Tozasertib

CHF 60.00
In stock
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Product Details
Synonyms MK-0457; VX-680
Product Type Chemical
Properties
Formula C23H28N8OS
MW 464.6
CAS 639089-54-6
Purity Chemicals ≥95%
Appearance Solid.
Solubility Soluble in DMSO or ethanol.
Declaration Manufactured by SynKinase.
Other Product Data Target: Aurora A | Kinase Group: Other | Substrate: Serine-Threonine

Click here for Original Manufacturer Product Datasheet
Our product description may differ slightly from the original manufacturers product datasheet.
InChi Key GCIKSSRWRFVXBI-UHFFFAOYSA-N
Shipping and Handling
Shipping AMBIENT
Short Term Storage +4°C
Long Term Storage -20°C
Use/Stability Stable for at least 2 years after receipt when stored at -20°C.
Documents
MSDS Download PDF
Product Specification Sheet
Datasheet Download PDF
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.
Product References
  1. VX-680, a potent and selective small-molecule inhibitor of the Aurora kinases, suppresses tumor growth in vivo: E.A. Harrington, et al.; Nat. Med. 10, 262 (2004)
  2. Novel series of pyrrolotriazine analogs as highly potent pan-Aurora kinase inhibitors: S. Abraham, et al.; Bioorg. Med. Chem. Lett. 21, 5296 (2011)
  3. Development of o-chlorophenyl substituted pyrimidines as exceptionally potent aurora kinase inhibitors: H.R. Lawrence, et al.; J. Med. Chem. 55, 7392 (2012)
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