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TG-101209

Chemical Structure : TG-101209

CAS No.: 936091-14-4

TG-101209 (SAR-317461)

Catalog No.: PC-42570Not For Human Use, Lab Use Only.

A potent, selective, orally bioavailable JAK2 inhibitor with IC50 of 6 nM.

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10 mg $108 In stock
50 mg $324 In stock
100 mg $600 In stock

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

Biological Activity

A potent, selective, orally bioavailable JAK2 inhibitor with IC50 of 6 nM; also inhibits FLT3 (IC50=25 nM) and RET (IC50=17 nM) kinases, weakly inhibits JAK3 (IC50=168 nM); inhibits growth of Ba/F3 cells expressing JAK2V617F or MPLW515L mutations with IC50 of 200 nM, induces cell cycle arrest and apoptosis, and inhibits phosphorylation of JAK2V617F, STAT5 and STAT3; attenuates myelofibrosis in murine model of JAK2V617F-induced polycythemia vera; also potently inhibits BRD4 with Kd of 123 nM.

Bone Cancer

Preclinical

Physicochemical Properties

M.Wt 509.6668
Formula C26H35N7O2S
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

10 mM in DMSO

Chemical Name/SMILES

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

References

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

2. Libani IV, et al. Blood. 2008 Aug 1;112(3):875-85.

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

4. Wang Y, et al. Blood. 2009 Dec 3;114(24):5024-33.

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