TG101209

TG101209 is a selective JAK2 inhibitor with IC50 of 6 nM, less potent to Flt3 and RET with IC50 of 25 nM and 17 nM, appr 30-fold selective for JAK2 than JAK3, and sensitive to JAK2V617F and MPLW515L/K mutations.

936091-14-4

12352005

H302, H315, H319, H335

Apoptosis; Autophagy; FLT3; JAK; RET

Reference compound

Apoptosis; Autophagy; Epigenetics; JAK/STAT Signaling; Protein Tyrosine Kinase/RTK; Stem Cell/Wnt

Cancer-Kinase/protease

Cancer

https://www.medchemexpress.com/TG101209.html

10mM

98.81

DMSO : ≥ 50 mg/mL

O=S(C1=CC=CC(NC2=NC(NC3=CC=C(C=C3)N4CCN(CC4)C)=NC=C2C)=C1)(NC(C)(C)C)=O

C26H35N7O2S

509.67

H302, H315, H319, H335

[1]Pardanani A, et al. TG101209, a small molecule JAK2-selective kinase inhibitor potently inhibits myeloproliferative disorder-associated JAK2V617F and MPLW515L/K mutations. Leukemia. 2007 Aug;21 (8) :1658-68.|[2]Ma AC, et al. A novel zebrafish jak2a (V581F) model shared features of human JAK2 (V617F) polycythemia vera. Exp Hematol. 2009 Dec;37 (12) :1379-1386.e4.|[3]Sun Y, et al. Inhibition of JAK2 signaling by TG101209 enhances radiotherapy in lung cancer models. J Thorac Oncol. 2011 Apr;6 (4) :699-706|[4]Cuesta-Dominguez A, et al. Transforming and tumorigenic activity of JAK2 by fusion to BCR: molecular mechanisms of action of a novel BCR-JAK2 tyrosine-kinase. PLoS One. 2012;7 (2) :e3245

Room Temperature

-20°C, 3 years; 4°C, 2 years (Powder)

http://file.medchemexpress.com/batch_PDF/HY-10410/TG101209-SDS-MedChemExpress.pdf

Reference compound1

No Development Reported

JAK2; JAK3