TABLE 1C

pSMAD2 inhibition in tumor cell line and in cross-species immune cells

Cell LineIC50 (Total Drug, nM)IC50 (Unbound Drug, nM)c
MDA-MB-23146.09 ± 2.0517.28 ± 0.77
SpeciesIC50 (Total Drug, nM)IC50 (Unbound Drug, nM)c
Humana151.4 ± 20.6256.78 ± 7.73
Cynomolgus monkeya68.30 ± 3.1825.61 ± 1.19
Ratb101.65 ± 38.2138.12 ± 14.33
Mouseb42.91 ± 15.1016.09 ± 5.66

  • ↵a pSMAD2 inhibition in hTGFβ1 stimulated human or cynomolgus monkey PBMCs.

  • ↵b pSMAD2 inhibition in mTGFβ1 stimulated mouse splenocytes; unbound IC50 (IC50u) concentrations were calculated using the formula: IC50 = IC50 × fu media, where fu media for PF-06952229 is 0.375.