2366216-76-2
Chemical Structure
JND4135
- CAS No.: 2366216-76-2
- Formula:C37H39N7O
- Molecular Weight:597.75
IUPAC Name: 3-((6-(4-aminophenyl)imidazo[1,2-a]pyrazin-3-yl)ethynyl)-N-(3-isopropyl-5-((4-methylpiperazin-1-yl)methyl)phenyl)-2-methylbenzamide
InChIKey: KDFREDAEEQQCFD-UHFFFAOYSA-N
SMILES: CC1=C(C(NC2=CC(CN3CCN(C)CC3)=CC(C(C)C)=C2)=O)C=CC=C1C#CC4=CN=C5N4C=C(C6=CC=C(N)C=C6)N=C5
Biological Activity:
JND4135 is a Type II TRK inhibitor with IC50 values of 2.79, 3.19, and 3.01 nM against TRKA, TRKB, TRKC, respectively. JND4135 can overcome resistance from TRK xDFG and other mutant forms in the BaF3 stable model, inhibiting phosphorylation of both WT and xDFG mutant TRKs, along with their downstream signaling molecules. JND4135 can induce G0/G1 phase arrest and apoptosis in BaF3–CD74-TRKA-G667C cells. JND4135 shows tumor growth inhibition activity in the BaF3-CD74-TRKA-G667C mouse xenograft model[1].
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JND4135 | JND4135 is a Type II TRK inhibitor with IC50 values of 2.79, 3.19, and 3.01 nM against TRKA, TRKB, TRKC, respectively. JND4135 can overcome resistance from TRK xDFG and other mutant forms in the BaF3 stable model, inhibiting phosphorylation of both WT and xDFG mutant TRKs, along with their downstream signaling molecules. JND4135 can induce G0/G1 phase arrest and apoptosis in BaF3–CD74-TRKA-G667C cells. JND4135 shows tumor growth inhibition activity in the BaF3-CD74-TRKA-G667C mouse xenograft model. |
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Keywords
