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Cat. No. Name Size Price Add Cart
KI1124TG1013485 mg$176
TG10134810 mg$272
TG10134825 mg$592
TG10134850 mg$912

Chemical Characteristic

Product NameTG101348
SynonymsSAR302503
CAS No.936091-26-8
Molecular Weight 524.68
FormulaC27H36N6O3S
Chemical NameN-tert-butyl-3-[[5-methyl-2-[4-(2-pyrrolidin-1-ylethoxy)anilino]pyrimidin-4-yl]amino]benzenesulfonamide
Smilesc1(cc(ccc1)Nc1nc(ncc1C)Nc1ccc(cc1)OCCN1CCCC1)S(=O)(=O)NC(C)(C)C
Chemical Structure

Biological activities

TG101348 is a selective small-molecule inhibitor of JAK2. The IC50 of TG101348 is 3 nM against JAK2. TG101348 also inhibits JAK2V617F with an IC50 of 3 nM. In contrast, TG101348 prevents Flt3 and Ret with IC50 of 15 and 48 nM, respectively. TG101348 has an IC50∼300-fold higher for the closely related JAK3. TG101348 is a less potent inhibitor of the JAK1 and TYK2 family members. TG101348 inhibits proliferation of both of a human erythroblast leukemia (HEL) cell line that harbors the JAK2V617F mutation and a murine pro-B cell line expressing human JAK2V617F (Ba/F3 JAK2V617F) The IC50 of TG101348 is 300 nM for either line.[1] TG10134 inhibits the growth of KITD816V-dependent mast cell leukemia cells by blocking JAK-STAT signaling.[2] TG101348 is well tolerated and produces significant reduction in disease burden of myelofibrosis.[3] TG101348 prevents the cytokine-independent growth of human erythroleukemia and Ba/F3-JAK2V617F cells with IC50 of 0.3 and 0.58 µM, respectively. TG101348 inhibits Ba/F3-MPLW515L cells with an IC50 of 0.62 µM. TG101348 significantly decreases the size of erythroid colonies (erythroid burst-forming unit) obtained from PV progenitor cells.[4]

References

[1] Wernig G, et al. Efficacy of TG101348, a selective JAK2 inhibitor, in treatment of a murine model of JAK2V617F-induced polycythemia vera. Cancer Cell. 2008, (4): 11-20.
[2] Lasho T, 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(7): 1378-1380.
[3] Pardanani A, et al. Safety and efficacy of TG101348, a selective JAK2 inhibitor, in myelofibrosis. J Clin Oncol. 2011, 29(7): 789-796.
[4] Lasho TL, 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(9): 1790-1792.

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