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 53 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 NV\RZnNkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2jv[2lEPTB;MD6wNFM{QCEQvF2= NFnFVohUSU6JUlXS
RS4-11 NH7kUmFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{TwSWlEPTB;MD6wNFQxPCEQvF2= MkjJV2FPT1KHUh?=
MFH-ino NXLhdnZnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX;JR|UxRTBwMEC5PUDPxE1? MnfrV2FPT1KHUh?=
NTERA-S-cl-D1 MlHES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHOwRndKSzVyPUCuNFE1OzRizszN MYrTRW5IWkWU
697 M3X6VWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{j2WmlEPTB;MD6wNlQ4OSEQvF2= MW\TRW5IWkWU
NALM-6 NEnycY9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHz1TYRKSzVyPUCuNFI2PTJizszN NVjIOVl[W0GQR2LFVi=>
ES8 M3jHcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3LPV2lEPTB;MD6wOFYyOyEQvF2= M32ybHNCVkeURWK=
HUTU-80 M3PiN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mo[2TWM2OD1yLkC1Nlk6KM7:TR?= M2fKXnNCVkeURWK=
MV-4-11 NUnSXoRpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWTJR|UxRTBwMEe3PFIh|ryP MkjoV2FPT1KHUh?=
MONO-MAC-6 M{TncWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGHCSppKSzVyPUCuNFc5PzlizszN NFHDR2xUSU6JUlXS
LC-2-ad MoDBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWDJR|UxRTBwMEi3PFkh|ryP M36xeHNCVkeURWK=
BL-41 M2\5RWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXXsO3dGUUN3ME2wMlExPDR3IN88US=> NEnZNHdUSU6JUlXS
A4-Fuk M4nXN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MofvTWM2OD1yLkGxOVY{KM7:TR?= M2jhWXNCVkeURWK=
SW954 M2XRbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUjJR|UxRTBwMUKyNlkh|ryP NUHJNW1DW0GQR2LFVi=>
BV-173 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIPXPGJKSzVyPUCuNVI3PDFizszN MkKwV2FPT1KHUh?=
TE-11 NVn1dFI2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn7NTWM2OD1yLkG0PVgzKM7:TR?= NXXTXlFrW0GQR2LFVi=>
SK-UT-1 M2LxO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV;lfWpWUUN3ME2wMlE2QTZ3IN88US=> NUC3Xmc6W0GQR2LFVi=>
SIG-M5 NULm[Y97T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{jhVWlEPTB;MD6xOlcxPyEQvF2= MXnTRW5IWkWU
OCUB-M NX21TW5DT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml;wTWM2OD1yLkG2PVg{KM7:TR?= MV;TRW5IWkWU
K052 MnLFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVy2V3Y3UUN3ME2wMlE6PDhizszN NYm3W2tRW0GQR2LFVi=>
VA-ES-BJ MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3rhW2lEPTB;MD6yNFA5PiEQvF2= NIrU[GVUSU6JUlXS
SW982 MoTKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEjDNI1KSzVyPUCuNlE{QCEQvF2= M{ji[HNCVkeURWK=
LB647-SCLC M1nZS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFTi[ZhKSzVyPUCuNlE2OjNizszN M1zqOXNCVkeURWK=
PSN1 M1nadmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFPTcoZKSzVyPUCuNlIxOjZizszN MXnTRW5IWkWU
BB30-HNC M17wSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4fsfGlEPTB;MD6yNlU6OSEQvF2= MUPTRW5IWkWU
ST486 NWLDeHZjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnLnTWM2OD1yLkKzNFg4KM7:TR?= NVzHTnd5W0GQR2LFVi=>
MOLT-4 M4HsVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUjJR|UxRTBwMkOzN|ch|ryP NYr6VY55W0GQR2LFVi=>
EW-16 NWS5[|llT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIXaSWtKSzVyPUCuNlM4PjhizszN NX7wXpBbW0GQR2LFVi=>
KS-1 M4nrSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV3EToU2UUN3ME2wMlI{Pzh3IN88US=> M{nFcHNCVkeURWK=
SR NEHuUpdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVnJR|UxRTBwMkS1OlQh|ryP MVHTRW5IWkWU
KM12 NFzObnVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4DWV2lEPTB;MD6yOlM3KM7:TR?= M2K3[HNCVkeURWK=
EM-2 NID2[XRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVjJR|UxRTBwMk[2OFEh|ryP MnK3V2FPT1KHUh?=
MEG-01 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1L5U2lEPTB;MD6yO|g1QSEQvF2= M4SyZ3NCVkeURWK=
NB13 MkP6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHjvVnRKSzVyPUCuNlc6QDRizszN M3fBSnNCVkeURWK=
RKO NXvvRVFTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUL3WFBxUUN3ME2wMlMxQDF|IN88US=> M1\j[HNCVkeURWK=
CESS MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUXJR|UxRTBwM{GzNlgh|ryP NUK1ZZFUW0GQR2LFVi=>
EoL-1-cell MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4jZS2lEPTB;MD6zN|Q2QSEQvF2= NH72UFdUSU6JUlXS
DOHH-2 NFjVZZRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYr2XGpmUUN3ME2wMlM{PzhzIN88US=> Ml;LV2FPT1KHUh?=
A388 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYXHUXNkUUN3ME2wMlM1ODh4IN88US=> M{jHR3NCVkeURWK=
LAMA-84 M2fYSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4[zR2lEPTB;MD6zOVE4QCEQvF2= NIT3[oZUSU6JUlXS
IMR-5 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3HZVGlEPTB;MD6zOVU1KM7:TR?= M{nnbnNCVkeURWK=
KARPAS-422 Mkj3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkH4TWM2OD1yLkO3NlczKM7:TR?= M2m1eXNCVkeURWK=
MRK-nu-1 MmrBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2nZRWlEPTB;MD6zPFE{KM7:TR?= M1XiNHNCVkeURWK=
BL-70 MnW1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF3wPVJKSzVyPUCuN|g6PzRizszN M1Ox[nNCVkeURWK=
LXF-289 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHPUXYRKSzVyPUCuOFA1ODZizszN M2DWTnNCVkeURWK=
RL95-2 M{TFTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH7LV|FKSzVyPUCuOFA2PjdizszN NEC3VnZUSU6JUlXS
QIMR-WIL MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFnmXmdKSzVyPUCuOFI3PzZizszN M2C4RXNCVkeURWK=
K-562 M3TqWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXj2SohNUUN3ME2wMlQ{PDd{IN88US=> MVvTRW5IWkWU
NCI-H510A MlL6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYLJR|UxRTBwNEO4NlMh|ryP MkP2V2FPT1KHUh?=
NCI-H524 Mn\ZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFPLcXhKSzVyPUCuOVEyPDdizszN M2PhN3NCVkeURWK=
KE-37 MkjWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1nBVGlEPTB;MD61NlExOiEQvF2= MWHTRW5IWkWU
KP-N-YS M3O2N2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4fINmlEPTB;MD61OFM6OiEQvF2= NFLGRZNUSU6JUlXS
LS-411N M4nSR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlzITWM2OD1yLkW3O|UzKM7:TR?= MnyzV2FPT1KHUh?=
CTV-1 M13GWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXvUTVkyUUN3ME2wMlU5Pzd|IN88US=> NV;Tb3p7W0GQR2LFVi=>
NCI-SNU-16 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYXEe2FLUUN3ME2wMlY{PTdzIN88US=> NY\rbGprW0GQR2LFVi=>
HT-144 MnLuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3myemlEPTB;MD62N|c6QCEQvF2= Mnj6V2FPT1KHUh?=
NCI-H187 MmPRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXW4[HR{UUN3ME2wMlY1OTNizszN MkmyV2FPT1KHUh?=
OCI-AML2 NFnmN4lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYfN[5J[UUN3ME2wMlY1PDB|IN88US=> MkP4V2FPT1KHUh?=
CCRF-CEM MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M33hd2lEPTB;MD62OVM1PiEQvF2= MnPzV2FPT1KHUh?=
ONS-76 NFrDTHlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2rmTmlEPTB;MD62OlQ2QCEQvF2= NWixWHdDW0GQR2LFVi=>
IST-SL2 MlXoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXXkNpN1UUN3ME2wMlcyQTh{IN88US=> MoXHV2FPT1KHUh?=
NB6 M13uZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3:0XmlEPTB;MD63O|I2PCEQvF2= MnH0V2FPT1KHUh?=
SK-PN-DW MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmTmTWM2OD1yLke5NVQh|ryP MYnTRW5IWkWU
HCC1599 NYHzdnJ5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUD1eGdrUUN3ME2wMlgxQDd2IN88US=> Mm\iV2FPT1KHUh?=
MC116 M4jMOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGDJe5ZKSzVyPUCuPFUxOTFizszN MkDIV2FPT1KHUh?=
TE-15 M4L2Z2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXTBPZViUUN3ME2wMlg2ODl6IN88US=> NV\DUnhOW0GQR2LFVi=>
HOP-62 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVrJR|UxRTBwOE[zNlkh|ryP MmLWV2FPT1KHUh?=
TGBC24TKB NVf6[Wk4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3\0emlEPTB;MD64OlM5PSEQvF2= MojjV2FPT1KHUh?=
HCE-4 MlHwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH3PZoFKSzVyPUCuPFgxPjNizszN Ml;TV2FPT1KHUh?=
ALL-PO M2rETWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXXmbpdtUUN3ME2wMlg5OTd3IN88US=> MWXTRW5IWkWU
KGN MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWfCZ4FnUUN3ME2wMlg6QTl3IN88US=> MknzV2FPT1KHUh?=
ML-2 M1nmNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmDyTWM2OD1yLkmwNlU6KM7:TR?= NXq2[YMzW0GQR2LFVi=>
ES4 Mkf0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{LPPGlEPTB;MD65NVEzQCEQvF2= MXnTRW5IWkWU
SF126 NF;YfW9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MW\JR|UxRTBwOUS4NVkh|ryP NIW2XpRUSU6JUlXS
SK-N-DZ MmLKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlK5TWM2OD1yLkm2NVg6KM7:TR?= NHzrfWdUSU6JUlXS
HCC1187 NWjlSWt1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEGxNYxKSzVyPUGuNFA2ODVizszN NWG5RXhsW0GQR2LFVi=>
DU-4475 NHnzdGNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NE[2folKSzVyPUGuNFE4PTZizszN NW\4[GVtW0GQR2LFVi=>
NKM-1 NE\tbWlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlPBTWM2OD1zLkCyO|c2KM7:TR?= NFraSlhUSU6JUlXS
HL-60 M2\RSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnTuTWM2OD1zLkC2OVc1KM7:TR?= MWHTRW5IWkWU
SBC-1 NXSyZZpXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWnHd5ljUUN3ME2xMlEzPTR{IN88US=> MWTTRW5IWkWU
TE-10 M3PSWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{j4VmlEPTB;MT6xNlk1PiEQvF2= MXfTRW5IWkWU
ETK-1 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUXJR|UxRTFwMUO2NVMh|ryP NEPVfI9USU6JUlXS
HAL-01 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2TybmlEPTB;MT6xOlcxQSEQvF2= M2TxSHNCVkeURWK=
BB65-RCC Mlm5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF34RYVKSzVyPUGuNVgxODVizszN MXnTRW5IWkWU
EW-1 NHXQSWxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoLqTWM2OD1zLkG4OVYzKM7:TR?= MnvFV2FPT1KHUh?=
SK-NEP-1 Mk\6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWPJR|UxRTFwMkGxNVEh|ryP Mn3VV2FPT1KHUh?=
SK-LMS-1 NF3RPHBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVn0PFZwUUN3ME2xMlIzOjF{IN88US=> M1K1TXNCVkeURWK=
DEL NX7NfpVpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFTLZ21KSzVyPUGuNlU3PDNizszN NYnVOVYyW0GQR2LFVi=>
GT3TKB MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHr3Zm9KSzVyPUGuNlgxPTdizszN MWjTRW5IWkWU
MOLT-16 M1mzRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFTXflNKSzVyPUGuN|U1ODVizszN NIn6TZlUSU6JUlXS
CMK M4jPd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXLJR|UxRTFwNEKxNVch|ryP MmjBV2FPT1KHUh?=
NB5 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkLQTWM2OD1zLk[0NlI6KM7:TR?= MXzTRW5IWkWU
NCI-H1963 M4jRPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWTjNJNDUUN3ME2xMlcxPTh|IN88US=> NHTBUYlUSU6JUlXS
KURAMOCHI Ml\yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{\ONWlEPTB;MT63PFkyOSEQvF2= MXHTRW5IWkWU
TE-8 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NW\LVlVbUUN3ME2xMlgxOzZ6IN88US=> MYrTRW5IWkWU
NCI-H1304 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWHJR|UxRTFwOEOwO|Mh|ryP NYjJS3pvW0GQR2LFVi=>
A101D NH;0fnNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1iy[GlEPTB;MT64O|M6PSEQvF2= M2rGdXNCVkeURWK=
SCLC-21H NF;YSHlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVHJR|UxRTFwOUewOVch|ryP M3jCZXNCVkeURWK=
GB-1 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFvIVmxKSzVyPUKuNFE3PDdizszN M2PLdHNCVkeURWK=
KARPAS-45 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1Hp[WlEPTB;Mj6wNlY2PCEQvF2= NWfKUZc6W0GQR2LFVi=>
ATN-1 MoD2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX;lfIJOUUN3ME2yMlAzQDV6IN88US=> MoLDV2FPT1KHUh?=
NCI-H720 NITaN3JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGLHS2hKSzVyPUKuNFYzPDRizszN MmjnV2FPT1KHUh?=
RPMI-6666 M4i2VGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXzJR|UxRTJwMU[yNFch|ryP M4P4VnNCVkeURWK=
NB17 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYnJR|UxRTJwMkmyO{DPxE1? MknXV2FPT1KHUh?=
IST-SL1 M2jL[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEnEd5ZKSzVyPUKuNlk4PjVizszN MlfZV2FPT1KHUh?=
SH-4 MmnTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWfJR|UxRTJwM{K0Olkh|ryP MVzTRW5IWkWU
K5 MlWzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVnJR|UxRTJwNECzNVkh|ryP NUfMXJNxW0GQR2LFVi=>
OVCAR-4 NHj4fldIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M162dWlEPTB;Mj60OlE{KM7:TR?= M33LWHNCVkeURWK=
ACN MmPGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYWwOmhtUUN3ME2yMlUxOjF|IN88US=> NIrqRm5USU6JUlXS
TGW NFXRVpVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NE\sOG5KSzVyPUKuOlU5OzJizszN NGrvS3JUSU6JUlXS
NCI-H2107 NV7UTmpTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXXQXIFoUUN3ME2yMlg{PzFzIN88US=> MUPTRW5IWkWU
NCI-H82 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGrxW|lKSzVyPUKuPFM5OzhizszN MV;TRW5IWkWU
SK-N-FI MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2DNXGlEPTB;Mj64Olg3QCEQvF2= MlPZV2FPT1KHUh?=
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TE-6 NVrQN2R5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV;JR|UxRTR6LkS0OkDPxE1? NXHIcFdkW0GQR2LFVi=>
NCI-H345 M4HYdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV;ydlN7UUN3ME20PE41PjhizszN NETLbVdUSU6JUlXS
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... 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 (mg) = Concentration (mM) × Volume (mL) × 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

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