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FL118

Cat. No. M10394
FL118 Structure
Synonym:

FL-118; CAS# 151636-76-9

Size Price Availability Quantity
10mg USD 700  USD700 In stock
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Quality Control & Documentation
Biological Activity

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.

Chemical Information
Molecular Weight 392.36
Formula C21H16N2O6
CAS Number 135415-73-5
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
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.

References

[1] Rabi Thangaiyan, et al. Am J Transl Res. Kras mutation subtypes distinctly affect colorectal cancer cell sensitivity to FL118, a novel inhibitor of survivin, Mcl-1, XIAP, cIAP2 and MdmX

[2] Zhenxue Tang, et al. Life Sci. Pyroptosis is involved in the inhibitory effect of FL118 on growth and metastasis in colorectal cancer

[3] Qi Weng, et al. Cancer Chemother Pharmacol. In vitro evaluation of FL118 and 9-Q20 cytotoxicity and cellular uptake in 2D and 3D different cell models

[4] Xiang Ling, et al. J Exp Clin Cancer Res. An ABCG2 non-substrate anticancer agent FL118 targets drug-resistant cancer stem-like cells and overcomes treatment resistance of human pancreatic cancer

[5] Zhihong Yang, et al. Biosci Trends. 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

[6] Jin Wang, et al. Am J Transl Res. FL118, a novel survivin inhibitor, wins the battle against drug-resistant and metastatic lung cancers through inhibition of cancer stem cell-like properties

[7] David Westover, et al. Mol Cancer. 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

[8] Xiang Ling, et al. Cancer Res. FL118 induces p53-dependent senescence in colorectal cancer cells by promoting degradation of MdmX

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Keywords: FL118, FL-118; CAS# 151636-76-9 supplier, p53, inhibitors, activators


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