RET-IN-22
RET-IN-22 (compound 17b) is a potent, selective and orally active RET inhibitor with an IC50 of 20.9 nM and 18.3 nM for wild-type RET and RET-V804M, respectively. RET-IN-22 shows highly selective profile to most kinases, especially to EGFR and VEGFR2. RET-IN-22 has anticancer effects.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
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: 2918281-79-3
- 分子式: C29H31F3N6O4
- 分子量:584.59
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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
IC50: 20.9 nM (wild-type RET) and 18.3 nM (RET-V804M)[1]
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Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| BaF3 | IC50 |
12.1 nM
Compound: 17b
|
Antiproliferative activity against mouse BaF3 cells expressing CCDC6-RET-V804M incubated for 72 hrs by CCK8 assay
Antiproliferative activity against mouse BaF3 cells expressing CCDC6-RET-V804M incubated for 72 hrs by CCK8 assay
|
[PMID: 36905915] |
| BaF3 | IC50 |
13.6 nM
Compound: 17b
|
Antiproliferative activity against mouse BaF3 cells expressing CCDC6-RET incubated for 72 hrs by CCK8 assay
Antiproliferative activity against mouse BaF3 cells expressing CCDC6-RET incubated for 72 hrs by CCK8 assay
|
[PMID: 36905915] |
| BaF3 | IC50 |
3870 nM
Compound: 17b
|
Antiproliferative activity against mouse BaF3 cells incubated for 72 hrs by CCK8 assay
Antiproliferative activity against mouse BaF3 cells incubated for 72 hrs by CCK8 assay
|
[PMID: 36905915] |
| BaF3 | IC50 |
401 nM
Compound: 17b
|
Antiproliferative activity against mouse BaF3 cells expressing CCDC6-RET-G810R incubated for 72 hrs by CCK8 assay
Antiproliferative activity against mouse BaF3 cells expressing CCDC6-RET-G810R incubated for 72 hrs by CCK8 assay
|
[PMID: 36905915] |
| BaF3 | IC50 |
84.6 nM
Compound: 17b
|
Antiproliferative activity against mouse BaF3 cells expressing CCDC6-RET-G810C incubated for 72 hrs by CCK8 assay
Antiproliferative activity against mouse BaF3 cells expressing CCDC6-RET-G810C incubated for 72 hrs by CCK8 assay
|
[PMID: 36905915] |
化学情報
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CAS 番号 2918281-79-3
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分子量 584.59
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分子式 C29H31F3N6O4
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SMILES
O=C(NC1=CC=C(C2=NNC(C3=CC=C(OCCN4CCOCC4)C=C3)=C2)C=C1)NC5=NOC(C(C)(C(F)(F)F)C)=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)