Tozasertib (VX-680, MK-0457)

Catalog No.S1048

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

Molecular Weight(MW): 464.59

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

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Cited by 38 Publications

16 Customer Reviews

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

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

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

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

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

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

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

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

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

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

     

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

Purity & Quality Control

Choose Selective Aurora Kinase Inhibitors

Biological Activity

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

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

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
BE-13 M{CxPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mmq1TWM2OD1yLkCwN|M5KM7:TR?= M4\RWHNCVkeURWK=
RS4-11 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4P5O2lEPTB;MD6wNFQxPCEQvF2= M1rQXXNCVkeURWK=
MFH-ino MmLNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHPsNodKSzVyPUCuNFA6QSEQvF2= MlP4V2FPT1KHUh?=
NTERA-S-cl-D1 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NY\4fnRRUUN3ME2wMlAyPDN2IN88US=> NY\xe|A2W0GQR2LFVi=>
697 M3r4fmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2rG[mlEPTB;MD6wNlQ4OSEQvF2= MYLTRW5IWkWU
NALM-6 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHrONVNKSzVyPUCuNFI2PTJizszN MlnHV2FPT1KHUh?=
ES8 M{\3N2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXnYNXI2UUN3ME2wMlA1PjF|IN88US=> MUHTRW5IWkWU
HUTU-80 NU[2NZAyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGTQRWNKSzVyPUCuNFUzQTlizszN NGHHTohUSU6JUlXS
MV-4-11 M3vrdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVPJR|UxRTBwMEe3PFIh|ryP NY\sXZRqW0GQR2LFVi=>
MONO-MAC-6 M4fmc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4fXR2lEPTB;MD6wO|g4QSEQvF2= MnjOV2FPT1KHUh?=
LC-2-ad NEXLPJNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWOwcXV5UUN3ME2wMlA5Pzh7IN88US=> NHPXU5NUSU6JUlXS
BL-41 NWPidFk4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkfWTWM2OD1yLkGwOFQ2KM7:TR?= NUXLZnpNW0GQR2LFVi=>
A4-Fuk NWPmNINRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mmf3TWM2OD1yLkGxOVY{KM7:TR?= MVfTRW5IWkWU
SW954 M2GxTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVPzNmJHUUN3ME2wMlEzOjJ7IN88US=> NYrSbpg{W0GQR2LFVi=>
BV-173 MmG0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1uyW2lEPTB;MD6xNlY1OSEQvF2= NVTPd4ZRW0GQR2LFVi=>
TE-11 NVmySWFWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGDybFBKSzVyPUCuNVQ6QDJizszN Mn\MV2FPT1KHUh?=
SK-UT-1 NGS5WpdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3XLTGlEPTB;MD6xOVk3PSEQvF2= MVvTRW5IWkWU
SIG-M5 Moj2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYPJR|UxRTBwMU[3NFch|ryP NWXuW4VpW0GQR2LFVi=>
OCUB-M NWX6TWdoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXjJR|UxRTBwMU[5PFMh|ryP M3HMRnNCVkeURWK=
K052 NWDu[IlrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkHvTWM2OD1yLkG5OFgh|ryP MVfTRW5IWkWU
VA-ES-BJ M3:1TWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIfMTGNKSzVyPUCuNlAxQDZizszN M3;Ne3NCVkeURWK=
SW982 MlTZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlfXTWM2OD1yLkKxN|gh|ryP M4ezNHNCVkeURWK=
LB647-SCLC NUXMTWlsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVXDWndoUUN3ME2wMlIyPTJ|IN88US=> MkLuV2FPT1KHUh?=
PSN1 NVvXd|dET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{e1TGlEPTB;MD6yNlAzPiEQvF2= MmryV2FPT1KHUh?=
BB30-HNC NWjTdnJ7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGCxS4xKSzVyPUCuNlI2QTFizszN MUnTRW5IWkWU
ST486 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHf2XFVKSzVyPUCuNlMxQDdizszN MlfuV2FPT1KHUh?=
MOLT-4 NIHOTJBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGrVO4FKSzVyPUCuNlM{OzdizszN M13xTnNCVkeURWK=
EW-16 NInqR5pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnvpTWM2OD1yLkKzO|Y5KM7:TR?= M3i2c3NCVkeURWK=
KS-1 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1yzcGlEPTB;MD6yN|c5PSEQvF2= NVrSPWx7W0GQR2LFVi=>
SR NHvhV2pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4[1OGlEPTB;MD6yOFU3PCEQvF2= MmTpV2FPT1KHUh?=
KM12 NILyO|ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUPJR|UxRTBwMk[zOkDPxE1? M4KyV3NCVkeURWK=
EM-2 M4La[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2PzOmlEPTB;MD6yOlY1OSEQvF2= NUXM[2lYW0GQR2LFVi=>
MEG-01 NF;oTHZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml;jTWM2OD1yLkK3PFQ6KM7:TR?= NXXabIdVW0GQR2LFVi=>
NB13 MoTWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4q2WGlEPTB;MD6yO|k5PCEQvF2= M4\wSXNCVkeURWK=
RKO NWDKUGk4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWnHVmkyUUN3ME2wMlMxQDF|IN88US=> NGCwdXpUSU6JUlXS
CESS NV3jTmJ1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlS3TWM2OD1yLkOxN|I5KM7:TR?= MXrTRW5IWkWU
EoL-1-cell NELIZ4JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{WwS2lEPTB;MD6zN|Q2QSEQvF2= M1q2Z3NCVkeURWK=
DOHH-2 NGLFbGVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHixepFKSzVyPUCuN|M4QDFizszN M{S0UHNCVkeURWK=
A388 M4W5WGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3PVemlEPTB;MD6zOFA5PiEQvF2= MkTMV2FPT1KHUh?=
LAMA-84 M{O5PGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3zYbWlEPTB;MD6zOVE4QCEQvF2= MWjTRW5IWkWU
IMR-5 M{DONmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYHVVYd1UUN3ME2wMlM2PTRizszN NFHIUXRUSU6JUlXS
KARPAS-422 NH7jSFhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3TsNmlEPTB;MD6zO|I4OiEQvF2= MXjTRW5IWkWU
MRK-nu-1 M4T0fmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGK0OmlKSzVyPUCuN|gyOyEQvF2= NIL0c49USU6JUlXS
BL-70 M2nVV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlPPTWM2OD1yLkO4PVc1KM7:TR?= MmLBV2FPT1KHUh?=
LXF-289 Mnn0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MULJR|UxRTBwNEC0NFYh|ryP NVH2NZRHW0GQR2LFVi=>
RL95-2 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEjCSJlKSzVyPUCuOFA2PjdizszN NEjNZWNUSU6JUlXS
QIMR-WIL NWHGXGh4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlP1TWM2OD1yLkSyOlc3KM7:TR?= Ml\GV2FPT1KHUh?=
K-562 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{nWVmlEPTB;MD60N|Q4OiEQvF2= MnHiV2FPT1KHUh?=
NCI-H510A M2O5bmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHvZbpdKSzVyPUCuOFM5OjNizszN NHHqd5NUSU6JUlXS
NCI-H524 MkD0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXTac2lmUUN3ME2wMlUyOTR5IN88US=> MV7TRW5IWkWU
KE-37 NXn0dVlpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3LXVWlEPTB;MD61NlExOiEQvF2= M{TLeXNCVkeURWK=
KP-N-YS Mn3sS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYHJR|UxRTBwNUSzPVIh|ryP NIfLSHRUSU6JUlXS
LS-411N M2jj[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnrJTWM2OD1yLkW3O|UzKM7:TR?= NGXZenpUSU6JUlXS
CTV-1 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmK2TWM2OD1yLkW4O|c{KM7:TR?= NVXQZYVoW0GQR2LFVi=>
NCI-SNU-16 M3LqbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MomzTWM2OD1yLk[zOVcyKM7:TR?= MV;TRW5IWkWU
HT-144 Mlv6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUnMZ5IzUUN3ME2wMlY{Pzl6IN88US=> MXPTRW5IWkWU
NCI-H187 M33tVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVjIbVBQUUN3ME2wMlY1OTNizszN M1WxPHNCVkeURWK=
OCI-AML2 M1PZO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWOwZpJbUUN3ME2wMlY1PDB|IN88US=> MnHTV2FPT1KHUh?=
CCRF-CEM MojmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYnTZVQyUUN3ME2wMlY2OzR4IN88US=> MUHTRW5IWkWU
ONS-76 NV[4TlV2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIn1[HNKSzVyPUCuOlY1PThizszN M1q2e3NCVkeURWK=
IST-SL2 MmDQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmHnTWM2OD1yLkexPVgzKM7:TR?= MVvTRW5IWkWU
NB6 NHm1bGxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NITtUYlKSzVyPUCuO|czPTRizszN MVrTRW5IWkWU
SK-PN-DW MkLhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGPpdG5KSzVyPUCuO|kyPCEQvF2= NUPYWVV{W0GQR2LFVi=>
HCC1599 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXf4b|J7UUN3ME2wMlgxQDd2IN88US=> Mny5V2FPT1KHUh?=
MC116 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFP3OIJKSzVyPUCuPFUxOTFizszN MlrPV2FPT1KHUh?=
TE-15 MljZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MW\JR|UxRTBwOEWwPVgh|ryP NUfZWWIxW0GQR2LFVi=>
HOP-62 MnHSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHT0[JBKSzVyPUCuPFY{OjlizszN MlrZV2FPT1KHUh?=
TGBC24TKB NEH4eFVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2HjPWlEPTB;MD64OlM5PSEQvF2= Mn;WV2FPT1KHUh?=
HCE-4 M13KW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1S3SmlEPTB;MD64PFA3OyEQvF2= MmfQV2FPT1KHUh?=
ALL-PO NIizfJJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NI\JRlBKSzVyPUCuPFgyPzVizszN MV7TRW5IWkWU
KGN MlTTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3Pu[mlEPTB;MD64PVk6PSEQvF2= NVLKTm51W0GQR2LFVi=>
ML-2 NV3WUpFKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXzJR|UxRTBwOUCyOVkh|ryP MnXMV2FPT1KHUh?=
ES4 M1\1T2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NE\WZppKSzVyPUCuPVEyOjhizszN NFexeFBUSU6JUlXS
SF126 MlixS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEPaN2FKSzVyPUCuPVQ5OTlizszN NHTuVHhUSU6JUlXS
SK-N-DZ MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NITMXHhKSzVyPUCuPVYyQDlizszN NYTKZlBrW0GQR2LFVi=>
HCC1187 NX23OJlvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1y4cGlEPTB;MT6wNFUxPSEQvF2= NYLtO|JFW0GQR2LFVi=>
DU-4475 MlPLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXvJR|UxRTFwMEG3OVYh|ryP MnfkV2FPT1KHUh?=
NKM-1 NHH3c5RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M17sSmlEPTB;MT6wNlc4PSEQvF2= NHjETZJUSU6JUlXS
HL-60 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGK0VGpKSzVyPUGuNFY2PzRizszN MmHhV2FPT1KHUh?=
SBC-1 NX72TFRXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1\lXGlEPTB;MT6xNlU1OiEQvF2= M4\NdnNCVkeURWK=
TE-10 MnnhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkPiTWM2OD1zLkGyPVQ3KM7:TR?= MVTTRW5IWkWU
ETK-1 NUTVZVZZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV;JR|UxRTFwMUO2NVMh|ryP NX\ySpdGW0GQR2LFVi=>
HAL-01 NYPNeoN1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUPJR|UxRTFwMU[3NFkh|ryP M3zGZXNCVkeURWK=
BB65-RCC MoPES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkK3TWM2OD1zLkG4NFA2KM7:TR?= NXfGdG1KW0GQR2LFVi=>
EW-1 NVf5eohVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV;JR|UxRTFwMUi1OlIh|ryP NIr5TotUSU6JUlXS
SK-NEP-1 NFqyO|RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MY\JR|UxRTFwMkGxNVEh|ryP NWDnVmY5W0GQR2LFVi=>
SK-LMS-1 NFPp[pZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1GwR2lEPTB;MT6yNlIyOiEQvF2= MUnTRW5IWkWU
DEL MnPjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1fMcGlEPTB;MT6yOVY1OyEQvF2= M1HSTHNCVkeURWK=
GT3TKB Mn;wS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mnr3TWM2OD1zLkK4NFU4KM7:TR?= MmXsV2FPT1KHUh?=
MOLT-16 NFHzR2NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFj3SWVKSzVyPUGuN|U1ODVizszN MkXIV2FPT1KHUh?=
CMK NEi3XY9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkPNTWM2OD1zLkSyNVE4KM7:TR?= MV3TRW5IWkWU
NB5 M2iyZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVrJR|UxRTFwNkSyNlkh|ryP NYToXYY4W0GQR2LFVi=>
NCI-H1963 NVi1b4UzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmTyTWM2OD1zLkewOVg{KM7:TR?= NEmyW4FUSU6JUlXS
KURAMOCHI Mn7OS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUfudGRmUUN3ME2xMlc5QTFzIN88US=> NV\HXZhoW0GQR2LFVi=>
TE-8 NHPycW1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYnxU4JPUUN3ME2xMlgxOzZ6IN88US=> MUnTRW5IWkWU
NCI-H1304 M1TKUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEL2Wo9KSzVyPUGuPFMxPzNizszN MULTRW5IWkWU
A101D MlTpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUHJR|UxRTFwOEezPVUh|ryP NVTDSYFJW0GQR2LFVi=>
SCLC-21H MmPCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUfJR|UxRTFwOUewOVch|ryP NY[1fG9{W0GQR2LFVi=>
GB-1 Mm\BS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHyyeFRKSzVyPUKuNFE3PDdizszN NWPnZ254W0GQR2LFVi=>
KARPAS-45 M{\DeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXvvRm1pUUN3ME2yMlAzPjV2IN88US=> NFXP[nRUSU6JUlXS
ATN-1 NH61NVBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX3ZdVhEUUN3ME2yMlAzQDV6IN88US=> MYrTRW5IWkWU
NCI-H720 NVHjOWJbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4HLRWlEPTB;Mj6wOlI1PCEQvF2= M{K0XHNCVkeURWK=
RPMI-6666 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mnm3TWM2OD1{LkG2NlA4KM7:TR?= NHuxbXlUSU6JUlXS
NB17 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4S0V2lEPTB;Mj6yPVI4KM7:TR?= M4PGXnNCVkeURWK=
IST-SL1 NE\4WIpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVrVUo9nUUN3ME2yMlI6PzZ3IN88US=> MoTrV2FPT1KHUh?=
SH-4 M1[xUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWnJR|UxRTJwM{K0Olkh|ryP MV3TRW5IWkWU
K5 M1LiTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHnGdWJKSzVyPUKuOFA{OTlizszN NHXIWodUSU6JUlXS
OVCAR-4 MmOwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NG\vfGFKSzVyPUKuOFYyOyEQvF2= NFrtOodUSU6JUlXS
ACN NUm0WIxnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV3JR|UxRTJwNUCyNVMh|ryP MWnTRW5IWkWU
TGW NWfXbFhOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1LDW2lEPTB;Mj62OVg{OiEQvF2= M3\uPXNCVkeURWK=
NCI-H2107 M4rGNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWfJR|UxRTJwOEO3NVEh|ryP NVPhdGI3W0GQR2LFVi=>
NCI-H82 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX3HNVVCUUN3ME2yMlg{QDN6IN88US=> NH;rTpRUSU6JUlXS
SK-N-FI M1XDfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUjFNnhpUUN3ME2yMlg3QDZ6IN88US=> NITT[ZRUSU6JUlXS
LB1047-RCC MmP4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV;0XXNLUUN3ME2yMlg5OTJ4IN88US=> MYHTRW5IWkWU
LU-134-A NHW0enhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWrEXYtxUUN3ME2yMlg6OjZizszN NFnBfVRUSU6JUlXS
NCI-H209 MoLKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmHsTWM2OD1{LkmxNlU{KM7:TR?= NGf0d3lUSU6JUlXS
NOMO-1 M1\XUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mlr4TWM2OD1|LkCyNlc1KM7:TR?= NX6xUpNuW0GQR2LFVi=>
RH-1 M1rMUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmjFTWM2OD1|LkG3NlkyKM7:TR?= NF;iS4xUSU6JUlXS
LOUCY M2GwZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkK4TWM2OD1|LkG4Olk{KM7:TR?= NE\EN5ZUSU6JUlXS
TE-9 Mn7SS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3zxZ2lEPTB;Mz6yOlc{PiEQvF2= M2PHcHNCVkeURWK=
PF-382 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGTNXplKSzVyPUOuN|U4PzhizszN MmTXV2FPT1KHUh?=
RPMI-8402 MljsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHzhfmpKSzVyPUOuOVg3ODNizszN MV3TRW5IWkWU
HEL MmXxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX7JR|UxRTNwNkOyJO69VQ>? MWXTRW5IWkWU
NOS-1 NGrlV3ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGnGbW5KSzVyPUOuPFQ4PTRizszN MoT1V2FPT1KHUh?=
ES1 NGi5SW1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3HBWWlEPTB;Mz65NlI6OyEQvF2= MnizV2FPT1KHUh?=
NCI-H2171 NIfXd|BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4j5U2lEPTB;Mz65NlQzOyEQvF2= MXTTRW5IWkWU
NCI-H747 MnLXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkLETWM2OD1|Lkm0NlIyKM7:TR?= MnLJV2FPT1KHUh?=
MHH-NB-11 M2T5U2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVi0bIxQUUN3ME2zMlk2OzF{IN88US=> MXjTRW5IWkWU
MZ1-PC MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVLGS2xnUUN3ME2zMlk6OjRizszN MV;TRW5IWkWU
MMAC-SF NUPpOFhJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2XRXGlEPTB;ND6wNlQ3PyEQvF2= NIntfHVUSU6JUlXS
NMC-G1 NHHuPYtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkC4TWM2OD12LkKyO|I{KM7:TR?= Mkn4V2FPT1KHUh?=
SW872 M3:wPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnzJTWM2OD12LkO0N|Qh|ryP MofwV2FPT1KHUh?=
TE-12 NWjKO4pST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NETib3ZKSzVyPUSuOVY{QTRizszN MUjTRW5IWkWU
LU-139 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH\hZllKSzVyPUSuOlE5OzVizszN MmqyV2FPT1KHUh?=
HC-1 M4Lve2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXvJR|UxRTRwNkm0PVQh|ryP MoH1V2FPT1KHUh?=
COR-L279 NVjENWpGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWDJR|UxRTRwN{W4PVEh|ryP M4\jSnNCVkeURWK=
SF268 NXnM[Ww1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGnMS4FKSzVyPUSuO|k6OTZizszN Ml3iV2FPT1KHUh?=
MC-CAR NIDDZodIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHmxT2NKSzVyPUWuNFY4PTdizszN MlP6V2FPT1KHUh?=
TK10 NX3SfVNRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnLyTWM2OD13LkO1OFY6KM7:TR?= M2LPTnNCVkeURWK=
TE-1 NIXPW5pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlOyTWM2OD13LkS5NFA1KM7:TR?= Mo\tV2FPT1KHUh?=
NCI-H2126 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUPJR|UxRTVwNkS1O|Qh|ryP MlnZV2FPT1KHUh?=
Daudi Mn;YS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{LDcWlEPTB;NT62PVEzKM7:TR?= MoPqV2FPT1KHUh?=
NCI-H1648 NFPrPWRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYr2Ulk3UUN3ME21MlgyPDV2IN88US=> M3:2cHNCVkeURWK=
OS-RC-2 MnrzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGm2VG1KSzVyPUWuPVg2QTdizszN M3;vcnNCVkeURWK=
DJM-1 NWLYfZlJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2fmc2lEPTB;Nj6zOFY3PiEQvF2= NEHRZ2RUSU6JUlXS
LS-1034 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MljYTWM2OD14Lke1OlYh|ryP NHq5XYxUSU6JUlXS
NCI-H1581 M4e5U2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHj1XmhKSzVyPU[uO|g1ODVizszN MlzEV2FPT1KHUh?=
UACC-257 M4\IbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml7uTWM2OD15LkC0OVEzKM7:TR?= NGj3dlJUSU6JUlXS
KM-H2 MlXhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXKzXmNRUUN3ME23MlE5PDV5IN88US=> MoPsV2FPT1KHUh?=
NCI-H1436 NVXvXFlQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnnJTWM2OD15Lk[5PVMzKM7:TR?= MWDTRW5IWkWU
IA-LM Mn3wS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3q3WmlEPTB;Nz64OVkh|ryP MmnjV2FPT1KHUh?=
NCI-H526 NUXTWXNQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYC5UnJFUUN3ME24MlI2PjN5IN88US=> MYrTRW5IWkWU
GCIY NWfDb4FHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{G1bGlEPTB;OD6zOlk3PSEQvF2= M1HzPHNCVkeURWK=
CP67-MEL NGG3OZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4PvV2lEPTB;OD61N|I3KM7:TR?= NYGxdmc{W0GQR2LFVi=>
KALS-1 NUOwXYNrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX3DN2s1UUN3ME24Mlg{QDVzIN88US=> M1zhSHNCVkeURWK=
NCI-H1770 MmizS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4DGT2lEPTB;OD65NFI3PSEQvF2= M4XvUnNCVkeURWK=
8-MG-BA M1\4Smdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWfJR|UxRTlwM{K4OFQh|ryP M3HxfXNCVkeURWK=
KY821 M3\nWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFXxfIFKSzVyPUmuO|c1QDRizszN NVj5WIZPW0GQR2LFVi=>
SNB75 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYLJR|UxRTFyLkC3OkDPxE1? NFqwUllUSU6JUlXS
NCCIT MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1;1eGlEPTB;MUGuNFU5OiEQvF2= NVi0ZYZiW0GQR2LFVi=>
SJSA-1 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{DJO2lEPTB;MUGuNlg6OSEQvF2= MW\TRW5IWkWU
LB373-MEL-D MnKxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnvWTWM2OD1zMT6zPFI4KM7:TR?= NF3MUXlUSU6JUlXS
TALL-1 Ml7BS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXHVcZNmUUN3ME2xNU41ODV6IN88US=> M{jkeHNCVkeURWK=
NB69 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{HwO2lEPTB;MUGuO|cxPSEQvF2= NUXpOYp3W0GQR2LFVi=>
NCI-H1355 NVPIWXhrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH[xWHRKSzVyPUGxMlk1OjZizszN MnPWV2FPT1KHUh?=
DMS-153 M1jqRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFHWZnZKSzVyPUGyMlA1OjZizszN NIXpbVdUSU6JUlXS
OPM-2 M1LkRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUXJR|UxRTF{LkG1PVYh|ryP NVfGbpR[W0GQR2LFVi=>
NB1 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoXXTWM2OD1zMj6yPUDPxE1? NEHEcZNUSU6JUlXS
A3-KAW MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NW\WdWprUUN3ME2xNk4{OjN4IN88US=> Ml70V2FPT1KHUh?=
NCI-H1882 NWfPR4w5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHjwdG9KSzVyPUGyMlQxPjZizszN NHPUSpFUSU6JUlXS
KG-1 NU\JeYtxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NInRd3JKSzVyPUGyMlY2PDVizszN MnrHV2FPT1KHUh?=
LC4-1 NXPUfpR5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4iyV2lEPTB;MUKuO|cxPiEQvF2= MoLsV2FPT1KHUh?=
HCE-T NUK0OZBtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUfaRmVDUUN3ME2xN{4xODR7IN88US=> NHj2bYlUSU6JUlXS
NEC8 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmHrTWM2OD1zMz6xNFM5KM7:TR?= NFrV[XNUSU6JUlXS
IST-MEL1 NYDyRYsxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH[3[WZKSzVyPUGzMlU4QDhizszN MWHTRW5IWkWU
EW-3 NVjiVYRGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVXJR|UxRTF|Lke0NFIh|ryP NX70VIRVW0GQR2LFVi=>
CTB-1 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{HMe2lEPTB;MUSuNFMzQSEQvF2= NGDnPHZUSU6JUlXS
LS-123 M{\LUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFvyZ2tKSzVyPUG0MlE2QDhizszN NVrFSWpEW0GQR2LFVi=>
NCI-H1417 NEC3O4pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlvJTWM2OD1zND6zNFUzKM7:TR?= M3LkeHNCVkeURWK=
MZ7-mel MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYGzXo81UUN3ME2xOE41PDN|IN88US=> NIHvdVBUSU6JUlXS
JiyoyeP-2003 NUjiOZhUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXnkNm97UUN3ME2xOU43OzJ4IN88US=> NHu1d|RUSU6JUlXS
ES6 MljNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIPxW4hKSzVyPUG2MlI{PjFizszN NXPZZlJXW0GQR2LFVi=>
HH M3r4Omdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWrJR|UxRTF5LkG5OlMh|ryP M3zHVHNCVkeURWK=
SF539 MmjDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGO5c3dKSzVyPUG3Mlk6OjJizszN M2nY[3NCVkeURWK=
Calu-6 NXznfpN{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGfCfG1KSzVyPUG5MlI{QSEQvF2= Mn6wV2FPT1KHUh?=
SK-MM-2 NGrnTW9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M13KbGlEPTB;MUmuOVU2KM7:TR?= MWDTRW5IWkWU
IST-MES1 MnvlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4fqW2lEPTB;MUmuOlY3OyEQvF2= MonUV2FPT1KHUh?=
GI-ME-N NWjaWXJHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUDJR|UxRTF7LkiyNlch|ryP MXvTRW5IWkWU
CAL-148 M4\XU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIXoe4hKSzVyPUKwMlk6OzRizszN M1vhfHNCVkeURWK=
EVSA-T MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYDDN4JoUUN3ME2yNU4yPDl7IN88US=> MWfTRW5IWkWU
LP-1 NXixZ3lRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXzKS5ZpUUN3ME2yNU4{PDN{IN88US=> NWnKOZNEW0GQR2LFVi=>
BOKU NUi1WJVKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1S0TGlEPTB;MkGuOFU{OyEQvF2= M3PYT3NCVkeURWK=
KLE MorrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1fXUWlEPTB;MkKuNVkxOyEQvF2= NF7PXYhUSU6JUlXS
LB831-BLC NGPkTIRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkTJTWM2OD1{NT6xOVI3KM7:TR?= NVLNd2VsW0GQR2LFVi=>
NCI-H889 NVntc3ZxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmXrTWM2OD1{NT6xPVMyKM7:TR?= MYjTRW5IWkWU
REH M{TsO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2TWUGlEPTB;MkWuOFY4OSEQvF2= NFLZSFNUSU6JUlXS
KP-N-RT-BM-1 NI\3bYJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWPHb4hDUUN3ME2yOU41PzV{IN88US=> NXjTWo5NW0GQR2LFVi=>
MPP-89 NHnkRlJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoX1TWM2OD1{NT61N|E1KM7:TR?= MmTOV2FPT1KHUh?=
no-11 MkDGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFrUd4pKSzVyPUK1Mlc1PyEQvF2= M{PjOXNCVkeURWK=
NCI-H748 M2\ZU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2\G[2lEPTB;MkWuO|YzPyEQvF2= MlrPV2FPT1KHUh?=
LB2518-MEL MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIC4SlFKSzVyPUK3MlE4PzNizszN NVTxPGRuW0GQR2LFVi=>
TGBC1TKB MoTnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX\vTnVRUUN3ME2yO{42PTh3IN88US=> M2LFfXNCVkeURWK=
MHH-PREB-1 M{j4XWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGO0WVBKSzVyPUK4MlA4OzRizszN NFPrOWxUSU6JUlXS
MZ2-MEL Mn\pS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Moe5TWM2OD1{OD62NVQ{KM7:TR?= NXfRU49VW0GQR2LFVi=>
U-266 M33Ld2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWrZ[W5YUUN3ME2yPE43OzZ4IN88US=> M3jmNHNCVkeURWK=
SNU-C1 NGfYdINIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{TDbmlEPTB;MkiuPVQ{KM7:TR?= NUPtVJBYW0GQR2LFVi=>
SW962 M3fGPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXnJR|UxRTNyLkK3OFch|ryP MVXTRW5IWkWU
Raji MnjES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3HwcmlEPTB;M{CuOVU6OiEQvF2= NV3neZNrW0GQR2LFVi=>
KNS-42 M1m3V2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEHBZohKSzVyPUOwMlg6PTZizszN MlzlV2FPT1KHUh?=
LB996-RCC MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUPzeGFHUUN3ME2zNU4yPzB{IN88US=> M4nHPXNCVkeURWK=
CHP-126 NWm5cIRET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml7LTWM2OD1|MT6xPVg1KM7:TR?= NWrVPWtqW0GQR2LFVi=>
RXF393 NU\nSItXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYPM[pFZUUN3ME2zNk41QTdizszN NXm2UFdIW0GQR2LFVi=>
COLO-684 NXzacGp[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3H1SmlEPTB;M{KuOlQ{QCEQvF2= NHvQc2tUSU6JUlXS
A704 NUfNcIh2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVPWNHo6UUN3ME2zN{42PTN6IN88US=> NWnxZYtEW0GQR2LFVi=>
A253 NHW5eYtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXnJR|UxRTN|LkW4OVIh|ryP NWHyUFJ6W0GQR2LFVi=>
KNS-81-FD NHXBWoFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEHIWlRKSzVyPUO0MlU1PTZizszN M2K0SnNCVkeURWK=
TE-441-T NXL4enVUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWTCWnFNUUN3ME2zOE43OzdzIN88US=> MX3TRW5IWkWU
HCC2157 M1Kwfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVXEUVI6UUN3ME2zOU41PjF7IN88US=> MYLTRW5IWkWU
ES3 NFzFfIdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXXpTJZkUUN3ME2zOk43PzVizszN Ml7HV2FPT1KHUh?=
NCI-H1155 M3rNXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXzJR|UxRTN5LkixOUDPxE1? M13oSXNCVkeURWK=
SNU-C2B MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkT6TWM2OD1|OD6xOlU1KM7:TR?= MoHOV2FPT1KHUh?=
JAR MoDBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mo\YTWM2OD1|OD6yOFQ6KM7:TR?= NIC1dmVUSU6JUlXS
GDM-1 NUDPTlI4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2WyeGlEPTB;M{iuPVEyPiEQvF2= NUnw[G1{W0GQR2LFVi=>
KU812 M2\lTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGnHdGpKSzVyPUSxMlUxPyEQvF2= NHPkcYlUSU6JUlXS
BC-1 M1G5c2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX\JR|UxRTR{Lk[3N|Eh|ryP MkTaV2FPT1KHUh?=
GI-1 M4\OSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MW\JR|UxRTR{LkmxPVIh|ryP MkD1V2FPT1KHUh?=
NCI-H1694 MknoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mkm0TWM2OD12ND65OFczKM7:TR?= NYHzUlNSW0GQR2LFVi=>
DG-75 NXX3d4ZRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXnJR|UxRTR3LkG1O|ch|ryP Mli4V2FPT1KHUh?=
COR-L88 NHnVVW1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWXJR|UxRTR3LkK3O|gh|ryP MX\TRW5IWkWU
LS-513 NE\HT2hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1\rbmlEPTB;NEWuPVE2PiEQvF2= NYK4PI9TW0GQR2LFVi=>
HD-MY-Z NFPpdWtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkTKTWM2OD12Nj60OlEzKM7:TR?= MoPLV2FPT1KHUh?=
L-363 NXTNdVNQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWLJR|UxRTR4Lki4NUDPxE1? MkT0V2FPT1KHUh?=
TE-6 M3LNd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MknNTWM2OD12OD60OFYh|ryP NUH3TGt1W0GQR2LFVi=>
NCI-H345 M3LN[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlHPTWM2OD12OD60Olgh|ryP MmfVV2FPT1KHUh?=
TE-5 NHXlO4pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{\KdmlEPTB;NEmuO|EyQCEQvF2= MXHTRW5IWkWU

... Click to View More Cell Line Experimental Data

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

Protocol

Kinase Assay:

[3]

+ Expand

Kinase inhibition assays:

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

[2]

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

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


    (Only for Reference)
Animal Research:

[1]

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

Solubility (25°C)

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

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

Chemical Information

Molecular Weight 464.59
Formula

C23H28N8OS

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

Bio Calculators

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Molarity Calculator

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

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

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

Dilution Calculator

Dilution Calculator

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

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

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

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Molecular Weight Calculator

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

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Mass Concentration Volume Molecular Weight

Clinical Trial Information

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

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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

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Aurora Kinase Signaling Pathway Map

Aurora Kinase Inhibitors with Unique Features

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID