推荐产品
质量水平
方案
≥98% (HPLC)
表单
powder
颜色
white to beige
溶解性
DMSO: 2 mg/mL, clear
储存温度
2-8°C
SMILES字符串
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
生化/生理作用
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.
储存分类代码
11 - Combustible Solids
闪点(°F)
Not applicable
闪点(°C)
Not applicable
历史批次信息供参考:
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
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
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
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
Daniel E Lopes de Menezes et al.
Clinical cancer research : an official journal of the American Association for Cancer Research, 11(14), 5281-5291 (2005-07-22)
Fms-like tyrosine kinase 3 (FLT3) encodes a receptor tyrosine kinase (RTK) for which activating mutations have been identified in a proportion of acute myelogenous leukemia (AML) patients and associated with poor clinical prognosis. Given the relevance of FLT3 mutations in
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