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.
For research use only. We do not sell to patients.
- CAS No.: 2366216-76-2
- Formula: C37H39N7O
- Molecular Weight:597.75
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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TrkA |
TrkB |
TrkC |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| SH-SY5Y | IC50 |
58 nM
Compound: 9o
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Antiproliferative activity against human SH-SY5Y cells transfected with TrkB (unknown origin) assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay
Antiproliferative activity against human SH-SY5Y cells transfected with TrkB (unknown origin) assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay
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[PMID: 31271959] |
Chemical Information
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CAS No. 2366216-76-2
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Molecular Weight 597.75
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Formula C37H39N7O
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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
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Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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