耗材描述
Sulanemadlin
产品活性:Sulanemadlin (ALRN-6924) 是一种可穿透细胞膜的,基于 p53 的强效拟肽大环。Sulanemadlin 是 p53-MDM2,p53-MDMX,或 p53 和 MDM2 和 MDMX 蛋白-蛋白相互作用的抑制剂。Sulanemadlin 可用于癌症研究。
产品来源: https://www.medchemexpress.cn/sulanemadlin.html
研究领域:Apoptosis
作用靶点:MDM-2/p53
In Vitro: Sulanemadlin (0-10 μM, 24 h) induces reversible, dose-dependent cell cycle arrest in CD34+ human bone marrow cells, and protects cells from Topotecan (HY-13768)-induced DNA damage.
In Vivo: Sulanemadlin (5-20 mg/kg, i.v.) shows antitumor activity in multiple TP53-WT subcutaneous mouse xenograft models.
Sulanemadlin (2.4 mg/kg, daily with for 5 days, 24 h prior to daily 1.5 mg/kg Topotecan) protects mice against Topotecan-induced neutropenia and gastrointestinal toxicity in mice, without diminishing Topotecan antitumor activity in TP53-mutant cancer models.
PK properties of Sulanemadlin.
Species
Dose (mg/kg)
Cmax (μg/mL)
AUCall (μg·h/mL)
T1/2 (h)
CL (mL/h/kg)
Mouse
5
67.8
450
2.2
11
Rat
5
95.9
223
2.0
24
Monkey
5
137
914
4.9
5.9
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