2. Cytoskeleton Cell Cycle/DNA Damage Immunology/Inflammation NF-κB Metabolic Enzyme/Protease Apoptosis
  3. Microtubule/Tubulin Reactive Oxygen Species (ROS) Apoptosis PERK Eukaryotic Initiation Factor (eIF) IRE1
  4. FC-116

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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FC-116

FC-116 Chemical Structure

CAS No. : 2417298-29-2

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
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Based on 1 publication(s) in Google Scholar

FC-116 Related Antibodies

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Description

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[1].

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 (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.

FC-116 Related Antibodies

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-APCmin/+ 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-APCmin/+ 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.
Molecular Weight

369.39

Formula

C21H20FNO4
CAS No.
Appearance

Solid

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.7072 mL 13.5358 mL 27.0717 mL
5 mM 0.5414 mL 2.7072 mL 5.4143 mL
View the 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.

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Purity & Documentation
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
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FC-116 Related Classifications

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

FC-1162417298-29-2FC116FC 116Microtubule/TubulinReactive Oxygen Species (ROS)ApoptosisPERKEukaryotic Initiation Factor (eIF)IRE1Protein kinase R-like endoplasmic reticulum kinasePKR-like endoplasmic reticulum kinaseInositol requiring enzyme 1apoptosisROSCRCcancercolorectal cancerInhibitorinhibitorinhibit

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