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Dovitinib

Chemical Structure : Dovitinib

CAS No.: 405169-16-6

Dovitinib (CHIR-258, TKI258, TKI-258, CHIR258)

Catalog No.: PC-45899Not For Human Use, Lab Use Only.

Dovitinib (CHIR-258, TKI258) is a multitargeted RTK inhibitor of class III, IV, and V RTKs with IC50 of 1/2/36/8/9 nM for FLT3/c-KIT/c-Fms/FGFR1/FGFR3, respectively.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

Dovitinib (CHIR-258, TKI258) is a multitargeted RTK inhibitor of class III, IV, and V RTKs with IC50 of 1/2/36/8/9 nM for FLT3/c-KIT/c-Fms/FGFR1/FGFR3, respectively.
Dovitinib (CHIR-258, TKI258) also inhibits VEGFR1/2/3 (IC50=10/13/8 nM) and PDGFRβ/α (IC50=27/210 nM).
Dovitinib (CHIR-258, TKI258) selectively inhibits the growth of B9 cells and human myeloma cell lines expressing wild-type (WT) or activated mutant FGFR3.
Dovitinib (CHIR-258, TKI258) inhibits downstream ERK 1/2 phosphorylation and induces cytostatic and cytotoxic effects; demonstrates activity in a xenograft mouse model of FGFR3 MM; orally active.

Physicochemical Properties

M.Wt 392.4294
Formula C21H21FN6O
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

DMSO: 25 mg/mL

Chemical Name/SMILES

2(1H)-Quinolinone, 4-amino-5-fluoro-3-[6-(4-methyl-1-piperazinyl)-1H-benzimidazol-2-yl]-

References

1. Trudel S, et al. Blood. 2005 Apr 1;105(7):2941-8.

2. Lopes de Menezes DE, et al. Clin Cancer Res. 2005 Jul 15;11(14):5281-91.

3. Xin X, et al. Clin Cancer Res. 2006 Aug 15;12(16):4908-15.

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