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. Author manuscript; available in PMC: 2021 Apr 23.

Published in final edited form as: J Med Chem. 2020 Apr 8;63(8):4256–4292. doi: 10.1021/acs.jmedchem.0c00193

Table 7.

Antiproliferative Activities of Selected Dual Inhibitors against Various Human Cancer Cell Lines at NCI-60^a

		GI₅₀ (μM)
cancer type	cell line	28d	46b	48b	48c	48o	Idelalisib	Vorinostat (SAHA)
leukemia	CCRF-CEM	3.1	0.4	1.6	0.7	0.05	22.3	0.7
	SR	2.5	1.2	1.4	0.7	0.6		0.4
non-small cell lung cancer	HOP-62	11.8	2.7	1.9	2.4	1.4	>100.0	1.6
	HOP-92	2.2	0.2	1.1	0.9	0.3	14.1	2.9
colon cancer	HCT-2998	3.0	2.2	1.7	2.1	1.8	38.5	1.9
	KM-12	2.3	4.0	1.9	1.7	0.4	1.2	0.8
CNS cancer	SNB-75	3.0	0.3	1.3	0.7	0.4	1.2	0.8
	U251	2.5	1.5	1.7	1.7	1.4	53.2	1.6
melanoma	LOX IMVI	1.8	1.4	1.8	1.6	1.5	33.5	1.2
	M14	5.5	1.8	2.3	1.8	1.5	37.8	1.3
ovarian cancer	IGROV1	2.3	0.5	1.9	1.5	0.9	4.8	1.1
	OVCAR3	3.4	1.2	2.2	1.2	1.3	17.7	1.4
renal cancer	A498	6.1	0.2	1.4	1.0	0.7	1.1	1.4
	CAKI-1	14.6	1.3	3.2	1.3	0.8	20.5	1.2
	RXF 393	3.2	0.2	1.4	1.2	0.5	1.4	1.3
breast cancer	MDA-MB-231/ATCC	2.8	1.8	2.3	1.8	1.5	42.3	2.5
	HS 578T	4.5	0.4	2.5	2.0	0.9	6.0	3.6
	T-47D	1.7	0.3	1.6	1.2	0.3	5.2	0.5

^a

Compounds were tested at NCI-60 panel in singlet 5-dose IC₅₀ mode with 10-fold serial dilution starting at a concentration of 100 μM.