Art. -Nr.: HY-155068

FC-116

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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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Reinheit: 98.04%
CAS. Nr.: 2417298-29-2
Formel: C₂₁H₂₀FNO₄
Molecular Weight:369.39

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

FC-116 Chemical Structure

CAS. Nr.: 2417298-29-2

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Biologische Aktivität
- Beschreibung
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Cellular Effect

Cell Line	Type	Value	Description	References
CT26	IC₅₀	18.69 nM Compound: 17; FC116	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	[PMID: 37301075]
HCT-116	GI₅₀	0.079 μM Compound: 17; FC116	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	[PMID: 37301075]
HCT-116	IC₅₀	4.52 nM Compound: 17; FC116	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	[PMID: 37301075]

In Vitro

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 (K_d = 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.

Apoptosis Analysis^[1]

Cell Line:

HCT116 and CT26 cells
Concentration:

2.5, 5, 10, 20, 40 nM
Incubation Time:

24 h
Result:

Increased the apoptosis rate.
Up-regulated the expression of apoptosis-related protein Cleaved-Caspase 3.

Cell Cycle Analysis^[1]

Cell Line:

HCT116 and CT26 cells
Concentration:

2.5, 5, 10, 20, 40 nM
Incubation Time:

24 h
Result:

Blocked the cell cycle of HCT116 and CT26 cells in the G2/M phase.

Western Blot Analysis^[1]

Cell Line:

HCT116 and CT26 cells
Concentration:

2.5, 5, 10, 20, 40 nM
Incubation Time:

24 h
Result:

Increased phosphorylation of PERK, eIF2α, and IRE1α.

In Vivo

FC-116 (1.5-3 mg/kg, i.p., once daily, 21 days) exerts significant anti-tumor efficacy in HCT116 xenograft model^[1].
FC-116 (1.5-3 mg/kg, i.p., once daily, 45 days) shows potent inhibitory effect on intestinal tumorigenesis in C57BL/6-APC^min/+ mice^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

HCT116 cells (5 × 10⁶) were subcutaneously injected into the right flank of 5-week-old male BALB/c nude mice^[1].
Dosage:

1.5, 3 mg/kg
Administration:

i.p., once daily, 21 days
Result:

Achieved tumor growth inhibition.
Showed no significant changes in body weight.
Reduced the Ki67 expression.

Animal Model:

C57BL/6-APC^min/+ mice with a mutation (replacing amino acid L at position 850 of the Apc gene with a termination codon X) were used^[1].
Dosage:

1.5, 3 mg/kg
Administration:

i.p., once daily, 45 days
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

CAS. Nr. 2417298-29-2
Appearance Solid
Molecular Weight 369.39
Formel C₂₁H₂₀FNO₄
Color Off-white to light yellow
SMILES

COC1=C(OC)C(OC)=CC(C(/C(C)=C/C2=CNC3=C2C=CC(F)=C3)=O)=C1
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.7072 mL

13.5358 mL

27.0717 mL

5 mM

0.5414 mL

2.7072 mL

5.4143 mL

10 mM

0.2707 mL

1.3536 mL

2.7072 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Liu X, et al. Fluoroindole chalcone analogues targeting the colchicine binding site of tubulin for colorectal oncotherapy. Eur J Med Chem. 2023 Sep 5;257:115540. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

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FC-116

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

Metabolism/Protease Compound Library

NF-κB Signaling Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Endoplasmic Reticulum Stress Compound Library

Cytoskeleton Compound Library

Anti-Lung Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Protein-protein Interaction Inhibitor Library

Cell Death Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

High-Efficiency Gene Editing Compound Library

Lactylation Compound Library

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

FC-116

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

Metabolism/Protease Compound Library

NF-κB Signaling Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Endoplasmic Reticulum Stress Compound Library

Cytoskeleton Compound Library

Anti-Lung Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Protein-protein Interaction Inhibitor Library

Cell Death Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

High-Efficiency Gene Editing Compound Library

Lactylation Compound Library

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

FC-116 Related Classifications

HY-155068 Related Classifications