|
ChemicalBook Optimization Suppliers |
| 名前: |
BOC Sciences |
| 電話番号: |
1-631-485-4226; 16314854226 |
| 電子メール: |
info@bocsci.com |
|
| 化学名: | Chb-M′ | | 英語化学名: | CB-6644 | | 别名: | CB-6644;CB-6644
(CB6644;Chb-M';CB6644,CB-6644,Inhibitor,CB 6644,inhibit;Benzamide, 5-chloro-N-[4-[[6,7-dihydro-3-(methoxymethyl)-1-oxo-1H,5H-pyrazolo[1,2-a][1,2]benzodiazepin-2-yl]amino]-2,2-dimethyl-4-oxobutyl]-2-ethoxy-4-fluoro-;5-Chloro-2-ethoxy-4-fluoro-N-(4-((3-(methoxymethyl)-1-oxo-6,7-dihydro-1H,5H-benzo[c]pyrazolo[1,2-a][1,2]diazepin-2-yl)amino)-2,2-dimethyl-4-oxobutyl)benzamide;CB-6644, 10 mM in DMSO | | CAS番号: | 2316817-88-4 | | 分子式: | C29H34ClFN4O5 | | 分子量: | 573.06 | | EINECS: | | | カテゴリ情報: | | | Mol File: | 2316817-88-4.mol |  |
| 比重(密度) | 1.34±0.1 g/cm3(Predicted) | | 貯蔵温度 | Store at -20°C | | 溶解性 | DMSO:100.0(Max Conc. mg/mL);174.5(Max Conc. mM) | | 外見 | A solid | | 酸解離定数(Pka) | 13.13±0.20(Predicted) | | 色 | White to light yellow |
| | Chb-M′ Usage And Synthesis |
| 使用 | CB-6644 is a selective inhibitor of RUVBL1/2 complex with anti-cancer activity. CB-6644 blocks the ATPase activity of RUVBL1/2 with an IC50 of 15 nM[1]. | | 生物活性 | CB-6644 is a selective RUVBL1/2 complex inhibitor. It inhibits the ATPase activity of RUVBL1/2 with IC50 of 15 nM; it also has anticancer activity. | | in vitro | 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. | | | in vivo | 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: < /td> | 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. | | | 参考文献 | [1] Assimon VA, et al. CB-6644 Is a Selective Inhibitor of the RUVBL1/2 Complex with Anticancer Activity. ACS Chem Biol. 2019 Feb 15;14(2):236-244. DOI:10.1021/acschembio.8b00904 |
|