| Bioactivity | XYD190 (Compound 14g) is an orally active degrader for CBP/p300. XYD190 inhibits CBP/p300 bromodomain with IC50 of 483.7 nM. XYD190 exhibits antitumor activity against acute myeloid leukemia. (Structure: Pink, CBP/p300 ligand 4 (HY-161495); Blue, E3 ligase ligand (HY-14658); Black: linker (HY-161496))[1]. |
| Invitro | XYD190 (0-1 μM，72-120 h) 抑制急性髓系白血病 (AML) 细胞 MV4;11，MOLM-13 和 MOLM-16 的增殖，IC50 分别为 1.8、26.9 和 4.6 nM[1]。XYD190 (0-150 nM，6 h) CRBN 和蛋白酶依赖地诱导溴结构域蛋白家族中 CBP 和 p300 的降解[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> XYD190 相关抗体: Cell Proliferation Assay[1] Cell Line: |
| In Vivo | CBP/p300 ligand 4 (5 mg/kg，口服，两天一次，持续 2 周) 在 MV4;11 异种移植小鼠模型中表现出抗肿瘤活性，肿瘤生长抑制率 TGI 为 88%[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: |
| Formula | C55H50F2N10O7 |
| Molar Mass | 1001.05 |
| 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]. Hu J, et al., Discovery of Highly Potent and Efficient CBP/p300 Degraders with Strong In Vivo Antitumor Activity. J Med Chem. 2024 May 9;67(9):6952-6986. |