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TG101348 (SAR302503) | JAK2 inhibitor

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Price:
$109.00
Catalog #:
C8134-5
Quantity:


Product Description

TG101348 is an orally-available, aminopyrimidine-based inhibitor of JAK2 and JAK2V617F at an IC50 of 3 nM, with marked selectivity over JAK3 (IC50 >1 uM). [1, 2] TG101348 inhibits proliferation of HMC-1.1 and HMC-1.2 cells at IC50s of 740 and 407 nM, respectively. [1]

In a UT7/EPO cell line, TG101348 inhibited STAT5 phosphorylation much more potently at lower concentrations than known JAK2/3 inhibitor AG490 (600 nM vs 100 uM). In the same study, TG101348 inhibited AKT phosphorylation while reducing GATA-1 S310 phosphorylation. [2]

In human erythroleukemia and Ba/F3-JAK2V617F cells, TG101348 inhibited the cytokine-independent growth at IC50s of 300 and 580 nM, respectively. [3]

TG101348 induces apoptosis in both HEL and Ba/F3 JAK2V617F cells, but not in normal human dermal fibroblasts at concentrations up to 10 uM; antiproliferative IC50 against fibroblasts is > 5 uM.


Technical information:

Chemical Formula:   C27H36N6O3S
CAS #:   936091-26-8
Molecular Weight:   524.68
Purity:   >98%
Appearance:   Pale Yellow
Chemical Name:   N-tert-butyl-3-(5-methyl-2-(4-(2-(pyrrolidin-1-yl)ethoxy)phenylamino)pyrimidin-4-ylamino)benzenesulfonamide
Solubility:   Up to 100mM in DMSO
Synonyms:   TG101348, TG-101348, SAR302503

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. Lasho et al., Inhibition of JAK-STAT signaling by TG101348: a novel mechanism for inhibition of KITD816V-dependent growth in mast cell leukemia cells. Leukemia, 2010, 24, 1378-1380. Pubmed ID: 20485374
2. Geron et al., Selective inhibition of JAK2-driven erythroid differentiation of polycythemia vera progenitors. Cancer Cell, 2008, 13(4), 321-330. Pubmed ID: 18394555
3. Lasho et al., TG101348, a JAK2-selective antagonist, inhibits primary hematopoietic cells derived from myeloproliferative disorder patients with JAK2V617F, MPLW515K or JAK2 exon 12 mutations as well as mutation negative patients. Leukemia, 2008, 22, 1790-1792. Pubmed ID: 18354492
4. Wernig et al., Efficacy of TG101348, a selective JAK2 inhibitor, in treatment of a murine model of JAK2V617F-induced polycythemia vera. Cancer Cell 2008, 13(4), 311-320. Pubmed ID: 18394555

Other Information:

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

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