| Size | Price | |
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| 500mg | ||
| 1g | ||
| Other Sizes |
| Targets |
As an ADC linker component, FL118-C3-OC-amide-C-NH2 itself does not have an independent pharmacological target. Upon conjugation to an antibody and internalization into target cells, the FL118 payload is released and targets multiple oncogenic proteins. Similar to its parent compound FL118, the released payload selectively inhibits key anti-apoptotic proteins including survivin, Mcl-1, XIAP, and cIAP2, and targets the DDX5/p68 oncoprotein through ubiquitin-mediated degradation pathways.
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| ln Vitro |
As an ADC linker, its in vitro activity is typically evaluated following conjugation to a targeting antibody, with efficacy assessed by target cell cytotoxicity and selectivity. The parent payload FL118 has demonstrated potent cytotoxicity against various cancer cell lines with IC₅₀ values in the low nanomolar range.
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| ln Vivo |
The compound is designed for use in ADC development, where in vivo antitumor efficacy would be assessed following conjugation to a tumor-targeting antibody.
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| Enzyme Assay |
The compound is a synthetic intermediate for ADC preparation rather than a direct biological testing agent.
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| Cell Assay |
For cell-based studies, FL118-C3-OC-amide-C-NH2 is typically dissolved in DMSO as a stock solution. The working solution can be prepared by diluting the stock in appropriate cell culture media. Since this compound is an ADC linker, cellular activity studies are typically conducted after it is conjugated to a targeting antibody to form a complete ADC. Standard ADC characterization includes target cell binding assays, internalization studies, and cytotoxicity assessments using MTT or similar viability assays.
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| Animal Protocol |
For in vivo administration of ADCs synthesized using FL118-C3-OC-amide-C-NH2, standard ADC formulation protocols apply. The unconjugated linker can be formulated using various injection vehicles: (1) DMSO : Tween 80 : Saline = 10 : 5 : 85; (2) DMSO : PEG300 : Tween 80 : Saline = 10 : 40 : 5 : 45; or (3) DMSO : Corn oil = 10 : 90. For oral administration, the compound can be suspended in 0.5% CMC Na (carboxymethylcellulose sodium) or dissolved in PEG400. The complete ADC conjugates are typically administered via intravenous injection. Dosing frequency and duration vary depending on the specific ADC construct and tumor model.
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| ADME/Pharmacokinetics |
As an ADC linker, the pharmacokinetic properties of the final ADC conjugate are primarily determined by the antibody component rather than the linker-payload alone.
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| Toxicity/Toxicokinetics |
The product is for research use only and should be handled with appropriate safety precautions. Standard laboratory safety practices including the use of personal protective equipment (gloves, lab coat, eye protection) should be followed when handling this compound.
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| References | |
| Additional Infomation |
FL118-C3-OC-amide-C-NH2 (compound 6a) is an ADC linker used in the synthesis of antibody-drug conjugates (ADCs). The compound has a molecular formula of C₂₇H₂₈N₄O₈ and a molecular weight of 536.53 g/mol. Synonyms include (S)-2-Amino-N-((3-(7-ethyl-7-hydroxy-8,11-dioxo-7,8,11,13-tetrahydro-10H-[1,3]dioxolo[4,5-g]pyrano[3',4':6,7]indolizino[1,2-b]quinolin-14-yl)propoxy)methyl)acetamide. The compound should be stored as a powder at -20°C (stable for up to 3 years) or at 4°C (stable for up to 2 years), protected from light and moisture. Solubility: typically soluble in DMSO (e.g., 10 mM). Purity is typically ≥98%. The compound is categorized as an ADC linker, pharmaceutical standard, intermediate, and fine chemical. Reference: WO2023143208 A1.
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| Molecular Formula |
C27H28N4O8
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|---|---|
| Molecular Weight |
536.533226966858
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| CAS # |
2821769-41-7
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| Appearance |
Typically exists as solid at room temperature
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| SMILES |
CC[C@@]1(C2C=C3C4C(=C(C5C(N=4)=CC4OCOC=4C=5)CCCOCNC(CN)=O)CN3C(=O)C=2COC1=O)O
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| Synonyms |
FL-118-C3-O-C-amide-C-NH2 formate
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ~100 mg/mL (171.7 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8638 mL | 9.3191 mL | 18.6383 mL | |
| 5 mM | 0.3728 mL | 1.8638 mL | 3.7277 mL | |
| 10 mM | 0.1864 mL | 0.9319 mL | 1.8638 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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