| Description | ND-646 is an orally bioavailable and allosteric inhibitor of the ACC enzymes ACC1 and ACC2(IC50s of 3.5 nM and 4.1 nM for recombinant hACC1 and hACC2, respectively) |
| In vivo | ND-646是ACC酶ACC1和ACC2的非竞争性抑制剂，通过阻止ACC亚单位二聚体的形成来抑制体外和体内的脂肪酸合成。长期ND-646治疗移植瘤和基因工程小鼠模型的非小细胞肺癌(NSCLC)显示出抑制肿瘤生长的效果。无论是单独使用还是与标准治疗药物卡铂联合使用，ND-646在KRAS p53(Kras;Trp53-/-)和KRAS Lkb1(Kras;Stk11-/-)的非小细胞肺癌(NSCLC)小鼠模型中显著抑制了肺部肿瘤的生长。 |
| Target activity | ACC2 (human):4.1 nM , ACC1 (human):3.5 nM |
| molecular weight | 568.64 |
| Molecular formula | C28H32N4O7S |
| CAS | 1434639-57-2 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 95 mg/mL (167.06 mM) |
| References | 1. Svensson RU, et al. Inhibition of acetyl-CoA carboxylase suppresses fatty acid synthesis and tumor growth of non-small-cell lung cancer in preclinical models. Nat Med. 2016 Oct;22(10):1108-1119. |