Famitinib - CAS 945380-27-8
Catalog number: 945380-27-8
Category: Inhibitor
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Molecular Formula:
C23H27FN4O2
Molecular Weight:
410.493
COA:
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Description:
Famitinib is a novel multi-targeted receptor tyrosine kinase inhibitor under development for cancer treatment.  Famitinib is a structural analogue ofsunitinib, is a novel and potent multi-targeted RTK inhibitor that is currently undergoing phase II clinical trials in China for the treatment of renal cell carcinoma, gastrointestinal stromal tumours, pancreatic cancer, and nasopharyngeal carcinoma. Compared with sunitinib, famitinib exhibits superior inhibition activities against multiple RTKs.
Synonyms:
Famitinib; SHR1020; SHR 1020; SHR-1020
MSDS:
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InChIKey:
GKEYKDOLBLYGRB-LGMDPLHJSA-N
InChI:
InChI=1S/C23H27FN4O2/c1-4-27(5-2)10-11-28-9-8-19-21(23(28)30)14(3)20(25-19)13-17-16-12-15(24)6-7-18(16)26-22(17)29/h6-7,12-13,25H,4-5,8-11H2,1-3H3,(H,26,29)/b17-13-
Canonical SMILES:
CCN(CC)CCN1CCC2=C(C1=O)C(=C(N2)C=C3C4=C(C=CC(=C4)F)NC3=O)C
Current Developer:
Jiangsu Hengrui Medicine Co. Ltd. China
1.Famitinib enhances nasopharyngeal cancer cell radiosensitivity by attenuating radiation-induced phosphorylation of platelet-derived growth factor receptor and c-kit and inhibiting microvessel formation.
Mu X1,2, Ma J1, Zhang Z1, Zhou H1, Xu S1, Qin Y1, Huang J1, Yang K1, Wu G1. Int J Radiat Biol. 2015;91(9):771-6. doi: 10.3109/09553002.2015.1062574. Epub 2015 Sep 21.
PURPOSE: Famitinib is a novel tyrosine kinase inhibitor. We investigated the effects of famitinib on the radiosensitivity of human nasopharyngeal carcinoma (NPC) cell radiosensitivity in vitro and in vivo, and explored its possible mechanisms.
2.Hypothyroidism as a potential biomarker of efficacy of famitinib, a novel VEGFR-2 inhibitor in metastatic breast cancer.
Cao J1, Zhang J, Wang Z, Wang B, Lv F, Wang L, Hu X. Cancer Chemother Pharmacol. 2014 Aug;74(2):389-98. doi: 10.1007/s00280-014-2505-x. Epub 2014 Jun 18.
PURPOSE: Hypothyroidism is a common adverse event in patients treated with anti-VEGFR-2 targeting agents and may be a valuable predictive factor of efficacy. Famitinib is an inhibitor of multiple tyrosine kinases mainly targeting VEGFR-2. The objectives of this study were to assess the efficacy and safety of famitinib in patients with pretreated HER2-negative metastatic breast cancer (MBC) and to explore potential of famitinib-induced hypothyroidism and serum vascular endothelial growth factor (VEGF) level for efficacy prediction.
3.[Predicting pharmacokinetics of anti-cancer drug, famitinib in human using physiologically based pharmacokinetic model].
Yu MM, Gao ZW, Chen XY, Zhong DF. Yao Xue Xue Bao. 2014 Dec;49(12):1684-8.
This study is to establish physiologically based pharmacokinetic (PBPK) models of famitinib in rat and monkey, and then to predict the pharmacokinetics and tissue distribution of famitinib in human based on the PBPK models. According to published paper, previous studies and the chemical properties of famitinib predicted by ACD/ADME suite and SimCYP, the PBPK models of rat and monkey were established and optimized using GastroPlus. And then, the PBPK models were applied to predict the pharmacokinetic and tissue distribution of famitinib in human. The results showed that the PBPK models of rat and monkey can fit the observed data well, and the AUC0-∞, ratios of observed and calculated data in rat and monkey were 1.00 and 0.97, respectively. The AUC0-∞, ratios of observed and predicted data in human were 1.63 (rat to human) and 1.57 (monkey to human), respectively. The rat and monkey PBPK models of famitinib were well established, and the PBPK models were applied in predicting pharmacokinetic of famitinib in human successfully.
4.Metabolism and bioactivation of famitinib, a novel inhibitor of receptor tyrosine kinase, in cancer patients.
Xie C1, Zhou J, Guo Z, Diao X, Gao Z, Zhong D, Jiang H, Zhang L, Chen X. Br J Pharmacol. 2013 Apr;168(7):1687-706. doi: 10.1111/bph.12047.
BACKGROUND AND PURPOSE: Famitinib is a novel multi-targeted receptor tyrosine kinase inhibitor under development for cancer treatment. This study aims to characterize the metabolic and bioactivation pathways of famitinib.
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CAS 945380-27-8 Famitinib

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