Pulrodemstat
基本信息
产品名称：
Pulrodemstat
英文名称：
Pulrodemstat
国产/进口：
进口
产地/品牌：
美国/TargetMol
型号：
参考报价：
面议
销售商：
总点击数：
17
更新日期：
2025-05-27
产品类别：
性能参数
Product Introduction
Bioactivity
英文名: Pulrodemstat
描述: Pulrodemstat (CC-90011) is a highly potent and selective inhibitor of lysine specific demethylase-1 (LSD1). It exhibits a reversible mode of action and can be administered orally. With an impressive IC50 of 0.25 nM, Pulrodemstat effectively suppresses the enzymatic activity of LSD1. Notably, it demonstrates minimal inhibition against LSD2, MOA-A, and MAO-B enzymes. Moreover, Pulrodemstat possesses remarkable anticancer properties, promoting differentiation in acute myeloid leukemia (AML) and small cell lung cancer (SCLC) cells.
体外活性: Pulrodemstat (CC-90011, Compound 11) shows potent induction of on-target cellular differentiation marker CD11b in THP-1 cell line with an EC 50 of 7 nM, antiproliferative activity in AML kasumi-1 cells with an EC 50 of 2 nM[1]. Suppression of GRP is observed with treatment of Pulrodemstat (4 days) in a dose-dependent manner and at pharmacologically useful concentrations (EC 50 =3 nM, H209 and 4 nM, H1417). Pulrodemstat (12 days) treatment of SCLC cells results in potent antiproliferative activity (EC 50 =6 nM, H1417) that correlated with GRP suppression[1].
体内活性: Pulrodemstat (CC-90011; 5 mg/kg; oral administration; daily; for 30 days; for 30 days) treatment inhibits tumor growth in patient-derived xenograft SCLC models[1]. Pulrodemstat (once a day; for 4 days) treatment results in robust downregulation of GRP mRNA levels at 2.5 mg/kg and maximum suppression of GRP at 5 mg/kg in a SCLC human tumor xenograft (H1417) mice[1]. After i.v. administration, Pulrodemstat (Compound 11; 5 mg/kg) has systemic clearance of 32.4 mL/min/kg, elimination half-life of 2 h, and a high volume of distribution of 7.5 L/kg. Pulrodemstat (Compound 11; 5 mg/kg) is readily absorbed after oral administration with an AUC 0-24h of 1.8 μM·h, C/sub>max of 0.36 μM, and oral bioavailability of 32%[1]. Animal Model: BALB/c nude mice bearing small cell lung carcinoma (SCLC)[1]Dosage: 5 mg/kg Administration: Oral administration; daily; for 30 days Result: Showed a tumor growth inhibition (TGI) of 78% at 5 mg/kg with no body weight loss.
存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year
关键字: CC90011 | Pulrodemstat | CC 90011
Bioactivity
英文名: Pulrodemstat
描述: Pulrodemstat (CC-90011) is a highly potent and selective inhibitor of lysine specific demethylase-1 (LSD1). It exhibits a reversible mode of action and can be administered orally. With an impressive IC50 of 0.25 nM, Pulrodemstat effectively suppresses the enzymatic activity of LSD1. Notably, it demonstrates minimal inhibition against LSD2, MOA-A, and MAO-B enzymes. Moreover, Pulrodemstat possesses remarkable anticancer properties, promoting differentiation in acute myeloid leukemia (AML) and small cell lung cancer (SCLC) cells.
体外活性: Pulrodemstat (CC-90011, Compound 11) shows potent induction of on-target cellular differentiation marker CD11b in THP-1 cell line with an EC 50 of 7 nM, antiproliferative activity in AML kasumi-1 cells with an EC 50 of 2 nM[1]. Suppression of GRP is observed with treatment of Pulrodemstat (4 days) in a dose-dependent manner and at pharmacologically useful concentrations (EC 50 =3 nM, H209 and 4 nM, H1417). Pulrodemstat (12 days) treatment of SCLC cells results in potent antiproliferative activity (EC 50 =6 nM, H1417) that correlated with GRP suppression[1].
体内活性: Pulrodemstat (CC-90011; 5 mg/kg; oral administration; daily; for 30 days; for 30 days) treatment inhibits tumor growth in patient-derived xenograft SCLC models[1]. Pulrodemstat (once a day; for 4 days) treatment results in robust downregulation of GRP mRNA levels at 2.5 mg/kg and maximum suppression of GRP at 5 mg/kg in a SCLC human tumor xenograft (H1417) mice[1]. After i.v. administration, Pulrodemstat (Compound 11; 5 mg/kg) has systemic clearance of 32.4 mL/min/kg, elimination half-life of 2 h, and a high volume of distribution of 7.5 L/kg. Pulrodemstat (Compound 11; 5 mg/kg) is readily absorbed after oral administration with an AUC 0-24h of 1.8 μM·h, C/sub>max of 0.36 μM, and oral bioavailability of 32%[1]. Animal Model: BALB/c nude mice bearing small cell lung carcinoma (SCLC)[1]Dosage: 5 mg/kg Administration: Oral administration; daily; for 30 days Result: Showed a tumor growth inhibition (TGI) of 78% at 5 mg/kg with no body weight loss.
存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year
关键字: CC90011 | Pulrodemstat | CC 90011
公司简介
TargetMol（陶术）作为一家全球性的生物医药领域高科技企业，我们致力于为高校、研究所、医院、企业等各类生物医药研发机构提供优质的产品和服务，为全球医药科学家更高效地完成科研工作助力。可提供20,000+种 抑制剂和激动剂 、800+种 化合物库 、19,000+种 天然产物 ，以及9,000+种 重组蛋白 、多种 多肽 、抗体 和 生命科学试剂盒 等。此外，在上海，TargetMol研发中心配备了 CADD & AIDD研究中心、药理实验室和药物化学合成 平台三大技术中心，可提供虚拟筛选、化合物活性测试、分子间结合力检测和化合物结构优化等技术服务，多方位满足用户的研发需求。
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