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TG101348 (SAR302503)JAK-2 inhibitor,potent and selective

TG101348 (SAR302503)

Catalog No. A4136
Size Price Stock Qty
Evaluation Sample $28.00 In stock
5mg $70.00 In stock
10mg $110.00 In stock
25mg $230.00 In stock
50mg $350.00 In stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

TG101348 (SAR302503)

Related Biological Data

TG101348 (SAR302503)

Related Biological Data

TG101348 (SAR302503)

Related Biological Data

TG101348 (SAR302503)

Biological Activity

Description TG-101348 (SAR302503) is a selective inhibitor of JAK2 with IC50 of 3 nM, 35- and 334-fold more selective for JAK2 versus JAK1 and JAK3.
Targets JAK2          
IC50 3 nM          

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Chemical Properties

Cas No. 936091-26-8 SDF Download SDF
Synonyms Tg-101348,SAR-302503
Chemical Name N-tert-butyl-3-[[5-methyl-2-[4-(2-pyrrolidin-1-ylethoxy)anilino]pyrimidin-4-yl]amino]benzenesulfonamide
Canonical SMILES CC1=CN=C(N=C1NC2=CC(=CC=C2)S(=O)(=O)NC(C)(C)C)NC3=CC=C(C=C3)OCCN4CCCC4
Formula C27H36N6O3S M.Wt 524.68
Solubility Soluble in DMSO > 10 mM Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

Background

TG101348, also known as SAR302503, is a potent and selective inhibitor of janus kinase 2 (JAK2), one member of a family of 4 cytoplasmic tyrosine kinases including janus kinase 1(JAK1), JAK2, janus kinase 3 (JAK3) and tyrosine kinase 2 (Tyk2), with the inhibition constant IC50 of 3 nM. Comparing to other close related kinases, the selectivity of TG101348 for JAK2 is 35- and 334-fold stronger than that for JAK3 and JAK1 respectively.  TG10348 is capable of inducing apoptosis in HEL cells as well BaF/3 cells harboring JAK2V617 mutation and inhibiting hematopoietic progenitor colony formation and erythroid engraftment in samples from polycythemia vera (PV) patients.

Reference

Srdan Verstovsek. Therapeutic potential of JAK2 inhibitors. Hematology Am Soc Hematol Educ Program 2009:636-642