZ7IN88US=> MkOxV2FPT1KHUh?=
TE-1 NVvPXWhST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NILaVFhKSzVyPUWuOFkxODRizszN MlnKV2FPT1KHUh?=
NCI-H2126 NUjGNZcxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGW3VYpKSzVyPUWuOlQ2PzRizszN NUfufVhQW0GQR2LFVi=>
Daudi MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnTTTWM2OD13Lk[5NVIh|ryP MUPTRW5IWkWU
NCI-H1648 NET1So9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4PrdGlEPTB;NT64NVQ2PCEQvF2= NI\2RmlUSU6JUlXS
OS-RC-2 NHy5[oFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlnOTWM2OD13Lkm4OVk4KM7:TR?= NHj1SmJUSU6JUlXS
DJM-1 M{T4Z2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml\wTWM2OD14LkO0OlY3KM7:TR?= NYnac3BVW0GQR2LFVi=>
LS-1034 NH;SRlhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYSxfItrUUN3ME22Mlc2PjZizszN MX;TRW5IWkWU
NCI-H1581 MmDrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnO1TWM2OD14Lke4OFA2KM7:TR?= Mnm2V2FPT1KHUh?=
UACC-257 MkXDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXOxW|BqUUN3ME23MlA1PTF{IN88US=> MXPTRW5IWkWU
KM-H2 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGLve5NKSzVyPUeuNVg1PTdizszN NIXDUVZUSU6JUlXS
NCI-H1436 NYjtSJVxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWnJR|UxRTdwNkm5N|Ih|ryP MoLiV2FPT1KHUh?=
IA-LM NVj5SJRMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUfJR|UxRTdwOEW5JO69VQ>? M3f0OnNCVkeURWK=
NCI-H526 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWDJR|UxRThwMkW2N|ch|ryP NYDweJJlW0GQR2LFVi=>
GCIY M2HlVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV\JR|UxRThwM{[5OlUh|ryP NXmxTlRSW0GQR2LFVi=>
CP67-MEL M1n2fGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGW4OG1KSzVyPUiuOVMzPiEQvF2= NF3MbldUSU6JUlXS
KALS-1 Mn;NS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYHtWGRzUUN3ME24Mlg{QDVzIN88US=> NH\wWWZUSU6JUlXS
NCI-H1770 M1;6Smdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{XMcGlEPTB;OD65NFI3PSEQvF2= NX;rWZRTW0GQR2LFVi=>
8-MG-BA M{DkfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlzYTWM2OD17LkOyPFQ1KM7:TR?= MUnTRW5IWkWU
KY821 NWjxbHY6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUDOWpNlUUN3ME25Mlc4PDh2IN88US=> NWnx[VB5W0GQR2LFVi=>
SNB75 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2TPZmlEPTB;MUCuNFc3KM7:TR?= MkPmV2FPT1KHUh?=
NCCIT NHLxPY5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIGzNZJKSzVyPUGxMlA2QDJizszN M4W3bnNCVkeURWK=
SJSA-1 NV\Z[mZGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEnmWFVKSzVyPUGxMlI5QTFizszN M{f3N3NCVkeURWK=
LB373-MEL-D NX;GZW1[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYDae3BqUUN3ME2xNU4{QDJ5IN88US=> M4DCZXNCVkeURWK=
TALL-1 M4C4T2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX[4N5N{UUN3ME2xNU41ODV6IN88US=> Mln2V2FPT1KHUh?=
NB69 Mo\GS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEjRfpVKSzVyPUGxMlc4ODVizszN NIP6cIRUSU6JUlXS
NCI-H1355 Mm\qS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkLkTWM2OD1zMT65OFI3KM7:TR?= MXzTRW5IWkWU
DMS-153 NUjMWGlFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXPJR|UxRTF{LkC0NlYh|ryP MkH6V2FPT1KHUh?=
OPM-2 M{nKS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXrJR|UxRTF{LkG1PVYh|ryP NFf3V41USU6JUlXS
NB1 NEDrSopIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFXWc2RKSzVyPUGyMlI6KM7:TR?= MU\TRW5IWkWU
A3-KAW NITETotIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3y1fWlEPTB;MUKuN|I{PiEQvF2= Mlm0V2FPT1KHUh?=
NCI-H1882 NFTJV|lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MW\JR|UxRTF{LkSwOlYh|ryP NVnIZ|JpW0GQR2LFVi=>
KG-1 M2PrSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml3XTWM2OD1zMj62OVQ2KM7:TR?= Mle4V2FPT1KHUh?=
LC4-1 Ml\PS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX3CeHlQUUN3ME2xNk44PzB4IN88US=> NXPSV|lXW0GQR2LFVi=>
HCE-T M4\YPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NU\6XJZFUUN3ME2xN{4xODR7IN88US=> Ml3uV2FPT1KHUh?=
NEC8 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGHtbVBKSzVyPUGzMlExOzhizszN NFnY[JpUSU6JUlXS
IST-MEL1 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVHJR|UxRTF|LkW3PFgh|ryP MnzHV2FPT1KHUh?=
EW-3 M4LQfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NETTXWZKSzVyPUGzMlc1ODJizszN NUnuXYZbW0GQR2LFVi=>
CTB-1 NFnCOXRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mln3TWM2OD1zND6wN|I6KM7:TR?= M2jIeHNCVkeURWK=
LS-123 NI\rZ4VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUPBXZlsUUN3ME2xOE4yPTh6IN88US=> MVXTRW5IWkWU
NCI-H1417 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkDuTWM2OD1zND6zNFUzKM7:TR?= NETYR4tUSU6JUlXS
MZ7-mel MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoryTWM2OD1zND60OFM{KM7:TR?= NFK3ZYFUSU6JUlXS
JiyoyeP-2003 NXHGU3RKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlO4TWM2OD1zNT62N|I3KM7:TR?= MnP1V2FPT1KHUh?=
ES6 NVm0cVZYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVnIPItsUUN3ME2xOk4zOzZzIN88US=> MlHLV2FPT1KHUh?=
HH MmrRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NULqOlZ1UUN3ME2xO{4yQTZ|IN88US=> NVLuNWpWW0GQR2LFVi=>
SF539 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYC2cHpzUUN3ME2xO{46QTJ{IN88US=> MlG3V2FPT1KHUh?=
Calu-6 NXeyTnF[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYrJR|UxRTF7LkKzPUDPxE1? NEXIPItUSU6JUlXS
SK-MM-2 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUm0V25iUUN3ME2xPU42PTVizszN MmjCV2FPT1KHUh?=
IST-MES1 MlTqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVriZmo2UUN3ME2xPU43PjZ|IN88US=> NXzZcZFNW0GQR2LFVi=>
GI-ME-N MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVXJR|UxRTF7LkiyNlch|ryP M1i4UnNCVkeURWK=
CAL-148 Mn7iS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{nydWlEPTB;MkCuPVk{PCEQvF2= MoLUV2FPT1KHUh?=
EVSA-T Mn3qS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH3XPWRKSzVyPUKxMlE1QTlizszN M3\IWHNCVkeURWK=
LP-1 NWPjWllsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXLYdnlSUUN3ME2yNU4{PDN{IN88US=> NIfMZ|dUSU6JUlXS
BOKU MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4nEdGlEPTB;MkGuOFU{OyEQvF2= NU\sWZlCW0GQR2LFVi=>
KLE NYfQfWJVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWjOPGZUUUN3ME2yNk4yQTB|IN88US=> MXfTRW5IWkWU
LB831-BLC NELsOZpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{TkZmlEPTB;MkWuNVUzPiEQvF2= NFezNndUSU6JUlXS
NCI-H889 NHjkUVZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3Ty[WlEPTB;MkWuNVk{OSEQvF2= NW\DXGNlW0GQR2LFVi=>
REH NEfZ[HdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVj2emJpUUN3ME2yOU41PjdzIN88US=> NFvWeVhUSU6JUlXS
KP-N-RT-BM-1 Mlv6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3\jRWlEPTB;MkWuOFc2OiEQvF2= M4PjR3NCVkeURWK=
MPP-89 M3PLeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVLJR|UxRTJ3LkWzNVQh|ryP NGjVRXlUSU6JUlXS
no-11 NUHsWFBET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4\sUmlEPTB;MkWuO|Q4KM7:TR?= M37HXHNCVkeURWK=
NCI-H748 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHjNO49KSzVyPUK1Mlc3OjdizszN NIf2RVNUSU6JUlXS
LB2518-MEL MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUDn[5c3UUN3ME2yO{4yPzd|IN88US=> NXfmc|VIW0GQR2LFVi=>
TGBC1TKB NXPSR3lFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX3JR|UxRTJ5LkW1PFUh|ryP NFK5UldUSU6JUlXS
MHH-PREB-1 M4HYUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVXJR|UxRTJ6LkC3N|Qh|ryP Ml;BV2FPT1KHUh?=
MZ2-MEL MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoHiTWM2OD1{OD62NVQ{KM7:TR?= M3TBZXNCVkeURWK=
U-266 NEPhWIlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1jXXmlEPTB;MkiuOlM3PiEQvF2= M3rVXnNCVkeURWK=
SNU-C1 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NULhWY8zUUN3ME2yPE46PDNizszN M3ux[nNCVkeURWK=
SW962 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVXJR|UxRTNyLkK3OFch|ryP MUDTRW5IWkWU
Raji NUS4OoxJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{XYTmlEPTB;M{CuOVU6OiEQvF2= M3i4UnNCVkeURWK=
KNS-42 NHf2[5pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NInhOoFKSzVyPUOwMlg6PTZizszN MULTRW5IWkWU
LB996-RCC NUXYZotsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWHJR|UxRTNzLkG3NFIh|ryP MVzTRW5IWkWU
CHP-126 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXvBfm5pUUN3ME2zNU4yQTh2IN88US=> MknsV2FPT1KHUh?=
RXF393 NH3Z[HlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1voVmlEPTB;M{KuOFk4KM7:TR?= MlKzV2FPT1KHUh?=
COLO-684 M1TZUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGCw[FRKSzVyPUOyMlY1OzhizszN MWnTRW5IWkWU
A704 MkPhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYGwU2xwUUN3ME2zN{42PTN6IN88US=> M1LsVXNCVkeURWK=
A253 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH:1e4xKSzVyPUOzMlU5PTJizszN NIG4Z4JUSU6JUlXS
KNS-81-FD M4jxSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MknjTWM2OD1|ND61OFU3KM7:TR?= MYDTRW5IWkWU
TE-441-T MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mm\sTWM2OD1|ND62N|cyKM7:TR?= NVrkSHZ5W0GQR2LFVi=>
HCC2157 M2SzWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEHLOJdKSzVyPUO1MlQ3OTlizszN M{TFOXNCVkeURWK=
ES3 M{nqTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFGx[lJKSzVyPUO2MlY4PSEQvF2= Mn\6V2FPT1KHUh?=
NCI-H1155 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3\BcWlEPTB;M{euPFE2KM7:TR?= NIHV[VFUSU6JUlXS
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JAR MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MY\JR|UxRTN6LkK0OFkh|ryP NXu1TVFlW0GQR2LFVi=>
GDM-1 NYPGe2xmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIjtZopKSzVyPUO4MlkyOTZizszN NHfoe4VUSU6JUlXS
KU812 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MknvTWM2OD12MT61NFch|ryP MWjTRW5IWkWU
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NCI-H1694 M{izfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXPJR|UxRTR2Lkm0O|Ih|ryP NYHw[Y1sW0GQR2LFVi=>
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LS-513 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF7xRnNKSzVyPUS1MlkyPTZizszN M2TldXNCVkeURWK=
HD-MY-Z MnrjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYLST3k1UUN3ME20Ok41PjF{IN88US=> NX72VXpyW0GQR2LFVi=>
L-363 M3TYZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mnz4TWM2OD12Nj64PFEh|ryP M3W3UXNCVkeURWK=
TE-6 M1TOOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVPJR|UxRTR6LkS0OkDPxE1? NISxSIxUSU6JUlXS
NCI-H345 MkPsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoTpTWM2OD12OD60Olgh|ryP M{PNTXNCVkeURWK=
TE-5 NGLN[3lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEewb5BKSzVyPUS5MlcyOThizszN MmjaV2FPT1KHUh?=

... 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
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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
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  • 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
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  • 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

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

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
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    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
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Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

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To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00500006 Terminated Chronic Myelogenous Leukemia|Leukemia, Lymphoblastic, Acute, Philadelphia-Positive Merck Sharp & Dohme Corp. October 2007 Phase 1
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
NCT00104351 Terminated Cancer Merck Sharp & Dohme Corp. May 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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Aurora Kinase Signaling Pathway Map

Aurora Kinase Inhibitors with Unique Features

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID