TDP1-IN-6
TDP1-IN-6 is a TDP1 inhibitor with an IC50 of 1.52 μM. Combination of TDP1-IN-6 with Topotecan (HY-13768) enhances DNA damage, induces Apoptosis, triggers S-phase cell cycle arrest, and promotes Ferroptosis. TDP1-IN-6 can be used for the research of cervical cancer.
For research use only. We do not sell to patients.
- Formula: C29H30N8O2
- Molecular Weight:522.60
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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
- Purity & Documentation
- References
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Biological Activity
TDP1-IN-6 (Compound 16b) potently inhibits purified TDP1 enzyme by stably binding to the catalytic domain and DNA-binding domain of the protein, with an IC50 of 1.52 μM[1].
TDP1-IN-6 inhibits the viability of HeLa cervical cancer cells with an IC50 of 14.85 μM; it exerts synergistic cytotoxic effects when combined with Topotecan[1].
TDP1-IN-6 (used at 2-4 μM in combination with 2 μM TPT) enhances Topotecan-induced apoptosis of HeLa cervical cancer cells in a dose-dependent manner by regulating apoptosis-related proteins, including downregulating BCL-2, upregulating BAX, and activating caspases[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HeLa cervical cancer cells
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Concentration:2-4 μM TDP1-IN-6; 2 μM TPT
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Incubation Time:72 h (wound healing)
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Result:Had no effect on colony formation, wound healing, or cell invasion when used alone.
Significantly reduced colony formation rates when combined with TPT: 0.50 for 2 μM TPT + 2 μM TDP1-IN-6; 0.33 for 2 μM TPT + 4 μM TDP1-IN-6.
Slowed wound healing when combined with TPT: 0.46 and 0.28 wound healing rates at 72 h for 2 μM TPT + 2 μM TDP1-IN-6 and 2 μM TPT + 4 μM TDP1-IN-6, respectively.
Reduced invasive cell counts by ~81.5% for 2 μM TPT + 4 μM TDP1-IN-6 compared to control when combined with TPT.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female nude mice (SPF grade)[1]
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Dosage:5 mg/kg (monotherapy; combination with TPT); 10 mg/kg (monotherapy; combination with TPT); 0.3 mg/kg (TPT, combination)
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Administration:i.p.; every 2 days
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Result:Did not significantly reduce tumor growth compared to control group (monotherapy at 5 mg/kg or 10 mg/kg).
Significantly inhibited tumor growth when combined with 0.3 mg/kg TPT, resulting in significantly lower tumor weights at study end point (5 mg/kg and 10 mg/kg).
Caused only slight decreases in mouse body weight (monotherapy).
Did not exacerbate body weight loss when coadministered with TPT.
Showed extensive necrotic areas and inflammatory cell infiltration in tumors from combination treatment groups.
Chemical Information
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Molecular Weight 522.60
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Formula C29H30N8O2
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SMILES
CC1=NC(N)=CC(N2CCN(CC2)CCOC(C3=CC4=C(N5CCC6=C(C5=N4)NC7=CC=CC=C76)C=C3)=O)=N1
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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.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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