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M-7007 Masitinib, Free Base, >99%

[AB-1010] [Masatinib]

M.W. 498.64

C28H30N6OS

[790299-79-5]

Storage:  Store at or below -20 ºC.  Solubility:  Soluble in DMSO at 200 mg/mL; very poorly soluble in ethanol or water; maximum solubility in plain water is estimated to be about 10-20 µM; buffers, serum, or other additives may increase or decrease the aqueous solubility.  Disposal:  A

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• Masitinib mesylate (AB1010) is a protein tyrosine kinase inhibitor.  In vitro it has greater activity and selectivity than imatinib mesylate against the wild-type c-Kit receptor and the mutated form in the juxtamembrane region.  It also inhibits the PDGF and FGFR3 receptors.  BUI, B.N., et al.  "Preliminary efficacy and safety results of Masitinib administered, front line in patients with advanced GIST.  A phase II study."  J. of Clin. Oncology 25:  10025 (ASCO Annual Meeting Proceedings Part I 2007).

• A placebo-controlled phase III clinical trial of masitinib was performed in the dogs with nonmetastatic recurrent or nonresectable grade II or III mast cell tumors (MCT).  Masitinib significantly increased overall time to tumor progression (TTP) compared with placebo, regardless of whether the tumors expressed mutant or wild-type KIT.  Masitinib was generally well tolerated, with the most common adverse events being mild or moderate diarrhea or vomiting.  Hahn, K.A., et al.  "Masitinib is safe and effective for the treatment of canine mast cell tumors."  J. Vet. Intern. Med. 22:  1301-1309 (2008).

• Masitinib treatment of patients with imatinib-resistant tumors was encouraging.  The safety profile of masitinib at 12mg/kg/day b.i.d. was favorable and compatible with a long-term regimen for the treatment of solid cancers.  Soria, J.C., et al.  "Phase 1 dose-escalation study of oral tyrosine kinase inhibitor masitinib in advanced and/or metastatic solid cancers."  Eur. J. Cancer  Jun 19 (2009) [Epub ahead of print].

• Masitinib showed an oral bioavailability of ~60% in cats.  Bellamy, F., et al.  "Pharmacokinetics of masitinib in cats."  Vet. Res. Commun.  Jun 16 (2009) [Epub ahead of print].

• Sold for laboratory or manufacturing purposes only; not for human, medical, 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.