CH-0793076
CAS No. : 534605-78-2
(Synonyms: TP3076)
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| Cat. No. : | HY-107096 |
| M.Wt: | 458.51 |
| Formula: | C26H26N4O4 |
| Purity: | >98 % |
| Solubility: | 10 mM in DMSO |
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]. In Vitro:CH0793076 (TP3076) (6 days at 37°C) shows antiproliferative activity against PC-6/BCRP and PC-6/pRC cells, with IC50s of 0.35 and 0.18 nM, respectively[1]. In Vivo:TP300 (1-100 mg/kg; bolus intravenous injection once per week for 3 weeks, for a total of three doses), a water-soluble prodrug of CH0793076, 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].
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