(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 allostericCD11bagonist. (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[1]. |
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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[1].
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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[1].
(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[1].
| Animal Model: | KPC mice [p48-CRE/Lox-stop-Lox(LSL)-KrasG12D/p53flox/flox][1] | | Dosage: | 30, 60, or 120 mg/kg | | Administration: | Oral gavage; 60 days | | Result: | Delayed tumor progression, leading to a significantly decreased tumor burden in time-point analysis and improved overall survival. |
| Animal Model: | Male rats[1] | | Dosage: | 30, 100 mg/kg (Pharmacokinetic Analysis) | | Administration: | Oral gavage twice a day; on days 1 and 5 | | Result: | Had 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. |
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| 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 | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 4.55 mg/mL(10.80 mM;ultrasonic and warming and heat to 60℃) 配制储备液 | 1 mM | 2.3725 mL | 11.8627 mL | 23.7254 mL | | 5 mM | 0.4745 mL | 2.3725 mL | 4.7451 mL | | 10 mM | 0.2373 mL | 1.1863 mL | 2.3725 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 |
