2316817-88-4
中文名稱
CB-6644
英文名稱
CB-6644
CAS
2316817-88-4
分子式
C29H34ClFN4O5
分子量
573.06
MOL 文件
2316817-88-4.mol
更新日期
2023/03/20 15:41:25
2316817-88-4 結(jié)構式
物理化學性質(zhì)
密度1.34±0.1 g/cm3(Predicted)
儲存條件-20°C儲存
溶解度DMSO:100.0(Max Conc. mg/mL);174.5(Max Conc. mM)
酸度系數(shù)(pKa)13.13±0.20(Predicted)
形態(tài)固體
顏色White to light yellow
常見問題列表
生物活性
CB-6644 一種選擇性的 RUVBL1/2 復合體抑制劑。抑制 RUVBL1/2 的 ATP 酶活性，IC50 為 15 nM。具有抗癌活性。體外研究
CB-6644 (20 μM) interacts with the RUVBL1/2 complex in Ramos cells.
CB-6644 (0.001-10 μM; 72 hours) potently kills 123 cell lines (including HCT116, NCI-1975, and HT29 cells) with an EC
50
range of 41 to 785 nM.
Cell Viability Assay
| Cell Line: | 123 cell lines such as HCT116, NCI-1975, and HT29 cells |
| Concentration: | 0.001, 0.01, 0.1, 1, and 10 μM |
| Incubation Time: | 72 hours |
| Result: | Potently killed cells with an EC 50 range of 41 to 785 nM. |
體內(nèi)研究
CB-6644 (150 mg/kg, oral administration, 10 days of treatment for SCID-beige mice bearing Ramos xenograft models, 30 days of treatment for SCID-beige mice bearing RPMI8226 xenograft models) has antitumor activity in xenograft tumor models with tumor growth inhibitions (TGIs) of 68 and 81%, respectively in Ramos xenograft models and RPMI8226 xenograft models.
| Animal Model: | SCID-beige mice bearing human tumor xenografts derived from either Burkitt’s lymphoma (Ramos) or multiple myeloma (RPMI8226) cell lines |
| Dosage: | 150 mg/kg |
| Administration: | Oral gavage once (qd) or twice (BID) daily, 10 days of treatment for Ramos, 30 days of treatment for RPMI8226 |
| Result: | There was no significant bodyweight loss in mice. TGI of 68 and 81% in Ramos and RPMI8226, respectively. |