| Bioactivity | YCH1899 is an orally active PARP inhibitor, with an IC50< 0.001 nM for PARP1/2. YCH1899 exhibits distinct antiproliferation activity against Olaparib (HY-10162)-resistant and Talazoparib (HY-16106)-resistant Capan-1 cells (Capan-1/OP and Capan-1/TP cells) , with IC50 values of 0.89 and 1.13 nM, respectively. YCH1899 has acceptable pharmacokinetic properties in rats[1]. |
| Invitro | YCH1899 (7天) 对Capan-1、Capan-1/OP、Capan-1/TP 细胞表现出明显的抗增殖活性，IC50 分别为0.10、0.89、1.13 nM[1]。YCH1899 (0.001-1 nM, 4 h) 稳定PARP1-DNA复合物，抑制PARP的形成[1]。YCH1899 (3.5 h) 对BRCA突变/野生型细胞 (V−C8, V79, HCT-15, HCC1937) 的增殖有抑制作用, IC50s 范围为1.19-44.24 nM[1]。YCH1899 (1 μM, 24 h) 在 Capan-1、Capan-1/OP、Capan-1/TP 细胞中诱导 DNA 损伤，使 γH2AX 数量大量增加[1]。YCH1899 (1 μM, 48 h) 在 U2OS-DR-GFP 细胞中诱导 HR (Homologous Recombination, 同源重组) 修复活性显著降低[1]。 0 --> YCH1899 相关抗体: Cell Proliferation Assay[1] Cell Line: |
| In Vivo | YCH1899 (5 mg/kg, 静脉给药) 在大鼠中具有中等清除力[1]。 YCH1899在MDA-MB-436/OP (6.25, 12.5和25 mg/kg, 口服给药，每天一次，持续27天) 和Capan-1/R（12.5和25 mg/kg, 口服给药，每天一次，持续21天） 异种移植小鼠肿瘤模型中克服了Talazoparib耐药，肿瘤体积显著下降[1]。 Animal Model: |
| Name | YCH1899 |
| Formula | C25H18BrFN6O3 |
| Molar Mass | 549.35 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Sun Y, et al. YCH1899, a Highly Effective Phthalazin-1(2H)-one Derivative That Overcomes Resistance to Prior PARP Inhibitors. J Med Chem. 2023 Aug 21. |