TRK/ALK-IN-1
TRK/ALK-IN-1 (compound 21) is a potent and dual inhibitor of TRK and ALK. TRK/ALK-IN-1 in the enzymatic assays is in good accordance with anti-proliferative activity with IC50 values of 2.2, 9.3 and 38 nM towards TRKA, ALKWT and ALKL1196M, respectively. TRK/ALK-IN-1 has the potential for the research of cancer diseases.
For research use only. We do not sell to patients.
- CAS No.: 3052405-64-5
- Formula: C31H35ClF2N8O2S
- Molecular Weight:657.18
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
IC50 & Target
|
TrkA |
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
>10 μM
Compound: 21
|
Antiproliferative activity against EGFR-positive human A549 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
Antiproliferative activity against EGFR-positive human A549 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
|
[PMID: 34534734] |
| KARPAS-299 | IC50 |
0.072 μM
Compound: 21
|
Antiproliferative activity against NPM-ALK addicted human KARPAS-299 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
Antiproliferative activity against NPM-ALK addicted human KARPAS-299 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
|
[PMID: 34534734] |
| KM12 | IC50 |
0.086 μM
Compound: 21
|
Antiproliferative activity against TPM3-NTRK1-addicted human KM12 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
Antiproliferative activity against TPM3-NTRK1-addicted human KM12 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
|
[PMID: 34534734] |
| NCI-H2228 | IC50 |
0.141 μM
Compound: 21
|
Antiproliferative activity against EML4-ALK addicted human H2228 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
Antiproliferative activity against EML4-ALK addicted human H2228 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
|
[PMID: 34534734] |
Chemical Information
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CAS No. 3052405-64-5
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Molecular Weight 657.18
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Formula C31H35ClF2N8O2S
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SMILES
CN1CCN(CC1)C2=CC=C(C=C2C(N3CCSCC3)=O)NC([C@@H]4CCCN4C5=NC(NC6=CC(F)=CC(F)=C6)=NC=C5Cl)=O
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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 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.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)