Table 1 R723 activity in cell-based... | American Society of Hematology

Table 1

R723 activity in cell-based assays

Assay	Target	IC₅₀, nM
Ba/F3-EPOR-JAK2V617F proliferation	JAK2 V617F	191
UKE1 proliferation	JAK2 V617F	168
SET2 proliferation	JAK2 V617F	139
EPO-dependent human CD34⁺ progenitor proliferation	JAK2	124
Ba/F3-EPOR-JAK2V617F pSTAT5 FACS	JAK2 V617F	390
SET2 pSTAT5 FACS	JAK2 V617F	39
IL-2 CTLL2 proliferation	JAK1/JAK3	528
IL-2 human primary T-cell proliferation	JAK1/JAK3	1260
IL-2 CTLL2 pSTAT5 FACS	JAK1/JAK3	2300
IL-2 human primary T-cell pSTAT5 FACS	JAK1/JAK3	2700
Ba/F3-JAK1V658F proliferation	JAK1 V658F	885
CMK proliferation	JAK3 A572V	2340
A549 proliferation	Multiple	3680
H1299 proliferation	Multiple	4100
IgE CHMC tryptase	Syk	760
Insulin HeLa pAKT in cell western	InsR	10 800
VEGF HUVEC pVEGFR in cell western	VEGFR	3250

Assay	Target	IC₅₀, nM
Ba/F3-EPOR-JAK2V617F proliferation	JAK2 V617F	191
UKE1 proliferation	JAK2 V617F	168
SET2 proliferation	JAK2 V617F	139
EPO-dependent human CD34⁺ progenitor proliferation	JAK2	124
Ba/F3-EPOR-JAK2V617F pSTAT5 FACS	JAK2 V617F	390
SET2 pSTAT5 FACS	JAK2 V617F	39
IL-2 CTLL2 proliferation	JAK1/JAK3	528
IL-2 human primary T-cell proliferation	JAK1/JAK3	1260
IL-2 CTLL2 pSTAT5 FACS	JAK1/JAK3	2300
IL-2 human primary T-cell pSTAT5 FACS	JAK1/JAK3	2700
Ba/F3-JAK1V658F proliferation	JAK1 V658F	885
CMK proliferation	JAK3 A572V	2340
A549 proliferation	Multiple	3680
H1299 proliferation	Multiple	4100
IgE CHMC tryptase	Syk	760
Insulin HeLa pAKT in cell western	InsR	10 800
VEGF HUVEC pVEGFR in cell western	VEGFR	3250