EasySep™小鼠TIL（CD45）正选试剂盒
产品号 #73472_C
JAK/STAT通路抑制剂；抑制JAK2
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总览
TG101348是Janus激酶2（JAK2）的抑制剂，IC₅₀为6 nM。它能抑制活性较低的相关激酶，例如fms相关酪氨酸激酶3（FLT3）、RET和JAK3，IC₅₀值分别为25 nM、17 nM和169 nM（Pardanani et al.）。据推测，TG101348可与其激酶靶标的ATP结合位点结合（Zhou et al.）。
癌症研究
·抑制表达JAK2 V617F或MPL W515L突变的Ba/F3细胞的生长（Pardanani et al.）。
·在JAK2 V617F诱发的造血和骨髓增生性疾病小鼠模型中，降低肿瘤细胞负担并提高生存率（Pardanani et al.; Wernig et al.）。
·在体外和小鼠异种移植模型中，提高对厄洛替尼耐药的非小细胞肺癌细胞对厄洛替尼治疗的敏感性（Zhang et al.）。
·在体外，从染色质中取代BRD4，并抑制多发性骨髓瘤细胞中的c-MYC表达（Ciceri et al.）。
细胞类型
癌细胞及细胞系，白血病/淋巴瘤细胞
种属
人，小鼠，非人灵长类，其他物种，大鼠
研究领域
癌症
CAS 编号
936091-26-8
化学式
C₂₇H₃₆N₆O₃S
纯度
≥98%
通路
JAK/STAT
靶点
JAK2
产品说明书及文档
请在《产品说明书》中查找相关支持信息和使用说明，或浏览下方更多实验方案。
相关材料与文献
技术资料 (2)
文献 (5)
TG101209, a small molecule JAK2-selective kinase inhibitor potently inhibits myeloproliferative disorder-associated JAK2V617F and MPLW515L/K mutations.
Leukemia 2007
Abstract
JAK2V617F and MPLW515L/K represent recently identified mutations in myeloproliferative disorders (MPD) that cause dysregulated JAK-STAT signaling,which is implicated in MPD pathogenesis. We developed TG101209,an orally bioavailable small molecule that potently inhibits JAK2 (IC(50)=6 nM),FLT3 (IC(50)=25 nM) and RET (IC(50)=17 nM) kinases,with significantly less activity against other tyrosine kinases including JAK3 (IC(50)=169 nM). TG101209 inhibited growth of Ba/F3 cells expressing JAK2V617F or MPLW515L mutations with an IC(50) of approximately 200 nM. In a human JAK2V617F-expressing acute myeloid leukemia cell line,TG101209-induced cell cycle arrest and apoptosis,and inhibited phosphorylation of JAK2V617F,STAT5 and STAT3. Therapeutic efficacy of TG101209 was demonstrated in a nude mouse model. Furthermore,TG101209 suppressed growth of hematopoietic colonies from primary progenitor cells harboring JAK2V617F or MPL515 mutations.
Efficacy of TG101348, a selective JAK2 inhibitor, in treatment of a murine model of JAK2V617F-induced polycythemia vera.
Cancer cell 2008
Abstract
We report that TG101348,a selective small-molecule inhibitor of JAK2 with an in vitro IC50 of approximately 3 nM,shows therapeutic efficacy in a murine model of myeloproliferative disease induced by the JAK2V617F mutation. In treated animals,there was a statistically significant reduction in hematocrit and leukocyte count,a dose-dependent reduction/elimination of extramedullary hematopoiesis,and,at least in some instances,evidence for attenuation of myelofibrosis. There were no apparent toxicities and no effect on T cell number. In vivo responses were correlated with surrogate endpoints,including reduction/elimination of JAK2V617F disease burden assessed by quantitative genomic PCR,suppression of endogenous erythroid colony formation,and in vivo inhibition of JAK-STAT signal transduction as assessed by flow cytometric measurement of phosphorylated Stat5.
Specificity and mechanism-of-action of the JAK2 tyrosine kinase inhibitors ruxolitinib and SAR302503 (TG101348).
Leukemia 2014
Abstract
更多信息
| 物种 | 人, 其它物种, 大鼠, 小鼠, 非人灵长类 |
|---|---|
| Cas Number | 936091-26-8 |
| Chemical Formula | C₂₇H₃₆N₆O₃S |
| 纯度 | ≥ 98% |
| Target | JAK2 |
| Pathway | JAK/STAT |
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