JND4135
Product Specifications
CAS Number
2366216-76-2
Target
Trk receptor, Apoptosis
Related Pathways
Apoptosis, Tyrosine Kinase/Adaptors
Bioactivity
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.
Smiles
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
Molecular Formula
C37H39N7O
Molecular Weight
597.75
Shipping Conditions
Ice Packs
Storage Temperature
-20°C
Available Sizes
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