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TG101209

JAK2 and 3 inhibitor, also inhibits Flt3 and RET

TG101209

Catalog No. A4145
Size Price Stock Qty
Evaluation Sample $28.00 In stock
5mg $110.00 In stock
10mg $190.00 In stock
50mg $590.00 In stock
200mg $1,490.00 In stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

TG101209

Related Biological Data

TG101209

Related Biological Data

TG101209

Biological Activity

Description TG101209 is a selective inhibitor of JAK2 with IC50 of 6 nM.
Targets   Flt3 RET JAK3    
IC50 6 nM 25 nM 17 nM 169 nM    

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Chemical Properties

Cas No. 936091-14-4 SDF Download SDF
Synonyms TG-101209
Chemical Name N-tert-butyl-3-[[5-methyl-2-[4-(4-methylpiperazin-1-yl)anilino]pyrimidin-4-yl]amino]benzenesulfonamide
Canonical SMILES CC1=CN=C(N=C1NC2=CC(=CC=C2)S(=O)(=O)NC(C)(C)C)NC3=CC=C(C=C3)N4CCN(CC4)C
Formula C26H35N7O2S M.Wt 509.67
Solubility Soluble in DMSO Storage Store at -20°C
Shipping Condition: Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

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Background

TG101209, a small-molecule identified by structure based design, is a selective inhibitor of janus kinase 2 (Jak2) that potently inhibits Jak/Stat pathway in multiple myeloma (MM) cell lines, such as cell harboring JAK2V617F or MPLW515L/K mutations which are commonly associated with polycythemia vera (PV) and primary myelofibrosis (PMF) respectively. According to results of multiple studies, it has revealed that TG101209 exhibits a dose and time dependent cyctoxicity, which is associated with inhibited cell cycle progrgression and induced apoptosis, in a wild range of MM cell lines through suppressing the expression of pJak2, pStat3 and Bcl-xl and inducing the overexpression of pErk and pAkt.

Reference

Ramakrishnan V, Kimlinger T, Haug J, Timm M, Wellik L, Halling T, Pardanani A, Tefferi A, Rajkumar SV, Kumar S. TG101209, a novel JAK2 inhibitor, has significant in vitro activity in multiple myeloma and displays preferential cytotoxicity for CD45+ myeloma cells. Am J Hematol. 2010;85(9):675-686.