Art. -Nr.: HY-10207

Dovitinib lactate

(Synonyms: CHIR-258 lactate; TKI-258 lactate)

11 Cited Publications

Kundenbewertung

Based on 11 publication(s) in Google Scholar

Dovitinib lactate (TKI258 lactate) is a multi-targeted tyrosine kinase inhibitor with IC₅₀s of 1, 2, 8/9, 10/13/8, 27/210 nM for FLT3, c-Kit, FGFR1/3, VEGFR1/2/3 and PDGFRα/β, respectively.

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Reinheit: 99.75%
CAS. Nr.: 692737-80-7
Formel: C₂₄H₂₇FN₆O₄
Molecular Weight:482.51

Speicherung:

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Dovitinib lactate Chemical Structure

CAS. Nr.: 692737-80-7

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (11)
Lösungsmittel & Löslichkeit
- In Vitro
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

FLT3

1 nM (IC₅₀)

c-Kit

2 nM (IC₅₀)

FGFR1

8 nM (IC₅₀)

FGFR3

9 nM (IC₅₀)

VEGFR1

1 nM (IC₅₀)

VEGFR3

8 nM (IC₅₀)

VEGFR2

13 nM (IC₅₀)

PDGFRα

27 nM (IC₅₀)

PDGFRβ

210 nM (IC₅₀)

Alle VEGFR Isoform-spezifische Produkte anzeigen :

Alle PDGFR Isoform-spezifische Produkte anzeigen :

In Vitro

Dovitinib potently inhibits the FGF-stimulated growth of WT and F384L-FGFR3-expressing B9 cells with IC₅₀ values of 25 nM. B9-MINV cells are resistant to the inhibitory activity of Dovitinib at concentrations up to 1 μM. Dovitinib inhibits cell proliferation of KMS11 (FGFR3-Y373C), OPM2 (FGFR3-K650E), and KMS18 (FGFR3-G384D) cells with IC₅₀ of values of 90 nM (KMS11 and OPM2) and 550 nM, respectively^[1]. Treatment of SK-HEP1 cells with dovitinib results in G2/M cell cycle arrest, inhibition of colony formation in soft agar and blockade of bFGF-induced cell migration. Dovitinib inhibits basal expression and FGF-induced phosphorylation of FGFR-1, FRS2-α and ERK1/2^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Dovitinib (10 mg/kg, 30 mg/kg, 60 mg/kg, p.o.) shows significant antitumor effect in the KMS11-bearing mice model, and the growth inhibition is 48%, 78.5%, and 94% in the 10 mg/kg, 30 mg/kg, and 60 mg/kg treatment arms, respectively, compared with the placebo-treated mice^[1]. Dovitinib demonstrates significant antitumor and antimetastatic activities in HCC xenograft models. Dovitinib potently inhibits tumor growth of six HCC lines. Inhibition of angiogenesis correlates with inactivation of FGFR/PDGFR-β/VEGFR-2 signaling pathways. Dovitinib also causes dephosphorylation of retinoblastoma, upregulation of p-histone H2A-X and p27, and downregulation of p-cdk-2 and cyclin B1, which results in a reduction in cellular proliferation and the induction of tumor cell apoptosis^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS. Nr. 692737-80-7
Appearance Solid
Molecular Weight 482.51
Formel C₂₄H₂₇FN₆O₄
Color Light yellow to yellow
SMILES

O=C(N1)C(C(NC2=C3)=NC2=CC=C3N4CCN(C)CC4)=C(N)C5=C1C=CC=C5F.O=C(O)C(C)O
Synonyms

CHIR-258 lactate; TKI-258 lactate
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Publications (11)

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Journal Impact Factor

Nat Commun

PEAK1 maintains tight junctions in intestinal epithelial cells and resists colitis by inhibiting autophagy-mediated ZO-1 degradation. [Abstract]

2025 Jul 24;16(1):6777. PMID: 40707483
Sci Transl Med

PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]

2018 Jul 18;10(450):eaaq1093. PMID: 30021885
Theranostics

Jujuboside A promotes Aβ clearance and ameliorates cognitive deficiency in Alzheimer's disease through activating Axl/HSP90/PPARγ pathway. [Abstract]

2018 Jul 30;8(15):4262-4278. PMID: 30128052

Dovitinib lactate purchased from MedChemExpress. Usage Cited in: Theranostics. 2018 Jul 30;8(15):4262-4278. [Abstract]

BV2 cells are pretreated with 0.1% DMSO (Ctrl), JuA (25 µM) or JuA (25 µM) with the indicated antagonist of RTKs (Dovitinib at 1 µM, Gefinitib at 2.5 µM, Sunitinib at 2.5 µM and LDC1267 at 1 µM) for 30 min, followed by administration of Aβ42 (5 μM) for 12 h.
Acta Pharm Sin B

2026 Feb 10.
NPJ Precis Oncol

Comprehensive functional evaluation of variants of fibroblast growth factor receptor genes in cancer. [Abstract]

2021 Jul 16;5(1):66. PMID: 34272467
Front Cell Dev Biol

An FGFR/AKT/SOX2 Signaling Axis Controls Pancreatic Cancer Stemness. [Abstract]

2020 May 7:8:287. PMID: 32457900

Dovitinib lactate purchased from MedChemExpress. Usage Cited in: Front Cell Dev Biol. 2020 May 7:8:287. [Abstract]

Determination in L3.6 cells of FGF2-induced FGFR phosphorylation by Western blot in the presence of Dovitinib. FGFR1 and alpha-Tubulin are used as loading controls.
J Biol Chem

Activation of Gcn2 by small molecules designed to be inhibitors. [Abstract]

2023 Apr;299(4):104595 PMID: 36898579
BMJ Open Ophthalmol

Impact of anticancer drugs on human Tenon's fibroblast proliferation: implications for glaucoma surgery. [Abstract]

2026 Jan 12;11(1):e002307. PMID: 41526033
University of Düsseldorf

2024.
bioRxiv

2024 June 09.
Biochemistry for Health, NOVA University of Lisbon

2019 Jul.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 25 mg/mL (51.81 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.0725 mL

10.3625 mL

20.7250 mL

5 mM

0.4145 mL

2.0725 mL

4.1450 mL

10 mM

0.2072 mL

1.0362 mL

2.0725 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Protokoll

Cell Assay^[2]

To determine IC₅₀ for SK-HEP1 cells, cells are plated at a density of 2×10⁴ cells per dish. After 48 h, cells are treated with 0, 0.01, 0.1, 1, 5, 10, 50, 100 μM dovitinib in DMEM containing 1% FBS for 24 h. Cell viability is determined with Cell Proliferation Assay. IC₅₀ is calculated by nonlinear regression analysis using GraphPad Prism software^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration^[2]

Mice: Six HCC lines (06-0606, 26-0808A, 26-1004, 25-0705A, 5-1318, 21-0208) are used to establish tumors in male SCID mice. or dose-esponse experiments, mice bearing the 06-0606 xenografts re orally given vehicle (5% dextrose) or two doses of dovitinib (50 and 75 mg/kg) daily for 14 days. For time-dependent inhibition of dovitinib targets, mice bearing 06-0606 tumors are given orally 200 μL of either vehicle (n=6) or 50 mg/kg/day of dovitinib (n=10)^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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. [Content Brief]

[2]. Huynh H, et al. Dovitinib demonstrates antitumor and antimetastatic activities in xenograft models of hepatocellular carcinoma. J Hepatol. 2012, 56(3), 595-601. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.0725 mL	10.3625 mL	20.7250 mL	51.8124 mL
	5 mM	0.4145 mL	2.0725 mL	4.1450 mL	10.3625 mL
	10 mM	0.2072 mL	1.0362 mL	2.0725 mL	5.1812 mL
	15 mM	0.1382 mL	0.6908 mL	1.3817 mL	3.4542 mL
	20 mM	0.1036 mL	0.5181 mL	1.0362 mL	2.5906 mL
	25 mM	0.0829 mL	0.4145 mL	0.8290 mL	2.0725 mL
	30 mM	0.0691 mL	0.3454 mL	0.6908 mL	1.7271 mL
	40 mM	0.0518 mL	0.2591 mL	0.5181 mL	1.2953 mL
	50 mM	0.0414 mL	0.2072 mL	0.4145 mL	1.0362 mL

Keywords

Dovitinib lactate

11 Cited Publications

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Dovitinib lactate

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Reprogramming Compound Library

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Anti-Lung Cancer Compound Library

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Anti-Blood Cancer Compound Library

Angiogenesis-Related Compound Library

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Human Metabolite Library

Anti-Prostate Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

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Protein Kinase Compound Library

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Posttranslational Modification Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Publications Citing Use of MedChemExpress (MCE) Dovitinib lactate

Alle VEGFR Isoform-spezifische Produkte anzeigen

Alle PDGFR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (11)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Dovitinib lactate Related Classifications

HY-10207 Related Classifications