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Dovitinib

Dovitinib (CHIR-258) is an orally active, potent multi-targeted tyrosine kinase (RTK) inhibitor with IC50s of 1, 2, 36, 8/9, 10/13/8, 27/210 nM for FLT3, c-Kit, CSF-1R, FGFR1/FGFR3, VEGFR1/VEGFR2/VEGFR3 and PDGFRα/PDGFRβ, respectively. Dovitinib has potent antitumor activity[1][2].

Product Specifications

CAS Number

[405169-16-6]

Product Name Alternative

CHIR-258; TKI258

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

C-Fms; c-Kit; FGFR; FLT3; PDGFR; VEGFR

Type

Reference compound

Related Pathways

Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/Dovitinib.html

Purity

99.88

Solubility

DMSO : 23.33 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

O=C1NC(C=CC=C2F)=C2C(N)=C1C3=NC4=CC=C(N5CCN(C)CC5)C=C4N3

Molecular Formula

C21H21FN6O

Molecular Weight

392.43

Precautions

H302, H315, H319, H335

References & Citations

[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.|[2]Huynh H, et al. Dovitinib demonstrates antitumor and antimetastatic activities in xenograft models of hepatocellular carcinoma. J Hepatol. 2012, 56 (3), 595-601.|[3]Lee Y, et al. A Receptor Tyrosine Kinase Inhibitor, Dovitinib (TKI-258), Enhances BMP-2-Induced Osteoblast Differentiation In Vitro. Mol Cells. 2016 May 31;39 (5) :389-94|[4]Chon HJ, et al. Traf2- and Nck-interacting kinase (TNIK) is involved in the anti-cancer mechanism of dovitinib in human multiple myeloma IM-9 cells. Amino Acids. 2016 Jul;48 (7) :1591-9.

Shipping Conditions

Room Temperature

Storage Conditions

-20°C, 3 years; 4°C, 2 years (Powder)

Product Datasheet

http://file.medchemexpress.com/batch_PDF/HY-50905/Dovitinib-DataSheet-MedChemExpress.pdf

Product MSDS

http://file.medchemexpress.com/batch_PDF/HY-50905/Dovitinib-SDS-MedChemExpress.pdf

Scientific Category

Reference compound1

Clinical Information

Phase 3

Isoform

PDGFRα; PDGFRβ; VEGFR1/Flt-1; VEGFR2/KDR/Flk-1; VEGFR3/Flt-4

Citation 01

Biochemistry for Health, NOVA University of Lisbon. 2019 Jul.|bioRxiv. 2024 June 09.|Front Cell Dev Biol. 2020 May 7:8:287.|Harvard Medical School LINCS LIBRARY|J Biol Chem. 2023 Apr;299 (4) :104595|NPJ Precis Oncol. 2021 Jul 16;5 (1) :66.|Sci Transl Med. 2018 Jul 18;10 (450) :eaaq1093.|Theranostics. 2018 Jul 30;8 (15) :4262-4278.|University of Düsseldorf. 2024.|Nat Commun. 2025 Jul 24;16 (1) :6777.

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