FC-116
Based on 1 Customer Validation
FC-11 is a tubulin inhibitor. FC-116 inhibits the proliferation of colorectal cancer (CRC) cells, with IC50 values of 4.52 nM for HCT116 cells and 18.69 nM for CT26 cells. FC-11 can induce ER stress to generate excess ROS, leading to mitochondrial damage, thereby promoting apoptosis in colorectal cancer (CRC) cells by targeting microtubules. FC-116 exerts potent anti-tumor effects in vivo. FC-11 can be used for the study of colorectal cancer.
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- Purity: 98.04%
- CAS No.: 2417298-29-2
- 화학식: C21H20FNO4
- 분자량:369.39
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CT26 | IC50 |
18.69 nM
Compound: 17; FC116
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Antiproliferative activity against mouse CT26 cells assessed as inhibition of proliferation measured after 24 hrs by CCK-8 assay
Antiproliferative activity against mouse CT26 cells assessed as inhibition of proliferation measured after 24 hrs by CCK-8 assay
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[PMID: 37301075] |
| HCT-116 | GI50 |
0.079 μM
Compound: 17; FC116
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Cytotoxicity against human HCT-116 cells assessed as growth inhibition measured after 48 hrs by CCK-8 assay
Cytotoxicity against human HCT-116 cells assessed as growth inhibition measured after 48 hrs by CCK-8 assay
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[PMID: 37301075] |
| HCT-116 | IC50 |
4.52 nM
Compound: 17; FC116
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Antiproliferative activity against human HCT116 cells assessed as inhibition of proliferation measured after 24 hrs by CCK-8 assay
Antiproliferative activity against human HCT116 cells assessed as inhibition of proliferation measured after 24 hrs by CCK-8 assay
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[PMID: 37301075] |
FC-116 (24 h) exerts superior antiproliferative activity against HCT116 cells (IC50 = 4.52 nM), and CT26 cells (IC50 = 18.69 nM), and shows no cytotoxicity to normal NCM460 cells and PC12 cells at the same dose[1].
FC-116 (2.5-40 nM, 24 h) significantly induces apoptosis, ER stress, ROS production and blocks the cell cycle of HCT116 and CT26 cells in the G2/M phase[1].
FC-116 (12.5-100 μM, 24 h) directly binds to the colchicine binding site of tubulin (Kd = 136 nM) via Cys239 and Cys354, inhibits tubulin polymerization in a dose-dependent manner, and disrupts the microtubule network of HCT116 and CT26 cells[1].
FC-116 (2.540 nM, 24 h) reduces mitochondrial membrane potential (MMP), inhibits mitochondrial respiration (decreases oxygen consumption rate, OCR), and causes mitochondrial swelling and vacuolization in HCT116 cells and CT26 cells[1].
FC-116 (0.3-30 nM, 3 days) exhibits potent inhibitory activity against three colorectal cancer (CRC) organoid models (21JW91CRT1, 21Q4MGCRT1, 22G5AECRT1), with IC50 values of 2.5 nM, 1.8 nM, and 1.9 nM, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HCT116 and CT26 cells
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Concentration:2.5, 5, 10, 20, 40 nM
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Incubation Time:24 h
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Result:Increased the apoptosis rate.
Up-regulated the expression of apoptosis-related protein Cleaved-Caspase 3.
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Cell Line:HCT116 and CT26 cells
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Concentration:2.5, 5, 10, 20, 40 nM
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Incubation Time:24 h
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Result:Blocked the cell cycle of HCT116 and CT26 cells in the G2/M phase.
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Cell Line:HCT116 and CT26 cells
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Concentration:2.5, 5, 10, 20, 40 nM
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Incubation Time:24 h
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Result:Increased phosphorylation of PERK, eIF2α, and IRE1α.
FC-116 (1.5-3 mg/kg, i.p., once daily, 45 days) shows potent inhibitory effect on intestinal tumorigenesis in C57BL/6-APCmin/+ mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:HCT116 cells (5 × 106) were subcutaneously injected into the right flank of 5-week-old male BALB/c nude mice[1].
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Dosage:1.5, 3 mg/kg
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Administration:i.p., once daily, 21 days
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Result:Achieved tumor growth inhibition.
Showed no significant changes in body weight.
Reduced the Ki67 expression.
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Animal Model:C57BL/6-APCmin/+ mice with a mutation (replacing amino acid L at position 850 of the Apc gene with a termination codon X) were used[1].
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Dosage:1.5, 3 mg/kg
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Administration:i.p., once daily, 45 days
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Result:Achieved adenoma number inhibition.
Showed no significant changes in body weight.
Increased phosphorylation of endoplasmic reticulum (ER) stress-related molecules eIF2α and IRE1α in intestinal tissues.
Increased the necrotic area and apoptosis in tumor tissues.
Chemical Information
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CAS No. 2417298-29-2
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Appearance Solid
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분자량 369.39
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화학식 C21H20FNO4
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Color Off-white to light yellow
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SMILES
COC1=C(OC)C(OC)=CC(C(/C(C)=C/C2=CNC3=C2C=CC(F)=C3)=O)=C1
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
DMSO : 66.67 mg/mL (180.49 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
순도&문서
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Data Sheet (278 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.7072 mL | 13.5358 mL | 27.0717 mL | 67.6791 mL |
| 5 mM | 0.5414 mL | 2.7072 mL | 5.4143 mL | 13.5358 mL | |
| 10 mM | 0.2707 mL | 1.3536 mL | 2.7072 mL | 6.7679 mL | |
| 15 mM | 0.1805 mL | 0.9024 mL | 1.8048 mL | 4.5119 mL | |
| 20 mM | 0.1354 mL | 0.6768 mL | 1.3536 mL | 3.3840 mL | |
| 25 mM | 0.1083 mL | 0.5414 mL | 1.0829 mL | 2.7072 mL | |
| 30 mM | 0.0902 mL | 0.4512 mL | 0.9024 mL | 2.2560 mL | |
| 40 mM | 0.0677 mL | 0.3384 mL | 0.6768 mL | 1.6920 mL | |
| 50 mM | 0.0541 mL | 0.2707 mL | 0.5414 mL | 1.3536 mL | |
| 60 mM | 0.0451 mL | 0.2256 mL | 0.4512 mL | 1.1280 mL | |
| 80 mM | 0.0338 mL | 0.1692 mL | 0.3384 mL | 0.8460 mL | |
| 100 mM | 0.0271 mL | 0.1354 mL | 0.2707 mL | 0.6768 mL |
FC-116 Related Classifications
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