Tozasertib

MK-0457; VX-680

Solid.

639089-54-6

32160000

liquid

GHS07

H303, H317, H333

InChI=1S/C23H28N8OS/c1-15-13-20(29-28-15)25-19-14-21(31-11-9-30(2)10-12-31)27-23(26-19)33-18-7-5-17(6-8-18)24-22(32)16-3-4-16/h5-8,13-14,16H,3-4,9-12H2,1-2H3,(H,24,32)(H2,25,26,27,28,29)

GCIKSSRWRFVXBI-UHFFFAOYSA-N

Chemical. CAS: 639089-54-6. Formula: C23H28N8OS. MW: 464.6. In mammals, three Aurora kinases, Aurora A, Aurora B, and Aurora C, are expressed. Aurora C expression is mainly restricted to testis, where it functions during meiosis, whereas Aurora A and B play key functions regulating mitosis. Aurora A is localized to the centrosome and spindle poles, where it drives centrosome maturation, separation, and bipolar spindle assembly. Aurora B is the central component of the chromosomal passenger complex (CPC) that also contains the inner centromere protein (INCENP), borealin, and survivin. These non-enzymatic components of the CPC play a key role in regulating kinase activity and localization. Over-expression of Aurora kinases can be oncogeneic and they have thus long been targets for cancer thearpy. Tozasertib, or VX-680, is a potent and selective inhibitor of Aurora kinases, particularly Aurora A and B. In vitro, VX-680 blocks cell cycle progression and induces apoptosis in a wide range of human tumor types at low IC(50) values (i.e. 3.38nM for human BE-13 cells, and 14.34nM for NTERA cells). Moreover, VX680, also has very potent Ki values, with inhibition constants (Ki) of 0.6, 18, and 46nM for Aurora A, B, and C, respectively. VX-680 is also effective in vivo, being used in a Caki-1 xenograft model, VX-680 demonstrated a 75.7% (P < 0.001) decrease in Caki-1 xeno-graft tumor volume with no apparent alternation in animal body weight, peripheral blood counts, or other biological parameters.

C23H28N8OS

464.6

Plastic Vial

P261, P272, P280, P302, P352, P333, P313, P321, P363, P501

In mammals, three Aurora kinases, Aurora A, Aurora B, and Aurora C, are expressed. Aurora C expression is mainly restricted to testis, where it functions during meiosis, whereas Aurora A and B play key functions regulating mitosis. Aurora A is localized to the centrosome and spindle poles, where it drives centrosome maturation, separation, and bipolar spindle assembly. Aurora B is the central component of the chromosomal passenger complex (CPC) that also contains the inner centromere protein (INCENP), borealin, and survivin. These non-enzymatic components of the CPC play a key role in regulating kinase activity and localization. Over-expression of Aurora kinases can be oncogeneic and they have thus long been targets for cancer thearpy. Tozasertib, or VX-680, is a potent and selective inhibitor of Aurora kinases, particularly Aurora A and B. In vitro, VX-680 blocks cell cycle progression and induces apoptosis in a wide range of human tumor types at low IC(50) values (i.e. 3.38nM for human BE-13 cells, and 14.34nM for NTERA cells). Moreover, VX680, also has very potent Ki values, with inhibition constants (Ki) of 0.6, 18, and 46nM for Aurora A, B, and C, respectively. VX-680 is also effective in vivo, being used in a Caki-1 xenograft model, VX-680 demonstrated a 75.7% (P < 0.001) decrease in Caki-1 xeno-graft tumor volume with no apparent alternation in animal body weight, peripheral blood counts, or other biological parameters.

>95%

Warning

Soluble in DMSO or ethanol.

Non-hazardous

Protein Kinase Modulators

12352200

Stable for at least 2 years after receipt when stored at -20°C.