TRK-IN-12
TRK-IN-12 (Compound 9e) is a potent inhibitor of TRK (TRKG595R IC50 = 13.1 nM). TRK-IN-12 is a macrocyclic derivative compound. TRK-IN-12 shows significant antiproliferative activity in the Ba/F3-LMNA-NTRK1 cell line (IC50 = 0.080 μM). TRK-IN-12 has shown a better inhibitory effect (IC50 = 0.646 μM) than control agent LOXO-101 in Ba/F3-LMNA-NTRK1-G595R cell line.
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- CAS. Nr.: 2823342-34-1
- Formel: C18H19ClFN5O3S
- Molecular Weight:439.89
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
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Biologische Aktivität
Beschreibung
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| BaF3 | IC50 |
0.08 μM
Compound: 9e
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Antiproliferative activity against mouse BaF3 cells harboring LMNA fused NTRKA1
Antiproliferative activity against mouse BaF3 cells harboring LMNA fused NTRKA1
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[PMID: 34628036] |
| BaF3 | IC50 |
0.646 μM
Compound: 9e
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Antiproliferative activity against mouse BaF3 cells harboring LMNA fused NTRKA1 G595R mutant
Antiproliferative activity against mouse BaF3 cells harboring LMNA fused NTRKA1 G595R mutant
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[PMID: 34628036] |
Chemical Information
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CAS. Nr. 2823342-34-1
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Molecular Weight 439.89
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Formel C18H19ClFN5O3S
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SMILES
CN1CC2=CC(F)=CC=C2OCCN(CC3=C4N=C1C=CN4N=C3)S(=O)(CCl)=O
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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.
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Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
TRK-IN-12 Related Classifications
HY-144451 Related Classifications
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