534605-78-2

534605-78-2 structure

Name: CH-0793076
Chemical Name: CH-0793076
CAS Number: 534605-78-2
Molecular Formula: C₂₆H₂₆N₄O₄
Molecular Weight: 458.51
Catalog: Signaling Pathways Cell Cycle/DNA Damage Topoisomerase
Create Date: 2020-04-09 17:55:08
Modify Date: 2024-01-09 14:21:12
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].

Name	CH-0793076

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.

Molecular Formula	C₂₆H₂₆N₄O₄
Molecular Weight	458.51