CB-6644

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

CB-6644 是 RUVBL1/2 复合物的选择性抑制剂，可阻断 RUVBL1/2 的 ATP 酶活性 (IC50 = 15 nM)。

CB-6644 is a selective inhibitor of the RUVBL1/2 complex and blocks the ATPase activity of RUVBL1/2 (IC50 = 15 nM).(In Vitro):CB-6644 (20 μM) interacts with the RUVBL1/2 complex in Ramos cells. In 123 cell lines such as HCT116, NCI-1975, and HT29 cells, CB-6644 (0.001-10 μM; 72 hours) potently kills 123 cell lines (EC50: 41 to 785 nM).(In Vivo):Administration of oral gavage once (qd) or twice (BID) daily, 10 days of treatment for Ramos, 30 days of treatment for RPMI8226, CB-6644 has antitumor activity in xenograft tumor models. The tumor growth inhibitions (TGIs) are 68 and 81%, respectively in Ramos xenograft models and RPMI8226 xenograft models.

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 EC50 range of 41 to 785 nM.

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.

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Others

Other Targets

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2316817-88-4

573.06

C29H34ClFN4O5

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (174.50 mM)

CCOc1cc(F)c(Cl)cc1C(=O)NCC(C)(C)CC(=O)Nc1c(COC)n2CCCc3ccccc3-n2c1=O

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(-20℃)

With Ice Pack

≥ 2 years