FL118 is a novel camptothecin derivative, is insensitive to ABCG2 expression and shows improved efficacy in comparison with irinotecan in colon and lung cancer models with ABCG2-induced resistance. FL118 inhibits human survivinion expression and activates tumor suppressor p53 as a MOA in p53 wild-type cancer cells.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
Kras mutation subtypes distinctly affect colorectal cancer cell sensitivity to FL118, a novel inhibitor of survivin, Mcl-1, XIAP, cIAP2 and MdmX
Rabi Thangaiyan, et al. Am J Transl Res. 2021 Jul 15;13(7):7458-7474. PMID: 34377229.
Pyroptosis is involved in the inhibitory effect of FL118 on growth and metastasis in colorectal cancer
Zhenxue Tang, et al. Life Sci. 2020 Sep 15;257:118065. PMID: 32659366.
In vitro evaluation of FL118 and 9-Q20 cytotoxicity and cellular uptake in 2D and 3D different cell models
Qi Weng, et al. Cancer Chemother Pharmacol. 2019 Sep;84(3):527-537. PMID: 31030236.
An ABCG2 non-substrate anticancer agent FL118 targets drug-resistant cancer stem-like cells and overcomes treatment resistance of human pancreatic cancer
Xiang Ling, et al. J Exp Clin Cancer Res. 2018 Oct 3;37(1):240. PMID: 30285798.
FL118, a novel camptothecin analogue, suppressed migration and invasion of human breast cancer cells by inhibiting epithelial-mesenchymal transition via the Wnt/β-catenin signaling pathway
Zhihong Yang, et al. Biosci Trends. 2018;12(1):40-46. PMID: 29553100.
FL118, a novel survivin inhibitor, wins the battle against drug-resistant and metastatic lung cancers through inhibition of cancer stem cell-like properties
Jin Wang, et al. Am J Transl Res. 2017 Aug 15;9(8):3676-3686. PMID: 28861158.
FL118, a novel camptothecin derivative, is insensitive to ABCG2 expression and shows improved efficacy in comparison with irinotecan in colon and lung cancer models with ABCG2-induced resistance
David Westover, et al. Mol Cancer. 2015 Apr 28;14:92. PMID: 25928015.
FL118 induces p53-dependent senescence in colorectal cancer cells by promoting degradation of MdmX
Xiang Ling, et al. Cancer Res. 2014 Dec 15;74(24):7487-97. PMID: 25512388.
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PhiKan 083 is a p53 stabilizing agent.
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