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Cat. No. Name Size Price Add Cart
KI2840TKI-2585 mg$170
TKI-25810 mg$272
TKI-25820 mg$436
TKI-25850 mg$752
TKI-258100 mg$1204
TKI-258200 mg$1926
TKI-2581 g$7700

Chemical Characteristic

Product NameTKI-258
SynonymsDovitinib
CAS No.405169-16-6
Molecular Weight 392.43
FormulaC21H21FN6O
Chemical Name(3Z)-4-amino-5-fluoro-3-[5-(4-methylpiperazin-1-yl)-1,3-dihydrobenzimidazol-2-ylidene]quinolin-2-one
Smiles[nH]1c(=O)c(c(c2c(cccc12)F)N)c1nc2c([nH]1)ccc(c2)N1CCN(CC1)C
Chemical Structure

Biological activities

TKI-258 is a novel and multitargeted receptor tyrosine kinase (RTK) inhibitor. TKI-258 inhibits the class III RTKs including FLT3, c-Kit, CSF-1R, and PDGFRα/β with IC50 values ranging from 1 to 210 nM. TKI-258 potently inhibits class IV members FGFR1 and FGFR3 with IC50 values of 8 and 9 nM, respectively. TKI-258 also inhibits class V (VEGFR1-4) RTKs with IC50 values of 10 to 13 nM, respectively. In vitro, TKI-258 selectively inhibits the growth of B9 cells and human myeloma cell lines expressing wild-type (WT) or activated mutant FGFR3. In a xenograft mouse model of FGFR3 MM, TKI-258 has potent therapeutic efficacy in vivo.[1]

Protocols

In vitro: Prior to use, TKI-258 is dissolved in dimethyl sulfoxide (DMSO) at a stock concentration of 20 mM.[1]

References

[1] Trudel S, et al. CHIR-258, a novel, multitargeted tyrosine kinase inhibitor for the potential treatment of t(4;14) multiple myeloma. Blood. 2005, 105(7): 2941-2948.

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