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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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 2366216-76-2
- 分子式: C37H39N7O
- 分子量:597.75
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
製品説明
IC50 & Target
|
TrkA |
TrkB |
TrkC |
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| SH-SY5Y | IC50 |
58 nM
Compound: 9o
|
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
|
[PMID: 31271959] |
化学情報
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CAS 番号 2366216-76-2
-
分子量 597.75
-
分子式 C37H39N7O
-
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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輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)