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TG101209

CAT: 0804-HY-10410-01Size: 5 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-10410-01Size:5 mg
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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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.
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
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
JAK2; JAK3

Alternative Products

CatalogName
A4145-50TG101209

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