Tozasertib (VX-680, MK-0457)

For research use only.

Catalog No.S1048

96 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 BCR-ABL tyrosine kinase, which are inhibited by the Tozasertib with both Ki of 30 nM. Tozasertib induces apoptosis and autophagy. Phase 2.

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Selleck's Tozasertib (VX-680, MK-0457) has been cited by 96 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 BCR-ABL tyrosine kinase, which are inhibited by the Tozasertib with both Ki of 30 nM. 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 MmmxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mlf5TWM2OD1yLkCwN|M5KM7:TR?= NWT3W5FWW0GQR2LFVi=>
RS4-11 NFexUWpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MULJR|UxRTBwMEC0NFQh|ryP M4qw[3NCVkeURWK=
MFH-ino NEXLUZRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWrJR|UxRTBwMEC5PUDPxE1? NXS0RpQ4W0GQR2LFVi=>
NTERA-S-cl-D1 M4HENmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mo\qTWM2OD1yLkCxOFM1KM7:TR?= MX7TRW5IWkWU
697 NGDPSoJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlPUTWM2OD1yLkCyOFcyKM7:TR?= MUPTRW5IWkWU
NALM-6 M13FbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVXJR|UxRTBwMEK1OVIh|ryP MlHPV2FPT1KHUh?=
ES8 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkHkTWM2OD1yLkC0OlE{KM7:TR?= M1rmbHNCVkeURWK=
HUTU-80 NH7wWXNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2n2dmlEPTB;MD6wOVI6QSEQvF2= NVfHZmNSW0GQR2LFVi=>
MV-4-11 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXzUcnBkUUN3ME2wMlA4Pzh{IN88US=> MWnTRW5IWkWU
MONO-MAC-6 NUXVT3V6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWPJR|UxRTBwMEe4O|kh|ryP M4jTR3NCVkeURWK=
LC-2-ad M4qxTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGWzNZhKSzVyPUCuNFg4QDlizszN M13SVnNCVkeURWK=
BL-41 M{nyU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYf0OVdKUUN3ME2wMlExPDR3IN88US=> M3zwfnNCVkeURWK=
A4-Fuk NEnMN2NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWDJR|UxRTBwMUG1OlMh|ryP M3vWN3NCVkeURWK=
SW954 M2DCbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnjwTWM2OD1yLkGyNlI6KM7:TR?= MWLTRW5IWkWU
BV-173 M3;ON2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHmxZXpKSzVyPUCuNVI3PDFizszN MmnUV2FPT1KHUh?=
TE-11 NVy1emgyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHjTenVKSzVyPUCuNVQ6QDJizszN M4\iU3NCVkeURWK=
SK-UT-1 NVv6NJVPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NW\hXId{UUN3ME2wMlE2QTZ3IN88US=> MlzVV2FPT1KHUh?=
SIG-M5 M33kcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH7MRXZKSzVyPUCuNVY4ODdizszN MVLTRW5IWkWU
OCUB-M NH\3WZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1LONGlEPTB;MD6xOlk5OyEQvF2= NYTGd2FNW0GQR2LFVi=>
K052 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFW1RpNKSzVyPUCuNVk1QCEQvF2= MoXmV2FPT1KHUh?=
VA-ES-BJ NEjremRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4\0U2lEPTB;MD6yNFA5PiEQvF2= NHrqSm9USU6JUlXS
SW982 NG\3Z5lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUm3XXJrUUN3ME2wMlIyOzhizszN MkLRV2FPT1KHUh?=
LB647-SCLC NUjrbHN3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mm\FTWM2OD1yLkKxOVI{KM7:TR?= M1O2THNCVkeURWK=
PSN1 NWnsbYQzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFPyc4RKSzVyPUCuNlIxOjZizszN Mor2V2FPT1KHUh?=
BB30-HNC NF\3bYhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkHZTWM2OD1yLkKyOVkyKM7:TR?= NIjrXWpUSU6JUlXS
ST486 NG\XemJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnH1TWM2OD1yLkKzNFg4KM7:TR?= Ml7MV2FPT1KHUh?=
MOLT-4 NHzqZXdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUDJR|UxRTBwMkOzN|ch|ryP MmLHV2FPT1KHUh?=
EW-16 NHnwd4FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXjHc4VMUUN3ME2wMlI{PzZ6IN88US=> NX7SVGtzW0GQR2LFVi=>
KS-1 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXrJR|UxRTBwMkO3PFUh|ryP M2KzXnNCVkeURWK=
SR M1i5U2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4XCd2lEPTB;MD6yOFU3PCEQvF2= M133bHNCVkeURWK=
KM12 MoPTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHr3eY1KSzVyPUCuNlY{PiEQvF2= NVTjVmlmW0GQR2LFVi=>
EM-2 NHLwVYZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{\OdWlEPTB;MD6yOlY1OSEQvF2= MmPxV2FPT1KHUh?=
MEG-01 NHr4NZpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVj0[GZ1UUN3ME2wMlI4QDR7IN88US=> M1PaVnNCVkeURWK=
NB13 NXXOTJNwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoDoTWM2OD1yLkK3PVg1KM7:TR?= M{G0fXNCVkeURWK=
RKO NWfjblB[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWfsb5V7UUN3ME2wMlMxQDF|IN88US=> M4jLeHNCVkeURWK=
CESS NWC3NZk3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmDKTWM2OD1yLkOxN|I5KM7:TR?= NY\2WlVTW0GQR2LFVi=>
EoL-1-cell MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXPoUlBlUUN3ME2wMlM{PDV7IN88US=> MYXTRW5IWkWU
DOHH-2 NHW5OpBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWHJR|UxRTBwM{O3PFEh|ryP M4nucnNCVkeURWK=
A388 NVq2[ItMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWjJR|UxRTBwM{SwPFYh|ryP MmTJV2FPT1KHUh?=
LAMA-84 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUT6NlNHUUN3ME2wMlM2OTd6IN88US=> M3O5SnNCVkeURWK=
IMR-5 NIK2SnZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmrxTWM2OD1yLkO1OVQh|ryP MX\TRW5IWkWU
KARPAS-422 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{LDRmlEPTB;MD6zO|I4OiEQvF2= MXzTRW5IWkWU
MRK-nu-1 M3SwWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWDJR|UxRTBwM{ixN{DPxE1? NGTNOY5USU6JUlXS
BL-70 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYDlT5JDUUN3ME2wMlM5QTd2IN88US=> NELYe3lUSU6JUlXS
LXF-289 M2X4XGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4rMe2lEPTB;MD60NFQxPiEQvF2= NEHLT|JUSU6JUlXS
RL95-2 NXvwW3p[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFvVRphKSzVyPUCuOFA2PjdizszN NXThNItuW0GQR2LFVi=>
QIMR-WIL M1z2Xmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXL4VHczUUN3ME2wMlQzPjd4IN88US=> M4DUfXNCVkeURWK=
K-562 NHz6UJVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkmzTWM2OD1yLkSzOFczKM7:TR?= M3nRXXNCVkeURWK=
NCI-H510A NWnROGs5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2X1e2lEPTB;MD60N|gzOyEQvF2= MUPTRW5IWkWU
NCI-H524 MlqyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWfJR|UxRTBwNUGxOFch|ryP NF7JPGtUSU6JUlXS
KE-37 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3S0[mlEPTB;MD61NlExOiEQvF2= NUnRTYhLW0GQR2LFVi=>
KP-N-YS NYr6ZlhYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEjhZVdKSzVyPUCuOVQ{QTJizszN NWW3cow3W0GQR2LFVi=>
LS-411N MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYjvW4ZCUUN3ME2wMlU4PzV{IN88US=> M{n4SnNCVkeURWK=
CTV-1 MoD5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVvJR|UxRTBwNUi3O|Mh|ryP MVjTRW5IWkWU
NCI-SNU-16 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUnBbpplUUN3ME2wMlY{PTdzIN88US=> NXnFV41GW0GQR2LFVi=>
HT-144 M4HmUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWfJR|UxRTBwNkO3PVgh|ryP NX\LNGJmW0GQR2LFVi=>
NCI-H187 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4\oS2lEPTB;MD62OFE{KM7:TR?= NHzFb4hUSU6JUlXS
OCI-AML2 M{LWeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkHJTWM2OD1yLk[0OFA{KM7:TR?= MYXTRW5IWkWU
CCRF-CEM MofjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVrncZpqUUN3ME2wMlY2OzR4IN88US=> M4HweHNCVkeURWK=
ONS-76 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIDL[o5KSzVyPUCuOlY1PThizszN M{TreHNCVkeURWK=
IST-SL2 M{LHXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M37CT2lEPTB;MD63NVk5OiEQvF2= NVPFOmp[W0GQR2LFVi=>
NB6 MlnrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYj1WWVFUUN3ME2wMlc4OjV2IN88US=> Mkn3V2FPT1KHUh?=
SK-PN-DW MnmzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIWwOY9KSzVyPUCuO|kyPCEQvF2= NU\I[INnW0GQR2LFVi=>
HCC1599 NWHIU3BFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3rINGlEPTB;MD64NFg4PCEQvF2= NH\ibGxUSU6JUlXS
MC116 Mon4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MULJR|UxRTBwOEWwNVEh|ryP NFzZO5hUSU6JUlXS
TE-15 M4r1UGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlvnTWM2OD1yLki1NFk5KM7:TR?= MlrEV2FPT1KHUh?=
HOP-62 NVfweJg1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4DJR2lEPTB;MD64OlMzQSEQvF2= MonzV2FPT1KHUh?=
TGBC24TKB NUnZXXdYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmfjTWM2OD1yLki2N|g2KM7:TR?= M3\lc3NCVkeURWK=
HCE-4 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYrBVVFCUUN3ME2wMlg5ODZ|IN88US=> Ml;1V2FPT1KHUh?=
ALL-PO MlfHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXiyNJNVUUN3ME2wMlg5OTd3IN88US=> MYjTRW5IWkWU
KGN MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkjBTWM2OD1yLki5PVk2KM7:TR?= M33zPXNCVkeURWK=
ML-2 MnnpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M12xSWlEPTB;MD65NFI2QSEQvF2= NXO3XW5RW0GQR2LFVi=>
ES4 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX7JR|UxRTBwOUGxNlgh|ryP NIrydHNUSU6JUlXS
SF126 MlTwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3u3emlEPTB;MD65OFgyQSEQvF2= M1jpenNCVkeURWK=
SK-N-DZ MmfsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoDUTWM2OD1yLkm2NVg6KM7:TR?= M{TuSXNCVkeURWK=
HCC1187 NYe2T|hWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWTq[WVLUUN3ME2xMlAxPTB3IN88US=> MXTTRW5IWkWU
DU-4475 M1H2N2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NI\POlZKSzVyPUGuNFE4PTZizszN M2nTNXNCVkeURWK=
NKM-1 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYewOFNOUUN3ME2xMlAzPzd3IN88US=> MUPTRW5IWkWU
HL-60 MoLTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFLneFhKSzVyPUGuNFY2PzRizszN M1;CVHNCVkeURWK=
SBC-1 NXi4d2Z1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWPJR|UxRTFwMUK1OFIh|ryP NWPzTmlHW0GQR2LFVi=>
TE-10 NEjWXpFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4DkV2lEPTB;MT6xNlk1PiEQvF2= MUTTRW5IWkWU
ETK-1 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NInaWZlKSzVyPUGuNVM3OTNizszN NH7Dd4tUSU6JUlXS
HAL-01 MlLHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIXvNHlKSzVyPUGuNVY4ODlizszN NHjFV4hUSU6JUlXS
BB65-RCC MnXsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mm\MTWM2OD1zLkG4NFA2KM7:TR?= NXr0cXNkW0GQR2LFVi=>
EW-1 NX\EdGxMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4DDVmlEPTB;MT6xPFU3OiEQvF2= M3v0O3NCVkeURWK=
SK-NEP-1 MlHWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX\2dnN[UUN3ME2xMlIyOTFzIN88US=> MV\TRW5IWkWU
SK-LMS-1 MkjhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVjmbnB7UUN3ME2xMlIzOjF{IN88US=> NYe0U4Q{W0GQR2LFVi=>
DEL M1HKTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVfj[WtEUUN3ME2xMlI2PjR|IN88US=> M1u2bnNCVkeURWK=
GT3TKB MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVHJR|UxRTFwMkiwOVch|ryP MUfTRW5IWkWU
MOLT-16 MnrTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHLneHBKSzVyPUGuN|U1ODVizszN MoXmV2FPT1KHUh?=
CMK NIjJeHNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2jPSGlEPTB;MT60NlEyPyEQvF2= NGLHPGxUSU6JUlXS
NB5 NIHre5dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVPPfphbUUN3ME2xMlY1OjJ7IN88US=> M33kSnNCVkeURWK=
NCI-H1963 NEHOb2ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWf5[VNQUUN3ME2xMlcxPTh|IN88US=> MWPTRW5IWkWU
KURAMOCHI MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHyyVVBKSzVyPUGuO|g6OTFizszN MoT4V2FPT1KHUh?=
TE-8 MkLGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFTEUWhKSzVyPUGuPFA{PjhizszN NHz2OmpUSU6JUlXS
NCI-H1304 NFfUN5hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{LC[WlEPTB;MT64N|A4OyEQvF2= M4q2ZXNCVkeURWK=
A101D NFXQcIhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXvCWmdvUUN3ME2xMlg4Ozl3IN88US=> NHzDWXVUSU6JUlXS
SCLC-21H M1G3N2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXLjenoyUUN3ME2xMlk4ODV5IN88US=> MVzTRW5IWkWU
GB-1 MoPUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYTJR|UxRTJwMEG2OFch|ryP NVLLSIxqW0GQR2LFVi=>
KARPAS-45 NIG1VVBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3L3Z2lEPTB;Mj6wNlY2PCEQvF2= MVLTRW5IWkWU
ATN-1 NHjpbGxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFjPe49KSzVyPUKuNFI5PThizszN M4HnT3NCVkeURWK=
NCI-H720 NH\GbWdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVT6R2ZDUUN3ME2yMlA3OjR2IN88US=> MX7TRW5IWkWU
RPMI-6666 NH[2ZotIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mk\tTWM2OD1{LkG2NlA4KM7:TR?= M3fZVnNCVkeURWK=
NB17 MlvES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV;3SIRPUUN3ME2yMlI6OjdizszN MlrNV2FPT1KHUh?=
IST-SL1 M{HneGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV7QcYN4UUN3ME2yMlI6PzZ3IN88US=> MWnTRW5IWkWU
SH-4 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4LsXGlEPTB;Mj6zNlQ3QSEQvF2= MYTTRW5IWkWU
K5 NVOzZoNkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF\RSW9KSzVyPUKuOFA{OTlizszN Mo[3V2FPT1KHUh?=
OVCAR-4 M4f2WGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVnPRYlIUUN3ME2yMlQ3OTNizszN MWnTRW5IWkWU
ACN MmLjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIHSXlNKSzVyPUKuOVAzOTNizszN MXrTRW5IWkWU
TGW NGfSUFZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYKyPWFNUUN3ME2yMlY2QDN{IN88US=> MXzTRW5IWkWU
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LS-513 NWfhTIlWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFHGPWVKSzVyPUS1MlkyPTZizszN NFjQXohUSU6JUlXS
HD-MY-Z MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIC2b5FKSzVyPUS2MlQ3OTJizszN MY\TRW5IWkWU
L-363 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUXJR|UxRTR4Lki4NUDPxE1? NVHCSoxyW0GQR2LFVi=>
TE-6 M37EU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{fE[GlEPTB;NEiuOFQ3KM7:TR?= NETDdWRUSU6JUlXS
NCI-H345 Mo[0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn22TWM2OD12OD60Olgh|ryP NHLsSFVUSU6JUlXS
TE-5 M1XhSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEn0W4lKSzVyPUS5MlcyOThizszN NXXRcWw3W0GQR2LFVi=>

... 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