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Dovitinib

Product Name
Dovitinib
CAS No.
405169-16-6
Chemical Name
Dovitinib
Synonyms
CS-226;TKI-258;CHIR-258;dovitinib;PDovitinib;NCGC00249685;CHIR258 7.7G;Dovitinib base;Unii-I35H55G906;TKI258; CHIR-258
CBNumber
CB11512534
Molecular Formula
C21H21FN6O
Formula Weight
392.43
MOL File
405169-16-6.mol
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Dovitinib Property

Density 
1.386
storage temp. 
-20°
solubility 
Soluble in DMSO (up to 30 mg/ml).
pka
9.44±0.70(Predicted)
form 
solid
color 
Yellow-green
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 3 months.
InChI
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)
InChIKey
PIQCTGMSNWUMAF-UHFFFAOYSA-N
SMILES
N1C2=C(C(F)=CC=C2)C(N)=C(C2NC3=CC(N4CCN(C)CC4)=CC=C3N=2)C1=O
CAS DataBase Reference
405169-16-6
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
SML3012
Product name
Dovitinib
Purity
≥98% (HPLC)
Packaging
10 mg
Price
$82.3
Updated
2025/07/31
Sigma-Aldrich
Product number
SML3012
Product name
Dovitinib
Purity
≥98% (HPLC)
Packaging
50 mg
Price
$269
Updated
2025/07/31
Cayman Chemical
Product number
15220
Product name
Dovitinib
Purity
≥98%
Packaging
5mg
Price
$121
Updated
2024/03/01
Cayman Chemical
Product number
15220
Product name
Dovitinib
Purity
≥98%
Packaging
10mg
Price
$193
Updated
2024/03/01
Cayman Chemical
Product number
15220
Product name
Dovitinib
Purity
≥98%
Packaging
25mg
Price
$313
Updated
2024/03/01
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Dovitinib Chemical Properties,Usage,Production

Description

Dovitinib (405169-16-6) is a potent kinase inhibitor. Inhibits FLT3 (IC50 = 1 nM), c-KIT (IC50 = 2 nM), FGFR (IC50 = 8 nM), VEGFR1/2/3 (IC50 = 10 nM), PDGFRβ (IC50 = 27 nM), and CSF-1R (IC50 = 36 nM).1 Active in cell culture and in whole animals. Dovitinib selectively blocks the growth B9 cells transformed by wild type, or activated mutant FGFR3. Induces apoptosis, or sensitizes cells to induction of apoptosis by other means in a variety of cancer cell lines.

Uses

Compound used in treating melanoma

Uses

Dovitinib (TKI258, CHIR-258) is a multitargeted tyrosine kinase inhibitor of FLT3 and c-KIT with IC50 of 1 nM and 2 nM, respectively.

Uses

Dovitinib (TKI258, CHIR258) is a novel multi-target inhibitor for Flt3, c-Kit, FGFR1/3, VEGFR1/2/3, PDGFRα/β with IC50 of 1 nM, 2 nM, 8 nM/9 nM and 10 nM/13 nM/8 nM, 210 nM/27 nM respectively.

Uses

Dovitinib is a receptor tyrosine kinase inhibitor that targets vascular endothelial growth factor-2, basic fibroblast growth factor-1, and platelet-derived growth factor β receptors (IC50s = 65, 11, and 5 nM, respectively). At 0.04 μM, dovitinib can inhibit endothelial cell proliferation and motility. These antiangiogenic effects have been proposed to be the mechanism by which dovitinib inhibits hepatocellular carcinoma growth and metastasis. Dovitinib has been evaluated in clinical trials for the treatment of advanced solid tumors.

Definition

ChEBI: 4-amino-5-fluoro-3-[5-(4-methyl-1-piperazinyl)-1,3-dihydrobenzimidazol-2-ylidene]-2-quinolinone is a N-arylpiperazine.

Synthesis

402948-37-2

77326-36-4

405169-16-6

Ethyl 2-[5-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl]acetate (compound of formula 1, 68 g) and 2-amino-6-fluorobenzonitrile (compound of formula 2, 151 g) were added to 20 times the volume of toluene, and evaporated under reduced pressure at 60°C until the volume of the solution was halved. Subsequently, nitrogen was passed through and 10 times the volume of toluene was added, the internal temperature was controlled to be below 65°C, and the toluene was removed by continued distillation under reduced pressure. To the residue, 10 times the volume of toluene was added again and nitrogen was introduced, and the moisture content was tested to be less than 300 ppm. After reaching the standard, it was cooled down to 20 ℃, and potassium tert-butanolate solid (169 g) was added directly, and the reaction was carried out at 50 ℃ for 2 h. The reaction was completed with 5 times the volume of toluene and nitrogen was added. Upon completion of the reaction, the reaction was quenched with 5 times the volume of water at room temperature to 40 °C. Subsequently, 5 times the volume of tetrahydrofuran was added to the viscous reaction solution until the solution was clarified and then washed with water to separate the organic and aqueous phases. After the organic phase was washed with saturated sodium chloride solution, the tetrahydrofuran was evaporated and heated to precipitate a solid, which was cooled and filtered to give the final product 4-amino-5-fluoro-3-[5-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl]quinolin-2(1H)-one (Dovimatinib, 173 g) in 88.4% yield.

in vivo

the combination of tigatuzumab and tki258 inhibited huh-7 xenograft tumor growth [3]. tki258 reduced wm tumor progression [4].

target

FLT3

IC 50

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)

References

[1] SANG HOON LEE. In vivo target modulation and biological activity of CHIR-258, a multitargeted growth factor receptor kinase inhibitor, in colon cancer models.[J]. Clinical Cancer Research, 2005, 11 10: 3633-3641. DOI:10.1158/1078-0432.ccr-04-2129
[2] XIAOHUA XIN. CHIR-258 is efficacious in a newly developed fibroblast growth factor receptor 3-expressing orthotopic multiple myeloma model in mice.[J]. Clinical Cancer Research, 2006, 12 16: 4908-4915. DOI:10.1158/1078-0432.ccr-06-0957

Dovitinib Preparation Products And Raw materials

Raw materials

Preparation Products

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Dovitinib Suppliers

Canada 1 China 171 India 3 United Kingdom 3 United States 22 Global 200
Guangzhou Tomums Life Science Co., Ltd.
Tel
020-31155029 18902330969
Fax
020-31155029
Email
sales@tomums.cn
Country
China
ProdList
4696
Advantage
58
Tianjin Kailiqi Biotechnology Co., Ltd.
Tel
15076683720
Fax
022-23754520
Email
klq@cw-bio.com
Country
China
ProdList
8011
Advantage
55
Shanghai Boyle Chemical Co., Ltd.
Tel
Fax
86-21-57758967
Email
sales@boylechem.com
Country
China
ProdList
2922
Advantage
55
Yangzhou Siyu Chemical Co.,Ltd.
Tel
0514-87325867
Fax
0086-514-87325867
Email
sales@siyuchem.com
Country
China
ProdList
370
Advantage
55
ZHIWE CHEMTECH CO LTD
Tel
021-20221225 13917446399
Fax
QQ:115820162
Email
zwchem@163.com
Country
China
ProdList
617
Advantage
61
Chembest Research Laboratories Limited
Tel
+86-21-20908456
Fax
021-58180499
Email
sales@BioChemBest.com
Country
China
ProdList
6003
Advantage
61
Chemsky (shanghai) International Co.,Ltd
Tel
021-50135380
Email
shchemsky@sina.com
Country
China
ProdList
15402
Advantage
60
Jinan Trio PharmaTech Co., Ltd.
Tel
0531-88811783
Fax
+86 (531) 55696010 QQ 1762738062
Email
sales@trio-pharmatech.com
Country
China
ProdList
1856
Advantage
62
China Langchem Inc.
Tel
0086-21-58956006
Fax
0086-21-58956100
Country
China
ProdList
7811
Advantage
57
Dalian Meilun Biotech Co., Ltd.
Tel
0411-62910999 13889544652
Email
sales@meilune.com
Country
China
ProdList
4747
Advantage
58
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View Lastest Price from Dovitinib manufacturers

Nanjing Fred Technology Co., Ltd
Product
Dovitinib 405169-16-6
Price
US $0.00-0.00/kg
Min. Order
1kg
Purity
99%, Single impurity＜0.1
Supply Ability
1 ton
Release date
2023-12-28
Career Henan Chemical Co
Product
4-Amino-5-fluoro-3-[5-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl]quinolin-2(1H)-one 405169-16-6
Price
US $2.00/kg
Min. Order
1kg
Purity
99%
Supply Ability
100kg
Release date
2018-12-24

405169-16-6, DovitinibRelated Search:

ARRY-334543 AZD-4547 Gefitinib Nintedanib Dasatinib BI 2536 Ponatinib Decernotinib Selumetinib Sulfate Savolitinib Masitinib Lestaurtinib CAL-101 PLX3397 (Pexidartinib) CO-1686 Momelotinib 790299-79-5 Dovitinib

  • 4-Amino-5-fluoro-3-[5-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl]quinolin-2(1H)-one
  • dovitinib
  • 4-amino-5-fluoro-3-[6-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl]-1H-quinolin-2-one
  • CS-226
  • CHIR-258;CHIR 258
  • Unii-I35H55G906
  • CHIR258 7.7G
  • TKI-258
  • 4-amino-5-fluoro-3-[6-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl]quinolin-2(1H)-one
  • CHIR-258(Dovitinib,TKI258)
  • CHIR-258(Dovitinib)
  • TKI258; CHIR-258
  • Dovitinib (TKI-258)
  • NCGC00249685
  • Dovitinib (TKI-258, CHIR-258)
  • 1-aMino-5-fluoro-3-(6-(4-Methylpiperazin-1-yl)-1H-benzo[d]iMidazol-2-yl)quinolin-2(1H)-one
  • 2(1H)-Quinolinone,4-aMino-5-fluoro-3-[5-(4-Methyl-1-piperazinyl)-1H-benziMidazol-2-yl]- (9CI)
  • Dovitinib(CHIR-258,TKI258)
  • 4-Amino-5-fluoro-3-[5-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl]quinolin-2(1H)-one Dovitinib (TKI-258, CHIR-258)
  • Dovitinib 4-Amino-5-fluoro-3-[5-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl]quinolin-2(1H)-one
  • 4-amino-5-fluoro-3-(5-(4-methylpiperazin-1-yl)-1H-benzo[d]imidazol-2-yl)quinolin-2(1H)-one
  • CHIR-258
  • PDovitinib
  • 2(1H)-Quinolinone,4-amino-5-fluoro-3-[6-(4-methyl-1-piperazinyl)-1H-benzimidazol-2-yl]-
  • Dovitinib (CHIR-258)
  • Dovitinib base
  • CHIR-258;CHIR258;CHIR 258;TKI258;TKI-258;TKI 258
  • 4-Amino-5-fluoro-3-(6-(4-methylpiperazin-1-yl)-1H-benzo[d]imidazol-2-yl)quinolin-2(1H)-one
  • Dovitinib, class III-V receptor tyrosine kinase inhibitor
  • Dovitinib, 10 mM in DMSO
  • Dovitinib (TKI-258) ，S1018
  • 405169-16-6
  • C21H21FN6O
  • Inhibitors
  • Intermediates & Fine Chemicals
  • Pharmaceuticals
  • API intermediates