Topoisomerase I inhibitor 7

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Topoisomerase I inhibitor 7 (Compound 8) is a potent inhibitor of Topoisomerase I. Topoisomerase I inhibitor 7 significantly inhibits tumor growth (up to 79%) and increases the lifespan (153%) of mice bearing P388 lymphoma transplants. Topoisomerase I inhibitor 7 indicates prospects for further search of new antitumor agent candidates among the heteroarene-fused anthraquinones.

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Topoisomerase I inhibitor 7 Chemical Structure

CAS No. : 2408639-81-4

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Topoisomerase Topo I Topo II

Biological Activity
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Description

Cellular Effect

Cell Line	Type	Value	Description	References
CAPAN-1	IC₅₀	0.5 μM Compound: 8	Antiproliferative activity against human CAPAN-1 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against human CAPAN-1 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 32428792]
HCT-116	IC₅₀	0.8 μM Compound: 8	Antiproliferative activity against human HCT-116 cells with inactivated p53 gene assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against human HCT-116 cells with inactivated p53 gene assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 32428792]
HCT-116	IC₅₀	0.9 μM Compound: 8	Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 32428792]
HL-60	IC₅₀	0.9 μM Compound: 8	Antiproliferative activity against human HL-60 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against human HL-60 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 32428792]
K562	IC₅₀	0.8 μM Compound: 8	Antiproliferative activity against human K562 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against human K562 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 32428792]
NCI-H460	IC₅₀	0.9 μM Compound: 8	Antiproliferative activity against human NCI-H460 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against human NCI-H460 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 32428792]
TERT-RPE1	IC₅₀	15.8 μM Compound: 8	Cytotoxicity against human TERT-RPE1 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Cytotoxicity against human TERT-RPE1 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 32428792]

Molecular Weight

405.40

Formula

C₂₂H₁₉N₃O₅

CAS No.

2408639-81-4

SMILES

CC1=C(C2=C(C3=C(C(O)=C2N1)C(C4=C(C3=O)C=CC=C4)=O)O)C(N5CC[C@@H](C5)N)=O

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Tikhomirov AS, et al. Amides of pyrrole- and thiophene-fused anthraquinone derivatives: A role of the heterocyclic core in antitumor properties. Eur J Med Chem. 2020 Aug 1;199:112294. [Content Brief]