Cat. No.: HY-10161

Tozasertib

(Synonyms: VX 680; MK-0457)

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Tozasertib (VX 680; MK-0457) is an inhibitor of Aurora A/B/C kinases with K_is of 0.6, 18, 4.6 nM, respectively.

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Pureté: 99.92%
CAS No.: 639089-54-6
Formule: C₂₃H₂₈N₈OS
Masse moléculaire:464.59

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* In solvent : -80°C, 1 year; -20°C, 6 months (protect from light)

Tozasertib Chemical Structure

CAS No.: 639089-54-6

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Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- Essai clinique
Chemical Information
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Activité biologique

Description

Tozasertib (VX 680; MK-0457) is an inhibitor of Aurora A/B/C kinases with K_is of 0.6, 18, 4.6 nM, respectively.

IC₅₀ & Target^[1]

Aurora A

0.6 nM (Ki)

Aurora B

18 nM (Ki)

Aurora C

4.6 nM (Ki)

Voir tous les produits spécifiques à Isoform Aurora Kinase :

Cellular Effect

Cell Line	Type	Value	Description	References
A-431	IC₅₀	0.24 μM Compound: VX-680	Antiproliferative activity against human A431 cells after 48 hrs by CCK8 assay Antiproliferative activity against human A431 cells after 48 hrs by CCK8 assay	[PMID: 29358147]
A-431	IC₅₀	0.24 μM Compound: VX-680, MK-0457	Antiproliferative activity against human A431 cells assessed as cell viability after 72 hrs by CCK8 assay Antiproliferative activity against human A431 cells assessed as cell viability after 72 hrs by CCK8 assay	[PMID: 24681066]
A549	GI₅₀	35.8 μM Compound: VX-680	Antiproliferative activity against human A549 cells after 48 hrs by MTT assay Antiproliferative activity against human A549 cells after 48 hrs by MTT assay	[PMID: 30502115]
A549	IC₅₀	15.06 μM Compound: VX-680	Anticancer activity against human A549 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay Anticancer activity against human A549 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay	[PMID: 35476959]
A549	IC₅₀	19.4 μM Compound: VX-680	Cytotoxicity against human A549 cells after 48 hrs by MTT assay Cytotoxicity against human A549 cells after 48 hrs by MTT assay	[PMID: 25812967]
A549	IC₅₀	3.05 μM Compound: VX-680, MK-0457	Antiproliferative activity against human A549 cells assessed as cell viability after 72 hrs by CCK8 assay Antiproliferative activity against human A549 cells assessed as cell viability after 72 hrs by CCK8 assay	[PMID: 24681066]
A549	IC₅₀	3.9 μM Compound: VX-680	Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 72 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 31862411]
A549	IC₅₀	35.8 μM Compound: VX-680	Antiproliferative activity against human A549 cells after 48 hrs by MTT assay Antiproliferative activity against human A549 cells after 48 hrs by MTT assay	[PMID: 30728112]
A549	IC₅₀	6.9 μM Compound: VX680	Antiproliferative activity against human A549 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human A549 cells incubated for 72 hrs by MTT assay	[PMID: 32941989]
BaF3	IC₅₀	100 nM Compound: MK-0457	Antiproliferative activity against mouse BaF3 cells harbouring T315I mutant assessed as cell growth inhibition Antiproliferative activity against mouse BaF3 cells harbouring T315I mutant assessed as cell growth inhibition	[PMID: 35551036]
BaF3	IC₅₀	102 nM Compound: MK-0457; VX-680	Antiproliferative activity against parent mouse BaF3 cells assessed as inhibition of cell proliferation measured after 72 hrs in presence of IL-3 by MTT assay Antiproliferative activity against parent mouse BaF3 cells assessed as inhibition of cell proliferation measured after 72 hrs in presence of IL-3 by MTT assay	[PMID: 21481795]
BaF3	IC₅₀	104 nM Compound: MK-0457; VX-680	Antiproliferative activity against native mouse BaF3 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against native mouse BaF3 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 21481795]
BaF3	IC₅₀	110 nM Compound: MK-0457; VX-680	Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 L248R mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 L248R mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 21481795]
BaF3	IC₅₀	130 nM Compound: MK-0457; VX-680	Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 F359C mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 F359C mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 21481795]
BaF3	IC₅₀	130 nM Compound: MK-0457; VX-680	Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 Q252H mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 Q252H mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 21481795]
BaF3	IC₅₀	160 nM Compound: MK-0457; VX-680	Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 H396P mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 H396P mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 21481795]
BaF3	IC₅₀	180 nM Compound: MK-0457; VX-680	Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 G250E mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 G250E mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 21481795]
BaF3	IC₅₀	190 nM Compound: MK-0457; VX-680	Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 E255V mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 E255V mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 21481795]
BaF3	IC₅₀	190 nM Compound: MK-0457; VX-680	Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 Y253H mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 Y253H mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 21481795]
BaF3	IC₅₀	200 nM Compound: MK-0457; VX-680	Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 V299L mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 V299L mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 21481795]
BaF3	IC₅₀	30 nM Compound: VX-680, MK-0457	Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl T315I mutant Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl T315I mutant	[PMID: 20604564]
BaF3	IC₅₀	5 μM Compound: VX-680, MK-0457	Inhibition of Bcr-Abl T315I mutant autophosphorylation in mouse BA/F3 cells Inhibition of Bcr-Abl T315I mutant autophosphorylation in mouse BA/F3 cells	[PMID: 20604564]
BaF3	IC₅₀	65 nM Compound: MK-0457; VX-680	Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 M351T mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 M351T mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 21481795]
BaF3	IC₅₀	74 nM Compound: MK-0457; VX-680	Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 T315I mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 T315I mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 21481795]
BaF3	IC₅₀	80 nM Compound: MK-0457; VX-680	Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 Y253F mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 Y253F mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 21481795]
BaF3	IC₅₀	84 nM Compound: MK-0457; VX-680	Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 E255K mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 E255K mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 21481795]
BaF3	IC₅₀	84 nM Compound: MK-0457; VX-680	Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 F317L mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 F317L mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 21481795]
BaF3	IC₅₀	88 nM Compound: MK-0457; VX-680	Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 T315A mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 T315A mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 21481795]
COLO 205	IC₅₀	0.019 μM Compound: 44, MK-0457 (VX-680)	Antiproliferative activity against human COLO205 cells by [3H]thymidine uptake assay Antiproliferative activity against human COLO205 cells by [3H]thymidine uptake assay	[PMID: 19447622]
DU-145	IC₅₀	0.4 μM Compound: VX-680, MK-0457	Antiproliferative activity against human DU145 cells assessed as cell viability after 72 hrs by CCK8 assay Antiproliferative activity against human DU145 cells assessed as cell viability after 72 hrs by CCK8 assay	[PMID: 24681066]
HCT-116	EC₅₀	120 nM Compound: 1, VX-680	Antiproliferative activity against human HCT116 cells after 96 hrs by MTS assay Antiproliferative activity against human HCT116 cells after 96 hrs by MTS assay	[PMID: 23808327]
HCT-116	IC₅₀	0.053 μM Compound: 39, VX-680	Antiproliferative activity against human HCT116 cells Antiproliferative activity against human HCT116 cells	[PMID: 18630890]
HCT-116	IC₅₀	0.3 μM Compound: VX-680	Cytotoxicity against human HCT116 cells after 48 hrs by MTT assay Cytotoxicity against human HCT116 cells after 48 hrs by MTT assay	[PMID: 22572580]
HCT-116	IC₅₀	0.45 μM Compound: VX 680	Cytotoxicity against human HCT116 cells assessed as reduction in cell viability after 48 hrs by MTT assay Cytotoxicity against human HCT116 cells assessed as reduction in cell viability after 48 hrs by MTT assay	[PMID: 30143423]
HCT-116	IC₅₀	1.49 μM Compound: VX-680	Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability after 72 hrs by MTT assay Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 31862411]
HCT-116	IC₅₀	120 nM Compound: Tozasertib	Cytotoxicity against human HCT116 cells by MTS assay Cytotoxicity against human HCT116 cells by MTS assay	[PMID: 20550212]
HCT-116	IC₅₀	120 nM Compound: 1, VX-680	Antiproliferative activity against human HCT116 cells Antiproliferative activity against human HCT116 cells	[PMID: 23808327]
HCT-116	IC₅₀	2.79 μM Compound: VX680	Antiproliferative activity against human HCT116 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human HCT116 cells incubated for 72 hrs by MTT assay	[PMID: 32941989]
HCT-116	IC₅₀	24 nM Compound: 1, VX- 680, MK-0457	Cytotoxicity against human HCT116 cells assessed as number of colonies after 10 to 14 days by colony forming assay Cytotoxicity against human HCT116 cells assessed as number of colonies after 10 to 14 days by colony forming assay	[PMID: 19143567]
HCT-116	IC₅₀	28 nM Compound: VX-680, MK-0457	Antiproliferative activity against human HCT116 cells Antiproliferative activity against human HCT116 cells	[PMID: 21802948]
HCT-116	IC₅₀	4.32 μM Compound: VX-680	Antiproliferative activity against human HCT116 cells after 48 hrs by CCK8 assay Antiproliferative activity against human HCT116 cells after 48 hrs by CCK8 assay	[PMID: 29358147]
HCT-116	IC₅₀	4.32 μM Compound: VX-680, MK-0457	Antiproliferative activity against human HCT116 cells assessed as cell viability after 72 hrs by CCK8 assay Antiproliferative activity against human HCT116 cells assessed as cell viability after 72 hrs by CCK8 assay	[PMID: 24681066]
HCT-116	IC₅₀	55 nM Compound: VX-680, MK-0457	Inhibition of Aurora B kinase assessed as reduction in histone H3 phosphorylation in human HCT116 cells Inhibition of Aurora B kinase assessed as reduction in histone H3 phosphorylation in human HCT116 cells	[PMID: 21802948]
HCT-15	IC₅₀	1.23 μM Compound: VX 680	Cytotoxicity against human HCT15 cells assessed as reduction in cell viability after 48 hrs by MTT assay Cytotoxicity against human HCT15 cells assessed as reduction in cell viability after 48 hrs by MTT assay	[PMID: 30143423]
HCT-8	IC₅₀	44.6 μM Compound: VX-680	Cytotoxicity against human HCT8 cells after 48 hrs by MTT assay Cytotoxicity against human HCT8 cells after 48 hrs by MTT assay	[PMID: 25812967]
HeLa	GI₅₀	46.2 μM Compound: VX-680	Antiproliferative activity against human HeLa cells after 48 hrs by MTT assay Antiproliferative activity against human HeLa cells after 48 hrs by MTT assay	[PMID: 30502115]
HeLa	IC₅₀	0.013 μM Compound: VX-680	Inhibition of Aurora A phosphorylation at Thr288 residue in human HeLa cells after 12 hrs by ELISA Inhibition of Aurora A phosphorylation at Thr288 residue in human HeLa cells after 12 hrs by ELISA	[PMID: 30502115]
HeLa	IC₅₀	0.148 μM Compound: VX-680	Inhibition of Aurora B phosphorylation at Thr232 residue in human HeLa cells after 12 hrs by ELISA Inhibition of Aurora B phosphorylation at Thr232 residue in human HeLa cells after 12 hrs by ELISA	[PMID: 30502115]
HeLa	IC₅₀	0.261 μM Compound: VX-680	Inhibition of Aurora A in human HeLa cells after 12 hrs by ELISA method Inhibition of Aurora A in human HeLa cells after 12 hrs by ELISA method	[PMID: 25812967]
HeLa	IC₅₀	0.453 μM Compound: VX-680	Inhibition of Aurora B in human HeLa cells after 12 hrs by ELISA method Inhibition of Aurora B in human HeLa cells after 12 hrs by ELISA method	[PMID: 25812967]
HeLa	IC₅₀	2.93 μM Compound: VX-680	Antiproliferative activity against human HeLa cells after 48 hrs by CCK8 assay Antiproliferative activity against human HeLa cells after 48 hrs by CCK8 assay	[PMID: 29358147]
HeLa	IC₅₀	2.93 μM Compound: VX-680, MK-0457	Antiproliferative activity against human HeLa cells assessed as cell viability after 72 hrs by CCK8 assay Antiproliferative activity against human HeLa cells assessed as cell viability after 72 hrs by CCK8 assay	[PMID: 24681066]
HeLa	IC₅₀	27.3 μM Compound: VX-680	Cytotoxicity against human HeLa cells after 48 hrs by MTT assay Cytotoxicity against human HeLa cells after 48 hrs by MTT assay	[PMID: 25812967]
HeLa	IC₅₀	46.2 μM Compound: VX-680	Antiproliferative activity against human HeLa cells after 48 hrs by MTT assay Antiproliferative activity against human HeLa cells after 48 hrs by MTT assay	[PMID: 30728112]
HeLa	IC₅₀	6.24 μM Compound: VX-680	Anticancer activity against human HeLa cells assessed as reduction in cell viability measured after 24 hrs by MTT assay Anticancer activity against human HeLa cells assessed as reduction in cell viability measured after 24 hrs by MTT assay	[PMID: 35476959]
HeLa	IC₅₀	9.5 μM Compound: VX-680	Antiproliferative activity against human HeLa cells assessed as cell growth inhibition after 72 hrs by MTT assay Antiproliferative activity against human HeLa cells assessed as cell growth inhibition after 72 hrs by MTT assay	[PMID: 32035750]
HepG2	GI₅₀	53.3 μM Compound: VX-680	Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay	[PMID: 30502115]
HepG2	IC₅₀	12.8 μM Compound: VX-680	Antiproliferative activity against human HepG2 cells assessed as cell growth inhibition after 72 hrs by MTT assay Antiproliferative activity against human HepG2 cells assessed as cell growth inhibition after 72 hrs by MTT assay	[PMID: 32035750]
HepG2	IC₅₀	16.11 μM Compound: VX680	Antiproliferative activity against human HepG2 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human HepG2 cells incubated for 72 hrs by MTT assay	[PMID: 32941989]
HepG2	IC₅₀	18.01 μM Compound: VX-680	Anticancer activity against human HepG2 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay Anticancer activity against human HepG2 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay	[PMID: 35476959]
HepG2	IC₅₀	53.3 μM Compound: VX-680	Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay	[PMID: 30728112]
HepG2	IC₅₀	63.4 μM Compound: VX-680	Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay	[PMID: 25812967]
HL-60	IC₅₀	0.0382 μM Compound: VX-680, MK-0457	Antiproliferative activity against human HL60 cells assessed as cell viability after 72 hrs by CCK8 assay Antiproliferative activity against human HL60 cells assessed as cell viability after 72 hrs by CCK8 assay	[PMID: 24681066]
HL-60	IC₅₀	1.88 μM Compound: VX-680	Anticancer activity against human HL-60 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay Anticancer activity against human HL-60 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay	[PMID: 35476959]
HT-29	IC₅₀	0.15 μM Compound: 39, VX-680	Antiproliferative activity against human HT29 cells Antiproliferative activity against human HT29 cells	[PMID: 18630890]
K562	IC₅₀	0.079 μM Compound: VX-680	Antiproliferative activity against human K562 cells after 48 hrs by CCK8 assay Antiproliferative activity against human K562 cells after 48 hrs by CCK8 assay	[PMID: 29358147]
K562	IC₅₀	0.0791 μM Compound: VX-680, MK-0457	Antiproliferative activity against human K562 cells assessed as cell viability after 72 hrs by CCK8 assay Antiproliferative activity against human K562 cells assessed as cell viability after 72 hrs by CCK8 assay	[PMID: 24681066]
LoVo	GI₅₀	45.3 μM Compound: VX-680	Antiproliferative activity against human LoVo cells after 48 hrs by MTT assay Antiproliferative activity against human LoVo cells after 48 hrs by MTT assay	[PMID: 30502115]
LoVo	IC₅₀	13.6 μM Compound: VX-680	Antiproliferative activity against human LoVo cells assessed as cell growth inhibition after 72 hrs by MTT assay Antiproliferative activity against human LoVo cells assessed as cell growth inhibition after 72 hrs by MTT assay	[PMID: 32035750]
LoVo	IC₅₀	45.3 μM Compound: VX-680	Antiproliferative activity against human LoVo cells after 48 hrs by MTT assay Antiproliferative activity against human LoVo cells after 48 hrs by MTT assay	[PMID: 30728112]
MCF7	IC₅₀	0.048 μM Compound: 39, VX-680	Antiproliferative activity against human MCF7 cells Antiproliferative activity against human MCF7 cells	[PMID: 18630890]
MCF7	IC₅₀	0.38 μM Compound: VX-680	Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay	[PMID: 22572580]
MCF7	IC₅₀	1.02 μM Compound: VX-680	Anticancer activity against human MCF7 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay Anticancer activity against human MCF7 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay	[PMID: 35476959]
MCF7	IC₅₀	1.3 μM Compound: VX-680	Antiproliferative activity against human MCF7 cells after 48 hrs by CCK8 assay Antiproliferative activity against human MCF7 cells after 48 hrs by CCK8 assay	[PMID: 29358147]
MCF7	IC₅₀	1.3 μM Compound: VX-680, MK-0457	Antiproliferative activity against human MCF7 cells assessed as cell viability after 72 hrs by CCK8 assay Antiproliferative activity against human MCF7 cells assessed as cell viability after 72 hrs by CCK8 assay	[PMID: 24681066]
MCF7	IC₅₀	17.39 μM Compound: VX-680	Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 31862411]
MCF7	IC₅₀	39.78 μM Compound: VX680	Antiproliferative activity against human MCF-7 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human MCF-7 cells incubated for 72 hrs by MTT assay	[PMID: 32941989]
MDA-MB-231	IC₅₀	0.127 μM Compound: VX-680	Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by CCK8 assay Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by CCK8 assay	[PMID: 29358147]
MDA-MB-231	IC₅₀	0.127 μM Compound: VX-680, MK-0457	Antiproliferative activity against human MDA-MB-231 cells assessed as cell viability after 72 hrs by CCK8 assay Antiproliferative activity against human MDA-MB-231 cells assessed as cell viability after 72 hrs by CCK8 assay	[PMID: 24681066]
MOLT-4	IC₅₀	0.0212 μM Compound: VX-680, MK-0457	Antiproliferative activity against human MOLT4 cells assessed as cell viability after 72 hrs by CCK8 assay Antiproliferative activity against human MOLT4 cells assessed as cell viability after 72 hrs by CCK8 assay	[PMID: 24681066]
NCI-N87	IC₅₀	11.6 μM Compound: VX-680, MK-0457	Antiproliferative activity against human NCI-N87 cells assessed as cell viability after 72 hrs by CCK8 assay Antiproliferative activity against human NCI-N87 cells assessed as cell viability after 72 hrs by CCK8 assay	[PMID: 24681066]
PANC-1	IC₅₀	4.13 μM Compound: VX-680, MK-0457	Antiproliferative activity against human PANC1 cells assessed as cell viability after 72 hrs by CCK8 assay Antiproliferative activity against human PANC1 cells assessed as cell viability after 72 hrs by CCK8 assay	[PMID: 24681066]
PC-3	IC₅₀	5.81 μM Compound: VX-680, MK-0457	Antiproliferative activity against human PC3 cells assessed as cell viability after 72 hrs by CCK8 assay Antiproliferative activity against human PC3 cells assessed as cell viability after 72 hrs by CCK8 assay	[PMID: 24681066]
Sf9	IC₅₀	0.023 μM Compound: Tozasertib	Inhibition of GST-tagged AURORA A (unknown origin) expressed in baculovirus infected Sf9 cells using MBP as substrate Inhibition of GST-tagged AURORA A (unknown origin) expressed in baculovirus infected Sf9 cells using MBP as substrate	[PMID: 30234987]
Sf9	IC₅₀	20 nM Compound: 1, VX-680	Inhibition of GST-tagged Aurora kinase A catalytic domain (123 to 401 amino acids) (unknown origin) expressed in sf9 cells using tetra(LRRWSLG) as substrate preincubated for 15 mins prior to substrate addition measured after 90 mins by luminescence assay Inhibition of GST-tagged Aurora kinase A catalytic domain (123 to 401 amino acids) (unknown origin) expressed in sf9 cells using tetra(LRRWSLG) as substrate preincubated for 15 mins prior to substrate addition measured after 90 mins by luminescence assay	[PMID: 23808327]
SK-BR-3	IC₅₀	9.99 μM Compound: VX-680, MK-0457	Antiproliferative activity against human SKBR3 cells assessed as cell viability after 72 hrs by CCK8 assay Antiproliferative activity against human SKBR3 cells assessed as cell viability after 72 hrs by CCK8 assay	[PMID: 24681066]
U-87MG ATCC	IC₅₀	14.5 μM Compound: VX-680	Antiproliferative activity against human U87 cells assessed as cell growth inhibition after 72 hrs by MTT assay Antiproliferative activity against human U87 cells assessed as cell growth inhibition after 72 hrs by MTT assay	[PMID: 32035750]
U-937	IC₅₀	0.036 μM Compound: VX-680	Antiproliferative activity against human U937 cells after 48 hrs by CCK8 assay Antiproliferative activity against human U937 cells after 48 hrs by CCK8 assay	[PMID: 29358147]
U-937	IC₅₀	0.036 μM Compound: VX-680, MK-0457	Antiproliferative activity against human U937 cells assessed as cell viability after 72 hrs by CCK8 assay Antiproliferative activity against human U937 cells assessed as cell viability after 72 hrs by CCK8 assay	[PMID: 24681066]

In Vitro

Tozasertib 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. Tozasertib prevents the CAL-62 proliferation in a time-dependent manner. Tozasertib 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 Tozasertib inhibits proliferation with the IC₅₀ between 25 and 150 nM. The Tozasertib significantly impairs the ability of the different cell lines to form colonies in soft agar. Analysis of caspase-3 activity indicates that Tozasertib induces apoptosis in the different cell lines. CAL-62 cells exposed for 12 hours to Tozasertib show an accumulation of cells with ≥ 4N DNA content. Time-lapse analysis demonstrates that Tozasertib-treated CAL-62 cells exit metaphase without dividing. Moreover, histone H3 phosphorylation is abrogated following Tozasertib treatment^[2]. Tozasertib has significant inhibitory activity against BCR-Abl bearing the T315I mutation in patient-derived samples^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 639089-54-6
Appearance Solid
Masse moléculaire 464.59
Formule C₂₃H₂₈N₈OS
Color White to off-white
SMILES

CC1=CC(NC2=NC(SC3=CC=C(C=C3)NC(C4CC4)=O)=NC(N5CCN(CC5)C)=C2)=NN1
Synonyms

VX 680; MK-0457
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

4°C, protect from light

* In solvent : -80°C, 1 year; -20°C, 6 months (protect from light)

Publications (16)

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Journal Impact Factor

Exp Mol Med

Cancer-associated fibroblast-derived extracellular vesicles regulate lipophagy through PLIN2 to modulate dormancy in salivary gland adenoid cystic carcinoma cells. [Abstract]

2025 Dec 18. PMID: 41408408
Cell Discov

Single-cell profiling reveals molecular basis of malignant phenotypes and tumor microenvironments in small bowel adenocarcinomas. [Abstract]

2022 Sep 14;8(1):92. PMID: 36104333

Tozasertib purchased from MedChemExpress. Usage Cited in: Cell Discov. 2022 Sep 14;8(1):92. [Abstract]

Cell survival curve for HUTU-80 cells treated with the indicated inhibitors with Tozasertib (0.01-100 μM).
Mol Cell

Splice-switching ASOs targeting the AURKA 5' UTR collapse an SRSF1-AURKA-MYC oncogenic circuit in pancreatic cancer. [Abstract]

2026 Jan 8;86(1):60-77.e7. PMID: 41475344

Tozasertib purchased from MedChemExpress. Usage Cited in: Mol Cell. 2026 Jan 8;86(1):60-77.e7. [Abstract]

Western blotting of AURKA, AURKA phosphorylated at Thr288 (pT288), SRSF1, MYC, and VINC from SUIT2 cells after treatment with Tozasertib (VX 680) (1 μM; 6-48 h).
Sci Transl Med

PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]

2018 Jul 18;10(450):eaaq1093. PMID: 30021885
NPJ Breast Cancer

SIMD: Synergistic integration mutualistic platform based on single-cell and proteotranscriptomics for drug repositioning. [Abstract]

2025 Dec 24;12(1):4. PMID: 41444222
Cell Rep

circPRKAA1 activates a Ku80/Ku70/SREBP-1 axis driving de novo fatty acid synthesis in cancer cells. [Abstract]

2022 Nov 22;41(8):111707. PMID: 36417875
Br J Pharmacol

Aurora kinase inhibitor tozasertib suppresses mast cell activation in vitro and in vivo. [Abstract]

2020 Jun;177(12):2848-2859. PMID: 32017040

Tozasertib purchased from MedChemExpress. Usage Cited in: Br J Pharmacol. 2020 Jun;177(12):2848-2859. [Abstract]

Tozasertib (5-10 μM; 1 h) suppressed CD63 expression in activated RBLs and LAD2 mast cells.

Tozasertib purchased from MedChemExpress. Usage Cited in: Br J Pharmacol. 2020 Jun;177(12):2848-2859. [Abstract]

Tozasertib (5-10 μM; 1 h) inhibited histamine release from IgE/Ag-stimulated RBLs and PMACI-stimulated LAD2 cells in a concentration‐dependent manner.

Tozasertib purchased from MedChemExpress. Usage Cited in: Br J Pharmacol. 2020 Jun;177(12):2848-2859. [Abstract]

Tozasertib (5-20 μM; 1 h) inhibited activation of MAPKs (p38, JNK, and ERK) in BMMCs, as shown by decreased levels of p-p38, p-JNK, p-ERK1/2.
Cancers (Basel)

Stratification of Tamoxifen Synergistic Combinations for the Treatment of ER+ Breast Cancer. [Abstract]

2023 Jun 14;15(12):3179. PMID: 37370789
ACS Infect Dis

Human Polo-like Kinase Inhibitors as Antiplasmodials. [Abstract]

2023 Apr 14;9(4):1004-1021. PMID: 36919909
Am J Cancer Res

Epigenetic heterogeneity promotes acquired resistance to BET bromodomain inhibition in ovarian cancer. [Abstract]

2021 Jun 15;11(6):3021-3038. PMID: 34249442
bioRxiv

2025 April 15.
bioRxiv

Spindle morphology changes between meiosis and mitosis driven by CK2 regulation of the Ran pathway. [Abstract]

2024 Jul 25:2024.07.25.605073. PMID: 39211121
Patent

US20210299273A1.
bioRxiv

2021 Feb 5.
Patent

US20180263995A1.
J Biomol Screen

Differential determinants of cancer cell insensitivity to antimitotic drugs discriminated by a one-step cell imaging assay. [Abstract]

2013 Oct;18(9):1062-71. PMID: 23788527

Solvant et solubilité

In Vitro:

DMSO : 100 mg/mL (215.24 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.1524 mL

10.7622 mL

21.5244 mL

5 mM

0.4305 mL

2.1524 mL

4.3049 mL

10 mM

0.2152 mL

1.0762 mL

2.1524 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months (protect from light). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.08 mg/mL (4.48 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.08 mg/mL (4.48 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (4.48 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protocole

Kinase Assay^[3]

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 Tozasertib in 100% DMSO or DMSO alone. Ki values are calculated as follows, K_i=IC₅₀/(1+[S]/K_d), where [S]=[ATP]=2.2 mM, and K_d (of ATP to Abl)=70 μM. These values are calculated assuming a K_d (ATP) of 70 μM for wild type and H396P Abl kinase domain.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay^[2]

The CAL-62 cells are cultured in the absence (dimethyl sulfoxide, DMSO) or the presence of 500 nM Tozasertib for different periods of time (1-5 days). The dose-dependent effects of Tozasertib 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 Tozasertib-treated cells are compared with those observed in control cells and expressed as a fold of variation versus control.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration^[1]

For the HL-60 study, female athymic NCr-nu mice are inoculated subcutaneously with 107 HL-60(TB) leukemia cells into the right axillary area. Treatment is administered i.p. b.i.d. after tumors reached 150−200 mm³. Tozasertib is prepared in a vehicle of 50% PEG 300 in 50 mM phosphate buffer. Cisplatin, formulated in saline, is administered i.p. q.4.d. for a total of three injections, at a dose of 5.4 mg/kg. For the MIA PaCa-2 studies, female MF1 nude mice are inoculated with 10⁷ MIA PaCa-2 cells into the dorsal flank. Treatment is administered i.p. b.i.d. after tumors reach 175 mm³. Tozasertib is prepared in a vehicle of 50% PEG 300 in 50 mM phosphate buffer. 5-fluorouracil, formulated in saline, is administered i.v. q.4.d. at a dose of 50 mg/kg. For the HCT116 study, female Hsd RH rnu/nu rats are inoculated with 10⁷ HCT116 cells into the right flank. Treatment is administered once the tumors reached 700−950 mm³. Tozasertib is administered continuously through an indwelling femoral catheter, followed by a saline infusion for 4 d before repeating the dose cycle. For all studies, tumor volume is determined by caliper measurements three times a week.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (280 KB)
SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Harrington EA, et al. VX-680, a potent and selective smallmolecule inhibitor of the Aurora kinases, suppresses tumor growth in vivo. Nat Med. 2004; 10:262-7. [Content Brief]

[2]. Salah E, et al. Crystal structures of ABL-related gene (ABL2) in complex with imatinib, tozasertib (VX-680), and a type I inhibitor of the triazole carbothioamide class.J Med Chem. 2011 Apr 14;54(7):2359-67. Epub 2011 Mar 18. [Content Brief]

[3]. Arlot-Bonnemains Y, et al. Effects of the Aurora kinase inhibitor VX-680 on anaplastic thyroid cancer-derived cell lines. Endocr Relat Cancer. 2008 Jun;15(2):559-68 [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.1524 mL	10.7622 mL	21.5244 mL	53.8109 mL
	5 mM	0.4305 mL	2.1524 mL	4.3049 mL	10.7622 mL
	10 mM	0.2152 mL	1.0762 mL	2.1524 mL	5.3811 mL
	15 mM	0.1435 mL	0.7175 mL	1.4350 mL	3.5874 mL
	20 mM	0.1076 mL	0.5381 mL	1.0762 mL	2.6905 mL
	25 mM	0.0861 mL	0.4305 mL	0.8610 mL	2.1524 mL
	30 mM	0.0717 mL	0.3587 mL	0.7175 mL	1.7937 mL
	40 mM	0.0538 mL	0.2691 mL	0.5381 mL	1.3453 mL
	50 mM	0.0430 mL	0.2152 mL	0.4305 mL	1.0762 mL
	60 mM	0.0359 mL	0.1794 mL	0.3587 mL	0.8968 mL
	80 mM	0.0269 mL	0.1345 mL	0.2691 mL	0.6726 mL
	100 mM	0.0215 mL	0.1076 mL	0.2152 mL	0.5381 mL

Keywords

Tozasertib

16 Cited Publications

100 mg Obtenir un devis

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Tozasertib

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Publications Citing Use of MedChemExpress (MCE) Tozasertib

Voir tous les produits spécifiques à Isoform Aurora Kinase

Activité biologique

Chemical Information

Publications (16)

Solvant et solubilité

Protocole

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Tozasertib

Anti-COVID-19 Compound Library

Cytoskeleton Compound Library

Anti-Blood Cancer Compound Library

Targeted Diversity Library

Heterocyclic Compound Library

Cell Death Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Anti-Aging Compound Library Mini

Epigenetics Compound Library Mini

Cell Cycle/DNA Damage Compound Library

Epigenetics Compound Library

Kinase Inhibitor Library

Anti-Cancer Compound Library

Clinical Compound Library

Autophagy Compound Library

Anti-Aging Compound Library

Drug Repurposing Compound Library

Publications Citing Use of MedChemExpress (MCE) Tozasertib

Voir tous les produits spécifiques à Isoform Aurora Kinase

Activité biologique

Chemical Information

Publications (16)

Solvant et solubilité

Protocole

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Tozasertib Related Classifications

HY-10161 Related Classifications