SML3012
Dovitinib
≥98% (HPLC)
Synonym(s):
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
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About This Item
Empirical Formula (Hill Notation):
C21H21FN6O
CAS Number:
Molecular Weight:
392.43
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
Quality Level
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
2-8°C
SMILES string
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)
InChI key
PIQCTGMSNWUMAF-UHFFFAOYSA-N
Biochem/physiol Actions
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.).
Orally active, potent inhibitor against class III-V receptor tyrosine kinases (FLT3, KIT, PDGFR1/2, CSFR, FGFR1/3, VEGFR1/2/3) with efficacy in vitro and in vivo.
Storage Class
11 - Combustible Solids
flash_point_f
Not applicable
flash_point_c
Not applicable
Regulatory Information
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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)
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
Yi-Han Chiu et al.
Journal of oncology, 2019, 2024648-2024648 (2019-09-06)
Breast cancer is the most common cancer and the leading cause of cancer deaths in women worldwide. The rising incidence rate and female mortality make it a significant public health concern in recent years. Dovitinib is a novel multitarget receptor
Global Trade Item Number
| SKU | GTIN |
|---|---|
| SML3012-10MG | 04065265878227 |
| SML3012-50MG | 04065265878234 |