Epacadostat (Synonyms: INCB 024360)
目录号: PL04502 纯度: ≥99%
CAS No. :1204669-58-8
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中文名称
Epacadostat
中文别名
Epacadostat (INCB024360) 抑制剂;艾卡哚司他;500mg年底促销,8折;[C(Z)]-4-[[2-[(氨基磺酰基)氨基]乙基]氨基]-N-(3-溴-4-氟苯基)-N'-羟基-1,2,5-恶二唑-3-甲脒
英文名称
Epacadostat
英文别名
HY-15689;Epacadostat;INCB-24360(INCB-024360);Epacadostat (INCB024360);IDO inhibitor 1;INCB024360;INCB-024360;INCB-24360;INCB 024360;Epacadostat(INCB 024360);AK174791;71596A9R13;N-(3-bromo-4-fluorophenyl)-N'-hydroxy-4-{[2-(sulfamoylamino)ethyl]amino}-1,2,5-oxadiazole-3-carboximidamide;Epacadostat [USAN:INN];Epacadostat; INCB024360;Epacadostat (JAN/USAN/INN);GTPL8221;FBKMWOJEPMPVTQ-UHFFFAOYSA-N;INCB 24360;BDBM222999;BCP1
Cas No.
1204669-58-8
分子式
C11H13BrFN7O4S
分子量
438.23
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
Epacadostat (INCB 024360) 是一种有效,选择性的 IDO1 抑制剂, IC50 为 71.8 nM。
生物活性
Epacadostat (INCB 024360) is a potent and selective indoleamine 2,3-dioxigenase 1 (IDO1) inhibitor with an IC 50 of 71.8 nM.
性状
Solid
IC50 & Target[1][2]
IDO1 71.8 nM (IC50)
体外研究(In Vitro)
In cellular assays, Epacadostat (INCB 024360) selectively inhibits human IDO1 with IC50 values of approximately 10 nM, demonstrating little activity against other related enzymes such as IDO2 or tryptophan 2,3-dioxygenase (TDO). Epacadostat (INCB 024360) also exhibits significant activity toward mouse IDO1, with an IC50 value of 52.4 nM±15.7 nM, in a similar assay using mouse IDO1-transfected HEK293/MSR cells. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
Female Balb/c mice bearing CT26 tumors are treated orally twice daily for 12 d with Epacadostat at 100 mg/kg. Epacadostat (INCB 024360) suppresses kynurenine equivalently in plasma, tumors, and lymph nodes. In na?ve C57BL/6 mice, 50 mg/kg Epacadostat (INCB 024360) decreases plasma kynurenine levels within 1 hour and those levels stay at least 50% suppressed through the 8-hour time course. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
ClinicalTrial
参考文献
[1]. Liu X, et al. Selective inhibition of IDO1 effectively regulates mediators of antitumor immunity. Blood. 2010 Apr 29;115(17):3520-30.
[2]. Koblish HK, et al. Hydroxyamidine inhibitors of indoleamine-2,3-dioxygenase potently suppress systemic tryptophan catabolism and the growth of IDO-expressing tumors. Mol Cancer Ther. 2010 Feb;9(2):489-98.
溶解度数据
In Vitro: DMSO : 100 mg/mL (228.19 mM; Need ultrasonic)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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