| Bioactivity | XYD198 (Compound 14h) is an orally active degrader for CBP/p300. XYD198 inhibits CBP/p300 bromodomain with IC50 of 213.5 nM. XYD198 exhibits antitumor activity against acute myeloid leukemia. (Structure: Pink, CBP/p300 ligand 4 (HY-161495); Blue, E3 ligase ligand (HY-14658); Black: linker (HY-161499))[1] |
| Invitro | XYD198 (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 0.9，47 和 5.5 nM[1]。XYD198 (0-150 nM，6 h) CRBN 和蛋白酶体依赖地诱导溴结构域蛋白家族中 CBP 和 p300 的降解i[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> XYD198 相关抗体: Cell Proliferation Assay[1] Cell Line: |
| In Vivo | CBP/p300 ligand 4 (5 mg/kg，口服，每 2 天一次，共 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 93%[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: |
| Formula | C54H49F2N11O7 |
| Molar Mass | 1002.03 |
| 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. |