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

Physicochemical Properties

CAS #	2740278-76-4
Related CAS #	CH-0793076;534605-78-2
Appearance	Brown to orange solid powder
HS Tariff Code	2934.99.9001
Storage	Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture.
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity

Targets	Topoisomerase I 2.3 μM (IC50)
ln Vitro	CH0793076 (TP3076) TFA (6 days at 37°C) demonstrates antiproliferative efficacy with IC50s of 0.35 and 0.18 nM, respectively, against PC-6/BCRP and PC-6/pRC cells[1].
References	[1]. 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.

Solubility Data

Solubility (In Vitro)

DMSO : 30 mg/mL (52.40 mM)

Solubility (In Vivo)

Solubility in Formulation 1: 3 mg/mL (5.24 mM) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 30.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 + to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.  (Please use freshly prepared in vivo formulations for optimal results.)