Table 1 Mutant JAK3s are sensitive to... | American Society of Hematology

Table 1

Mutant JAK3s are sensitive to JAK3, PI3K, and mTOR inhibitors

	Tofacitinib, μM		BEZ-235, nM		BKM-120, μM		CI-1040, nM
	JAK3		PI3K/mTOR		PI3K		ERK 1/2
	IC₅₀	R²	IC₅₀	R²	IC₅₀	R²	IC₅₀	R²
BaF3	ND	0.77	ND	0.60	ND	0.55	ND	0.88
WT	0.18	0.84	ND	0.44	ND	0.65	ND	0.72
A572V	0.22	0.99	12.55	0.86	3.12	0.92	ND	0.73
L156P	0.27	0.99	11.96	0.90	2.51	0.93	ND	0.64
E183G	0.09	0.99	18.14	0.96	1.99	0.91	ND	0.62
R172Q	0.08	0.90	19.21	0.84	9.12	0.96	ND	0.50

	Tofacitinib, μM		BEZ-235, nM		BKM-120, μM		CI-1040, nM
	JAK3		PI3K/mTOR		PI3K		ERK 1/2
	IC₅₀	R²	IC₅₀	R²	IC₅₀	R²	IC₅₀	R²
BaF3	ND	0.77	ND	0.60	ND	0.55	ND	0.88
WT	0.18	0.84	ND	0.44	ND	0.65	ND	0.72
A572V	0.22	0.99	12.55	0.86	3.12	0.92	ND	0.73
L156P	0.27	0.99	11.96	0.90	2.51	0.93	ND	0.64
E183G	0.09	0.99	18.14	0.96	1.99	0.91	ND	0.62
R172Q	0.08	0.90	19.21	0.84	9.12	0.96	ND	0.50

mTOR indicates mammalian target of rapamycin; WT, wild type; and ND, IC₅₀ not determined due to poor curve-fitting models.

Live cells were quantified by the MTT assay after 24 hours on inhibitor. IC₅₀ and goodness-of-fit (R²) values for each mutant transduced into BaF3 cells were calculated based on best fit curves (see supplemental Figures 4,Figure 5–6 for individual curves.).

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