Cat. No.: HY-50905

Dovitinib

(Synonyms: CHIR-258; TKI258)

11 Cited Publications

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Based on 11 publication(s) in Google Scholar

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.

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Pureté: 99.88%
CAS No.: 405169-16-6
Formule: C₂₁H₂₁FN₆O
Masse moléculaire:392.43

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months

Dovitinib Chemical Structure

CAS No.: 405169-16-6

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Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (11)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Bioz

Activité biologique

Description

IC₅₀ & Target^[1]

FLT3

1 nM (IC₅₀)

c-Kit

2 nM (IC₅₀)

FGFR1

8 nM (IC₅₀)

FGFR3

9 nM (IC₅₀)

VEGFR3

8 nM (IC₅₀)

VEGFR1

10 nM (IC₅₀)

VEGFR2

13 nM (IC₅₀)

PDGFRβ

27 nM (IC₅₀)

PDGFRα

210 nM (IC₅₀)

CSF-1R

36 nM (IC₅₀)

Voir tous les produits spécifiques à Isoform VEGFR :

Voir tous les produits spécifiques à Isoform PDGFR :

Cellular Effect

Cell Line	Type	Value	Description	References
DU-145	ED₅₀	23 mg/kg Compound: 5	Antitumor activity against human DU145 cells xenografted nude mouse Antitumor activity against human DU145 cells xenografted nude mouse	[PMID: 19113866]
HL-60	IC₅₀	0.911 μM Compound: Dovitinib	Antiproliferative activity against human HL-60 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay Antiproliferative activity against human HL-60 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay	[PMID: 35339838]
K562	IC₅₀	2.018 μM Compound: Dovitinib	Antiproliferative activity against human K562 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay Antiproliferative activity against human K562 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay	[PMID: 35339838]
KCL-22	IC₅₀	2.552 μM Compound: Dovitinib	Antiproliferative activity against human KCL-22 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay Antiproliferative activity against human KCL-22 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay	[PMID: 35339838]
KG-1	IC₅₀	0.035 μM Compound: Dovitinib	Antiproliferative activity against human KG-1 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay Antiproliferative activity against human KG-1 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay	[PMID: 35339838]
KG-1a	IC₅₀	0.033 μM Compound: Dovitinib	Antiproliferative activity against human KG-1a cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay Antiproliferative activity against human KG-1a cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay	[PMID: 35339838]
MOLM-13	IC₅₀	0.005 μM Compound: Dovitinib	Antiproliferative activity against human MOLM-13 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay Antiproliferative activity against human MOLM-13 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay	[PMID: 35339838]
MOLM-13	IC₅₀	794.7 nM Compound: DOV	Antiproliferative activity against human MOLM-13 cells incubated for 48 hrs by CCK-8 assay Antiproliferative activity against human MOLM-13 cells incubated for 48 hrs by CCK-8 assay	[PMID: 34694800]
MOLT-4	IC₅₀	0.266 μM Compound: Dovitinib	Antiproliferative activity against human MOLT-4 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay Antiproliferative activity against human MOLT-4 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay	[PMID: 35339838]
MV4-11	ED₅₀	3 mg/kg Compound: 5	Antitumor activity against human MV4-11 cells xenografted SCID-NOD mouse Antitumor activity against human MV4-11 cells xenografted SCID-NOD mouse	[PMID: 19113866]
MV4-11	IC₅₀	0.004 μM Compound: Dovitinib	Antiproliferative activity against human MV4-11 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay Antiproliferative activity against human MV4-11 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay	[PMID: 35339838]
MV4-11	IC₅₀	184.5 nM Compound: DOV	Antiproliferative activity against human MV4-11 cells incubated for 48 hrs by CCK-8 assay Antiproliferative activity against human MV4-11 cells incubated for 48 hrs by CCK-8 assay	[PMID: 34694800]
NOMO-1	IC₅₀	1.493 μM Compound: Dovitinib	Antiproliferative activity against human NOMO-1 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay Antiproliferative activity against human NOMO-1 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay	[PMID: 35339838]
OCI-AML2	IC₅₀	0.568 μM Compound: Dovitinib	Antiproliferative activity against human OCI-AML2 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay Antiproliferative activity against human OCI-AML2 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay	[PMID: 35339838]
RPMI-8226	IC₅₀	2139 nM Compound: Chemical probe : CHIR-258	Cytotoxicity against human RPMI-8226 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay Cytotoxicity against human RPMI-8226 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay	[PMID: 26254279]
THP-1	IC₅₀	1.936 μM Compound: Dovitinib	Antiproliferative activity against human THP-1 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay Antiproliferative activity against human THP-1 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay	[PMID: 35339838]
U-266	IC₅₀	6761.8 nM Compound: Chemical probe : CHIR-258	Cytotoxicity against human U-266 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay Cytotoxicity against human U-266 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay	[PMID: 26254279]

In Vitro

Dovitinib (CHIR-258) shows more than 10-fold inhibition InsR (IC50=2 μM), EGFR1 (IC50=2 μM), c-Met (IC50>3 μM), EphrinA2 (EphA2; IC50=4 μM), Tie2 (IC50=4 μM), IGFR1 (IC50>10 μM), and HER2 (IC50>10 μM)^[1].
Dovitinib (12.5-400 nM; 48 hours) potently inhibits the FGF-stimulated growth of WT and F384L-FGFR3-expressing B9 cells with IC50 values of 25 nM^[1].
Dovitinib (100, 500 nM; 96 hours) inhibits FGF-mediated ERK1/2 phosphorylation and induces apoptosis of FGFR3-expressing human myeloma cell lines^[1].
Dovitinib (72 hours) 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].
Dovitinib (100 nM) augments Dexamethasone (0.5 μM) cytotoxicity in KMS11 cells^[1].
Dovitinib significantly reduces the basal phosphorylation levels of FGFR-1, FGFR substrate 2α (FRS2-α) and ERK1/2 but not Akt in both SK-HEP1 and 21-0208 cells^[2].
Dovitinib enhances the BMP-2-induced alkaline phosphatase (ALP) induction, which is a representative marker of osteoblast differentiation. Dovitinib also stimulates the translocation of phosphorylated Smad1/5/8 into the nucleus and phosphorylation of mitogen-activated protein kinases, including ERK1/2 and p38^[3].
Dovitinib strongly inhibits both the interaction of TNIK with ATP (K_i, 13 nM) and the activation of Wnt signaling effectors such as β-catenin and TCF4. Dovitinib also induces caspase-dependent apoptosis in IM-9 cells without significant cytotoxicity in PBMCs^[4].

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

Cell Viability Assay^[1]

Cell Line:

WT and F384L-FGFR3-expressing B9 cells
Concentration:

12.5, 25, 50, 100, 200, 300, 400 nM
Incubation Time:

48 hours
Result:

Potently inhibited the FGF-stimulated growth of the cells.

Apoptosis Analysis^[1]

Cell Line:

KMS11, OPM2, and KMS18 cells
Concentration:

100 nM or 500 nM
Incubation Time:

96 hours
Result:

Induced apoptosis of FGFR3-expressing human myeloma cell lines.

In Vivo

Dovitinib (CHIR-258; 10-60 mg/kg/day; gavage; for 21 days) has a significant antitumor effect^[1].
Dovitinib (50 and 75 mg/kg) results in 97% and 98% tumor growth inhibition, respectively, and the maximal efficacy is at 50 mg/kg^[2].

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

Animal Model:

6- to 8-week-old female BNX mice with KMS11 cells^[1]
Dosage:

10, 30, 60 mg/kg
Administration:

Gavage; daily for 21 days
Result:

Had a significant antitumor effect in all 3 dose groups with 48%, 78.5%, and 94% growth inhibition in the 10 mg/kg, 30 mg/kg, and 60 mg/kg treatment.

Chemical Information

CAS No. 405169-16-6
Appearance Solid
Masse moléculaire 392.43
Formule C₂₁H₂₁FN₆O
Color Light yellow to green yellow
SMILES

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

CHIR-258; TKI258
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

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
Acta Pharm Sin B

2026 Feb 10.
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 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.
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 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.

Solvant et solubilité

In Vitro:

DMSO : 23.33 mg/mL (59.45 mM; ultrasonic and warming and heat to 60°C; 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

2.5482 mL

12.7411 mL

25.4823 mL

5 mM

0.5096 mL

2.5482 mL

5.0965 mL

10 mM

0.2548 mL

1.2741 mL

2.5482 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (6.37 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (6.37 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (6.37 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (280 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)
- 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)
Instruction de manipulation (2659 KB)

Références

[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]

[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 [Content Brief]

[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. [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

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.5482 mL	12.7411 mL	25.4823 mL	63.7056 mL
	5 mM	0.5096 mL	2.5482 mL	5.0965 mL	12.7411 mL
	10 mM	0.2548 mL	1.2741 mL	2.5482 mL	6.3706 mL
	15 mM	0.1699 mL	0.8494 mL	1.6988 mL	4.2470 mL
	20 mM	0.1274 mL	0.6371 mL	1.2741 mL	3.1853 mL
	25 mM	0.1019 mL	0.5096 mL	1.0193 mL	2.5482 mL
	30 mM	0.0849 mL	0.4247 mL	0.8494 mL	2.1235 mL
	40 mM	0.0637 mL	0.3185 mL	0.6371 mL	1.5926 mL
	50 mM	0.0510 mL	0.2548 mL	0.5096 mL	1.2741 mL

Dovitinib

11 Cited Publications

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Dovitinib

Kinase Inhibitor Library

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Publications Citing Use of MedChemExpress (MCE) Dovitinib

Voir tous les produits spécifiques à Isoform VEGFR

Voir tous les produits spécifiques à Isoform PDGFR

Activité biologique

Chemical Information

Publications (11)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Dovitinib Related Classifications

Cat. No.: HY-50905