Products
Online Inquiry
Our Products Cannot Be Used As Medicines Directly For Personal Use.
Welcome! For price inquiries, please feel free to contact us through the form on the left side. We will get back to you as soon as possible.
TG101209
Cat No.
CEI-0194
Description
As a JAK2 selective inhibitor, TG101209 can inhibit JAK2 (IC50=6 nM), FLT3 (IC50=25 nM) and RET (IC50=17 nM) kinases and JAK3 (IC50=169 nM).
CAS No.
936091-14-4
Molecular Weight
509.67
Purity
>99%
Storage
2 years at -20 centigrade
Targets
JAK2, FLT3, RET
Molecular Formula
C26H35N7O2S
Chemical Name
N-tert-butyl-3-(5-methyl-2-(4-(4-methylpiperazin-1-yl)phenylamino)pyrimidin-4-ylamino)benzenesulfonamide
Solubility
DSMO 102 mg/mL Water
In vitro
As a JAK2 selective inhibitor, TG101209 can inhibit JAK2 (IC50=6 nM), FLT3 (IC50=25 nM) and RET (IC50=17 nM) kinases and JAK3 (IC50=169 nM). By inducing cell cycle arrest and apoptosis, and inhibiting phosphorylation of JAK2V617F, STAT5 and STAT3, TG101209 inhibit the cell proliferation of human JAK2V617F-expressing acute myeloid leukemia cell line. TG101209 inhibited growth of Ba/F3 cells expressing JAK2V617F or MPLW515L mutations with an IC50 of 200 nM.TG101209 can induce cytotoxicity in a variety of multiple myeloma (MM) cell lines in dose- and time-dependent manners. TG101209 can induce apoptosis and inhibit cell cycle progression in myeloma cell lines and patient-derived plasma cells. Co-treatment with BEZ235 and JAK2-TKI (TG101209 and SAR302503) synergistically induced lethal activity against the cultured and primary CD34+ MPN cells while relatively sparing the normal CD34+ HPCs.
In vivo
Treatment with TG101209 not only prevented bleomycin-induced fibrosis but also effectively reduced skin fibrosis in TSK-1 mice. addition of TG101209 to radiation in lung xenografts produced a significant tumor growth delay (>10 days) compared with radiation alone and was well tolerated. TG101209 increased apoptosis and decreased cell proliferation and vascular density.
Download
Download Datasheet