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TG101209 | JAK2/3 inhibitor

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Price:
$169.00
Catalog #:
C8120-5
Quantity:


Product Description

TG101209 is an orally-available, diaminopyrimidine-based inhibitor of JAK2 and Flt3 with IC50 values of 6, 25, and 17 nM, respectively. [1] In a human JAK2V617F-expressing acute myeloid leukemia cell line, TG101209 induced cell cycle arrest (G0/G1) and apoptosis, and inhibits phosphorylation of JAK2V617F, STAT5, and STAT3 at doses between 300-600 nM. In MM1S cells, however, a time-dependent cell cycle arrest was observed in the G2/M stages. [2]

TG101209 was recently utilized in studying a novel BCR-JAK2 tyrosine kinase in which the BCR oligomerization domain is fused to the JAK2 tyrosine-kinase domain. [3]

In lung cancers, TG101209 was shown to inhibit STAT3 activation and survivin expression, and sensitized HCC2429 and H460 cells to radation in clonogenic assays. [4]


Technical information:

Chemical Formula:   C26H35N7O2S
CAS #:   936091-14-4
Molecular Weight:   509.67
Purity:   >98%
Appearance:   White
Chemical Name:   N-tert-butyl-3-(5-methyl-2-(4-(4-methylpiperazin-1-yl)phenylamino)pyrimidin-4-ylamino)benzenesulfonamide
Solubility:   Up to 100mM in DMSO
Synonyms:   TG101209, TG-101209

Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.


Reference:

1. Pardanani et al., TG101209, a small molecule JAK2-selective kinase inhibitor potently inhibits myeloproliferative disorder-associated JAK2V617F and MPLW515L/K mutations. Leukemia 2007, 21, 1658-1668. Pubmed ID: 17541402
2. Ramakrishnan et al., 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. Pubmed ID: 20652971
3. Cuesta-Dominguez 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), e32451. Pubmed ID: 22384256
4. Sun et al., Inhibition of JAK2 signaling by TG101209 enhances radiotherapy in lung cancer models. J. Thorac. Oncol. 2011, 6(4), 699-706. Pubmed ID: 20652971

Other Information:

Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.

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