JND4135 is a Type II TRK inhibitor that effectively targets TRKA, TRKB, and TRKC with IC50 values of 2.79, 3.19, and 3.01 nM, respectively. This compound is capable of overcoming resistance associated with TRK xDFG and other mutant forms, inhibiting the phosphorylation of both wild-type and mutant TRKs, as well as their downstream signaling pathways. JND4135 induces G0/G1 phase cell cycle arrest and apoptosis in BaF3–CD74-TRKA-G667C cells and exhibits potent antitumor activity in a BaF3-CD74-TRKA-G667C mouse xenograft model, highlighting its potential for cancer research and therapy.
JND4135 is a Type II TRK inhibitor that effectively targets TRKA, TRKB, and TRKC with IC50 values of 2.79, 3.19, and 3.01 nM, respectively. This compound is capable of overcoming resistance associated with TRK xDFG and other mutant forms, inhibiting the phosphorylation of both wild-type and mutant TRKs, as well as their downstream signaling pathways. JND4135 induces G0/G1 phase cell cycle arrest and apoptosis in BaF3–CD74-TRKA-G667C cells and exhibits potent antitumor activity in a BaF3-CD74-TRKA-G667C mouse xenograft model, highlighting its potential for cancer research and therapy.
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