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  • TG101348(SAR302503)

    • Fedratinib;SAR 302503;TG-101348;TG 101348
    货号: abs812216
    CAS号: 936091-26-8
    分子式: C27H36N6O3S
    分子量: 524.68
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    货号-规格 货期 价格 数量
    abs812216-5mg 现货 ¥750.00
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    abs812216-10mg 现货 ¥1313.00
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    abs812216-25mg 现货 ¥2514.00
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    abs812216-50mg 现货 ¥3386.00
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    大包装询价
    产品描述
    描述

    Fedratinib (SAR302503, TG101348)是一种选择性JAK2抑制剂,在无细胞试验中IC50为3 nM,作用于JAK2比作用于JAK1和JAK3选择性高35和334倍。

    纯度
    >98%
    储存/保存方法
    Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
    基本信息
    别名
    Fedratinib;SAR 302503;TG-101348;TG 101348
    外观
    off-white powder
    可溶性/溶解性
    DMSO : 93 mg/mL (177.3 mM)
    生物活性
    靶点
    JAK2;JAK2 (V617F);FLT3;RET
    In vitro(体外研究)
    TG-101348 also significantly inhibits JAK2 V617F, Flt3, and Ret with IC50 of 3 nM, 15 nM, and 48 nM, respectively. TG101348 has an IC50 ~300-fold higher for the closely related JAK3 and is a less potent inhibitor of the JAK1 and TYK2 family members. TG101348 inhibits proliferation of a human erythroblast leukemia (HEL) cell line that harbors the JAK2V617F mutation, as well as a murine pro-B cell line expressing human JAK2V617F (Ba/F3 JAK2V617F), with IC50 of 305 nM and 270 nM, respectively. TG-101348 also inhibits proliferation of parental Ba/F3 cells to a comparable level, with IC50 of ~420 nM. TG101348 treatment reduces STAT5 phosphorylation at concentrations that parallel the concentrations required to inhibit cell proliferation. TG101348 induces apoptosis in both HEL and Ba/F3 JAK2V617F cells in a dose-dependent manner. TG101348 does not show proapoptotic activity in control normal human dermal fibroblasts at concentrations up to 10 μM, and the antiproliferative IC50 against fibroblasts is >5 μM. TG101348 treatment decreases GATA-1 expression, which is associated with erythroid-skewing of JAK2V617F+ progenitor differentiation, and inhibits STAT5 as well as GATA S310 phosphorylation. TG101348 inhibits the proliferation of HMC-1.1 (KITV560G) cells, with somewhat lower potency than HMC-1.2 (KITD816V, KITV560G) cells, with IC50 of 740 nM and 407 nM, respectively.
    In vivo(体内研究)
    TG101348 has potential for efficacious treatment of JAK2V617F-associated myeloproliferative diseases (MPD). In treated animals, there is 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, correlated with surrogate endpoints, including reduction/elimination of JAK2V617F disease burden, suppression of endogenous erythroid colony formation, and in vivo inhibition of JAK-STAT signal transduction. There are no apparent toxicities and no effect on T cell number. Oral administration of TG101348 (120 mg/kg) significantly inhibits PV progenitor erythroid differentiation in vivo.
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    参考文献
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