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]:
[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]
Chemical & Physical Properties
[ Molecular Formula ]:
C26H26N4O4
[ Molecular Weight ]:
458.51