Tozasertib (VX-680, MK-0457)

For research use only.

Catalog No.S1048

79 publications

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

CAS No. 639089-54-6

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. The only exceptions are Fms-related tyrosine kinase-3 (FLT-3) and c-ABL tyrosine kinase, which are inhibited by the Tozasertib with Ki of 30 nM and 20 nM, respectively. Tozasertib induces apoptosis and autophagy. Phase 2.

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Selleck's Tozasertib (VX-680, MK-0457) has been cited by 79 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. The only exceptions are Fms-related tyrosine kinase-3 (FLT-3) and c-ABL tyrosine kinase, which are inhibited by the Tozasertib with Ki of 30 nM and 20 nM, respectively. Tozasertib induces apoptosis and autophagy. 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 NWXNVHVsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVK5VVBYUUN3ME2wMlAxOzN6IN88US=> MoDuV2FPT1KHUh?=
RS4-11 NVK0eY91T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2\od2lEPTB;MD6wNFQxPCEQvF2= MU\TRW5IWkWU
MFH-ino NF;qdpFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFnDS2RKSzVyPUCuNFA6QSEQvF2= MlLVV2FPT1KHUh?=
NTERA-S-cl-D1 NHfSW4tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUfjU3drUUN3ME2wMlAyPDN2IN88US=> NITYcZNUSU6JUlXS
697 M1iwbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mm\LTWM2OD1yLkCyOFcyKM7:TR?= M2C2cHNCVkeURWK=
NALM-6 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1uzfmlEPTB;MD6wNlU2OiEQvF2= NVzLfIlvW0GQR2LFVi=>
ES8 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEfJU3RKSzVyPUCuNFQ3OTNizszN M4XzVXNCVkeURWK=
HUTU-80 M3r5e2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnO1TWM2OD1yLkC1Nlk6KM7:TR?= MWXTRW5IWkWU
MV-4-11 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX6xXXkxUUN3ME2wMlA4Pzh{IN88US=> NWHtVpZLW0GQR2LFVi=>
MONO-MAC-6 M4fDUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVfJR|UxRTBwMEe4O|kh|ryP MoLyV2FPT1KHUh?=
LC-2-ad NGnvR3VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml:0TWM2OD1yLkC4O|g6KM7:TR?= NYDjT4wyW0GQR2LFVi=>
BL-41 NYnzb|g1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEfyW4JKSzVyPUCuNVA1PDVizszN MonwV2FPT1KHUh?=
A4-Fuk MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYjrfXgxUUN3ME2wMlEyPTZ|IN88US=> MlvFV2FPT1KHUh?=
SW954 NI\STHZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUfOWYp7UUN3ME2wMlEzOjJ7IN88US=> NE\oTlFUSU6JUlXS
BV-173 NYLOTZl1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXnDcGRZUUN3ME2wMlEzPjRzIN88US=> M37Rb3NCVkeURWK=
TE-11 M2m4[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV6yUotIUUN3ME2wMlE1QTh{IN88US=> M1ftRnNCVkeURWK=
SK-UT-1 NIrU[lRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX7JR|UxRTBwMUW5OlUh|ryP NEexXIxUSU6JUlXS
SIG-M5 MmW3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHHLTmdKSzVyPUCuNVY4ODdizszN MYLTRW5IWkWU
OCUB-M NIjvV5RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFznNGJKSzVyPUCuNVY6QDNizszN MWjTRW5IWkWU
K052 NY\DWYtGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWHFSFNSUUN3ME2wMlE6PDhizszN MXLTRW5IWkWU
VA-ES-BJ Ml;0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYXJR|UxRTBwMkCwPFYh|ryP NXu0bYNTW0GQR2LFVi=>
SW982 MnfWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFHMVlRKSzVyPUCuNlE{QCEQvF2= NVe0TY5UW0GQR2LFVi=>
LB647-SCLC M1znZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1TRdGlEPTB;MD6yNVUzOyEQvF2= MVTTRW5IWkWU
PSN1 NIHKcGpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlfqTWM2OD1yLkKyNFI3KM7:TR?= MVTTRW5IWkWU
BB30-HNC MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHTXc2VKSzVyPUCuNlI2QTFizszN MVHTRW5IWkWU
ST486 MoLlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUjJR|UxRTBwMkOwPFch|ryP MYDTRW5IWkWU
MOLT-4 MnnlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYnkOZRbUUN3ME2wMlI{OzN5IN88US=> M2fJfXNCVkeURWK=
EW-16 MnvKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkTaTWM2OD1yLkKzO|Y5KM7:TR?= NGPvWmRUSU6JUlXS
KS-1 NITRNYlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{jwdGlEPTB;MD6yN|c5PSEQvF2= NV3RWI57W0GQR2LFVi=>
SR Mnz2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFrrXYNKSzVyPUCuNlQ2PjRizszN NGHaVo1USU6JUlXS
KM12 M3\Oemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmPVTWM2OD1yLkK2N|Yh|ryP M1vncXNCVkeURWK=
EM-2 NGf3Um9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGXk[|FKSzVyPUCuNlY3PDFizszN NXXVeVJ3W0GQR2LFVi=>
MEG-01 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVzJR|UxRTBwMke4OFkh|ryP MXHTRW5IWkWU
NB13 Mk\lS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXjJR|UxRTBwMke5PFQh|ryP MnfQV2FPT1KHUh?=
RKO NY[zXo06T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF\YZYZKSzVyPUCuN|A5OTNizszN NWe5dYd2W0GQR2LFVi=>
CESS MmfYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnfPTWM2OD1yLkOxN|I5KM7:TR?= NILRRYFUSU6JUlXS
EoL-1-cell MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEfSOotKSzVyPUCuN|M1PTlizszN NFr1TnZUSU6JUlXS
DOHH-2 M1[xbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2jnXGlEPTB;MD6zN|c5OSEQvF2= MVHTRW5IWkWU
A388 M1[3cmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGnxNZpKSzVyPUCuN|QxQDZizszN M1PMOnNCVkeURWK=
LAMA-84 M4rHN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmXqTWM2OD1yLkO1NVc5KM7:TR?= Mn3uV2FPT1KHUh?=
IMR-5 NU\DSpZ3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVP3R4Z4UUN3ME2wMlM2PTRizszN MYDTRW5IWkWU
KARPAS-422 NGjBRXJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWDHXYV4UUN3ME2wMlM4Ojd{IN88US=> MnTRV2FPT1KHUh?=
MRK-nu-1 NHHMUXNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVO0NGFQUUN3ME2wMlM5OTNizszN NHH2SGVUSU6JUlXS
BL-70 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1zh[WlEPTB;MD6zPFk4PCEQvF2= MUjTRW5IWkWU
LXF-289 NXnxXZQzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXPJR|UxRTBwNEC0NFYh|ryP MljyV2FPT1KHUh?=
RL95-2 M1vJ[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUjJR|UxRTBwNEC1Olch|ryP NV[4NI1nW0GQR2LFVi=>
QIMR-WIL MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUL3NoYzUUN3ME2wMlQzPjd4IN88US=> M4nM[3NCVkeURWK=
K-562 NYfkR5U2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3HHUGlEPTB;MD60N|Q4OiEQvF2= M2LwO3NCVkeURWK=
NCI-H510A NUDZWXhuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV\y[mpmUUN3ME2wMlQ{QDJ|IN88US=> NYq0N|RPW0GQR2LFVi=>
NCI-H524 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn\sTWM2OD1yLkWxNVQ4KM7:TR?= NITrc3hUSU6JUlXS
KE-37 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVPJR|UxRTBwNUKxNFIh|ryP MkXJV2FPT1KHUh?=
KP-N-YS NUX6VllzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV7IcXg2UUN3ME2wMlU1Ozl{IN88US=> MYLTRW5IWkWU
LS-411N NYPjbodDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoW3TWM2OD1yLkW3O|UzKM7:TR?= NEfGPXFUSU6JUlXS
CTV-1 MoXIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4XueWlEPTB;MD61PFc4OyEQvF2= MnX5V2FPT1KHUh?=
NCI-SNU-16 NYPuTHgxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVTJR|UxRTBwNkO1O|Eh|ryP NH\Ec3FUSU6JUlXS
HT-144 MnrqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXrJR|UxRTBwNkO3PVgh|ryP MnXlV2FPT1KHUh?=
NCI-H187 NXXBRlU{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFvZUWdKSzVyPUCuOlQyOyEQvF2= MnzHV2FPT1KHUh?=
OCI-AML2 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVnJR|UxRTBwNkS0NFMh|ryP NIfkRm5USU6JUlXS
CCRF-CEM M3zkN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVP4PYc1UUN3ME2wMlY2OzR4IN88US=> M4jEWnNCVkeURWK=
ONS-76 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGjEW|lKSzVyPUCuOlY1PThizszN MUTTRW5IWkWU
IST-SL2 NWOxTpVbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGTVelNKSzVyPUCuO|E6QDJizszN MYrTRW5IWkWU
NB6 MmnyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4P3d2lEPTB;MD63O|I2PCEQvF2= M3f2VHNCVkeURWK=
SK-PN-DW MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MorYTWM2OD1yLke5NVQh|ryP NYe1bHVnW0GQR2LFVi=>
HCC1599 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkXGTWM2OD1yLkiwPFc1KM7:TR?= M2nke3NCVkeURWK=
MC116 M2TGeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NITEeXlKSzVyPUCuPFUxOTFizszN M16ycnNCVkeURWK=
TE-15 Mo\tS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXPJR|UxRTBwOEWwPVgh|ryP MYXTRW5IWkWU
HOP-62 MkDFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mlf6TWM2OD1yLki2N|I6KM7:TR?= M1L0VXNCVkeURWK=
TGBC24TKB M2KwUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlTRTWM2OD1yLki2N|g2KM7:TR?= MX3TRW5IWkWU
HCE-4 NWXVUYpPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHjQOIRKSzVyPUCuPFgxPjNizszN NE\DdnFUSU6JUlXS
ALL-PO M2rTdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVPJR|UxRTBwOEixO|Uh|ryP NFz3RpZUSU6JUlXS
KGN MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEX6fY1KSzVyPUCuPFk6QTVizszN MmDGV2FPT1KHUh?=
ML-2 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3ezZ2lEPTB;MD65NFI2QSEQvF2= MVjTRW5IWkWU
ES4 NH2zR2hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEXWTGlKSzVyPUCuPVEyOjhizszN NIHCfopUSU6JUlXS
SF126 NXnIWZg{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHHNeZZKSzVyPUCuPVQ5OTlizszN NHnrUmRUSU6JUlXS
SK-N-DZ NEHHe5VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWnJR|UxRTBwOU[xPFkh|ryP NXfxU3ViW0GQR2LFVi=>
HCC1187 NH3yVHFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkCxTWM2OD1zLkCwOVA2KM7:TR?= M4HE[HNCVkeURWK=
DU-4475 NU\BXlFrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIjrWZVKSzVyPUGuNFE4PTZizszN Mn3IV2FPT1KHUh?=
NKM-1 NFXEXHRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEPKPJlKSzVyPUGuNFI4PzVizszN MXTTRW5IWkWU
HL-60 M3u0[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NU\WXIJpUUN3ME2xMlA3PTd2IN88US=> M3XrT3NCVkeURWK=
SBC-1 NYH5SZpGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFf5WoFKSzVyPUGuNVI2PDJizszN MU\TRW5IWkWU
TE-10 NX;aenRZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmXVTWM2OD1zLkGyPVQ3KM7:TR?= NVnNVZBPW0GQR2LFVi=>
ETK-1 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXLnOmVmUUN3ME2xMlE{PjF|IN88US=> M{TxNHNCVkeURWK=
HAL-01 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX3JR|UxRTFwMU[3NFkh|ryP MlHtV2FPT1KHUh?=
BB65-RCC NUT6WWRrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml\oTWM2OD1zLkG4NFA2KM7:TR?= Ml;MV2FPT1KHUh?=
EW-1 MmCyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXzIfYtMUUN3ME2xMlE5PTZ{IN88US=> Mm\YV2FPT1KHUh?=
SK-NEP-1 NEnlRYhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWntflVKUUN3ME2xMlIyOTFzIN88US=> NETaZlhUSU6JUlXS
SK-LMS-1 NHP2fYJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUnHXGVPUUN3ME2xMlIzOjF{IN88US=> MmTyV2FPT1KHUh?=
DEL NGnic2NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFT4WoxKSzVyPUGuNlU3PDNizszN MX;TRW5IWkWU
GT3TKB NUPyb417T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX7JR|UxRTFwMkiwOVch|ryP NUDlcmtYW0GQR2LFVi=>
MOLT-16 NHfWOlJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVzCPIpqUUN3ME2xMlM2PDB3IN88US=> M1n4VHNCVkeURWK=
CMK M2H6VWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIDKTIRKSzVyPUGuOFIyOTdizszN NVLRRlhZW0GQR2LFVi=>
NB5 NUHQOo9tT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MonwTWM2OD1zLk[0NlI6KM7:TR?= NYjabJVNW0GQR2LFVi=>
NCI-H1963 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3LYPGlEPTB;MT63NFU5OyEQvF2= NYnOcZQyW0GQR2LFVi=>
KURAMOCHI M4XMS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1Tne2lEPTB;MT63PFkyOSEQvF2= NHznTY9USU6JUlXS
TE-8 Mk\mS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkS0TWM2OD1zLkiwN|Y5KM7:TR?= M1K2WnNCVkeURWK=
NCI-H1304 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYTJR|UxRTFwOEOwO|Mh|ryP Mn7WV2FPT1KHUh?=
A101D NIHEe5JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkPiTWM2OD1zLki3N|k2KM7:TR?= NY[yUVg2W0GQR2LFVi=>
SCLC-21H NIDEVlBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXzhPVN[UUN3ME2xMlk4ODV5IN88US=> MU\TRW5IWkWU
GB-1 MnL3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4DlSmlEPTB;Mj6wNVY1PyEQvF2= MX7TRW5IWkWU
KARPAS-45 NYi4O2Y3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnPETWM2OD1{LkCyOlU1KM7:TR?= M13kN3NCVkeURWK=
ATN-1 MmjqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUO2fo5RUUN3ME2yMlAzQDV6IN88US=> M3TlXnNCVkeURWK=
NCI-H720 NFLXS4lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIracplKSzVyPUKuNFYzPDRizszN NHnCbFdUSU6JUlXS
RPMI-6666 NV[5TIlzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV7JR|UxRTJwMU[yNFch|ryP NWPZd|NRW0GQR2LFVi=>
NB17 Mon4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4LnWGlEPTB;Mj6yPVI4KM7:TR?= NGi1[FhUSU6JUlXS
IST-SL1 NUDvPFVUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MW\JR|UxRTJwMkm3OlUh|ryP M3GwRnNCVkeURWK=
SH-4 NETCVVJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWnicYtlUUN3ME2yMlMzPDZ7IN88US=> M1vMOHNCVkeURWK=
K5 M3OzNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn7MTWM2OD1{LkSwN|E6KM7:TR?= MVzTRW5IWkWU
OVCAR-4 M3y1bWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEn1RmhKSzVyPUKuOFYyOyEQvF2= NFH5dZVUSU6JUlXS
ACN NI\PZ3VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWPMRWhsUUN3ME2yMlUxOjF|IN88US=> Mm[4V2FPT1KHUh?=
TGW NV7MRYVzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3y0RmlEPTB;Mj62OVg{OiEQvF2= MlrTV2FPT1KHUh?=
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NB69 M{fROGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWrsZWdLUUN3ME2xNU44PzB3IN88US=> NHW5[49USU6JUlXS
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MPP-89 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVvBeolKUUN3ME2yOU42OzF2IN88US=> NHnTfYtUSU6JUlXS
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NCI-H748 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYDJR|UxRTJ3Lke2Nlch|ryP NYP0fYpXW0GQR2LFVi=>
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LB996-RCC NIO1cYJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml3tTWM2OD1|MT6xO|AzKM7:TR?= MXLTRW5IWkWU
CHP-126 MkD2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXPYNVFJUUN3ME2zNU4yQTh2IN88US=> MoDRV2FPT1KHUh?=
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SNU-C2B NGfuTJlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVvJR|UxRTN6LkG2OVQh|ryP MV3TRW5IWkWU
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BC-1 MoXoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVTudVB2UUN3ME20Nk43PzNzIN88US=> MkPEV2FPT1KHUh?=
GI-1 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYXuXJF[UUN3ME20Nk46OTl{IN88US=> M2[wbXNCVkeURWK=
NCI-H1694 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3PHdmlEPTB;NESuPVQ4OiEQvF2= NXe3T2pWW0GQR2LFVi=>
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COR-L88 M3jH[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWjmPIRCUUN3ME20OU4zPzd6IN88US=> NX\FUZBOW0GQR2LFVi=>
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HD-MY-Z Mk\VS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUfTUpZnUUN3ME20Ok41PjF{IN88US=> MXrTRW5IWkWU
L-363 M{iw[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVfJR|UxRTR4Lki4NUDPxE1? NEnmcHRUSU6JUlXS
TE-6 NEXITHZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYPJR|UxRTR6LkS0OkDPxE1? MoTqV2FPT1KHUh?=
NCI-H345 M1zFU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoLiTWM2OD12OD60Olgh|ryP NFLkcJpUSU6JUlXS
TE-5 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUjmT5prUUN3ME20PU44OTF6IN88US=> NFznOnZUSU6JUlXS

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
DLK / p-MKK7 / MKK7 / p-JNK / JNK ; 

PubMed: 23431148     


Western blot of the DLK pathway members in RGCs (retinal ganglion cells) 4 h after immunopanning in the presence of 0, 0.03, 0.06, 0.125, 0.25, 0.5, 1, or 2 μM tozasertib. 

p-AURKA / AURKA / Survivin ; 

PubMed: 28218735     


BGC823 cells were incubated with indicated doses of VX-680 for 24 h before subjected to western blotting with the indicated antibodies. Densitometry was used to quantify the Survivin and GAPDH levels. The relative expression shown (right panel) are means±s.e.m. of the ratios of Survivin to GAPDH. 

YAP; 

PubMed: 31160567     


Western blot analysis of YAP protein level in A549 cells treated with indicated doses of VX-680 for 24 h. 

p-AKT / p-GSK3β / Cleaved caspase-3 / Cleaved PARP ; 

PubMed: 21600017     


NB4-R2 cells were collected, lysed and subjected to Western blot analysis with cleaved caspase-3, cleaved-PARP, pAkt-1 (Ser473), pGSK-3β (Ser9) specific antibodies. GAPDH was used as a loading control. Data shown is a representative of three independent experiments.

23431148 28218735 31160567 21600017
Immunofluorescence
α-tubulin / Aurora-A ; 

PubMed: 21600017     


The morphology of mitotic spindle was shown by immunofluorescence staining with anti-α-tubulin antibody and anti-Aur-A antibodies. Microtubules were stained as green, Aur-A protein as red, and nucleus as blue.

21600017
Growth inhibition assay
Cell viability; 

PubMed: 21600017     


VX-680 significantly suppresses the proliferation in a number of leukemic cell types. OCI-AML3, NB4, HL-60 and ML-1 cells were incubated with increasing doses of VX-680 (1, 2, 5 and 10 nM) for 24 hr. Cell viability was measured by MTT assay. Data summarized three independent experiments, *p < 0.05, **p < 0.01, compared to control.

21600017
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]

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Kinase inhibition assays:

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

[2]

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

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


    (Only for Reference)
Animal Research:

[1]

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  • Animal Models: Female athymic NCr-nu mice bearing HL-60 leukemia cells
  • 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
Smiles CC1=CC(=NN1)NC2=CC(=NC(=N2)SC3=CC=C(C=C3)NC(=O)C4CC4)N5CCN(CC5)C

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O
CalculateReset

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 (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*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
    V1
    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

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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID