Table 2. Comparison of ABCG2 inhibitors described in the literature for in vivo experiments.

IC₅₀: Inhibitory concentration of 50% of the ABCG2 activity; IG₅₀: Inhibitory growth of 50% of the cell proliferation; I.V.: Intravenous; I.P.: Intraperitoneal; P.O.: Per Os.

Name	In vitro				In vivo Toxicity		In vivo Impact on
	Inhibition (IC50)		ABCG2 Specificity	Cytoxicity (IG50)	Acute	Chronic	Tumor growth	Pharmacokinetics
GF120918 [13, 21, 35, 45–48]	0.31 μM	Mitoxantrone	No	1–40 mM	> 5 mg/kg I.V.	> 400 mg oral (human)	Yes	Doxorubicin : No
					> 10 mg/kg I.P.			Topotecan: Yes
					> 50 mg/kg oral			CPT-11: Yes
Ko143 [6, 24, 49]	0.22 μM	Hoechst 3342	Yes	18–34 μM	> 50 mg/kg oral			Topotecan: Yes
	0.35 μM	Pheophorbide A			> 10 mg/kg I.P.
Telatinib [26, 50, 51]		[3H]-Mitoxantrone [3H]-E217BG	No	> 10 μM	>15 mg/kg oral	>1 500 mg (human)	Yes
Triclabendazole [7]	≈ 10 μM	Mitoxantrone			> 100 mg/kg I.P.			Nitrofurantoin: Yes
Sorafenib [25]			No	2–6 μM	> 25 mg/kg oral	> 25 mg/kg P.O.	Yes
YHO-13177 [40]	≈0.3 μM	Hoechst 3342	Yes	> 10 μM	> 200 mg/kg oral		Yes
					> 30 mg/kg I.V.
MBL-II-141	0.11 μM	Mitoxantrone	Yes	> 100 μM	> 10 mg/kg oral	> 10 mg/kg I.P.	Yes	CPT-11: Yes
					> 50 mg/kg I.P.	> 50 mg/kg I.P.