1. Cell Cycle/DNA Damage
  2. Topoisomerase
  3. Top1/2-IN-1

Top1/2-IN-1 (compound 23) is an orally available dual inhibitor of Top1/2 with antiproliferative activity. Top1/2-IN-1 damages DNA with increased levels of reactive oxygen species, inducing apoptosis and cell cycle arrest in cancer cells. Top1/2-IN-1 exhibits in vivo antitumor activity in xenograft models.

For research use only. We do not sell to patients.

Top1/2-IN-1

Top1/2-IN-1 Chemical Structure

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Description

Top1/2-IN-1 (compound 23) is an orally available dual inhibitor of Top1/2 with antiproliferative activity. Top1/2-IN-1 damages DNA with increased levels of reactive oxygen species, inducing apoptosis and cell cycle arrest in cancer cells. Top1/2-IN-1 exhibits in vivo antitumor activity in xenograft models[1].

IC50 & Target

Top1/2[1]

Cellular Effect
Cell Line Type Value Description References
A549 IC50
1.1 μM
Compound: 23
Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 96 hrs by MTT based ELISA
Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 96 hrs by MTT based ELISA
[PMID: 39106476]
BEAS-2B IC50
9.57 μM
Compound: 23
Antiproliferative activity against human BEAS-2B cells assessed as inhibition of cell growth incubated for 96 hrs by MTT based ELISA
Antiproliferative activity against human BEAS-2B cells assessed as inhibition of cell growth incubated for 96 hrs by MTT based ELISA
[PMID: 39106476]
DU-145 IC50
0.52 μM
Compound: 23
Antiproliferative activity against human DU-145 cells assessed as inhibition of cell growth incubated for 96 hrs by MTT based ELISA
Antiproliferative activity against human DU-145 cells assessed as inhibition of cell growth incubated for 96 hrs by MTT based ELISA
[PMID: 39106476]
HCT-116 IC50
0.21 μM
Compound: 23
Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth incubated for 96 hrs by MTT based ELISA
Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth incubated for 96 hrs by MTT based ELISA
[PMID: 39106476]
Huh-7 IC50
0.83 μM
Compound: 23
Antiproliferative activity against human Huh-7 cells assessed as inhibition of cell growth incubated for 96 hrs by MTT based ELISA
Antiproliferative activity against human Huh-7 cells assessed as inhibition of cell growth incubated for 96 hrs by MTT based ELISA
[PMID: 39106476]
MCF7 IC50
0.35 μM
Compound: 23
Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 96 hrs by MTT based ELISA
Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 96 hrs by MTT based ELISA
[PMID: 39106476]
MDA-MB-231 IC50
0.29 μM
Compound: 23
Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 96 hrs by MTT based ELISA
Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 96 hrs by MTT based ELISA
[PMID: 39106476]
NCI-H1650 IC50
0.88 μM
Compound: 23
Antiproliferative activity against human NCI-H1650 cells assessed as inhibition of cell growth incubated for 96 hrs by MTT based ELISA
Antiproliferative activity against human NCI-H1650 cells assessed as inhibition of cell growth incubated for 96 hrs by MTT based ELISA
[PMID: 39106476]
NCI-H1975 IC50
0.74 μM
Compound: 23
Antiproliferative activity against human NCI-H1975 cells assessed as inhibition of cell growth incubated for 96 hrs by MTT based ELISA
Antiproliferative activity against human NCI-H1975 cells assessed as inhibition of cell growth incubated for 96 hrs by MTT based ELISA
[PMID: 39106476]
NCI-H2228 IC50
0.88 μM
Compound: 23
Antiproliferative activity against human NCI-H2228 cells assessed as inhibition of cell growth incubated for 96 hrs by MTT based ELISA
Antiproliferative activity against human NCI-H2228 cells assessed as inhibition of cell growth incubated for 96 hrs by MTT based ELISA
[PMID: 39106476]
NCI-H446 IC50
0.09 μM
Compound: 23
Antiproliferative activity against human NCI-H446 cells assessed as inhibition of cell growth incubated for 96 hrs by MTT based ELISA
Antiproliferative activity against human NCI-H446 cells assessed as inhibition of cell growth incubated for 96 hrs by MTT based ELISA
[PMID: 39106476]
PC-3 IC50
0.4 μM
Compound: 23
Antiproliferative activity against human PC-3 cells assessed as inhibition of cell growth incubated for 96 hrs by MTT based ELISA
Antiproliferative activity against human PC-3 cells assessed as inhibition of cell growth incubated for 96 hrs by MTT based ELISA
[PMID: 39106476]
PC-9 IC50
0.76 μM
Compound: 23
Antiproliferative activity against human PC-9 cells assessed as inhibition of cell growth incubated for 96 hrs by MTT based ELISA
Antiproliferative activity against human PC-9 cells assessed as inhibition of cell growth incubated for 96 hrs by MTT based ELISA
[PMID: 39106476]
Molecular Weight

347.41

Formula

C21H21N3O2

SMILES

CN(C)CCCN1C2=C(C=C(OCO3)C3=C2)C4=C1C5=CC=CC=C5C=N4

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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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.

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Product Name:
Top1/2-IN-1
Cat. No.:
HY-161957
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