Tozasertib (VX-680, MK-0457)

Catalog No.S1048

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

Molecular Weight(MW): 464.59

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

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Cited by 36 Publications

16 Customer Reviews

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

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

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

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

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

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

     

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

Purity & Quality Control

Choose Selective Aurora Kinase Inhibitors

Biological Activity

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

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

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
BE-13 NGO3emFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml3UTWM2OD1yLkCwN|M5KM7:TR?= M{XtenNCVkeURWK=
RS4-11 NVrG[|hzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEjHbZRKSzVyPUCuNFA1ODRizszN MUHTRW5IWkWU
MFH-ino M2C5R2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUnJR|UxRTBwMEC5PUDPxE1? NHvhTWNUSU6JUlXS
NTERA-S-cl-D1 M{Pqe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVeyfIZkUUN3ME2wMlAyPDN2IN88US=> NIfDN5JUSU6JUlXS
697 NWq3b5BST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmeyTWM2OD1yLkCyOFcyKM7:TR?= NFHafZlUSU6JUlXS
NALM-6 NHjEcpNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXTJR|UxRTBwMEK1OVIh|ryP M13iNnNCVkeURWK=
ES8 NVvt[HEzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4P1S2lEPTB;MD6wOFYyOyEQvF2= MlTwV2FPT1KHUh?=
HUTU-80 MkXJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX;JR|UxRTBwMEWyPVkh|ryP MoXlV2FPT1KHUh?=
MV-4-11 NHvoT2hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWDLSHFUUUN3ME2wMlA4Pzh{IN88US=> NHTBPWJUSU6JUlXS
MONO-MAC-6 MkjGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnPLTWM2OD1yLkC3PFc6KM7:TR?= NFLvO3JUSU6JUlXS
LC-2-ad MnPjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MW\JR|UxRTBwMEi3PFkh|ryP MWPTRW5IWkWU
BL-41 M{\TfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXHNXI1yUUN3ME2wMlExPDR3IN88US=> MYnTRW5IWkWU
A4-Fuk MkDSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWrkc4d1UUN3ME2wMlEyPTZ|IN88US=> NEHBUohUSU6JUlXS
SW954 NEi5flFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3X2OWlEPTB;MD6xNlIzQSEQvF2= M3HyTHNCVkeURWK=
BV-173 M1;YWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVqxfHRKUUN3ME2wMlEzPjRzIN88US=> M17qXHNCVkeURWK=
TE-11 Ml7vS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWHJR|UxRTBwMUS5PFIh|ryP MUfTRW5IWkWU
SK-UT-1 NHvydFFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmXzTWM2OD1yLkG1PVY2KM7:TR?= NFX0R3JUSU6JUlXS
SIG-M5 NHTCc2JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2Li[mlEPTB;MD6xOlcxPyEQvF2= M4T6cnNCVkeURWK=
OCUB-M Mle4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVvVRXp5UUN3ME2wMlE3QTh|IN88US=> MlP2V2FPT1KHUh?=
K052 NXG0SHdET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYrSPGFnUUN3ME2wMlE6PDhizszN M2m5c3NCVkeURWK=
VA-ES-BJ MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYK3OYxtUUN3ME2wMlIxODh4IN88US=> MmDOV2FPT1KHUh?=
SW982 NUnJVlZJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mk\4TWM2OD1yLkKxN|gh|ryP Mn:xV2FPT1KHUh?=
LB647-SCLC M3ezR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUSzZlZzUUN3ME2wMlIyPTJ|IN88US=> M3H3fXNCVkeURWK=
PSN1 NWC1bZJQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{fSOmlEPTB;MD6yNlAzPiEQvF2= MkLTV2FPT1KHUh?=
BB30-HNC MnfCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoDqTWM2OD1yLkKyOVkyKM7:TR?= M3LEcXNCVkeURWK=
ST486 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWPSbWZSUUN3ME2wMlI{ODh5IN88US=> M4fsfnNCVkeURWK=
MOLT-4 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmKzTWM2OD1yLkKzN|M4KM7:TR?= MVHTRW5IWkWU
EW-16 MljqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXTJR|UxRTBwMkO3Olgh|ryP MVvTRW5IWkWU
KS-1 M2e0OGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVPJR|UxRTBwMkO3PFUh|ryP NEjpZ5BUSU6JUlXS
SR NYTvWVNqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXrJR|UxRTBwMkS1OlQh|ryP NYfpVGM6W0GQR2LFVi=>
KM12 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIHaPGVKSzVyPUCuNlY{PiEQvF2= NEHyUmJUSU6JUlXS
EM-2 NUjIWGZsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH73eJhKSzVyPUCuNlY3PDFizszN M2LzS3NCVkeURWK=
MEG-01 NYHKe4JMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV;uc5l5UUN3ME2wMlI4QDR7IN88US=> M2\XfHNCVkeURWK=
NB13 M1nBVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NI[ybXlKSzVyPUCuNlc6QDRizszN NUTuSYRSW0GQR2LFVi=>
RKO MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmXoTWM2OD1yLkOwPFE{KM7:TR?= NYf6T4JkW0GQR2LFVi=>
CESS NFrTcIlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIDBRldKSzVyPUCuN|E{OjhizszN NITMTVZUSU6JUlXS
EoL-1-cell MnjKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXHJR|UxRTBwM{O0OVkh|ryP MXjTRW5IWkWU
DOHH-2 M4T0[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUPJR|UxRTBwM{O3PFEh|ryP Ml71V2FPT1KHUh?=
A388 NYXkTHNqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2HRbmlEPTB;MD6zOFA5PiEQvF2= MUHTRW5IWkWU
LAMA-84 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV\JR|UxRTBwM{WxO|gh|ryP MkHxV2FPT1KHUh?=
IMR-5 NWfadlBST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUG4[VI6UUN3ME2wMlM2PTRizszN MoK4V2FPT1KHUh?=
KARPAS-422 M2HiW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEfifmRKSzVyPUCuN|czPzJizszN M2SycXNCVkeURWK=
MRK-nu-1 NVzTdYh6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH6xcVhKSzVyPUCuN|gyOyEQvF2= M1;LNXNCVkeURWK=
BL-70 NHnNPVRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHnaPFRKSzVyPUCuN|g6PzRizszN NIXobmRUSU6JUlXS
LXF-289 MnL1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{LvOmlEPTB;MD60NFQxPiEQvF2= MkXYV2FPT1KHUh?=
RL95-2 MnKwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXTJR|UxRTBwNEC1Olch|ryP NWrX[HlvW0GQR2LFVi=>
QIMR-WIL MnnZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXPJR|UxRTBwNEK2O|Yh|ryP MUnTRW5IWkWU
K-562 MnvmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mo[3TWM2OD1yLkSzOFczKM7:TR?= M3LRZnNCVkeURWK=
NCI-H510A MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV;JR|UxRTBwNEO4NlMh|ryP NWe1NXI4W0GQR2LFVi=>
NCI-H524 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEOwcopKSzVyPUCuOVEyPDdizszN MlvZV2FPT1KHUh?=
KE-37 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVTnW5hmUUN3ME2wMlUzOTB{IN88US=> MVnTRW5IWkWU
KP-N-YS M4DvWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NW\lOo1iUUN3ME2wMlU1Ozl{IN88US=> NIX3OGJUSU6JUlXS
LS-411N MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYPJR|UxRTBwNUe3OVIh|ryP MoDOV2FPT1KHUh?=
CTV-1 NHf5bIVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn7qTWM2OD1yLkW4O|c{KM7:TR?= MVPTRW5IWkWU
NCI-SNU-16 M1nmfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoTFTWM2OD1yLk[zOVcyKM7:TR?= NWfuT2hGW0GQR2LFVi=>
HT-144 MlnPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH7oPXBKSzVyPUCuOlM4QThizszN NFr4NXhUSU6JUlXS
NCI-H187 NXq1fYV2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1T4emlEPTB;MD62OFE{KM7:TR?= M3zYbnNCVkeURWK=
OCI-AML2 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWnwOnYyUUN3ME2wMlY1PDB|IN88US=> NIDzU2FUSU6JUlXS
CCRF-CEM MnHXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV3JR|UxRTBwNkWzOFYh|ryP M17PSXNCVkeURWK=
ONS-76 NY[5eWlNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXLJR|UxRTBwNk[0OVgh|ryP MV3TRW5IWkWU
IST-SL2 Mlq0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFu4cXVKSzVyPUCuO|E6QDJizszN M2DmW3NCVkeURWK=
NB6 Ml;DS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF[5UWZKSzVyPUCuO|czPTRizszN MlLiV2FPT1KHUh?=
SK-PN-DW NFrzUZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml7xTWM2OD1yLke5NVQh|ryP NVvWXHVYW0GQR2LFVi=>
HCC1599 NHzyOpFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV3JR|UxRTBwOEC4O|Qh|ryP NWH4c291W0GQR2LFVi=>
MC116 NV;SPIFrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH7KZ|ZKSzVyPUCuPFUxOTFizszN NXLIe3I3W0GQR2LFVi=>
TE-15 NFfOXJRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkTETWM2OD1yLki1NFk5KM7:TR?= MYDTRW5IWkWU
HOP-62 NETsRW1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYLJR|UxRTBwOE[zNlkh|ryP NGGxWItUSU6JUlXS
TGBC24TKB NG[5[ldIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlvKTWM2OD1yLki2N|g2KM7:TR?= NXS5NG91W0GQR2LFVi=>
HCE-4 MoezS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYjK[FBNUUN3ME2wMlg5ODZ|IN88US=> MVjTRW5IWkWU
ALL-PO MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIjyU45KSzVyPUCuPFgyPzVizszN NGn6WXNUSU6JUlXS
KGN M2XXN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NInMVJFKSzVyPUCuPFk6QTVizszN NVLySI9pW0GQR2LFVi=>
ML-2 NV7vZo95T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIWzbG1KSzVyPUCuPVAzPTlizszN MUPTRW5IWkWU
ES4 NX3iRo5lT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF65ToJKSzVyPUCuPVEyOjhizszN M2HRNnNCVkeURWK=
SF126 NW\SbXZFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFLFRpNKSzVyPUCuPVQ5OTlizszN NE\PRo1USU6JUlXS
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DU-4475 NGS1c4JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUKxenhqUUN3ME2xMlAyPzV4IN88US=> NEXvNYVUSU6JUlXS
NKM-1 M1vOTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX;JR|UxRTFwMEK3O|Uh|ryP NHTWc5VUSU6JUlXS
HL-60 NUL5dJZKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF\RW3pKSzVyPUGuNFY2PzRizszN M{nOZ3NCVkeURWK=
SBC-1 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1T2TWlEPTB;MT6xNlU1OiEQvF2= MnTJV2FPT1KHUh?=
TE-10 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn7jTWM2OD1zLkGyPVQ3KM7:TR?= NEHsbo5USU6JUlXS
ETK-1 NWDaNFlmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmO2TWM2OD1zLkGzOlE{KM7:TR?= NVHmXotyW0GQR2LFVi=>
HAL-01 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWHDVmRYUUN3ME2xMlE3PzB7IN88US=> M4LQUHNCVkeURWK=
BB65-RCC MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4XJcWlEPTB;MT6xPFAxPSEQvF2= NHPEV4hUSU6JUlXS
EW-1 NX7hW3huT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWjYWmVTUUN3ME2xMlE5PTZ{IN88US=> M3vGfHNCVkeURWK=
SK-NEP-1 MlHwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1GyXmlEPTB;MT6yNVEyOSEQvF2= NVTIXIxjW0GQR2LFVi=>
SK-LMS-1 NYizfFZWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmCyTWM2OD1zLkKyNlEzKM7:TR?= NGjxcHJUSU6JUlXS
DEL NWK1[5VbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFzNe25KSzVyPUGuNlU3PDNizszN Mm\WV2FPT1KHUh?=
GT3TKB NF:xN5JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXTJR|UxRTFwMkiwOVch|ryP M1fVTHNCVkeURWK=
MOLT-16 NIPibJhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2jvRWlEPTB;MT6zOVQxPSEQvF2= MV7TRW5IWkWU
CMK MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoPYTWM2OD1zLkSyNVE4KM7:TR?= MnfLV2FPT1KHUh?=
NB5 NXT3TGNFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWTr[WlkUUN3ME2xMlY1OjJ7IN88US=> NFeyPVRUSU6JUlXS
NCI-H1963 NX:wbJM3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV24Xml{UUN3ME2xMlcxPTh|IN88US=> NYrKWIk6W0GQR2LFVi=>
KURAMOCHI NE\RSo9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYXJR|UxRTFwN{i5NVEh|ryP NVzxdZdGW0GQR2LFVi=>
TE-8 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlWxTWM2OD1zLkiwN|Y5KM7:TR?= NYXCfGlYW0GQR2LFVi=>
NCI-H1304 M3\ifWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFX4cpRKSzVyPUGuPFMxPzNizszN MmHrV2FPT1KHUh?=
A101D NFzRdGxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUTJR|UxRTFwOEezPVUh|ryP NXP1eWMzW0GQR2LFVi=>
SCLC-21H NVX1SVRuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVfaNodvUUN3ME2xMlk4ODV5IN88US=> NW\TWVNUW0GQR2LFVi=>
GB-1 Ml3VS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH7KdFlKSzVyPUKuNFE3PDdizszN MnuzV2FPT1KHUh?=
KARPAS-45 MlzlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1zTXmlEPTB;Mj6wNlY2PCEQvF2= MYXTRW5IWkWU
ATN-1 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MULJR|UxRTJwMEK4OVgh|ryP MkO5V2FPT1KHUh?=
NCI-H720 NFjsfHdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXPDTGlqUUN3ME2yMlA3OjR2IN88US=> NW\EOFZ5W0GQR2LFVi=>
RPMI-6666 MmL5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2fsTGlEPTB;Mj6xOlIxPyEQvF2= NGL1d5BUSU6JUlXS
NB17 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUDJR|UxRTJwMkmyO{DPxE1? NGrxfXJUSU6JUlXS
IST-SL1 NFvETZVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2LZ[2lEPTB;Mj6yPVc3PSEQvF2= NWPFSIZyW0GQR2LFVi=>
SH-4 NH;JTYJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGPidW5KSzVyPUKuN|I1PjlizszN NEDOfFBUSU6JUlXS
K5 MlLBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFjneZJKSzVyPUKuOFA{OTlizszN NUjoPFU{W0GQR2LFVi=>
OVCAR-4 NUPBd3NCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVfJR|UxRTJwNE[xN{DPxE1? NH75VYlUSU6JUlXS
ACN M1;2fGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHTj[5NKSzVyPUKuOVAzOTNizszN M1PM[HNCVkeURWK=
TGW M{jZZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYHJR|UxRTJwNkW4N|Ih|ryP M{T3c3NCVkeURWK=
NCI-H2107 MkXTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3znSWlEPTB;Mj64N|cyOSEQvF2= M{XqVHNCVkeURWK=
NCI-H82 MkO1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWf0W2RIUUN3ME2yMlg{QDN6IN88US=> M4TpNHNCVkeURWK=
SK-N-FI MoHWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHXFbXFKSzVyPUKuPFY5PjhizszN MYHTRW5IWkWU
LB1047-RCC NIn6Oo9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYfJR|UxRTJwOEixNlYh|ryP NIjYbWNUSU6JUlXS
LU-134-A NHzibHNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXvJR|UxRTJwOEmyOkDPxE1? MmfWV2FPT1KHUh?=
NCI-H209 MoW1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3\aV2lEPTB;Mj65NVI2OyEQvF2= NGf2OWFUSU6JUlXS
NOMO-1 NHLMO49Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NI\QSFBKSzVyPUOuNFIzPzRizszN NEX1fHBUSU6JUlXS
RH-1 NHLpSHNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYHHTXI5UUN3ME2zMlE4OjlzIN88US=> MVfTRW5IWkWU
LOUCY NETLXGVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVvJR|UxRTNwMUi2PVMh|ryP MmK1V2FPT1KHUh?=
TE-9 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{LteGlEPTB;Mz6yOlc{PiEQvF2= NETn[4tUSU6JUlXS
PF-382 NYDrTIx5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2fu[GlEPTB;Mz6zOVc4QCEQvF2= NGTS[XdUSU6JUlXS
RPMI-8402 NF7FNmJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUfJR|UxRTNwNUi2NFMh|ryP NFfRXW9USU6JUlXS
HEL MlTCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3O1b2lEPTB;Mz62N|Ih|ryP NYPJN3BTW0GQR2LFVi=>
NOS-1 M4rGc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn;OTWM2OD1|Lki0O|U1KM7:TR?= M1Pl[3NCVkeURWK=
ES1 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnXtTWM2OD1|LkmyNlk{KM7:TR?= MnvVV2FPT1KHUh?=
NCI-H2171 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIPPO2dKSzVyPUOuPVI1OjNizszN NEPxcIpUSU6JUlXS
NCI-H747 M4fBfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml;FTWM2OD1|Lkm0NlIyKM7:TR?= M1fIXHNCVkeURWK=
MHH-NB-11 NIjUUZRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml;MTWM2OD1|Lkm1N|EzKM7:TR?= NX:ybpM3W0GQR2LFVi=>
MZ1-PC MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGTh[3FKSzVyPUOuPVkzPCEQvF2= M4XtSHNCVkeURWK=
MMAC-SF MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkPqTWM2OD12LkCyOFY4KM7:TR?= MnjLV2FPT1KHUh?=
NMC-G1 NIfoOotIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoXhTWM2OD12LkKyO|I{KM7:TR?= M1XnT3NCVkeURWK=
SW872 NG\xRXNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWfJR|UxRTRwM{SzOEDPxE1? NXuxOlVzW0GQR2LFVi=>
TE-12 NVP1V4JyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXruNVdFUUN3ME20MlU3Ozl2IN88US=> NXTtVmxJW0GQR2LFVi=>
LU-139 NF:yPFJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NULXWG9LUUN3ME20MlYyQDN3IN88US=> NVXETpFMW0GQR2LFVi=>
HC-1 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEfkWZhKSzVyPUSuOlk1QTRizszN NEXEWJlUSU6JUlXS
COR-L279 MoTYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYntdWZYUUN3ME20Mlc2QDlzIN88US=> M1\yU3NCVkeURWK=
SF268 MkTuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXvmeJFSUUN3ME20Mlc6QTF4IN88US=> NUTyTY5uW0GQR2LFVi=>
MC-CAR NH2wb5ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4e0XmlEPTB;NT6wOlc2PyEQvF2= MmrGV2FPT1KHUh?=
TK10 MlHXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4LpdmlEPTB;NT6zOVQ3QSEQvF2= NXfKcXg{W0GQR2LFVi=>
TE-1 MmXyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3zXZ2lEPTB;NT60PVAxPCEQvF2= NVXa[G9qW0GQR2LFVi=>
NCI-H2126 M3fMbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4jVVWlEPTB;NT62OFU4PCEQvF2= MoXvV2FPT1KHUh?=
Daudi NGqzUnlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFjVfnZKSzVyPUWuOlkyOiEQvF2= M1K0SHNCVkeURWK=
NCI-H1648 NEXsS4NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX\WO2tnUUN3ME21MlgyPDV2IN88US=> NFzBeYFUSU6JUlXS
OS-RC-2 MlLzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXvJR|UxRTVwOUi1PVch|ryP NVjYU25RW0GQR2LFVi=>
DJM-1 M2W3PGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3G5XmlEPTB;Nj6zOFY3PiEQvF2= MU\TRW5IWkWU
LS-1034 MnfjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV;RRWFEUUN3ME22Mlc2PjZizszN M{\6SnNCVkeURWK=
NCI-H1581 Mn3yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX3JR|UxRTZwN{i0NFUh|ryP NX\MUW1yW0GQR2LFVi=>
UACC-257 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFvJWmZKSzVyPUeuNFQ2OTJizszN NWT3VolMW0GQR2LFVi=>
KM-H2 Ml7oS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXrMdWJzUUN3ME23MlE5PDV5IN88US=> M4XucHNCVkeURWK=
NCI-H1436 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2G2WGlEPTB;Nz62PVk{OiEQvF2= NVvjfJZwW0GQR2LFVi=>
IA-LM MmTWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWXJR|UxRTdwOEW5JO69VQ>? MWnTRW5IWkWU
NCI-H526 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWXJR|UxRThwMkW2N|ch|ryP M4DS[nNCVkeURWK=
GCIY MmjKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2qxRmlEPTB;OD6zOlk3PSEQvF2= MnPxV2FPT1KHUh?=
CP67-MEL Ml\ES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWXGcVlMUUN3ME24MlU{OjZizszN MUPTRW5IWkWU
KALS-1 M4LqNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWq1R4YzUUN3ME24Mlg{QDVzIN88US=> NFP3XJJUSU6JUlXS
NCI-H1770 NUHoT2lXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV;JR|UxRThwOUCyOlUh|ryP NGO1PJpUSU6JUlXS
8-MG-BA M3HQWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NE\aVWFKSzVyPUmuN|I5PDRizszN MlnaV2FPT1KHUh?=
KY821 NYHpOnc1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnHjTWM2OD17Lke3OFg1KM7:TR?= M{XGTnNCVkeURWK=
SNB75 NGnlb3lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVe3bI5DUUN3ME2xNE4xPzZizszN NGTZT3JUSU6JUlXS
NCCIT Mo\6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NET3fINKSzVyPUGxMlA2QDJizszN NFu2WFVUSU6JUlXS
SJSA-1 MkDwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXfJR|UxRTFzLkK4PVEh|ryP NEjBUVlUSU6JUlXS
LB373-MEL-D M1f1dGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3\ITGlEPTB;MUGuN|gzPyEQvF2= MXzTRW5IWkWU
TALL-1 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH\pOmhKSzVyPUGxMlQxPThizszN M1zRbHNCVkeURWK=
NB69 NXjKd5Z1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEDqUG5KSzVyPUGxMlc4ODVizszN M3e2S3NCVkeURWK=
NCI-H1355 MmX0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWrJR|UxRTFzLkm0NlYh|ryP NF\iUFdUSU6JUlXS
DMS-153 MoDNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYPJR|UxRTF{LkC0NlYh|ryP MUHTRW5IWkWU
OPM-2 MluyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVrJR|UxRTF{LkG1PVYh|ryP NH75Zm1USU6JUlXS
NB1 NInDdodIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4TFeWlEPTB;MUKuNlkh|ryP MUfTRW5IWkWU
A3-KAW MoTrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnvQTWM2OD1zMj6zNlM3KM7:TR?= NI[4OWNUSU6JUlXS
NCI-H1882 NEW3TnlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mny1TWM2OD1zMj60NFY3KM7:TR?= M3;DOXNCVkeURWK=
KG-1 M13Jb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NE\GSIRKSzVyPUGyMlY2PDVizszN NXv5TGdWW0GQR2LFVi=>
LC4-1 Mn3oS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2faTWlEPTB;MUKuO|cxPiEQvF2= NGHMcFFUSU6JUlXS
HCE-T MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYDJR|UxRTF|LkCwOFkh|ryP NHfMOJVUSU6JUlXS
NEC8 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnraTWM2OD1zMz6xNFM5KM7:TR?= NXPxU2REW0GQR2LFVi=>
IST-MEL1 NVjJXFFUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkLFTWM2OD1zMz61O|g5KM7:TR?= MXfTRW5IWkWU
EW-3 NVzNXJg{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoLjTWM2OD1zMz63OFAzKM7:TR?= M1\ib3NCVkeURWK=
CTB-1 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHnyTmVKSzVyPUG0MlA{OjlizszN M13h[HNCVkeURWK=
LS-123 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWjQ[FhtUUN3ME2xOE4yPTh6IN88US=> M4\2PHNCVkeURWK=
NCI-H1417 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXnJR|UxRTF2LkOwOVIh|ryP NWq0[XFpW0GQR2LFVi=>
MZ7-mel NXrGR|JJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MorYTWM2OD1zND60OFM{KM7:TR?= NEmx[VBUSU6JUlXS
JiyoyeP-2003 NH7zd4NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUXJR|UxRTF3Lk[zNlYh|ryP NETFdJpUSU6JUlXS
ES6 Mmq4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUnJR|UxRTF4LkKzOlEh|ryP NI\1NZJUSU6JUlXS
HH M3;uSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHXNb3NKSzVyPUG3MlE6PjNizszN NXTWNWRUW0GQR2LFVi=>
SF539 NFW2d2FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Moj5TWM2OD1zNz65PVIzKM7:TR?= MlG0V2FPT1KHUh?=
Calu-6 NVjNd5pKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHPLdotKSzVyPUG5MlI{QSEQvF2= MnntV2FPT1KHUh?=
SK-MM-2 MmSxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1P3T2lEPTB;MUmuOVU2KM7:TR?= M4j3XnNCVkeURWK=
IST-MES1 NHiy[3hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXrJR|UxRTF7Lk[2OlMh|ryP MUjTRW5IWkWU
GI-ME-N NWXuWpRIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mo\1TWM2OD1zOT64NlI4KM7:TR?= NU\s[XN5W0GQR2LFVi=>
CAL-148 NYnoN2J[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXGyXphEUUN3ME2yNE46QTN2IN88US=> NX;aZY1xW0GQR2LFVi=>
EVSA-T NX7XeFRnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFi0OFBKSzVyPUKxMlE1QTlizszN MXXTRW5IWkWU
LP-1 NYLUOFZ2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3rMeGlEPTB;MkGuN|Q{OiEQvF2= NHW2fGlUSU6JUlXS
BOKU NHrHWHlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUTJR|UxRTJzLkS1N|Mh|ryP NUPxWW9WW0GQR2LFVi=>
KLE MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWfJR|UxRTJ{LkG5NFMh|ryP M3HBWXNCVkeURWK=
LB831-BLC NEiy[GFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUXJR|UxRTJ3LkG1NlYh|ryP NIjLVFBUSU6JUlXS
NCI-H889 NIPmNHpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn6yTWM2OD1{NT6xPVMyKM7:TR?= NYrOOpI2W0GQR2LFVi=>
REH MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHzj[W1KSzVyPUK1MlQ3PzFizszN M{KzZ3NCVkeURWK=
KP-N-RT-BM-1 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFPQclJKSzVyPUK1MlQ4PTJizszN NHTtZ5VUSU6JUlXS
MPP-89 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4LEZmlEPTB;MkWuOVMyPCEQvF2= MoPQV2FPT1KHUh?=
no-11 MnLRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXjBcYJbUUN3ME2yOU44PDdizszN MYjTRW5IWkWU
NCI-H748 MnPmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWfJR|UxRTJ3Lke2Nlch|ryP M3:3cnNCVkeURWK=
LB2518-MEL NU\XO2ttT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGjaXVFKSzVyPUK3MlE4PzNizszN MWnTRW5IWkWU
TGBC1TKB MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUj0N2N1UUN3ME2yO{42PTh3IN88US=> MVTTRW5IWkWU
MHH-PREB-1 M2XDR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHnqfYpKSzVyPUK4MlA4OzRizszN NV2wVlU6W0GQR2LFVi=>
MZ2-MEL MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFPobnlKSzVyPUK4MlYyPDNizszN NHHnTndUSU6JUlXS
U-266 MkDoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mnn0TWM2OD1{OD62N|Y3KM7:TR?= NWTFXWRIW0GQR2LFVi=>
SNU-C1 MmnBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn3TTWM2OD1{OD65OFMh|ryP MYXTRW5IWkWU
SW962 M2W2Smdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M13HWGlEPTB;M{CuNlc1PyEQvF2= M1;0VHNCVkeURWK=
Raji MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnfQTWM2OD1|MD61OVkzKM7:TR?= M1T4NHNCVkeURWK=
KNS-42 NEnDbHZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYHJR|UxRTNyLki5OVYh|ryP M2fRWHNCVkeURWK=
LB996-RCC MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHn4OFVKSzVyPUOxMlE4ODJizszN MUTTRW5IWkWU
CHP-126 NUnGfoRHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVTFb2ZFUUN3ME2zNU4yQTh2IN88US=> MYjTRW5IWkWU
RXF393 MnruS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVnMclZ1UUN3ME2zNk41QTdizszN M1HzenNCVkeURWK=
COLO-684 MkHwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEnNcGJKSzVyPUOyMlY1OzhizszN MXfTRW5IWkWU
A704 NX[wNpBzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnXNTWM2OD1|Mz61OVM5KM7:TR?= NVTGPHk4W0GQR2LFVi=>
A253 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHHZ[ItKSzVyPUOzMlU5PTJizszN MnrLV2FPT1KHUh?=
KNS-81-FD NU\SfFZMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYS5SnJkUUN3ME2zOE42PDV4IN88US=> NWrRVYhsW0GQR2LFVi=>
TE-441-T NF7oVVRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnS4TWM2OD1|ND62N|cyKM7:TR?= M{\T[HNCVkeURWK=
HCC2157 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIDDem1KSzVyPUO1MlQ3OTlizszN NVHXN3dHW0GQR2LFVi=>
ES3 NWSwNJVNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWfJR|UxRTN4Lk[3OUDPxE1? MYTTRW5IWkWU
NCI-H1155 M37Zd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{fkR2lEPTB;M{euPFE2KM7:TR?= M13BfnNCVkeURWK=
SNU-C2B MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVrJR|UxRTN6LkG2OVQh|ryP NYDxO3E3W0GQR2LFVi=>
JAR MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmnFTWM2OD1|OD6yOFQ6KM7:TR?= NEfD[WhUSU6JUlXS
GDM-1 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3vhOWlEPTB;M{iuPVEyPiEQvF2= MWTTRW5IWkWU
KU812 NEHDPJBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVj3WXF2UUN3ME20NU42ODdizszN MWrTRW5IWkWU
BC-1 MnHPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4G3[2lEPTB;NEKuOlc{OSEQvF2= M2PnOXNCVkeURWK=
GI-1 NYfXW|lST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXvJR|UxRTR{LkmxPVIh|ryP MmHiV2FPT1KHUh?=
NCI-H1694 M4HZc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkfYTWM2OD12ND65OFczKM7:TR?= NXTScmZmW0GQR2LFVi=>
DG-75 NXPu[YxnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVHMUXZ[UUN3ME20OU4yPTd5IN88US=> NGn5cnBUSU6JUlXS
COR-L88 NHvlXFlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV;v[2VIUUN3ME20OU4zPzd6IN88US=> NVLh[plZW0GQR2LFVi=>
LS-513 NWDDRZNTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXnWOFhtUUN3ME20OU46OTV4IN88US=> MYXTRW5IWkWU
HD-MY-Z M3vLUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWnJR|UxRTR4LkS2NVIh|ryP MUjTRW5IWkWU
L-363 NXHaSFYzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIPGeGxKSzVyPUS2Mlg5OSEQvF2= NIn5PHRUSU6JUlXS
TE-6 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mo\CTWM2OD12OD60OFYh|ryP NETSWI9USU6JUlXS
NCI-H345 NWnxN5FiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUXBUFB{UUN3ME20PE41PjhizszN M4TFNHNCVkeURWK=
TE-5 NGfob4pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIi2WIRKSzVyPUS5MlcyOThizszN MXvTRW5IWkWU

... 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 individually and in order:
5% DMSO+30% PEG 300+2% Tween 80+ddH2O
15mg/mL

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

Chemical Information

Molecular Weight 464.59
Formula

C23H28N8OS

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

Bio Calculators

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Molarity Calculator

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

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

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Dilution Calculator

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

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

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

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Molecular Weight Calculator

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Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00500006 Terminated Chronic Myelogenous Leukemia|Leukemia, Lymphoblastic, Acute, Philadelphia-Positive Merck Sharp & Dohme Corp. October 2007 Phase 1
NCT00405054 Terminated Leukemia Merck Sharp & Dohme Corp. December 2006 Phase 2
NCT00290550 Terminated Carcinoma, Non-Small-Cell Lung Merck Sharp & Dohme Corp. June 2006 Phase 2
NCT00111683 Completed Chronic Myelogenous Leukemia in Blast Crisis|Lymphocytic Leukemia, B Cell, Acute|Myelodysplastic Syndromes|Myelogenous Leukemia, Chronic Merck Sharp & Dohme Corp. June 2005 Phase 1
NCT02532868 Terminated Cancer Merck Sharp & Dohme Corp. May 2005 Phase 1
NCT00099346 Terminated Colorectal Cancer|Advanced Solid Tumors Merck Sharp & Dohme Corp. January 2005 Phase 1

Tech Support

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

Handling Instructions

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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID