JND4135 - CAS 2366216-76-2

JND4135, a type II TRK inhibitor, exhibits IC50 values targeting TRKA, TRKB, and TRKC at 2.79, 3.19, and 3.01 nM, respectively. It can overcome resistance due to TRKxDFG and other mutations in the BaF3 stable model, inhibiting the phosphorylation of TRKs WT, xDFG mutations, and their downstream signaling molecules. Additionally, JND4135 induces G0/G1 phase arrest and cell apoptosis (apoptosis) in BaF3–CD74-TRKA-G667C cells. This compound also demonstrates antitumor activity in a BaF3-CD74-TRKA-G667C mouse xenograft model by suppressing tumor growth.

Trk receptor, Apoptosis

Apoptosis, Tyrosine Kinase/Adaptors

2366138

C37H39N7O

597.75

O=C(NC=1C=C(C=C(C1)C(C)C)CN2CCN(C)CC2)C=3C=CC=C(C#CC4=CN=C5C=NC(=CN45)C=6C=CC(N)=CC6)C3C

-20°C

Ice Packs

Small Compound