Target intelligence / Profile preview

HCT116 colorectal carcinoma cell line (HCT116)

Target
HCT116
Molecular classification
Cell line, Colorectal cancer model
01

Overview

HCT116 is a human colorectal carcinoma cell line widely utilized in biomedical research and drug discovery as a model for colon cancer (ATCC, 2023). Derived from an adult male patient, these cells exhibit an epithelial morphology and are characterized by rapid proliferation and the ability to form tumors in xenograft models (PubMed: 6248960). Genetically, HCT116 is notable for being microsatellite unstable (MSI) due to a deficiency in the MLH1 mismatch repair gene and for harboring oncogenic mutations in KRAS and PIK3CA (NCBI: PMC2824443). In pharmacological contexts, HCT116 proliferation refers to a phenotypic assay used to evaluate the anti-tumor efficacy of small molecules or biologics. Because it represents a complex cellular system rather than a single protein or receptor, it is classified as a biological assay readout rather than a discrete therapeutic target (Nature Communications, 2019).

Other names
HCT-116HCT 116Human colorectal carcinoma cell line HCT116
02

Mechanism of action

Compounds tested against HCT116 proliferation typically act by inducing DNA damage, inhibiting DNA synthesis, or disrupting oncogenic signaling pathways such as the MAPK or PI3K/AKT pathways (PubMed: 25639211).

03

Biological functions

Cell proliferationApoptosisTumorigenesisDNA mismatch repair
04

Disease associations

Colorectal cancer
05

Safety considerations

Lack of selectivity for cancerous vs. healthy cellsPotential for systemic toxicity in vivoAssay results may not fully translate to complex human tumor microenvironments
06

Interacting drugs

5-Fluorouracil

4 more in the full profile.

07

Biomarkers

Microsatellite instability (MSI-H)KRAS mutation (G13D)PIK3CA mutation (H1047R)MLH1 deficiency

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