In a 72-h MTT assay, dovitinib IC50 values were 130 nM in LoVo and 2530 nM in HT-29 cells. These model-specific results do not establish KRAS/BRAF mutation class as a response predictor. [2]
Dovitinib also increased G2/M DNA-content accumulation in nasopharyngeal carcinoma cell lines after 48 h at micromolar concentrations. The authors did not authenticate these cell lines. [3]
FGFR1-fusion target engagement
Cell-based study · CUX1-FGFR1-expressing Ba/F3 cells [1]
TKI258 reduced fusion-FGFR1 phosphorylation; total proteins and alpha-tubulin were controls.
Literature-Reported Treatment Conditions
- Treatment concentration
- 0, 50, 100, 500, 1000, 5000 nM
- Exposure duration
- 90 min
- Method
- Immunoblot
- Vehicle
- DMSO stock; final vehicle fraction unspecified
- Reported limits
- Tested salt form and equivalence to catalog free base were not established; no dose conversion applied.
Methods and source locations
Compound reported in the paper: Dovitinib; Compound label in the paper: TKI258
Compound-level findings in the stated models; preparation-specific results do not validate an Adooq lot or salt equivalence.
Figure 2C; Western Blotting; Results and Discussion
Fusion-FGFR1 phosphorylation: Immunoblot with total FGFR1 and alpha-tubulin controls — Figure 2C; Results and Discussion
STAT5 and RPS6K phosphorylation: Phospho/total immunoblot comparison — Figure 2C; Results and Discussion
FGFR1-fusion growth inhibition with IL-3 rescue
Cell-based study · CUX1-FGFR1-expressing Ba/F3 cells, with or without IL-3 [1]
IL-3 rescued TKI258 growth inhibition; PKC412 did not show the same rescue. This supports FGFR1-dependent activity within this model.
Literature-Reported Treatment Conditions
- Treatment concentration
- Dose-response series (Figure 2B)
- Exposure duration
- 48 h
- Method
- CellTiter AQueous One Solution assay
- Vehicle
- DMSO stock; final vehicle fraction unspecified
- Reported limits
- Tested salt form and equivalence to catalog free base were not established; no dose conversion applied.
Methods and source locations
Compound reported in the paper: Dovitinib; Compound label in the paper: TKI258
Compound-level findings in the stated models; preparation-specific results do not validate an Adooq lot or salt equivalence.
Figure 2B; Cell culture; Results and Discussion
Growth without IL-3: Two experiments in triplicate; bars SD — Figure 2B; Results and Discussion
Growth with IL-3 (2 ng/mL): Figure label; two experiments in triplicate; bars SD — Figure 2B and caption
Differential colorectal cell viability response
Cell-based study · LoVo and HT-29 colorectal cancer cells [2]
LoVo was more sensitive than HT-29 in the 72-h MTT assay. The broader panel did not establish mutation class as a predictor.
Literature-Reported Treatment Conditions
- Treatment concentration
- Serial dilutions; Figure 4A: 0–10000 nM
- Exposure duration
- 72 h
- Method
- MTT assay
- Vehicle
- Assay control at 0 drug; drug vehicle unspecified
- Reported limits
- Tested salt form and equivalence to catalog free base were not established; no dose conversion applied.
Methods and source locations
Compound reported in the paper: Dovitinib; Compound label in the paper: TKI258
Compound-level findings in the stated models; preparation-specific results do not validate an Adooq lot or salt equivalence.
Figures 2A and 4A; Cell-viability assay
LoVo viability: MTT; CalcuSyn interpolation — Figure 2A table; Figure 4A caption
HT-29 viability: MTT; CalcuSyn interpolation — Figure 2A table; Figure 4A caption
Nasopharyngeal carcinoma cell-cycle response
Cell-based study · HONE1, HNE1, CNE2 and C666-1 cells [3]
Micromolar dovitinib increased 4N DNA-content accumulation. This endpoint alone does not distinguish G2 arrest from mitotic delay or slippage.
Literature-Reported Treatment Conditions
- Treatment concentration
- 0.1, 1, 2.5, 5, 10 μM; control
- Exposure duration
- 48 h
- Method
- Propidium-iodide flow cytometry; trypan-blue counts
- Vehicle
- Control shown; vehicle not specified
- Reported limits
- Tested salt form and equivalence to catalog free base were not established; no dose conversion applied.
Methods and source locations
Compound reported in the paper: Dovitinib; Compound label in the paper: TKI258
Compound-level findings in the stated models; preparation-specific results do not validate an Adooq lot or salt equivalence.
Figure 1A-C and caption; Experimental procedures
4N DNA-content accumulation: Flow cytometry; percentage not inferred — Figure 1A and Results
HONE1 and C666-1 viable cell number: Trypan-blue exclusion; mean ± SD, three independent experiments — Figure 1B and caption
