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.

Product Specifications

CAS Number

[936091-14-4]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Apoptosis; Autophagy; FLT3; JAK; RET

Type

Reference compound

Related Pathways

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

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

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

Concentration

10mM

Purity

98.81

Solubility

DMSO : ≥ 50 mg/mL

Smiles

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

Molecular Formula

C26H35N7O2S

Molecular Weight

509.67

Precautions

H302, H315, H319, H335

References & Citations

[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