Characterization of the biological activity of a potent small molecule Hec1 inhibitor TAI-1

Huang, Lynn YL; Lee, Ying-Shuan; Huang, Jiann-Jyh; Chang, Chia-chi; Chang, Jia-Ming; Chuang, Shih-Hsien; Kao, Kuo-Jang; Tsai, Yung-Jen; Tsai, Pei-Yi; Liu, Chia-Wei; Lin, Her-Sheng; Lau, Johnson YN

doi:10.1186/1756-9966-33-6

Journal of Experimental & Clinical Cancer Research

Table 1 Characteristics of cell lines screened in Hec1 inhibitor drug assays

From: Characterization of the biological activity of a potent small molecule Hec1 inhibitor TAI-1

	Cell lines	Cell type	RB	P53	GI₅₀(nM)
Strong sensitivity (GI₅₀ < 50 nM)	K562	Chronic myeloid leukemia	WT	Mut	13
	HeLa	Cervical cancer	Mut	Inactivated	16
	T47D	Breast, metastatic-pleural, invasive ductal carcinoma	WT	Mut	17
	U-937	Acute myeloid leukemia	WT	Null	22
	MDA-MB-453	Breast, metastatic-effusion, adenocarcinoma	WT	Deletion	24
	RPMI8226	Acute myeloid leukemia	Mut	Mut	27
	KG-1	Myelogenous leukemia	Rearranged	Reduced/no	29
	MDA-MB-468	Breast, metastatic-pleural, invasive ductal carcinoma	Mut/no	Mut	34
	HCT116	Colorectal carcinoma	Low	WT	39
	COLO205	Colorectal carcinoma	WT	No	40
	MDA-MB-231	Breast, metastatic-pleural, invasive ductal carcinoma	WT	Mut	43
Moderate sensitivity (50 nM < GI₅₀ < 100 nM)	PC3	Prostate cancer	WT	Null	60
	MCF7	Breast, metastatic-pleural, invasive ductal carcinoma	WT	Heterogenous. WT	64
	NCI-H520	Non-small cell lung cancer	WT	Reduced mRNA	68
	ZR-75-30	Breast, metastatic-ascites, invasive ductal carcinoma	WT	WT	77
	ZR-75-1	Breast, metastatic-ascites, invasive ductal carcinoma	WT	WT	80
	Huh7	Hepatocellular carcinoma	WT	Mut	84
	BT474	Breast, primary, invasive ductal carcinoma	WT	Mut	86
	PLC/PRF/5	Hepatocellular carcinoma	WT	Inactivated	92
	Hep3B	Hepatocellular carcinoma	No	Deletion	96
Low sensitivity (100 nM < GI₅₀ < 1 μM)	U2OS	Osteosarcoma	Less active	WT	139
	Hs578T	Breast, metastatic, invasive ductal carcinoma	WT	Mut	143
	MV4-11	Acute myeloid leukemia	WT	Mut	231
	RS4;11	Acute myeloid leukemia	WT	Mut	254
	HepG2	Hepatocellular carcinoma	WT	WT	273
	MOLM-13	Acute myeloid leukemia	WT	Mut	315
Resistant (GI₅₀ > 1 μM)	A549	Non-small cell lung cancer	WT	WT	>10 μM
	HCC1954	Breast, invasive ductal carcinoma	Mut	WT	>10 μM
	MDA-MB-361	Breast, metastatic-brain, adenocarcinoma	WT	No	>10 μM
	MOLT-4	Acute lymphoblastic leukemia	WT	WT	>30 μM
	N87	Gastric cancer	WT	WT	>30 μM

*WT, wild type; Mut, mutated.

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ISSN: 1756-9966

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