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Chemical Structure : TG101209
CAS No.: 936091-14-4
Catalog No.: PC-42570Not For Human Use, Lab Use Only.
TG101209 (SAR-317461) is a potent, selective, orally bioavailable JAK2 inhibitor with IC50 of 6 nM.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 2 mg (Free Sample) | $28 | In stock | |
| 10 mg | $98 | In stock | |
| 25 mg | $158 | In stock | |
| 50 mg | $248 | In stock | |
| 100 mg | Get quote |
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TG101209 (SAR-317461) is a potent, selective, orally bioavailable JAK2 inhibitor with IC50 of 6 nM.
TG101209 also inhibits FLT3 (IC50=25 nM) and RET (IC50=17 nM) kinases, weakly inhibits JAK3 (IC50=168 nM).
TG101209 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.
TG101209 attenuates myelofibrosis in murine model of JAK2V617F-induced polycythemia vera.
TG101209 also potently inhibits BRD4 with Kd of 123 nM.
| M.Wt | 509.6668 | |
| Formula | C26H35N7O2S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
Benzenesulfonamide, N-(1,1-dimethylethyl)-3-[[5-methyl-2-[[4-(4-methyl-1-piperazinyl)phenyl]amino]-4-pyrimidinyl]amino]- |
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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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