TG-101209
A potent, selective, orally bioavailable JAK2 inhibitor with IC50 of 6 nM; also inhibits FLT3 (IC50=25 nM) and RET (IC50=17 nM) kinases, weakly inhibits JAK3 (IC50=168 nM) ; inhibits growth of Ba/F3 cells expressing JAK2V617F or MPLW515L mutations with IC50 of 200 nM, induces cell cycle arrest and apoptosis, and inhibits phosphorylation of JAK2V617F, STAT5 and STAT3; attenuates myelofibrosis in murine model of JAK2V617F-induced polycythemia vera; also potently inhibits BRD4 with Kd of 123 nM.Bone Cancer Preclinical.
Product Specifications
CAS Number
936091-14-4
Product Name Alternative
SAR-317461
Purity
>98% (HPLC)
Solubility
10 mM in DMSO
Smiles
O=S (C1=CC=CC (NC2=NC (NC3=CC=C (N4CCN (C) CC4) C=C3) =NC=C2C) =C1) (NC (C) (C) C) =O
Molecular Formula
C26H35N7O2S
Molecular Weight
509.6668
Storage Conditions
Storage temperature: -20°C. Stability: ≥ 2 years
Notes
For research use only.
Other Product Names
Benzenesulfonamide, N- (1,1-dimethylethyl) -3-[[5-methyl-2-[[4- (4-methyl-1-piperazinyl) phenyl]amino]-4-pyrimidinyl]amino]-
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