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CAS No. : 2097523-60-7
MCE 国际站:Pulrodemstat benzenesulfonate
产品活性:CC-90011 benzenesulfonate 是一种有效的,选择性的,可逆的和具有口服活性的赖氨酸特异性脱甲基酶-1 (LSD1) 抑制剂,IC50 为 0.25 nM。CC-90011 benzenesulfonate 对 LSD2,MOA-A 和 MAO-B 的酶抑制作用较小。CC-90011 benzenesulfonate 诱导急性髓细胞性白血病 (AML)和小细胞肺癌 (SCLC) 细胞分化,并具有有效的抗癌活性。
研究领域:Epigenetics
作用靶点:Histone Demethylase
In Vitro: CC-90011 (Compound 11) shows potent induction of on-target cellular differentiation marker CD11b in THP-1 cell line with an EC50 of 7 nM, antiproliferative activity in AML kasumi-1 cells with an EC50 of 2 nM.
Suppression of GRP is observed with treatment of CC-90011 (4 days) in a dose-dependent manner and at pharmacologically useful concentrations (EC50=3 nM, H209 and 4 nM, H1417). CC-90011 (12 days) treatment of SCLC cells results in potent antiproliferative activity (EC50=6 nM, H1417) that correlated with GRP suppression.
In Vivo: CC-90011 (5 mg/kg; oral administration; daily; for 30 days) treatment inhibits tumor growth in patient-derived xenograft SCLC models.
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%.
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