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托法替尼 Tofacitinib

2019/7/4 23:20:26发布133次查看
交易须知
tofacitinib产品活性:tofacitinib是 jak1/2/3 抑制剂,ic50 分别为1,20 和 112 nm。
研究领域:epigenetics  |  stem cell/wnt  |  jak/stat signaling
作用靶点:jak
in vitro: tofacitinib (cp-690550) citrate binds potentially at jak3 and jak2 as 2.2 nm and 5 nm (kd). the report includes additional binding for tofacitinib at camk1 (kd of 5,000 nm), dcamkl3 (kd of 4.5 nm), mst2 (kd of 4,300 nm), pkn1 (kd of 200 nm), rps6ka2 (kin.dom.2-c-terminal) (kd of 1,400 nm), rps6ka6 (kin.dom.2-c-terminal) (kd of 1,200 nm), snark (kd of 420 nm), tnk1 (kd of 640 nm) and tyk2 (kd of 620 nm).
in vivo: animals that are treated with tofacitinib show a significantly lower production of anti-drug antibodies (adas) compare with peg-treated control mice (for five weeks after initial immunization, p<0.01, n=8). moreover adas become detectable earliest on day 28. a difference of 1000- to 200-fold in titers to ss1p is apparent from days 21 through 35, respectively. compare to ss1p, mice injected with keyhole limpet hemocyanin (klh) generate a more rapid antibody response. yet, the administration of tofacitinib reduces anti-klh titers compare to controls (p<0.05 on day 21, p4 hours.
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