CC-90011 Methylbenzenesulfonate 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 Methylbenzenesulfonate 对 LSD2，MOA-A 和 MAO-B 的酶抑制作用较小。CC-90011 Methylbenzenesulfonate 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。
| 生物活性 | CC-90011 Methylbenzenesulfonate is a potent, selective, reversible and orally active inhibitor oflysine specific demethylase-1 (LSD1)with anIC50of 0.25 nM. CC-90011 Methylbenzenesulfonate is less enzymatic inhibition against LSD2, MOA-A, andMAO-B. CC-90011 Methylbenzenesulfonate induces acute myeloid leukemia (AML) and small cell lungcancer(SCLC) cells differentiation and has potent anticancer activity[1]. |
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体外研究
(In Vitro) | CC-90011 (Compound 11) shows potent induction of on-target cellular differentiation marker CD11b in THP-1 cell line with an EC50of 7 nM, antiproliferative activity in AML kasumi-1 cells with an EC50of 2 nM[1].
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[1].
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体内研究
(In Vivo) | 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[1].
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 AUC0-24hof 1.8 μM·h, C/sub>maxof 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. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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