Elzovantinib (TPX-0022, CSF1R-IN-2) is a potent inhibitor of MET/CSF1R/SRC with biochemical IC50 of 0.14, 0.76 and 0.12 nM, respectively. Elzovantinib (TPX-0022) inhibited both autophosphorylation of CSF1R with an IC50 <3 nM and cell growth with an IC50 of 14 nM in Ba/F3 ETV6-CSF1R cell model. TPX-0022 effectively inhibited the growth of Ba/F3 ETV6-CSF1R xenograft tumors in vivo. TPX-0022 not only exhibited potency with an IC50 of 0.3 nM, but also potently inhibited the growth of M-NFS-60 cells with an IC50 of 11.6 nM in the presence of exogenous CSF1 at 1 ng/mL in CSF1/CSF1R signaling-dependent M-NFS-60 model. TPX-0022 effectively reduced tumor associated macrophages (TAMs), altered the polarity of TAMs toward a more M1 phenotype, increased cytotoxic T cells and inhibited the growth of MC38 tumors in MC38 syngeneic mouse model.
Physicochemical Properties
M.Wt
409.42
Formula
C20H20FN7O2
Appearance
Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Month
Shipping
Solubility
Chemical Name/SMILES
References
1. Vikas K. Goel, et al. Cancer Res (2021) 81 (13_Supplement): 1444.
2. Wei Deng, et al. Cancer Res (2019) 79 (13_Supplement): 1325.
