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CH-0793076

Names

[ CAS No. ]:
534605-78-2

[ Name ]:
CH-0793076

Biological Activity

[Description]:

CH-0793076 (TP3076), a hexacyclic camptothecin analog, is active drug and major metabolite of TP300. CH-0793076 inhibits DNA topoisomerase I with an IC50 of 2.3 μM. CH-0793076 is efficacious against cells expressing BCRP (breast cancer resistance protein)[1].

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> Cell Cycle/DNA Damage >> Topoisomerase

[Target]

Topoisomerase I:2.3 μM (IC50)


[In Vitro]

CH0793076 (TP3076) (6 days at 37°C) shows antiproliferative activity against PC-6/BCRP and PC-6/pRC cells, with IC50 of 0.35 and 0.18 nM[1].

[In Vivo]

TP300 (1-100 mg/kg; bolus intravenous injection once per week for 3 weeks, for a total of three doses) shows more than 50% of tumor growth inhibition in all nine models, regardless of the expression of BCRP (WiDr, HT-29, NCI-H460 and AsPC-1, HCT116, COLO 201, HCT-15, Calu-6 and NCI-N87)[1].

[References]

[1]. Endo M, et al. A water soluble prodrug of a novel camptothecin analog is efficacious against breast cancer resistance protein-expressing tumor xenografts. Cancer Chemother Pharmacol. 2010 Jan;65(2):363-71.

Chemical & Physical Properties

[ Molecular Formula ]:
C26H26N4O4

[ Molecular Weight ]:
458.51

Related Compounds