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TG101348 (SAR302503)

Cat No.
CEI-0192
Description
TG-101348 (SAR302503) can selectively inhibit JAK2 with IC50 of 3 nM.
CAS No.
936091-26-8
Molecular Weight
524.68
Purity
>99%
Storage
2 years at -20 centigrade
Targets
JAK2
Molecular Formula
C27H36N6O3S
Chemical Name
N-tert-butyl-3-(5-methyl-2-(4-(2-(pyrrolidin-1-yl)ethoxy)phenylamino)pyrimidin-4-ylamino)benzenesulfonamide
Solubility
DSMO 105 mg/mL Water
In vitro
TG-101348 also significantly inhibits JAK2 V617F, Flt3, and Ret with IC50 of 3 nM, 15 nM, and 48 nM, respectively. TG-101348 also inhibits proliferation of parental Ba/F3 cells to a comparable level, with IC50 of ~420 nM. TG101348 treatment decreases GATA-1 expression, which is associated with erythroid-skewing of JAK2V617F+ progenitor differentiation, and inhibits STAT5 as well as GATA S310 phosphorylation.
In vivo
Oral administration of TG101348 (120 mg/kg) significantly inhibits PV progenitor erythroid differentiation in vivo.
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