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(Z)-3-(((4-(N-甲基-2-(4-甲基哌嗪-1-基)乙酰氨基)苯基)氨基)(苯基)亚甲基)-2-氧代吲哚啉-6-羧酸甲酯乙磺酸盐; 尼达尼布乙磺酸盐
Nintedanib Ethanesulfonate Salt (Synonyms: Intedanib; BIBF 1120)
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中文名称(Z)-3-(((4-(N-甲基-2-(4-甲基哌嗪-1-基)乙酰氨基)苯基)氨基)(苯基)亚甲基)-2-氧代吲哚啉-6-羧酸甲酯乙磺酸盐; 尼达尼布乙磺酸盐
英文名称 Nintedanib Ethanesulfonate Salt (Synonyms: Intedanib; BIBF 1120)
CAS号656247-18-6
分子式C31H33N5O4.C2H6O3S
分子量649.76 | 539.64(free)
MDLMFCD26142360
外观Yellow powder
储存条件4°C, sealed storage, away from moisture
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Nintedanib Ethanesulfonate Salt (BIBF 1120) is an inhibitor of the receptor tyrosine kinases VEGFR, FGFR, and PDGFR (IC50s = 13-34, 37-610, 59, and 65 nM for VEGFR1-3, FGFR1-4, PDGFRα, and PDGFRβ, respectively).1 It is selective for VEGFR, FGFR, and PDGFR over a panel of 33 kinases but does inhibit FLT3, LCK, LYN, and Src (IC50s = 16-156 nM). BIBF 1120 inhibits growth factor-dependent proliferation of human umbilical vascular endothelial cells (HUVECs), human microvascular skin endothelial cells (HSMECs), human umbilical artery smooth muscle cells (HUASMCs), and bovine retinal pericytes (BRPs; EC50s = 7-290 nM). In vivo, BIBF 1120 (100 mg/kg) reduces tumor microvessel density and the number of PDGFRβ-expressing perivascular cells in a FaDu head and neck small cell carcinoma mouse xenograft model. It also inhibits tumor growth in a Caki-1 renal cancer mouse xenograft model. Formulations containing BIBF 1120 have been used in the treatment of idiopathic pulmonary fibrosis and non-small cell lung cancer (NSCLC).
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相关文献
Effect of a novel oral chemotherapeutic agent containing a combination of trifluridine, tipiracil and the novel triple angiokinase inhibitor nintedanib, on human colorectal cancer xenografts
PMID: 27805254 PMCID: PMC5112602 DOI: 10.3892/or.2016.5208
Design, synthesis, and evaluation of indolinones as triple angiokinase inhibitors and the discovery of a highly specific 6-methoxycarbonyl-substituted indolinone (BIBF 1120).
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BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy.
PMID: 18559524 DOI: 10.1158/0008-5472.CAN-07-6307
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(Z)-3-(((4-(N-甲基-2-(4-甲基哌嗪-1-基)乙酰氨基)苯基)氨基)(苯基)亚甲基)-2-氧代吲哚啉-6-羧酸甲酯; 尼达尼布
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(Z)-3-(((4-(N-甲基-2-(4-甲基哌嗪-1-基)乙酰氨基)苯基)氨基)(苯基)亚甲基)-2-氧代吲哚啉-6-羧酸甲酯乙磺酸盐; 尼达尼布乙磺酸盐
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