Dovitinib

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Anticancer drugs

Product Name: Dovitinib
CAS No.: 915769-50-5
Chemical Name: Dovitinib
Synonyms: TKI258 Lactate;Unii-69vky8p7ea;Dovitinib USP/EP/BP;Dovitinib Lactate（b）;MultidiMensional iMatinib;Dovitinib lactate(TKI258);Dovitinib Lactate Hydrate;Dovitinib (TKI258) Lactate;Dovitinib(C3H6O3：H20)=1：1：1;Dovitinib lactate Monohydrate
CBNumber: CB31518505
Molecular Formula: C24H29FN6O5
Formula Weight: 500.5226632
MOL File: 915769-50-5.mol

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Dovitinib Property

storage temp.: Store at -20°C
solubility: insoluble in EtOH; ≥10.62 mg/mL in DMSO; ≥168.2 mg/mL in H2O
form: Powder

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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.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.

P302+P352IF ON SKIN: wash with plenty of soap and water.

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

Biosynth Carbosynth

Product number: FD65011
Product name: Dovitinib Lactate
Packaging: 10mg
Price: $86
Updated: 2021/12/16

ApexBio Technology

Product number: B5953
Product name: Dovitinib(TKI258)Lactate
Packaging: 25mg
Price: $150
Updated: 2021/12/16

Biosynth Carbosynth

Product number: FD65011
Product name: Dovitinib Lactate
Packaging: 50mg
Price: $259
Updated: 2021/12/16

American Custom Chemicals Corporation

Product number: API0017255
Product name: DOVITINIB LACTATE HYDRATE
Purity: 95.00%
Packaging: 5MG
Price: $497.72
Updated: 2021/12/16

Biorbyt Ltd

Product number: orb146142
Product name: Dovitinib (TKI258) Lactate
Purity: >99%
Packaging: 100mg
Price: $606.9
Updated: 2021/12/16

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Dovitinib Chemical Properties,Usage,Production

Anticancer drugs

Dovitinib is an orally active small molecule multi-targeted tyrosine kinase inhibitor which can act directly on the tumor cells and provide nutritional support for blood vessels and stromal tumor cells, it has inhibition effect on a variety of growth factors such as VEGFR1-3, FGFR1-3, PDGFRB, e-KIT, Ret, TraA and csf-1. At present, Dovitinib is in clinical trail phase III ,clinical studies show that it has significant therapeutic effect on breast cancer, urinary tract carcinoma, prostate cancer, multiple myeloma, melanoma. With the development of clinical researches, cancer treatment is expected to expand its scope.
Dovitinib performs its anti-tumor effects by anti-angiogenic activity and anti-proliferative survival activity . The drug is used for inoperable/local treatment of advanced hepatocellular carcinoma patients,it requires the lesion diameter greater than 1cm , blood, liver function is good, physical condition is good ,patients do not receive any systemic therapy (allow surgery 4 weeks outside and radiotherapy and intervention ).
Preparation: use 5-chloro-2-nitroaniline and N-methyl piperazine as raw materials,after substitution,and reduction, form a ring with β-ethoxy-β-imino-propionate hydrochloride .Finally,after cyclization with 2-amino-6-fluorobenzonitrileto, generate Dovitinib , a total yield of 44.1%.
The above information is edited by the chemicalbook of Tian Ye.

Uses

4-Amino-5-fluoro-3-(6-(4-methylpiperazin-1-yl)-1H-benzo[d]imidazol-2-yl)quinolin-2(1H)-one 2-hydroxypropanoate hydrate is a useful research chemical compound.

Biological Activity

fibroblast growth factor receptor 1 (fgfr1) and fgfr2 amplifications are observed in approximately 10% of breast cancers and are related to poor outcomes. dovitinib (tki258) is an oral tyrosine kinase inhibitor (tki) against fgfr1–3, vegfr1–3, and platelet-derived growth factor receptor (pdgfr).

in vitro

dovitinib decreased the concentrations of pfrs2 and perk/mapk in a dose-dependent manner in fgfr1 amplified and fgfr2 amplified cell lines. the ic50 for cell growth inhibition was 190 and 180 nmol/l in mda-mb-134 and sum52, respectively. conversely, ic50 values were more than 2,000 nmol/l in the 11 breast cancer cell lines that had neither fgfr1 nor fgfr2 amplification [1].

in vivo

in vivo model (hbcx-2 breast cancer primary xenograft, with 8 fgfr1 gene copies), dovitinib prevented tumor growth at the 30 mg/kg dose and caused tumor regression at the 50 mg/kg dose. similarly, dovitinib caused tumor regression in hbcx-3 xenografts when administered at a dose of 40 mg/kg daily until day 35 [1].

IC 50

~10 nmol/l for fgfr1–3

References

[1] andré f, bachelot t, campone m, dalenc f, perez-garcia jm, hurvitz sa, turner n, rugo h, smith jw, deudon s, shi m, zhang y, kay a, porta dg, yovine a, baselga j. targeting fgfr with dovitinib (tki258): preclinical and clinical data in breast cancer. clin cancer res. 2013 jul 1;19(13):3693-702.

Dovitinib Preparation Products And Raw materials

Raw materials

Preparation Products

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View Lastest Price from Dovitinib manufacturers

Nanjing Fred Technology Co., Ltd

Product: CHIR-258 (TKI-258,Dovitinib Lactate Hydrate) 915769-50-5
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

Dideu Industries Group Limited

Product: Dovitinib 915769-50-5
Price: US $1.10/g
Min. Order: 1g
Purity: 99.9%
Supply Ability: 100 Tons Min
Release date: 2021-07-06

Career Henan Chemical Co

Product: Dovitinib 915769-50-5
Price: US $2.00/kg
Min. Order: 1kg
Purity: 99%
Supply Ability: 100kg
Release date: 2018-12-24

915769-50-5, DovitinibRelated Search:

Acetonitrile Methanol Benzimidazole Methyl acrylate 8-Hydroxyquinoline Erlotinib Imatinib Dasatinib monohydrate Basic Violet 1 Sunitinib Methyl acetate Lapatinib Gefitinib Paraquat dichloride Kresoxim-methyl L(+)-Lactic acid Methylparaben 3-(4-Hydroxyphenyl)propionic acid

4-Amino-5-fluoro-3-[6-(4-methyl-1-piperazinyl)-1H-benzimidazol-2-yl]-2(1H)-quinolinone 2-hydroxypropanoate hydrate (1:1:1)

Unii-69vky8p7ea

Dovitinib lactate(TKI258)

Propanoic acid, 2-hydroxy-, coMpd. with 4-aMino-5-fluoro-3-[6-(4-Methyl-1-piperazinyl)-1H-benziMidazol-2-yl]-2(1H)-quinolinone, hydrate (1:1:1)

Propanoic acid, 2-hydroxy-, coMpd. with 4-aMino-5-fluoro-3-[6-(4-Methyl-1-piperazinyl)-1H-benziMidazol-2-yl]-2(1H)-quinolinone, hydrate

Dovitinib(C3H6O3：H20)=1：1：1

Dovitinib lactate Monohydrate

4-Amino-5-fluoro-3-(6-(4-methylpiperazin-1-yl)-1H-benzo[d]imidazol-2-yl)quinolin-2(1H)-one 2-hydr

4-AMino-5-fluoro-3-(6-(4-Methylpiperazin-1-yl)-1H-benzo[d]iMidazol-2-yl)quinolin-2(1H)-one 2-hydroxypropanoate hydrate

MultidiMensional iMatinib

Dovitinib lactate(TKI-258, CHIR-258)

4-Amino-5-fluoro-3-[6-(4-methyl-1-piperazinyl)-1H-benzimidazol-2-yl]-2(1H)-quinolinone 2-hydroxypropanoate

Dovitinib (TKI258) Lactate

Dovitinib 4-Amino-5-fluoro-3-[6-(4-methyl-1-piperazinyl)-1H-benzimidazol-2-yl]-2(1H)-quinolinone 2-hydroxypropanoate hydrate (1:1:1)

4-Amino-5-fluoro-3-(6-(4-methylpiperazin-1-yl)-1H-benzo[d]imidazol-2-yl)quinolin-2(1H)-one 2-h

TKI258 Lactate

TKI258;CHIR258;DOVITINIB (TKI 258;CHIR 258)

Dovitinib Lactate Hydrate

Dovitinib USP/EP/BP

VEGFR1,FGFR1,TKI258 lactate,SCFR,CD117,Dovitinib lactate hydrate,FGFR,Fms like tyrosine kinase 3,PDGFR,FGFR3,CD135,inhibit,CHIR-258 lactate,multi-targeted,VEGFR,Fibroblast growth factor receptor,Cluster of differentiation antigen 135,tyrosine,Platelet-derived growth factor receptor,PDGFRβ,Inhibitor,VEGFR3,Vascular endothelial growth factor receptor,PDGFRα,VEGFR2,FLT3,c-Kit,kinase

CHIR-258 (TKI-258,Dovitinib Lactate Hydrate)

Dovitinib Lactate（b）

915769-50-5

915769-45-6

C24H29FN6O5

C21H21FN6OC3H6O3H2O

Inhibitors

Anti-cancer&immunity