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CC-90011

    
10mM in DMSO

CC-90011

源叶(MedMol)
V51078 一键复制产品信息
2097523-60-7
C30H29F2N5O5S
609.64
Pulrodemstat benzenesulfonate
货号 规格 价格 上海 北京 珠海 重庆 武汉 购买数量
V51078-1ml
10mM in DMSO

¥1210.00

货期:3-5天 - - - -
产品介绍 参考文献 质检证书(COA) 摩尔浓度计算器 相关产品
产品描述:

CC-90011 benzenesulfonate is a potent, selective, reversible and orally active inhibitor of lysine specific demethylase-1 (LSD1) with an IC50 of 0.25 nM. CC-90011 benzenesulfonate is less enzymatic inhibition against LSD2, MOA-A, and MAO-B. CC-90011 benzenesulfonate induces acute myeloid leukemia (AML) and small cell lung cancer (SCLC) cells differentiation and has potent anticancer activity

靶点: IC50: 0.25 nM (LSD1)
体内研究: 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].CC-90011 (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.After i.v. administration, CC-90011 (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. CC-90011 (Compound 11; 5 mg/kg) is readily absorbed after oral administration with an AUC0-24h of 1.8 μM·h, C/sub>max of 0.36 μM, and oral bioavailability of 32%. Animal Model: BALB/c nude mice bearing small cell lung carcinoma (SCLC) 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.
参考文献: 1. Toufike Kanouni, et al. Discovery of CC-90011: A Potent and Selective Reversible Inhibitor of Lysine Specific Demethylase 1 (LSD1). J Med Chem. 2020 Dec 10;63(23):14522-14529.
溶解性: Soluble  in  DMSO
保存条件: -80℃(运输条件:冰袋低温运输)
配置溶液浓度参考:
1mg 5mg 10mg
1 mM 1.64 ml 8.202 ml 16.403 ml
5 mM 0.328 ml 1.64 ml 3.281 ml
10 mM 0.164 ml 0.82 ml 1.64 ml
50 mM 0.033 ml 0.164 ml 0.328 ml
注意: 部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。

参考文献

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