(Z)-Leukadherin-1 (Synonyms: ADH-503 free base)
目录号: PL04505 纯度: ≥98%
CAS No. :2055362-72-4
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中文名称
(Z)-Leukadherin-1
英文名称
(Z)-Leukadherin-1
英文别名
Leukadherin-1;Leukadherin 1;LA1;BDBM8427;C22H26Cl2N2O11;AOB4116;SYN5137;BCP18444;s8306;STL372026;4-(5-((3-Benzyl-4-oxo-2-thioxothiazolidin-5-ylidene)methyl)furan-2-yl)benzoic acid;(Z)-4-(5-((3-benzyl-4-oxo-2-thioxothiazolidin-5-ylidene)methyl)furan-2-yl)benzoic acid;4-[5-[[4-oxo-3-(phenylmethyl)-2-thioxo-5-thiazolidinylidene];ADH-503 free base;(Z)-Leukadherin-1
Cas No.
2055362-72-4
分子式
C22H15NO4S2
分子量
421.49
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
(Z)-Leukadherin-1 (ADH-503 free base) 是一种具有口服活性的,变构的 CD11b 激动剂。(Z)-Leukadherin-1 可以导致与肿瘤相关的巨噬细胞重新极化,减少肿瘤浸润性免疫抑制骨髓细胞的数量,并增强树突状细胞的反应。
生物活性
(Z)-Leukadherin-1 (ADH-503 free base) is an orally active and allosteric CD11b agonist. (Z)-Leukadherin-1 leads to the repolarization of tumor-associated macrophages, reduction in the number of tumor-infiltrating immunosuppressive myeloid cells, and enhances dendritic cell responses.
性状
Solid
IC50 & Target[1][2]
CD11b
体外研究(In Vitro)
(Z)-Leukadherin-1 (ADH-503 free base; 4 μM; 8 days) reduces the numbers of total tumor-infiltrating CD11b cells and subsets of CD11b monocytes, granulocytes, eosinophils, and macrophages. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
(Z)-Leukadherin-1 (ADH-503 free base; oral gavage; 30, 60, or 120 mg/kg; twice a day for 60 days) delayes tumor progression, leading to a significantly decreased tumor burden in time-point analysis and improved overall survival.
(Z)-Leukadherin-1 (oral gavage; 30, 100 mg/kg; twice a day; on days 1 and 5) has the mean half-life of 4.68 and 3.95 hours, a maximum concentration of 1716 and 2594 ng/ml and AUC0-t in the plasma of 6950 and 13962 ng.h/ml at 30 and 100 mg/kg dosing, respectively.
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
参考文献
[1]. Panni RZ, et al. Agonism of CD11b reprograms innate immunity to sensitize pancreatic cancer to immunotherapies. Sci Transl Med. 2019 Jul 3;11(499).
溶解度数据
In Vitro: DMSO : 4.55 mg/mL (10.80 mM; ultrasonic and warming and heat to 60°C)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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