Masitinib, Free Base **

产品名称：Masitinib, Free Base
产品货号：LC  M-7007    
产品规格：100 MG
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].
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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