Table 1 Growth inhibitory effects of... | American Society of Hematology

Table 1

Growth inhibitory effects of proteasome inhibitors and various anticancer/anti-inflammatory drugs for wild-type (WT) and bortezomib (BTZ)–resistant THP1 cells

	IC_50*	Resistance factor†
	THP1/WT	THP1/BTZ₅₀	THP1/BTZ₁₀₀	THP1/BTZ₂₀₀
Proteasome inhibitors
Bortezomib, nM	3.3 ± 0.6	45	79	129
MG132, nM	237 ± 54	8.1	11.9	15.8
MG262, nM	2.1 ± 0.6	8.3	10.3	10.8
ALLN, μM	3.7 ± 0.4	5.8	10.0	18.1
4A6, μM	0.26 ± 0.06	44	117	287
Miscellaneous drugs
Methotrexate, nM	8.0 ± 1.4	0.8	1.0
Sulfasalazine, μM	275 ± 49	1.3	0.8
Chloroquine, μM	56.3‡	1.1	1.1
Cyclosporin A, μM	3.9‡	0.9	0.8
5-Fluorouracil, μM	2.3‡	0.5	0.4
Methylprednisone, μM	0.69‡	1.1	1.0
Doxorubicin, nM	18.9 ± 6.2	1.3	1.5
Mitoxantrone, nM	2.5 ± 1.3	1.4	1.2
Bleomycin, μM	4.9 ± 2.9	0.6	0.5
Cisplatin, μM	0.84 ± 0.46	2.1	1.9
Gefitinib, μM	10.4 ± 4.6	1.3	1.3
Geldanamycin, nM	30.6 ± 13.1	1.0	1.1
AAF-cmk, μM	7.3 ± 1.8	1.4	1.9	1.1

	IC_50*	Resistance factor†
	THP1/WT	THP1/BTZ₅₀	THP1/BTZ₁₀₀	THP1/BTZ₂₀₀
Proteasome inhibitors
Bortezomib, nM	3.3 ± 0.6	45	79	129
MG132, nM	237 ± 54	8.1	11.9	15.8
MG262, nM	2.1 ± 0.6	8.3	10.3	10.8
ALLN, μM	3.7 ± 0.4	5.8	10.0	18.1
4A6, μM	0.26 ± 0.06	44	117	287
Miscellaneous drugs
Methotrexate, nM	8.0 ± 1.4	0.8	1.0
Sulfasalazine, μM	275 ± 49	1.3	0.8
Chloroquine, μM	56.3‡	1.1	1.1
Cyclosporin A, μM	3.9‡	0.9	0.8
5-Fluorouracil, μM	2.3‡	0.5	0.4
Methylprednisone, μM	0.69‡	1.1	1.0
Doxorubicin, nM	18.9 ± 6.2	1.3	1.5
Mitoxantrone, nM	2.5 ± 1.3	1.4	1.2
Bleomycin, μM	4.9 ± 2.9	0.6	0.5
Cisplatin, μM	0.84 ± 0.46	2.1	1.9
Gefitinib, μM	10.4 ± 4.6	1.3	1.3
Geldanamycin, nM	30.6 ± 13.1	1.0	1.1
AAF-cmk, μM	7.3 ± 1.8	1.4	1.9	1.1

Results depicted are the mean of at least 3 to 10 experiments plus or minus SD.

IC₅₀: drug concentration resulting in 50% growth inhibition compared with control.

†

Resistance factor: ratio IC₅₀ BTZ-resistant cell line over IC₅₀ THP1/WT cells.

‡

Mean of 2 experiments performed in duplicate.

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