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.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- CAS. Nr.: 2918281-79-3
- Formel: C29H31F3N6O4
- Molecular Weight:584.59
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biologische Aktivität
Beschreibung
IC50 & Target
IC50: 20.9 nM (wild-type RET) and 18.3 nM (RET-V804M)[1]
Cellular Effect
|
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] |
Chemical Information
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CAS. Nr. 2918281-79-3
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Molecular Weight 584.59
-
Formel 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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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Protokoll
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)