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T-2304 Tozasertib, Free Base, >99%

[VX-680] [MK-0457] [VX6] [VX680] [VX 680]

M.W. 464.59

C23H28N8OS

[639089-54-6]

Storage:  Store at or below -20 ºC.  Solubility:  Soluble in DMSO at 100 mg/mL; very poorly soluble in ethanol; very poorly soluble in water; maximum solubility in plain water is estimated to be about 10-30 µM; buffers, serum, or other additives may increase or decrease the aqueous solubility.  Disposal:  A

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• Tozasertib is a potent inhibitor of all aurora kinases, including the A, B and C isotypes (Ki = 0.6 nM, 18 nM and 4.6 nM, respectively).  It also inhibits ABL kinase (Ki = 30 nM), an imatinib-resistant ABL mutant (T315I) kinase (Ki = 42 nM), and Flt-3 (Ki = 30 nM).  Tozasertib binds to an inactive aurora conformation.  Cheetham, G.M., et al.  "Structural basis for potent inhibition of the aurora kinases and a T315I multi-drug resistant mutant form of Abl kinase by VX-680."  Cancer Lett. 251:  323-329 (2007).

• Tozasertib has a similar binding affinity to ABL1 kinase (Kd = 20 nM) and mutated ABL1 (T351I) kinase (Kd = 5 nM).  It inhibits the growth of cells expressing wild type and mutated BCR-ABL, including T315I, with an IC50 of 200 nM.  Carter, T.A., et al.  "Inhibition of drug-resistant mutants of ABL, KIT, and EGF receptor kinases."  Proc. Natl. Acad. Sci. USA 102:  11011-11016 (2005).

• Tozasertib inhibits cell cycle progression, induces apoptosis and blocks tumor growth in varieties of in vivo xenograft models, including leukemia, colon and pancreatic tumors.  Harrington, E.A., et al.  "VX-680, a potent and selective small-molecule inhibitor of the aurora kinases, suppresses tumor growth in vivo."  Nat. Med. 10:  262-267 (2004).

• Tozasertib has shown antitumor effects in patients with T315I ABL-mutated chronic myeloid leukemia (CML) or Philadelphia chromosome (Ph)–positive acute lymphocytic leukemia (ALL).  Giles, F.J., et al.  "MK-0457, a novel kinase inhibitor, is active in patients with chronic myeloid leukemia or acute lymphocytic leukemia with the T315I BCR-ABL mutation."  Blood 109:  500-502 (2007).

• Sold for laboratory or manufacturing purposes only; not for human, veterinary, food, or household use.

• This product is offered for R&D use in accordance with (i) 35 USC 271(e)+A13(1) in the U.S.; (ii) Section 69.1 of Japanese Patent Law in Japan; (iii) Section 11, No. 2 of the German Patent Act of 1981 in Germany; (iv) Section 60, Paragraph 5b of the U.K. Patents Act of 1977 in the U.K.; (v) Sections 55.2(1) and 55.2(6) and other common law exemptions of Canadian patent law; (vi) Section 68B of the Patents Act of 1953 in New Zealand together with the amendment of same by the Statutes Amendment Bill of 2002; (vii) such related legislation and/or case law as may be or become applicable in the aforementioned countries; and (viii) such similar laws and rules as may apply in various other countries.

• Not available in some countries; not available to some institutions; not available for some uses.