Article
R723, a selective JAK2 inhibitor, effectively treats JAK2V617F-induced murine myeloproliferative neoplasm.
Blood - 23 Jun 2011
Shide Kotaro, Kameda Takuro, Markovtsov Vadim, Shimoda Haruko K, Tonkin Elizabeth, Fang Shuling, Liu Chian, Gelman Marina, Lang Wayne, Romero Jason, McLaughlin John, Bhamidipati Somasekhar, Clough Jeffrey, Low Caroline, Reitsma Andrea, Siu Stacey, Pine Polly, Park Gary, Torneros Allan, Duan Matt, Singh Rajinder, Payan Donald G, Matsunaga Takuya, Hitoshi Yasumichi, Shimoda Kazuya
Abstract excerpt
The activating mutations in JAK2 (including JAK2V617F) that have been described in patients with myeloproliferative neoplasms (MPNs) are linked directly to MPN pathogenesis. We developed R723, an orally bioavailable small molecule that inhibits JAK2 activity in vitro by 50% at a concentration of 2nM, while having minimal effects on JAK3, TYK2, and JAK1 activity. R723 inhibited cytokine-independent CFU-E growth...
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