Table 2. Thermodynamic parameters extracted from the calorimetric evaluation of unphosphorylated Δ574–580, Δ559, and T670I mutant KITs titrated Imatinib.
KIT mutant | ΔGbind,ITC (kcal/mol) | ΔHbind,ITC (kcal/mol) | -TΔSbind,ITC (kcal/mol) | Kd,ITC (nM) | n |
---|---|---|---|---|---|
Δ574−580 | −8.80 | −10.73 | 1.93 | 359 | 1.12 |
Δ559 | −9.41 | −11.67 | 2.26 | 127 | 1.09 |
T670I | −6.18 | −7.25 | 1.07 | 29450 | 0.96 |
Experiments were performed in triplicate at 25°C. Standard deviation values are within 1–3% for ΔHbind,ITC, 3–5% for Kd,ITC, and 1–2% for n