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L-6307 Lestaurtinib, >99%

[CEP-701] [KT-5555]

M.W. 439.46

C26H21N3O4

[111358-88-4]

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

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• Lestaurtinib is a potent inhibitor of several tyrosine kinases, such as FLT-3 and TrkA, that are associated with cancer growth and progression.  Schmidt-Arras, D., et al.  "FLT-3 receptor tyrosine kinase as a drug target in leukemia."  Curr. Pharm. Des. 10:  1867-1883 (2004).

• Lestaurtinib inhibited tumor growth when administered at 10 mg/kg s.c. b.i.d. 5 days a week for 21-28 days in Panc-1, AsPc-1, BxPc-3, Colo 357, and MiaPaCa2 s.c. xenografts in athymic nude mice.  Reductions in tumor growth volume were 50-70%.  Miknyoczki, S.J., et al.  "The Trk tyrosine kinase inhibitor CEP-701 (KT-5555) exhibits significant antitumor efficacy in preclinical xenograft models of human pancreatic ductal adenocarcinoma."  Clin. Cancer Res. 5:  2205-2212 (1999).

• Lestaurtinib inhibited RET and RET phosphorylation in medullary thyroid carcinoma (MTC) cells.  It also blocked the growth of these MTC cells in culture and tumor growth in MTC cell xenografts.  Strock, C.J., et al.  "CEP-701 and CEP-751 Inhibit Constitutively Activated RET Tyrosine Kinase Activity and Block Medullary Thyroid Carcinoma Cell Growth."  Cancer Res. 63:  5559-5563 (2003).

• FLT3 inhibition by lestaurtinib is associated with its clinical activity in AML patients harboring FLT3-activating mutations.  Smith, B.D., et al.  "Single-agent CEP-701, a novel FLT-3 inhibitor, shows biologic and clinical activity in patients with relapsed or refractory acute myeloid leukemia."  Blood 103:  3669-3676 (2004).

• Lestaurtinib is a FLT3 inhibitor that is both potent (IC50 of 2 nM) and selective (no activity on the other members of the type III RTK family at >500 nM).  Levis, M. and Small, D.  "Novel FLT3 tyrosine kinase inhibitors."  Expert Opin. Investig. Drugs 12:  1951-1962 (2003).

• In TF-1/ITD cells, lestaurtinib potently inhibited the phosphorylation of FLT3/ITD (IC50 < 5 nM).  Lestaurtinib inhibited the proliferation of TF-1/ITD cells (IC50 ≈ 10 nM), but showed very little effect at 10 nM on TF-1 cells.  Chen, P., et al.  "FLT3/ITD Mutation Signaling Includes Suppression of SHP-1."  J. Biol. Chem. 280:  5361-5369 (2005).

• 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.