Tozasertib

Tozasertib
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Item number Size Datasheet Manual SDS Delivery time Quantity Price
SYN-1092-M001 1 mg -

3 - 9 business days*

66.00€
SYN-1092-M005 5 mg -

3 - 9 business days*

86.00€
SYN-1092-M010 10 mg -

3 - 9 business days*

99.00€
SYN-1092-M050 50 mg -

3 - 9 business days*

289.00€
SYN-1092-M100 100 mg -

3 - 9 business days*

-
 
Soluble in DMSO or ethanol. In mammals, three Aurora kinases, Aurora A, Aurora B, and Aurora C,... more
Product information "Tozasertib"
Soluble in DMSO or ethanol. 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. Target: Aurora A , Kinase Group: Other , Substrate: Serine-Threonine
Keywords: MK-0457, VX-680
Supplier: SYNkinase
Supplier-Nr: 1092

Properties

Application: Aurora inhibitor
MW: 464,6 D
Formula: C23H28N8OS
Purity: >95%
Format: Solid

Database Information

CAS : 639089-54-6| Matching products
KEGG ID : K11480 | Matching products

Handling & Safety

Storage: -20°C
Shipping: +20°C (International: +20°C)
Caution
Our products are for laboratory research use only: Not for administration to humans!
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