Tozasertib (VX-680, MK-0457)

For research use only. Not for use in humans.

Catalog No.S1048

70 publications

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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Selleck's Tozasertib (VX-680, MK-0457) has been cited by 70 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 MkLaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYjJR|UxRTBwMECzN|gh|ryP MkT4V2FPT1KHUh?=
RS4-11 NV7SZnFQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH\RXnRKSzVyPUCuNFA1ODRizszN Mnr1V2FPT1KHUh?=
MFH-ino MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3zNWGlEPTB;MD6wNFk6KM7:TR?= NH3IS2dUSU6JUlXS
NTERA-S-cl-D1 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2DEeWlEPTB;MD6wNVQ{PCEQvF2= MnPJV2FPT1KHUh?=
697 MmfoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWLJR|UxRTBwMEK0O|Eh|ryP M4PETXNCVkeURWK=
NALM-6 NF7kd3RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVz1UJhmUUN3ME2wMlAzPTV{IN88US=> NGLoPYVUSU6JUlXS
ES8 M3WwZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1vWTmlEPTB;MD6wOFYyOyEQvF2= MV3TRW5IWkWU
HUTU-80 NITMOY9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3:5cWlEPTB;MD6wOVI6QSEQvF2= NVXIRW94W0GQR2LFVi=>
MV-4-11 NH;wc|NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIj3TXZKSzVyPUCuNFc4QDJizszN M2L3SnNCVkeURWK=
MONO-MAC-6 M{fPNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXnJR|UxRTBwMEe4O|kh|ryP NX;sN5RZW0GQR2LFVi=>
LC-2-ad MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NG[zcmJKSzVyPUCuNFg4QDlizszN Mn35V2FPT1KHUh?=
BL-41 Mm[zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV7lbYdRUUN3ME2wMlExPDR3IN88US=> MUPTRW5IWkWU
A4-Fuk NI\yXJNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnzXTWM2OD1yLkGxOVY{KM7:TR?= M3;KWHNCVkeURWK=
SW954 NVrxN49{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWLXTmZ3UUN3ME2wMlEzOjJ7IN88US=> MXrTRW5IWkWU
BV-173 MmTiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH7xPY1KSzVyPUCuNVI3PDFizszN MoLUV2FPT1KHUh?=
TE-11 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlLjTWM2OD1yLkG0PVgzKM7:TR?= MkPkV2FPT1KHUh?=
SK-UT-1 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1i4bGlEPTB;MD6xOVk3PSEQvF2= M1\2V3NCVkeURWK=
SIG-M5 NHrnfYdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlHpTWM2OD1yLkG2O|A4KM7:TR?= NXqxRYtGW0GQR2LFVi=>
OCUB-M MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIDyfXpKSzVyPUCuNVY6QDNizszN MXLTRW5IWkWU
K052 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGW4dZFKSzVyPUCuNVk1QCEQvF2= MYHTRW5IWkWU
VA-ES-BJ M37EXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4DhS2lEPTB;MD6yNFA5PiEQvF2= M{TuPXNCVkeURWK=
SW982 NI\wWYdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2TSOGlEPTB;MD6yNVM5KM7:TR?= Mlq5V2FPT1KHUh?=
LB647-SCLC M{fEWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3fnWWlEPTB;MD6yNVUzOyEQvF2= M1vn[3NCVkeURWK=
PSN1 NFrtSHdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn6wTWM2OD1yLkKyNFI3KM7:TR?= M4jkOHNCVkeURWK=
BB30-HNC M13TU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkL5TWM2OD1yLkKyOVkyKM7:TR?= M1LMTnNCVkeURWK=
ST486 MmLhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXTu[3g5UUN3ME2wMlI{ODh5IN88US=> M{X4b3NCVkeURWK=
MOLT-4 NVzCV3pZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWnW[VZqUUN3ME2wMlI{OzN5IN88US=> M3L2VXNCVkeURWK=
EW-16 NWrYZ217T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFqzUXNKSzVyPUCuNlM4PjhizszN M2GwWHNCVkeURWK=
KS-1 MkG2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml\HTWM2OD1yLkKzO|g2KM7:TR?= MlnmV2FPT1KHUh?=
SR MmLGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3;rTmlEPTB;MD6yOFU3PCEQvF2= MWXTRW5IWkWU
KM12 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4HtRWlEPTB;MD6yOlM3KM7:TR?= NHTYT|BUSU6JUlXS
EM-2 Ml;tS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{\QUGlEPTB;MD6yOlY1OSEQvF2= MmqyV2FPT1KHUh?=
MEG-01 M4\6PGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHjyZnZKSzVyPUCuNlc5PDlizszN NE\QWItUSU6JUlXS
NB13 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEmwdHJKSzVyPUCuNlc6QDRizszN M4LpPHNCVkeURWK=
RKO NXXEXphDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFvCSItKSzVyPUCuN|A5OTNizszN NFq5cmdUSU6JUlXS
CESS MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV[3Z493UUN3ME2wMlMyOzJ6IN88US=> NWH2WnVQW0GQR2LFVi=>
EoL-1-cell NYrzSZl4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVH5e5ZqUUN3ME2wMlM{PDV7IN88US=> M{nte3NCVkeURWK=
DOHH-2 NEXMVY5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWjGW5RKUUN3ME2wMlM{PzhzIN88US=> M{K0T3NCVkeURWK=
A388 M{\WV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEDuWlZKSzVyPUCuN|QxQDZizszN MVTTRW5IWkWU
LAMA-84 NGLHNYpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX[wfIxzUUN3ME2wMlM2OTd6IN88US=> NHL3SY1USU6JUlXS
IMR-5 Mo\PS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUDJR|UxRTBwM{W1OEDPxE1? MUHTRW5IWkWU
KARPAS-422 M3XNXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXTJR|UxRTBwM{eyO|Ih|ryP MW\TRW5IWkWU
MRK-nu-1 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUfLRXBXUUN3ME2wMlM5OTNizszN NH;3OXVUSU6JUlXS
BL-70 M3XGU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF3ENJZKSzVyPUCuN|g6PzRizszN NEHVcGJUSU6JUlXS
LXF-289 NVXBTJhMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXrOcZg3UUN3ME2wMlQxPDB4IN88US=> MV7TRW5IWkWU
RL95-2 M3L5Vmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4nkXWlEPTB;MD60NFU3PyEQvF2= NVnVb5lHW0GQR2LFVi=>
QIMR-WIL NH7I[VhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUjDeo9TUUN3ME2wMlQzPjd4IN88US=> NFLBdFlUSU6JUlXS
K-562 M2K1Nmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWTGRXN5UUN3ME2wMlQ{PDd{IN88US=> M{\VOHNCVkeURWK=
NCI-H510A M{DINWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3KwPWlEPTB;MD60N|gzOyEQvF2= M{nFNHNCVkeURWK=
NCI-H524 M2\1OGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYnvTm1NUUN3ME2wMlUyOTR5IN88US=> M2HndXNCVkeURWK=
KE-37 MoXyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWjCeGNqUUN3ME2wMlUzOTB{IN88US=> MXvTRW5IWkWU
KP-N-YS MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1;5[2lEPTB;MD61OFM6OiEQvF2= M{nVUHNCVkeURWK=
LS-411N NYWzW2Z[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkHoTWM2OD1yLkW3O|UzKM7:TR?= MmD5V2FPT1KHUh?=
CTV-1 NGKxb3ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{HLOGlEPTB;MD61PFc4OyEQvF2= M37VV3NCVkeURWK=
NCI-SNU-16 NGLXR4VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVnJR|UxRTBwNkO1O|Eh|ryP NGPrVXBUSU6JUlXS
HT-144 MmXqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFTTOJlKSzVyPUCuOlM4QThizszN MV\TRW5IWkWU
NCI-H187 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWXJR|UxRTBwNkSxN{DPxE1? MYrTRW5IWkWU
OCI-AML2 NXz5XXc3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3LVZ2lEPTB;MD62OFQxOyEQvF2= M2O1XnNCVkeURWK=
CCRF-CEM NFnR[lJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmPTTWM2OD1yLk[1N|Q3KM7:TR?= MWHTRW5IWkWU
ONS-76 M4f5WGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXHJR|UxRTBwNk[0OVgh|ryP MUHTRW5IWkWU
IST-SL2 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkDSTWM2OD1yLkexPVgzKM7:TR?= NGDCe3BUSU6JUlXS
NB6 MoLYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlrYTWM2OD1yLke3NlU1KM7:TR?= NVPuUJNYW0GQR2LFVi=>
SK-PN-DW NWnSOIYxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M37HOmlEPTB;MD63PVE1KM7:TR?= MUTTRW5IWkWU
HCC1599 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFfQRXFKSzVyPUCuPFA5PzRizszN M{H2PHNCVkeURWK=
MC116 NIW5Vo1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MULJR|UxRTBwOEWwNVEh|ryP NGfkWVZUSU6JUlXS
TE-15 NV3YNZZ4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3;adGlEPTB;MD64OVA6QCEQvF2= M2DiN3NCVkeURWK=
HOP-62 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEezNVVKSzVyPUCuPFY{OjlizszN NIDhfVVUSU6JUlXS
TGBC24TKB Mmj3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEXmWpRKSzVyPUCuPFY{QDVizszN NEK2U3dUSU6JUlXS
HCE-4 M{\qWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXXJR|UxRTBwOEiwOlMh|ryP NUPjcldzW0GQR2LFVi=>
ALL-PO Mmm1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUnmU3ZJUUN3ME2wMlg5OTd3IN88US=> NET6To5USU6JUlXS
KGN NXjBTXlxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml3wTWM2OD1yLki5PVk2KM7:TR?= MlXEV2FPT1KHUh?=
ML-2 NV63UllbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlTyTWM2OD1yLkmwNlU6KM7:TR?= NIrueWtUSU6JUlXS
ES4 MkDuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlTlTWM2OD1yLkmxNVI5KM7:TR?= NY\qUXhSW0GQR2LFVi=>
SF126 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEfPNHJKSzVyPUCuPVQ5OTlizszN MmiyV2FPT1KHUh?=
SK-N-DZ NWPpSVRTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGPERVZKSzVyPUCuPVYyQDlizszN NUHoVm5XW0GQR2LFVi=>
HCC1187 M1vTT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWXJR|UxRTFwMEC1NFUh|ryP NX;RW297W0GQR2LFVi=>
DU-4475 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVHiO5M6UUN3ME2xMlAyPzV4IN88US=> MmjjV2FPT1KHUh?=
NKM-1 NHPTSYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVXJR|UxRTFwMEK3O|Uh|ryP M1nEZ3NCVkeURWK=
HL-60 NUXWdVJCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFv6UW1KSzVyPUGuNFY2PzRizszN NXn3Zm1lW0GQR2LFVi=>
SBC-1 Mnf4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXHEbml6UUN3ME2xMlEzPTR{IN88US=> NGrXXXRUSU6JUlXS
TE-10 MnjhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF\YUWpKSzVyPUGuNVI6PDZizszN MkD1V2FPT1KHUh?=
ETK-1 NVK5b3cyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4PJNGlEPTB;MT6xN|YyOyEQvF2= NVTQOFN4W0GQR2LFVi=>
HAL-01 MlrrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXLRZWlJUUN3ME2xMlE3PzB7IN88US=> NYrifmJGW0GQR2LFVi=>
BB65-RCC M130ZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYDldFFwUUN3ME2xMlE5ODB3IN88US=> MVjTRW5IWkWU
EW-1 NXr2[21vT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2rVcGlEPTB;MT6xPFU3OiEQvF2= MoG5V2FPT1KHUh?=
SK-NEP-1 NHrvfFVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MU\JR|UxRTFwMkGxNVEh|ryP NE\uTZNUSU6JUlXS
SK-LMS-1 Mmq5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV;JR|UxRTFwMkKyNVIh|ryP NXqw[XV[W0GQR2LFVi=>
DEL M134ZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV7hcVdNUUN3ME2xMlI2PjR|IN88US=> NIXUVVdUSU6JUlXS
GT3TKB M2jPSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mmm1TWM2OD1zLkK4NFU4KM7:TR?= MkPKV2FPT1KHUh?=
MOLT-16 NHHkRnlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV7WSWl6UUN3ME2xMlM2PDB3IN88US=> MkX3V2FPT1KHUh?=
CMK NIjHSZNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVPJR|UxRTFwNEKxNVch|ryP MUHTRW5IWkWU
NB5 MknyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV7JR|UxRTFwNkSyNlkh|ryP M3jBPXNCVkeURWK=
NCI-H1963 Ml;uS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHfoXXVKSzVyPUGuO|A2QDNizszN M2K4bHNCVkeURWK=
KURAMOCHI NGLIPYtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX;OeWFqUUN3ME2xMlc5QTFzIN88US=> NYHRdJVTW0GQR2LFVi=>
TE-8 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVLTXpJPUUN3ME2xMlgxOzZ6IN88US=> MVXTRW5IWkWU
NCI-H1304 M3r0bWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGGzRVNKSzVyPUGuPFMxPzNizszN MX7TRW5IWkWU
A101D NVLwVFR{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlXCTWM2OD1zLki3N|k2KM7:TR?= MV\TRW5IWkWU
SCLC-21H MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{nEN2lEPTB;MT65O|A2PyEQvF2= M1e1Z3NCVkeURWK=
GB-1 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MljpTWM2OD1{LkCxOlQ4KM7:TR?= NVKyUZdoW0GQR2LFVi=>
KARPAS-45 NY\pU|l5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYrJR|UxRTJwMEK2OVQh|ryP NYjUV4Q2W0GQR2LFVi=>
ATN-1 NGP6TXNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnjpTWM2OD1{LkCyPFU5KM7:TR?= Mnu0V2FPT1KHUh?=
NCI-H720 Mo\ZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mlm4TWM2OD1{LkC2NlQ1KM7:TR?= MVrTRW5IWkWU
RPMI-6666 M336O2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoG1TWM2OD1{LkG2NlA4KM7:TR?= MV\TRW5IWkWU
NB17 NXS3UFR[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnrITWM2OD1{LkK5Nlch|ryP NVHZVJNUW0GQR2LFVi=>
IST-SL1 NIfXSoxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGnQW|lKSzVyPUKuNlk4PjVizszN NGn0clVUSU6JUlXS
SH-4 MnrFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mk\tTWM2OD1{LkOyOFY6KM7:TR?= MWnTRW5IWkWU
K5 M{PZeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVrJR|UxRTJwNECzNVkh|ryP Ml7JV2FPT1KHUh?=
OVCAR-4 M1;4e2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV\JR|UxRTJwNE[xN{DPxE1? M2TMZXNCVkeURWK=
ACN NVuxdHl4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXr4SFhXUUN3ME2yMlUxOjF|IN88US=> MkXTV2FPT1KHUh?=
TGW Moi1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3:wcWlEPTB;Mj62OVg{OiEQvF2= MWrTRW5IWkWU
NCI-H2107 NGG4epdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX\JR|UxRTJwOEO3NVEh|ryP MVPTRW5IWkWU
NCI-H82 NYrFOGlxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWC4fm1rUUN3ME2yMlg{QDN6IN88US=> NHjZ[XFUSU6JUlXS
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TE-6 Mo[2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmrMTWM2OD12OD60OFYh|ryP MUjTRW5IWkWU
NCI-H345 NH;VbGFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3r6SWlEPTB;NEiuOFY5KM7:TR?= M3vZU3NCVkeURWK=
TE-5 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1vRVmlEPTB;NEmuO|EyQCEQvF2= MXHTRW5IWkWU

... 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
  • 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
Smiles CN1CCN(CC1)C2=NC(=NC(=C2)NC3=N[NH]C(=C3)C)SC4=CC=C(NC(=O)C5CC5)C=C4

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)

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

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

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

Molecular Weight Calculator

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

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Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

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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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selleck catalog

Aurora Kinase Signaling Pathway Map

Aurora Kinase Inhibitors with Unique Features

  • Pan Aurora Kinase Inhibitors

    Danusertib (PHA-739358) : Pan-Aurora kinase inhibitor, Aurora A/B/C, IC50=13 nM/79 nM/61 nM.

  • Pan Aurora Kinase Inhibitors

    SNS-314 Mesylate : Pan-Aurora kinase inhibitor, Aurora A/B/C, IC50=9 nM/31 nM/3 nM.

  • Most Potent Aurora Kinase Inhibitor

    MK-5108 (VX-689) : Aurora A, IC50=0.064 nM.

  • Aurora Kinase Inhibitor in Clinical Trial

    Alisertib (MLN8237) : Phase III for Relapsed/Refractory Peripheral T-Cell Lymphoma.

  • Classic Aurora Kinase Inhibitor

    Hesperadin : Potently inhibits Aurora B with IC50 of 250 nM.

Related Aurora Kinase Products

  • Ro-3306 New

    RO-3306 is an ATP-competitive, and selective CDK1 inhibitor with Ki of 20 nM, >15-fold selectivity against a diverse panel of human kinases.

  • CCG-1423 New

    CCG-1423 is a specific RhoA pathway inhibitor, which inhibits SRF-mediated transcription.

  • ML141 New

    ML141 (CID-2950007), is demonstrated to be a potent, selective and reversible non-competitive inhibitor of Cdc42 GTPase suitable for in vitro assays, with IC50 of 200 nM and selectivity against other members of the Rho family of GTPases (Rac1, Rab2, Rab7).

  • Alisertib (MLN8237)

    Alisertib (MLN8237) is a selective Aurora A inhibitor with IC50 of 1.2 nM in a cell-free assay. It has >200-fold higher selectivity for Aurora A than Aurora B. Phase 3.

    Features:First orally available inhibitor of Aurora A.

  • Barasertib (AZD1152-HQPA)

    Barasertib (AZD1152-HQPA) is a highly selective Aurora B inhibitor with IC50 of 0.37 nM in a cell-free assay, ~3700 fold more selective for Aurora B over Aurora A. Phase 1.

  • Danusertib (PHA-739358)

    Danusertib (PHA-739358) is an Aurora kinase inhibitor for Aurora A/B/C with IC50 of 13 nM/79 nM/61 nM in cell-free assays, modestly potent to Abl, TrkA, c-RET and FGFR1, and less potent to Lck, VEGFR2/3, c-Kit, CDK2, etc. Phase 2.

  • ZM 447439

    ZM 447439 is a selective and ATP-competitive inhibitor for Aurora A and Aurora B with IC50 of 110 nM and 130 nM, respectively. It is more than 8-fold selective for Aurora A/B than MEK1, Src, Lck and has little effect against CDK1/2/4, Plk1, Chk1, etc.

    Features:An Aurora selective ATP-competitive inhibitor.

  • MLN8054

    MLN8054 is a potent and selective inhibitor of Aurora A with IC50 of 4 nM in Sf9 insect cell. It is more than 40-fold selective for Aurora A than Aurora B. Phase 1.

  • MK-5108 (VX-689)

    MK-5108 (VX-689) is a highly selective Aurora A inhibitor with IC50 of 0.064 nM in a cell-free assay and is 220- and 190-fold more selective for Aurora A than Aurora B/C, while it inhibits TrkA with less than 100-fold selectivity. Phase 1.

  • Aurora A Inhibitor I (TC-S 7010)

    Aurora A Inhibitor I is a novel, potent, and selective inhibitor of Aurora A with IC50 of 3.4 nM in a cell-free assay. It is 1000-fold more selective for Aurora A than Aurora B.

    Features:Aurora A Inhibitor I is a novel, potent, and selective inhibitor to Aurora A.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID