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是DHODH的新型，有效且口服可生物利用的抑制剂，可用于AML（急性骨髓性白血病）的相关研究。
| 基本信息 | |
| CAS | No.1035688-66-4 |
| 英文名称 | ASLAN003 |
| 别名 | LAS 186323 |
| 分子式 | C19H14F2N2O3 |
| 分子量 | 356.32 |
| 溶解性 | Soluble in DMSO |
| 纯度 | ≥98% |
| 外观(性状) | White to off-white Solid |
| 货期 | 1-2个工作日 |
| 储存条件 | Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year |
| SMILES | COC1=CC=CC(=C1)C2=CC(=C(C(=C2)F)NC3=C(C=CC=N3)C(=O)O)F |
| InChIKey | OMPATGZMNFWVOH-UHFFFAOYSA-N |
| InChI | InChI=1S/C19H14F2N2O3/c1-26-13-5-2-4-11(8-13)12-9-15(20)17(16(21)10-12)23-18-14(19(24)25)6-3-7-22-18/h2-10H,1H3,(H,22,23)(H,24,25) |
| PubChem CID | 24986824 |
| 靶点 | Dihydroorotate dehydrogenase (DHODH) |
| 通路 | Metabolic Enzyme&Protease |
| 背景说明 | ASLAN003是DHODH的新型,有效且口服可生物利用的抑制剂,可用于AmL(急性骨髓性白血病)的相关研究。 |
| 生物活性 | Farudodstat (ASLAN003) is an orally active and potent Dihydroorotate Dehydrogenase (DHODH) inhibitor with an IC50 of 35 nM for human DHODH enzyme. [1] |
| IC50 | IC50: 35 nM (human DHODH enzyme)[1] |
| In Vitro | Farudodstat (1， 2 μM; pretreatment 1 h before OPP for 1 h) inhibits protein synthesis， as demonstrated by the reduced incorporation of O-propargyl-puromycin (OPP) at protein translation sites in both MOLM-14 and KG-1 cells. Farudodstat causes the downregulation of EIF4B， and RPL6 proteins[1]. |
| 细胞实验 | Farudodstat (50 mg/kg; oral gavage; once daily; from the day 3 to 30) substantially reduces the number of disseminated tumors and prolongs survival[1]. |
| 数据来源文献 | [1]. Jianbiao Zhou， et al. ASLAN003， a potent dihydroorotate dehydrogenase inhibitor for differentiation of acute myeloid leukemia. Haematologica. 2019 Nov7;haematol.2019.230482. |
| 单位 | 支 |