Passa al contenuto
Merck
Tutte le immagini(1)

Documenti

SML3012

Sigma-Aldrich

Dovitinib

≥98% (HPLC)

Sinonimo/i:

4-Amino-5-fluoro-3-[6-(4-methyl-1-piperazinyl)-1H-benzimidazol-2-yl]-2(1H)-quinolinone, CHIR 258, CHIR-258, CHIR258, TKI 258, TKI-258, TKI258

Autenticatiper visualizzare i prezzi riservati alla tua organizzazione & contrattuali
Tutte le immagini(1)

About This Item

Formula empirica (notazione di Hill):
C21H21FN6O
Numero CAS:
405169-16-6
Peso molecolare:
392.43
Numero MDL:
MFCD10565680
Codice UNSPSC:
12352200
NACRES:
NA.77

Livello qualitativo

100

Saggio

≥98% (HPLC)

Forma fisica

powder

Colore

white to beige

Solubilità

DMSO: 2 mg/mL, clear

Temperatura di conservazione

2-8°C

Stringa SMILE

O=C1NC2=C(C(N)=C1C3=NC4=CC=C(N5CCN(CC5)C)C=C4N3)C(F)=CC=C2

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)
PIQCTGMSNWUMAF-UHFFFAOYSA-N

Azioni biochim/fisiol

Dovitinib (CHIR-258) is an orally active and potent receptor tyrosine kinase (RTK) inhibitor against class III (FLT3/KIT/PDGFR1/CSFR/PDGFR2 IC50 = 1/2/27/36/200 nM), class IV (FGFR1/3 IC50 = 8/9 nM), and class V (VEGFR1/2/3 IC50 = 10/13/8 nM) RTKs, but not INSR, EGFR1, ErbB2 or Raf (IC50 = 2.1, 2.2, >20, >25 μM, respectively). Dovitinib inhibits target RTKs phosphorylation in cultured cells (pVEGFR1 and pPDGFRβ IC90 <50 nM; KM12L4a) and exhibits in vivo anti-tumor efficacy in mice bearing KM12L4a or HCT116 human cancer xenografts (10-120 mg/kg/day p.o.).

Codice della classe di stoccaggio

11 - Combustible Solids

Punto d’infiammabilità (°F)

Not applicable

Punto d’infiammabilità (°C)

Not applicable

Certificati d'analisi (COA)

Cerca il Certificati d'analisi (COA) digitando il numero di lotto/batch corrispondente. I numeri di lotto o di batch sono stampati sull'etichetta dei prodotti dopo la parola ‘Lotto’ o ‘Batch’.

Possiedi già questo prodotto?

I documenti relativi ai prodotti acquistati recentemente sono disponibili nell’Archivio dei documenti.

Visita l’Archivio dei documenti

Isadora C Silveira et al.
Anti-cancer agents in medicinal chemistry, 20(6), 751-755 (2020-02-14)
Identification of the antitumor role of tyrosine kinase inhibitors, such as TKI-258, may lead to novel therapeutics for Oral Squamous Cell Carcinoma (OSCC), which has high mortality rates. TKI-258 blocks Fibroblast Growth Factor Receptors (FGFRs), Platelet-Derived Growth Factor Receptors (PDGFRs)
Brian B Hasinoff et al.
Biochemical pharmacology, 84(12), 1617-1626 (2012-10-09)
Dovitinib (TKI258/CHIR258) is a multi-kinase inhibitor in phase III development for the treatment of several cancers. Dovitinib is a benzimidazole-quinolinone compound that structurally resembles the bisbenzimidazole minor groove binding dye Hoechst 33258. Dovitinib bound to DNA as shown by its
Xiaohua Xin et al.
Clinical cancer research : an official journal of the American Association for Cancer Research, 12(16), 4908-4915 (2006-08-18)
The ectopically expressed and deregulated fibroblast growth factor receptor 3 (FGFR3) results from a t(4;14) chromosomal translocation that occurs in approximately 15% of multiple myeloma (MM) patients and confers a particularly poor prognosis. This study assesses the antimyeloma activity of
Tiina E Kähkönen et al.
Journal of bone oncology, 16, 100232-100232 (2019-04-09)
Advanced breast cancer has a high incidence of bone metastases. In bone, breast cancer cells induce osteolytic or mixed bone lesions by inducing an imbalance in bone formation and resorption. Activated fibroblast growth factor receptors (FGFRs) are important in regulation
Arabinda Das et al.
Cancer investigation, 38(6), 349-355 (2020-05-23)
Background: Meningiomas represent ∼30% of primary central nervous system (CNS) tumors. Although advances in surgery and radiotherapy have significantly improved survival, there remains an important subset of patients whose tumors have more aggressive behavior and are refractory to conventional therapy.
Visualizza tutti i documenti correlati

Il team dei nostri ricercatori vanta grande esperienza in tutte le aree della ricerca quali Life Science, scienza dei materiali, sintesi chimica, cromatografia, discipline analitiche, ecc..

Contatta l'Assistenza Tecnica.