TG101209
Product Specifications
UNSPSC Description
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.
Target Antigen
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
Purity
99.22
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 Weight
509.67
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
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Product Datasheet
http://file.medchemexpress.com/batch_PDF/HY-10410/TG101209-DataSheet-MedChemExpress.pdf
Product MSDS
http://file.medchemexpress.com/batch_PDF/HY-10410/TG101209-SDS-MedChemExpress.pdf
Clinical Information
No Development Reported
CAS Number
936091-14-4
Available Sizes
Curated Selection
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