おすすめの製品
品質水準
アッセイ
≥98% (HPLC)
形状
powder
色
white to beige
溶解性
DMSO: 2 mg/mL, clear
保管温度
2-8°C
SMILES記法
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
生物化学的／生理学的作用
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.).
保管分類コード
11 - Combustible Solids
引火点(°F)
Not applicable
引火点(℃)
Not applicable
適用法令
試験研究用途を考慮した関連法令を主に挙げております。化学物質以外については、一部の情報のみ提供しています。 製品を安全かつ合法的に使用することは、使用者の義務です。最新情報により修正される場合があります。WEBの反映には時間を要することがあるため、適宜SDSをご参照ください。
Jan Code
SML3012-BULK:
SML3012-10MG:
SML3012-VAR:
SML3012-50MG:
試験成績書（COA）
製品のロット番号・バッチ番号を入力して、試験成績書（COA） を検索できます。ロット番号・バッチ番号は、製品ラベルに「Lot」または「Batch」に続いて記載されています。
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)
Berna Sahan et al.
Cornea, 38(9), 1161-1168 (2019-06-11)
To compare the inhibitory effects of dovitinib and bevacizumab for treatment of corneal neovascularization (CNV). Thirty-nine adult female Sprague Dawley rats weighing 180 to 250 g were used. CNV was induced by silver nitrate in the right eye of each
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
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
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