Antiproliferative agent-53-d3
Antiproliferative agent-53-d3 (Compound C1) is an inhibitor for theta-mediated end joining (TMEJ) in HEK293 cell with an IC50 of 0.14 µM. Antiproliferative agent-53-d3 is the inhibitor for CYP2C19 and CYP2C9 with IC50 of 0.77 and 3.1 µM. Antiproliferative agent-53-d3 inhibits the proliferation of DNA repair-compromised cells, with IC50 of 8.1 µM for BRCA2-/- DLD-1. Antiproliferative agent-53-d3 exhibits good pharmacokinetic characteristics in CD-1 mice.
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- CAS No.: 2923508-77-2
- Formula: C20H14D3ClF4N4O2
- Molecular Weight:459.84
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
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CYP2C19 0.77 μM (IC50) |
CYP2C9 3.1 μM (IC50) |
CYP3A4 14.6 μM (IC50) |
CYP2D6 17.3 μM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| DLD-1 | IC50 |
8.1 μM
Compound: C1
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Antiproliferative activity against BRCA2 deficient human DLD-1 cells assessed as inhibition of cell growth incubated for 7 days by Cell-titer glo luminescence assay
Antiproliferative activity against BRCA2 deficient human DLD-1 cells assessed as inhibition of cell growth incubated for 7 days by Cell-titer glo luminescence assay
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[PMID: 38493730] |
Application
1. This compound can be used as a tracer
2. This compound can be used as an internal standard for quantitative analysis by NMR, GC-MS, or LC-MS.
Chemical Information
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CAS No. 2923508-77-2
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Molecular Weight 459.84
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Formula C20H14D3ClF4N4O2
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SMILES
[2H]C([2H])([2H])N(C1=CC(Cl)=C(C=C1)F)C([C@H]2N(C3=C(C(C(F)(F)F)=CC(C)=N3)C#N)C[C@H]2CO)=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)
Antiproliferative agent-53-d3 Related Classifications
HY-163816 Related Classifications
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