TRK-IN-28
TRK-IN-28 (compound 30f) is a TRK inhibitor with the IC50 values of 0.55 nM, 25.1 nM and 5.4 nM against TRKWT, TRKG595R and TRKG667C, respectively. TRK-IN-2 shows antiproliferative activity with IC50 values of 9.5, 3.7, 205.0 and 48.3 nM against Ba/F3-ETV6-TRKAWT, Ba/F3-ETV6-TRKBWT, Ba/F3-LMNA-TRKG595R and Ba/F3-LMNA-TRKAG667C, respectively.
For research use only. We do not sell to patients.
- CAS No.: 2991504-43-7
- Formula: C27H25F2N7
- Molecular Weight:485.53
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| BaF3 | IC50 |
205 nM
Compound: 30f
|
Antiproliferative activity against mouse BaF3 cells harbouring LMNA-TRKA G595R mutant assessed as cell viability measured after 72 hrs by CCK-8 method
Antiproliferative activity against mouse BaF3 cells harbouring LMNA-TRKA G595R mutant assessed as cell viability measured after 72 hrs by CCK-8 method
|
[PMID: 38271867] |
| BaF3 | IC50 |
3.7 nM
Compound: 30f
|
Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKB wildtype assessed as cell viability measured after 72 hrs by CCK-8 method
Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKB wildtype assessed as cell viability measured after 72 hrs by CCK-8 method
|
[PMID: 38271867] |
| BaF3 | IC50 |
48.3 nM
Compound: 30f
|
Antiproliferative activity against mouse BaF3 cells harbouring LMNA-TRKA G667C mutant assessed as cell viability measured after 72 hrs by CCK-8 method
Antiproliferative activity against mouse BaF3 cells harbouring LMNA-TRKA G667C mutant assessed as cell viability measured after 72 hrs by CCK-8 method
|
[PMID: 38271867] |
| BaF3 | IC50 |
9.5 nM
Compound: 30f
|
Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKA wildtype assessed as cell viability measured after 72 hrs by CCK-8 method
Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKA wildtype assessed as cell viability measured after 72 hrs by CCK-8 method
|
[PMID: 38271867] |
Chemical Information
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CAS No. 2991504-43-7
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Molecular Weight 485.53
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Formula C27H25F2N7
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SMILES
FC1=CC(CC2=CC3=C(NN=C3NC4=C5C=CC(N6CCN(CC6)C)=CC5=NC=N4)C=C2)=CC(F)=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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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.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)