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Merck
CN

SML3012

Sigma-Aldrich

Dovitinib

≥98% (HPLC)

Synonym(s):

4-Amino-5-fluoro-3-[6-(4-methyl-1-piperazinyl)-1H-benzimidazol-2-yl]-2(1H)-quinolinone, CHIR 258, CHIR-258, CHIR258, TKI 258, TKI-258, TKI258

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About This Item

Empirical Formula (Hill Notation):
C21H21FN6O
CAS Number:
405169-16-6
Molecular Weight:
392.43
MDL number:
MFCD10565680
UNSPSC Code:
12352200
NACRES:
NA.77

Key Documents

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Quality Level

100

Assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

2-8°C

SMILES string

O=C1NC2=C(C(N)=C1C3=NC4=CC=C(N5CCN(CC5)C)C=C4N3)C(F)=CC=C2

InChI

1S/C21H21FN6O/c1-27-7-9-28(10-8-27)12-5-6-14-16(11-12)25-20(24-14)18-19(23)17-13(22)3-2-4-15(17)26-21(18)29/h2-6,11H,7-10H2,1H3,(H,24,25)(H3,23,26,29)

InChI key

PIQCTGMSNWUMAF-UHFFFAOYSA-N

Biochem/physiol Actions

Dovitinib (CHIR-258) is an orally active and potent receptor tyrosine kinase (RTK) inhibitor against class III (FLT3/KIT/PDGFR1/CSFR/PDGFR2 IC50 = 1/2/27/36/200 nM), class IV (FGFR1/3 IC50 = 8/9 nM), and class V (VEGFR1/2/3 IC50 = 10/13/8 nM) RTKs, but not INSR, EGFR1, ErbB2 or Raf (IC50 = 2.1, 2.2, >20, >25 μM, respectively). Dovitinib inhibits target RTKs phosphorylation in cultured cells (pVEGFR1 and pPDGFRβ IC90 <50 nM; KM12L4a) and exhibits in vivo anti-tumor efficacy in mice bearing KM12L4a or HCT116 human cancer xenografts (10-120 mg/kg/day p.o.).
Orally active, potent inhibitor against class III-V receptor tyrosine kinases (FLT3, KIT, PDGFR1/2, CSFR, FGFR1/3, VEGFR1/2/3) with efficacy in vitro and in vivo.

Storage Class Code

11 - Combustible Solids

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Regulatory Information

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Certificates of Analysis (COA)

Lot/Batch Number
0000188190
0000188190
0000123615
0000123616
0000120685

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Isadora C Silveira et al.
Anti-cancer agents in medicinal chemistry, 20(6), 751-755 (2020-02-14)
Identification of the antitumor role of tyrosine kinase inhibitors, such as TKI-258, may lead to novel therapeutics for Oral Squamous Cell Carcinoma (OSCC), which has high mortality rates. TKI-258 blocks Fibroblast Growth Factor Receptors (FGFRs), Platelet-Derived Growth Factor Receptors (PDGFRs)
Andrew Chase et al.
Blood, 110(10), 3729-3734 (2007-08-19)
The 8p11 myeloproliferative syndrome (EMS) is an aggressive, atypical stem cell myeloproliferative disorder associated with chromosome translocations that disrupt and constitutively activate FGFR1 by fusion to diverse partner genes. To explore the possibility of targeted therapy for EMS, we have
Daniel E Lopes de Menezes et al.
Clinical cancer research : an official journal of the American Association for Cancer Research, 11(14), 5281-5291 (2005-07-22)
Fms-like tyrosine kinase 3 (FLT3) encodes a receptor tyrosine kinase (RTK) for which activating mutations have been identified in a proportion of acute myelogenous leukemia (AML) patients and associated with poor clinical prognosis. Given the relevance of FLT3 mutations in
Xiaohua Xin et al.
Clinical cancer research : an official journal of the American Association for Cancer Research, 12(16), 4908-4915 (2006-08-18)
The ectopically expressed and deregulated fibroblast growth factor receptor 3 (FGFR3) results from a t(4;14) chromosomal translocation that occurs in approximately 15% of multiple myeloma (MM) patients and confers a particularly poor prognosis. This study assesses the antimyeloma activity of
Berna Sahan et al.
Cornea, 38(9), 1161-1168 (2019-06-11)
To compare the inhibitory effects of dovitinib and bevacizumab for treatment of corneal neovascularization (CNV). Thirty-nine adult female Sprague Dawley rats weighing 180 to 250 g were used. CNV was induced by silver nitrate in the right eye of each
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