TOP1/TDP1-IN-1
TOP1/TDP1-IN-1 is a DNA topoisomerase 1B (TOP1) and tyrosyl-DNA phosphodiesterase 1 (TDP1) inhibitor with a TDP1 IC50 of 17.8 μM. TOP1/TDP1-IN-1directly suppresses TOP1 catalytic activity without forming a DNA-TOP1 ternary complex, inhibits TDP1-mediated repair of TOP1-induced DNA damage, and exhibits low acute toxicity. TOP1/TDP1-IN-1 disrupts DNA repair pathways, induces apoptosis, suppresses clonogenic growth, and elicits antiproliferative effects in cancer cells. TOP1/TDP1-IN-1 can be used for the research of non-small cell lung cancer, cervical cancer, colon cancer.
For research use only. We do not sell to patients.
- CAS No.: 3110679-68-7
- Formula: C22H24N2O5
- Molecular Weight:396.44
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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Top1 |
Tyrosyl-DNA phosphodiesterase 1 (TDP1) 17.8 μM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| HCT-116 | GI50 |
0.31 μM
Compound: B11
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Cytotoxicity against human HCT-116 cells assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay
Cytotoxicity against human HCT-116 cells assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay
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[PMID: 40120150] |
TOP1/TDP1-IN-1 (C13) (6.25-100 μM; 30 min) strongly inhibits calf thymus TOP1 enzyme activity in a concentration-dependent manner, with greater potency than 50 μM CPT[1].
TOP1/TDP1-IN-1 (30 min) inhibits purified TDP1 enzyme activity with an IC50 of 17.8 μM[1].
TOP1/TDP1-IN-1 (48 h) potently inhibits the proliferation of A549, HeLa, and HCT116 cancer cells with IC50 values of 0.89 μM, 1.2 μM, and 1.1 μM, respectively[1].
TOP1/TDP1-IN-1 (0.125-0.5 μM; 48 h treatment, followed by 10 days of growth) effectively impairs the clonogenic survival of A549 cells in a concentration-dependent manner[1].
TOP1/TDP1-IN-1 (0.5-2 μM; 12, 24, 36 h post-treatment) effectively inhibits the migration of A549 cells in a concentration-dependent manner[1].
TOP1/TDP1-IN-1 (1-2 μM; 3 h) induces marked DNA damage in A549 cells, as measured by γ-H2AX foci formation, at 1 μM and 2 μM[1].
TOP1/TDP1-IN-1 (1-4 μM; 48 h) induces apoptosis in A549 cells in vitro in a concentration-dependent manner[1].
TOP1/TDP1-IN-1 (1 μM; 48 h) synergizes with Topotecan (HY-13768A) to inhibit A549 cell proliferation[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:A549
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Concentration:0.5, 1, 2 μM
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Incubation Time:12, 24, 36 h post-treatment
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Result:Significantly impaired wound healing; at 2 μM, the healing rate decreased to 18% after 36 h compared to 64% in untreated cells.
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Cell Line:A549
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Concentration:1, 2 μM
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Incubation Time:3 h
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Result:Produced a significantly intense γ-H2AX response; at 2 μM, the number of γ-H2AX foci was superior to that induced by 0.5 μM Topotecan (TPT).
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Cell Line:A549
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Concentration:1, 2, 4 μM
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Incubation Time:48 h
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Result:Induced apoptosis in a concentration-dependent manner; increasing concentrations from 1 μM to 4 μM resulted in an increase in apoptosis from 5.9% to 12.6%.
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Cell Line:A549
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Concentration:1 μM
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Incubation Time:48 h
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Result:Showed dose-dependent enhancement of Topotecan cytotoxicity.
TOP1/TDP1-IN-1 (123-300 mg/kg; i.p.; single dose) shows complete survival in Kunming mice at doses ≤154 mg/kg and 100% mortality at 192 mg/kg and above in a single-dose acute toxicity study[1].
TOP1/TDP1-IN-1 (4 mg/kg (i.v.); 20 mg/kg (i.g.); single dose) displays favorable pharmacokinetic properties in Sprague-Dawley rats with high oral bioavailability (91.3%) and prolonged systemic exposure[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Athymic nude mice (nu/nu genotype, male) bearing LLC cells[1]
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Dosage:20, 40, 80 mg/kg
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Administration:i.p.; daily
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Result:Elicited significant dose-dependent tumor growth inhibition; at 20 mg/kg, resulted in significantly less body weight loss.
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Animal Model:Kunming (male)[1]
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Dosage:123, 154, 192, 240, 300 mg/kg
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Administration:i.p.; single dose
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Result:Observed complete survival at doses ≤154 mg/kg during the 7-day observation period; 100% mortality occurred within 3 days at 192 mg/kg and within 2 days at 240 mg/kg.
Chemical Information
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CAS No. 3110679-68-7
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Molecular Weight 396.44
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Formula C22H24N2O5
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SMILES
COC1=C(C=C2C(C(OCCN3CCCC3)=NC4=C2C=CC5=C4OCO5)=C1)OC
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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)
TOP1/TDP1-IN-1 Related Classifications
HY-181080 Related Classifications
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