NPA101.3

NPA101.3 (0.632 nM-0.2 mM; 60 min) potently inhibits purified RET (IC₅₀ = 0.001 μM), RET^V804M (IC₅₀ = 0.008 μM), VEGFR2 (IC₅₀ = 0.003 μM), TRKA (IC₅₀ = 32 nM), and CSF1R (IC₅₀ = 46 nM) in a cell-free in vitro kinase assay^[1].
NPA101.3 (40 μM; 240 min) increases the thermal stability of purified wild type RET (ΔT_m = 16 °C) and RET^V804M mutant kinase domains to the same degree, confirming tight binding in a type 2 mode^[1].
NPA101.3 inhibits hERG channel conductibility with an IC₅₀ of 7.57 μM, showing minimal hERG activity relative to its RET inhibitory potency^[1].
NPA101.3 (0.1 nM-100 nM; 2 h) inhibits phosphorylation of RET^C634R, RET^M918T, RET^V804L, RET^V804M, and RET^A883F oncoproteins in RAT1 cells, with near-complete inhibition achieved at 3 nM for RET^C634R and 10 nM for the other mutants^[1].
NPA101.3 (1 nM-100 nM; 2 h) inhibits phosphorylation of rearranged CCDC6-RET, NCOA4-RET, and FGFR1OP-RET oncoproteins in NIH3T3 cells, with inhibition detectable at 1 nM^[1].
NPA101.3 (0.1 nM-100 nM; 2 h) inhibits ligand-induced VEGFR2 phosphorylation in HEK293 cells, with near-complete inhibition achieved at 10 nM^[1].
NPA101.3 inhibits RET autophosphorylation and downstream SHC/MAPK signaling in TT, MZ-CRC-1, and TPC-1 human cancer cells, and inhibits RET and SHC phosphorylation in Lc-2/ad cells, with no effect on RET-negative control cells^[1].
NPA101.3 potently inhibits proliferation of RET-positive TT, MZ-CRC-1, TPC-1, and Lc-2/ad human cancer cells (IC₅₀ = 0.67−3.6 nM) and has no effect on RET-negative human cancer cells at concentrations ≤100 nM^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.