2. Cell Cycle/DNA Damage Apoptosis
  3. Topoisomerase DNA/RNA Synthesis Apoptosis
  4. 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.

TOP1/TDP1-IN-1

TOP1/TDP1-IN-1 Chemical Structure

CAS No. : 3110679-68-7

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TOP1/TDP1-IN-1 Related Antibodies

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Description

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[1].

IC50 & Target[1]

Top1

 

Tyrosyl-DNA phosphodiesterase 1 (TDP1)

17.8 μM (IC50)

In Vitro

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.

TOP1/TDP1-IN-1 Related Antibodies

Cell Migration Assay[1]

Cell Line: A549
Concentration: 0.5, 1, 2 μM
Incubation Time: 12, 24, 36 h post-treatment
Result: Significantly impaired wound healing; at 2 μM, the healing rate decreased to 18% after 36 h compared to 64% in untreated cells.

Immunofluorescence[1]

Cell Line: A549
Concentration: 1, 2 μM
Incubation Time: 3 h
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).

Apoptosis Analysis[1]

Cell Line: A549
Concentration: 1, 2, 4 μM
Incubation Time: 48 h
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%.

Cell Proliferation Assay[1]

Cell Line: A549
Concentration: 1 μM
Incubation Time: 48 h
Result: Showed dose-dependent enhancement of Topotecan cytotoxicity.
Parmacokinetics
Species Dose Route T1/2 Tmax Cmax AUC0-t AUC0-∞ MRT0-∞ Bioavailability
Rat[1] 4 mg/kg i.v. 4.78 h 0.08 h 241.33 ng/mL 600 ng·h/mL 710 ng·h/mL 5.62 h /
Rat[1] 20 mg/kg i.g. 5.97 h 6.67 h 203 ng/mL 3009 ng·h/mL 3293 ng·h/mL 10.8 h 91.3 %
In Vivo

TOP1/TDP1-IN-1 (C13) (20-80 mg/kg; i.p.; daily; for 8 days) exhibits dose-dependent in vivo antitumor efficacy in a Lewis lung carcinoma xenograft model with favorable tolerability at 20 mg/kg[1].
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.

Animal Model: Athymic nude mice (nu/nu genotype, male) bearing LLC cells[1]
Dosage: 20, 40, 80 mg/kg
Administration: i.p.; daily
Result: Elicited significant dose-dependent tumor growth inhibition; at 20 mg/kg, resulted in significantly less body weight loss.
Animal Model: Kunming (male)[1]
Dosage: 123, 154, 192, 240, 300 mg/kg
Administration: i.p.; single dose
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.
Molecular Weight

396.44

Formula

C22H24N2O5
CAS No.
SMILES

COC1=C(C=C2C(C(OCCN3CCCC3)=NC4=C2C=CC5=C4OCO5)=C1)OC
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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TOP1/TDP1-IN-1 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

TOP1/TDP1-IN-13110679-68-7TopoisomeraseDNA/RNA SynthesisApoptosisKunming micecalf thymus TOP1HeLa cellsA549 cellsLewis lung carcinoma xenograft modelapoptosiscancer cellstyrosyl-DNA phosphodiesterase 1HCT116 cellsDNA topoisomerase 1BInhibitorinhibitorinhibit

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