Anticancer agent 333
Anticancer agent 333 is a tetrazinone anticancer agent with broad-spectrum anticancer activity, targeting MGMT/AGT-deficient cancer cells (IC50≤20 μM). Anticancer agent 333 exhibits favorable safety profiles in rat and canine animal models. Anticancer agent 333 can be used for the research of MGMT-deficient cancers and related tumors.
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- CAS. Nr.: 3075414-82-0
- Formel: C8H7F3N6O3
- Molecular Weight:292.17
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
MGMT |
In Vitro
Anticancer agent 333 (I-1) weakly inhibits viability of MGMT positive / MMR positive and MGMT positive / MMR negative LN229 glioblastoma cells, with an IC50 greater than 100 μM for both cell lines[1].
Anticancer agent 333 (I-1) exhibits broad anti-cancer activity across diverse human cancer cell lines, with the highest potency (EC50/IC50 ≤ 30 μM) in most lymphoma, small cell lung carcinoma, colon carcinoma, melanoma, and glioblastoma cell lines tested[1].
Anticancer agent 333 (I-1) (66.7 μM; 5 days) exhibits lineage-dependent anti-cancer activity across 885 human cancer cell lines, with the most potent effects (Log2 fold change -3.5 to -2.0) observed in a subset of tested cell lines when treated at 66.7 μM for 5 days[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:885 barcoded human cancer cell lines across over 45 lineages
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Concentration:66.7 μM; 8-point 3-fold dilution dose range
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Incubation Time:5 days
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Result:Caused log2 fold change -3.5 to -2.0 (highly significant anti-cancer effect) in a subset of cell lines.
Caused log2 fold change >-2.0 to -1.0 (significant anti-cancer effect) in a subset of cell lines.
Caused log2 fold change >-1.0 to -0.5 (moderate anti-cancer effect) in a subset of cell lines including KYSE510, LS180, HOS, ASPC1, and others.
Caused log2 fold change >-0.5 to -0.001 (weak anti-cancer effect) in a subset of cell lines including RD, NCI-H1563, MONOMAC6, and others.
Showed no detectable anti-cancer effect in a subset of cell lines.
Chemical Information
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CAS. Nr. 3075414-82-0
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Molecular Weight 292.17
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Formel C8H7F3N6O3
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SMILES
O=C(C(N=CN12)=C2N=NN(CCOC(F)(F)F)C1=O)N
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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.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Anticancer agent 333 Related Classifications
HY-186228 Related Classifications
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Keywords
- Anticancer agent 333
- 3075414-82-0
- Anticancer agent333
- Anticancer agent-333
- DNA Methyltransferase
- dogs
- MGMT-deficient cancer cells
- MGMT-negative/MMR-negative glioblastoma cells
- colon cancer
- MGMT-proficient cancer cells
- lung cancer
- rats
- head and neck squamous cell carcinoma
- glioma
- MGMT-negative/MMR-positive glioblastoma cells
- Inhibitor
- inhibitor
- inhibit