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TG-101348

Chemical Structure : TG-101348

CAS No.: 936091-26-8

TG-101348 (Fedratinib, SAR302503, TG101348)

Catalog No.: PC-42569Not For Human Use, Lab Use Only.

TG-101348 (Fedratinib, SAR302503) is a potent, selective JAK2 inhibitor with IC50 of 3 nM for both wt JAK2 and JAK2 V617F.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

TG-101348 (Fedratinib, SAR302503) is a potent, selective JAK2 inhibitor with IC50 of 3 nM for both wt JAK2 and JAK2 V617F.
TG-101348 also inhibits FLT3 (IC50=15 nM) and RET (IC50=48 nM) kinases, weakly inhibits JAK3 (IC50=168 nM), >35-fold selectivity over JAK1/3 and Tyk2.
TG-101348 shows therapeutic efficacy in a murine model of myeloproliferative disease induced by the JAK2V617F mutation.
TG-101348 also potently inhibits BRD4 with Kd of 168 nM.

Physicochemical Properties

M.Wt 524.6782
Formula C27H36N6O3S
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

DMSO: ≥ 42 mg/mL

Chemical Name/SMILES

Benzenesulfonamide, N-(1,1-dimethylethyl)-3-[[5-methyl-2-[[4-[2-(1-pyrrolidinyl)ethoxy]phenyl]amino]-4-pyrimidinyl]amino]-

References

1. Pardanani A, et al. Leukemia. 2007 Aug;21(8):1658-68.

2. Ciceri P, et al. Nat Chem Biol. 2014 Apr;10(4):305-12.

3. Wernig G, et al. Cancer Cell. 2008 Apr;13(4):311-20.

4. Geron I, et al. Cancer Cell. 2008 Apr;13(4):321-30.

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