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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In DMSO USD 134 In stock
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Cited by 39 Publications

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 Mn;KS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGDMWotKSzVyPUCuNFA{OzhizszN NXjVXlZoW0GQR2LFVi=>
RS4-11 MojoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWDJR|UxRTBwMEC0NFQh|ryP Mk\LV2FPT1KHUh?=
MFH-ino NUX4[|BVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2DLRmlEPTB;MD6wNFk6KM7:TR?= NIPwWnFUSU6JUlXS
NTERA-S-cl-D1 M1PEPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3f1PGlEPTB;MD6wNVQ{PCEQvF2= NUnYN2Y2W0GQR2LFVi=>
697 NGDkWG1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn3kTWM2OD1yLkCyOFcyKM7:TR?= NIjRVZFUSU6JUlXS
NALM-6 MnT3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkLOTWM2OD1yLkCyOVUzKM7:TR?= NH;HSZhUSU6JUlXS
ES8 MofvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGPBR5hKSzVyPUCuNFQ3OTNizszN NV7kcIR3W0GQR2LFVi=>
HUTU-80 MnLBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVeydm8zUUN3ME2wMlA2Ojl7IN88US=> NUjwSJF{W0GQR2LFVi=>
MV-4-11 M4LyWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHvONVlKSzVyPUCuNFc4QDJizszN NX23NIk1W0GQR2LFVi=>
MONO-MAC-6 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3nzd2lEPTB;MD6wO|g4QSEQvF2= NUiyUZI3W0GQR2LFVi=>
LC-2-ad M4HwfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXvNe2xmUUN3ME2wMlA5Pzh7IN88US=> MVfTRW5IWkWU
BL-41 NIPjWXJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUDiOFhjUUN3ME2wMlExPDR3IN88US=> NFHJ[41USU6JUlXS
A4-Fuk MonPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYDJR|UxRTBwMUG1OlMh|ryP NGTXUJZUSU6JUlXS
SW954 NHHGbVJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUnJR|UxRTBwMUKyNlkh|ryP NIO1NXRUSU6JUlXS
BV-173 Mn\XS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnXuTWM2OD1yLkGyOlQyKM7:TR?= MWnTRW5IWkWU
TE-11 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{jvcWlEPTB;MD6xOFk5OiEQvF2= NHnrR5NUSU6JUlXS
SK-UT-1 NI[xWo1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlzDTWM2OD1yLkG1PVY2KM7:TR?= NVP6Z|Q2W0GQR2LFVi=>
SIG-M5 NVP4RmhmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnS1TWM2OD1yLkG2O|A4KM7:TR?= Mnf4V2FPT1KHUh?=
OCUB-M NXT3ZnNwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFf2d5VKSzVyPUCuNVY6QDNizszN NFrZV4xUSU6JUlXS
K052 NX\uRWhNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2jtRWlEPTB;MD6xPVQ5KM7:TR?= NV7zflM1W0GQR2LFVi=>
VA-ES-BJ NI\YOpZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWG4Soo2UUN3ME2wMlIxODh4IN88US=> MoDGV2FPT1KHUh?=
SW982 NVP3Z5plT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnfuTWM2OD1yLkKxN|gh|ryP MVHTRW5IWkWU
LB647-SCLC NUPyblB7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1fEfGlEPTB;MD6yNVUzOyEQvF2= Mlm1V2FPT1KHUh?=
PSN1 M3LLcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnzrTWM2OD1yLkKyNFI3KM7:TR?= M3jBRXNCVkeURWK=
BB30-HNC MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NG\4fG1KSzVyPUCuNlI2QTFizszN MkX0V2FPT1KHUh?=
ST486 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEjuO|JKSzVyPUCuNlMxQDdizszN NWDL[VlrW0GQR2LFVi=>
MOLT-4 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX3JR|UxRTBwMkOzN|ch|ryP M2\V[HNCVkeURWK=
EW-16 M2O3PWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlraTWM2OD1yLkKzO|Y5KM7:TR?= M1u0fnNCVkeURWK=
KS-1 NVrVeZB{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnPBTWM2OD1yLkKzO|g2KM7:TR?= M4frfXNCVkeURWK=
SR NEXsU3BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX60Sno5UUN3ME2wMlI1PTZ2IN88US=> M1HXT3NCVkeURWK=
KM12 NIrSTGxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXTLNldVUUN3ME2wMlI3OzZizszN NHLXVXRUSU6JUlXS
EM-2 M321OGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHPr[XJKSzVyPUCuNlY3PDFizszN NGnaUI1USU6JUlXS
MEG-01 MoHPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWTJR|UxRTBwMke4OFkh|ryP MYTTRW5IWkWU
NB13 M1TOUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NU\ufmNCUUN3ME2wMlI4QTh2IN88US=> MlXrV2FPT1KHUh?=
RKO MoO5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYHJR|UxRTBwM{C4NVMh|ryP M4TGdnNCVkeURWK=
CESS NF21VHVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3;uUGlEPTB;MD6zNVMzQCEQvF2= NYXpdJdTW0GQR2LFVi=>
EoL-1-cell NFmwRYVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVzJR|UxRTBwM{O0OVkh|ryP MXLTRW5IWkWU
DOHH-2 M{jBNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NG\uTY5KSzVyPUCuN|M4QDFizszN NH\PNFFUSU6JUlXS
A388 NVTRXXhrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEPnWpBKSzVyPUCuN|QxQDZizszN NHfUcVNUSU6JUlXS
LAMA-84 NIXXd2tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NILVPVlKSzVyPUCuN|UyPzhizszN MVHTRW5IWkWU
IMR-5 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1:wZmlEPTB;MD6zOVU1KM7:TR?= NUH6PFlsW0GQR2LFVi=>
KARPAS-422 NVjjVodtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoHOTWM2OD1yLkO3NlczKM7:TR?= MV;TRW5IWkWU
MRK-nu-1 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFXaNJJKSzVyPUCuN|gyOyEQvF2= M3HZRXNCVkeURWK=
BL-70 MmWzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn6xTWM2OD1yLkO4PVc1KM7:TR?= MlHWV2FPT1KHUh?=
LXF-289 M{nYPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVjIW5YzUUN3ME2wMlQxPDB4IN88US=> NFPadVNUSU6JUlXS
RL95-2 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml7oTWM2OD1yLkSwOVY4KM7:TR?= NUPxTpJJW0GQR2LFVi=>
QIMR-WIL NWPHS|ZnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NW\FZXNnUUN3ME2wMlQzPjd4IN88US=> M4HMR3NCVkeURWK=
K-562 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NG\heVFKSzVyPUCuOFM1PzJizszN MWDTRW5IWkWU
NCI-H510A MnrxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVLJR|UxRTBwNEO4NlMh|ryP M2GxcHNCVkeURWK=
NCI-H524 MnTZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX3JR|UxRTBwNUGxOFch|ryP NEHnSJZUSU6JUlXS
KE-37 NIHiRoxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mo\vTWM2OD1yLkWyNVAzKM7:TR?= NYrMS|VrW0GQR2LFVi=>
KP-N-YS NGe1S4xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnLNTWM2OD1yLkW0N|kzKM7:TR?= NVHmfnVFW0GQR2LFVi=>
LS-411N NWLMVIxxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH3EO|hKSzVyPUCuOVc4PTJizszN M3TUNHNCVkeURWK=
CTV-1 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3ruPGlEPTB;MD61PFc4OyEQvF2= M3\1W3NCVkeURWK=
NCI-SNU-16 M{j6Smdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnPmTWM2OD1yLk[zOVcyKM7:TR?= MnLNV2FPT1KHUh?=
HT-144 MlrBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVvJR|UxRTBwNkO3PVgh|ryP Ml\4V2FPT1KHUh?=
NCI-H187 MmTyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUGxemxbUUN3ME2wMlY1OTNizszN M3;6d3NCVkeURWK=
OCI-AML2 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH36foJKSzVyPUCuOlQ1ODNizszN MXLTRW5IWkWU
CCRF-CEM NV73ZlJTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYrJR|UxRTBwNkWzOFYh|ryP NX\ZcYNQW0GQR2LFVi=>
ONS-76 M4\sN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF75UVVKSzVyPUCuOlY1PThizszN NYewc2hQW0GQR2LFVi=>
IST-SL2 M2PKUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NID1N2tKSzVyPUCuO|E6QDJizszN NEXKN|RUSU6JUlXS
NB6 M33lWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3vINGlEPTB;MD63O|I2PCEQvF2= MnTSV2FPT1KHUh?=
SK-PN-DW MnjWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGjaUIFKSzVyPUCuO|kyPCEQvF2= NYHVc2tXW0GQR2LFVi=>
HCC1599 Ml\pS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVHiT5IyUUN3ME2wMlgxQDd2IN88US=> MXPTRW5IWkWU
MC116 M4S0WWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MorYTWM2OD1yLki1NFEyKM7:TR?= MWjTRW5IWkWU
TE-15 NGPzXYlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIC0fZRKSzVyPUCuPFUxQThizszN NEi4[VJUSU6JUlXS
HOP-62 NX3hPIY6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYDJR|UxRTBwOE[zNlkh|ryP NUTZdoRKW0GQR2LFVi=>
TGBC24TKB MnXlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1vUdGlEPTB;MD64OlM5PSEQvF2= NVHiTYxEW0GQR2LFVi=>
HCE-4 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4T6R2lEPTB;MD64PFA3OyEQvF2= NH\wOoRUSU6JUlXS
ALL-PO NUDlSIZNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn;YTWM2OD1yLki4NVc2KM7:TR?= MYDTRW5IWkWU
KGN MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4rO[WlEPTB;MD64PVk6PSEQvF2= MoHzV2FPT1KHUh?=
ML-2 MkLkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXPJR|UxRTBwOUCyOVkh|ryP MULTRW5IWkWU
ES4 M3PySmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVzJR|UxRTBwOUGxNlgh|ryP MXXTRW5IWkWU
SF126 NXrNflZWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MljzTWM2OD1yLkm0PFE6KM7:TR?= MULTRW5IWkWU
SK-N-DZ M2KxXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1zucWlEPTB;MD65OlE5QSEQvF2= MWrTRW5IWkWU
HCC1187 MlXJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmrDTWM2OD1zLkCwOVA2KM7:TR?= MUjTRW5IWkWU
DU-4475 NH;qRphIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVrJR|UxRTFwMEG3OVYh|ryP M2fHOnNCVkeURWK=
NKM-1 NHT2eXpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUPJR|UxRTFwMEK3O|Uh|ryP NUnNeY1wW0GQR2LFVi=>
HL-60 NWTwbFF[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2PLV2lEPTB;MT6wOlU4PCEQvF2= M{LjUHNCVkeURWK=
SBC-1 MnnlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWjlTnRpUUN3ME2xMlEzPTR{IN88US=> MUjTRW5IWkWU
TE-10 NVHWUo12T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYPJR|UxRTFwMUK5OFYh|ryP NXXld3BOW0GQR2LFVi=>
ETK-1 NV3IN5BET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUTJR|UxRTFwMUO2NVMh|ryP NXfXU2RKW0GQR2LFVi=>
HAL-01 M4PqR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVjJR|UxRTFwMU[3NFkh|ryP MmC4V2FPT1KHUh?=
BB65-RCC M{K5[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4jiemlEPTB;MT6xPFAxPSEQvF2= NXHhUXhqW0GQR2LFVi=>
EW-1 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{\WUWlEPTB;MT6xPFU3OiEQvF2= NX2wcWhEW0GQR2LFVi=>
SK-NEP-1 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGPJco5KSzVyPUGuNlEyOTFizszN MYrTRW5IWkWU
SK-LMS-1 NXy4Z4o5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXHJR|UxRTFwMkKyNVIh|ryP MkXxV2FPT1KHUh?=
DEL MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{TTcGlEPTB;MT6yOVY1OyEQvF2= Mnn5V2FPT1KHUh?=
GT3TKB MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXPEUphjUUN3ME2xMlI5ODV5IN88US=> MWHTRW5IWkWU
MOLT-16 MkjmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mm[zTWM2OD1zLkO1OFA2KM7:TR?= NIPVOGpUSU6JUlXS
CMK NXnCNFU6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnPITWM2OD1zLkSyNVE4KM7:TR?= NVXiRmVTW0GQR2LFVi=>
NB5 NXvuUVNXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4rqNWlEPTB;MT62OFIzQSEQvF2= NEXsWYxUSU6JUlXS
NCI-H1963 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXLOPGtVUUN3ME2xMlcxPTh|IN88US=> NWq0PHpvW0GQR2LFVi=>
KURAMOCHI MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWTJR|UxRTFwN{i5NVEh|ryP M2XrXXNCVkeURWK=
TE-8 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYT4R2p3UUN3ME2xMlgxOzZ6IN88US=> M{n2RnNCVkeURWK=
NCI-H1304 NHzkcGhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVPJR|UxRTFwOEOwO|Mh|ryP MX;TRW5IWkWU
A101D NWj1TXVLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlTuTWM2OD1zLki3N|k2KM7:TR?= M33ubXNCVkeURWK=
SCLC-21H MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4S0R2lEPTB;MT65O|A2PyEQvF2= MVrTRW5IWkWU
GB-1 NWDZWo1UT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnfDTWM2OD1{LkCxOlQ4KM7:TR?= Mn;BV2FPT1KHUh?=
KARPAS-45 MnrUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXLrXIZ3UUN3ME2yMlAzPjV2IN88US=> NFX2cWxUSU6JUlXS
ATN-1 NF7GeZdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MW\JR|UxRTJwMEK4OVgh|ryP MYnTRW5IWkWU
NCI-H720 NXLrU3dOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYXJR|UxRTJwME[yOFQh|ryP NGToe4ZUSU6JUlXS
RPMI-6666 M2LTeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF7rcFdKSzVyPUKuNVYzODdizszN MlThV2FPT1KHUh?=
NB17 NUXZWYdWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVzQe5A6UUN3ME2yMlI6OjdizszN NUjjWXpnW0GQR2LFVi=>
IST-SL1 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVLTd3FEUUN3ME2yMlI6PzZ3IN88US=> M3\OXHNCVkeURWK=
SH-4 NVHmOGVlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYrJR|UxRTJwM{K0Olkh|ryP Mny4V2FPT1KHUh?=
K5 M3rYO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWDuPY1VUUN3ME2yMlQxOzF7IN88US=> NHjkdYtUSU6JUlXS
OVCAR-4 NVnibmNQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkDwTWM2OD1{LkS2NVMh|ryP MYTTRW5IWkWU
ACN NEHhU25Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2fWUGlEPTB;Mj61NFIyOyEQvF2= M3\0bnNCVkeURWK=
TGW NFXmNVBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3[wVmlEPTB;Mj62OVg{OiEQvF2= Mk\TV2FPT1KHUh?=
NCI-H2107 NVXSelhHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXfrVJVUUUN3ME2yMlg{PzFzIN88US=> NHXJfm5USU6JUlXS
NCI-H82 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXH4[nllUUN3ME2yMlg{QDN6IN88US=> MUnTRW5IWkWU
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NCI-H748 MlLQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NY\zOFhuUUN3ME2yOU44PjJ5IN88US=> M{HndXNCVkeURWK=
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TE-6 MnTxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NY\PdI1xUUN3ME20PE41PDZizszN Mn[1V2FPT1KHUh?=
NCI-H345 NUHLbZdMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYfJR|UxRTR6LkS2PEDPxE1? Mn7lV2FPT1KHUh?=
TE-5 M3TFOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml\sTWM2OD12OT63NVE5KM7:TR?= M{TybnNCVkeURWK=

... 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

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)

  • Mass
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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 )

  • C1
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    C2
    V2

* 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):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
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

Instructions to calculate molar mass (molecular weight) of a chemical compound:

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
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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID