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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- CAS No.: 2366216-76-2
- Formule: C37H39N7O
- Masse moléculaire:597.75
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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- Pureté et documentation
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Help & FAQs
Activité biologique
Description
IC50 & Target
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TrkA |
TrkB |
TrkC |
Cellular Effect
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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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Masse moléculaire 597.75
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Formule 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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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
JND4135 Related Classifications
HY-126287 Related Classifications
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