CB-6644

生物活性体外研究体内研究 CB-6644 试剂级价格

CB-6644

CAS号:2316817-88-4
英文名:CB-6644
中文名:CB-6644
CBNumber:CB24844617
分子式:C29H34ClFN4O5
分子量:573.06
MOL File:2316817-88-4.mol

CB-6644化学性质

密度 :1.34±0.1 g/cm3(Predicted)
储存条件 :Store at -20°C
溶解度 :DMSO:100.0(Max Conc. mg/mL);174.5(Max Conc. mM)
形态 :A solid
酸度系数(pKa) :13.13±0.20(Predicted)
颜色 :White to light yellow

CB-6644性质、用途与生产工艺

生物活性 CB-6644 一种选择性的 RUVBL1/2 复合体抑制剂。抑制 RUVBL1/2 的 ATP 酶活性，IC50 为 15 nM。具有抗癌活性。

体外研究

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.

体内研究

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.