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.
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- CAS No.: 2918281-79-3
- 화학식: C29H31F3N6O4
- 분자량:584.59
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
IC50: 20.9 nM (wild-type RET) and 18.3 nM (RET-V804M)[1]
|
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 No. 2918281-79-3
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분자량 584.59
-
화학식 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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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)