ASR-490 通过下调Notch1信号传导降低 HCT116 和 SW620 细胞的活力。ASR-490 克服 Notch1 的过表达并抑制 HCT/Notch1 转染子的生长。ASR-490 在异种移植小鼠中抑制对照 (pCMV/HCT116) 和 Notch1/HCT116 的肿瘤生长。

ASR-490 reduces the viability of HCT116 and SW620 cells by downregulating Notch1 signaling. ASR-490 overcomes Notch1 overexpression and inhibits the growth of HCT/Notch1 transfectants. ASR-490 inhibits the tumor growth in control (pCMV/HCT116) and Notch1/HCT116 in xenotransplanted mice [1].

ASR-490 (0-1.6 μM; 24 h, 48 h) reduces the viability of HCT116 and SW620 cells in 24h (IC 50 =750 nM in HCT116 cells, IC 50 =1.2 μM in SW620 cells) and 48h (IC 50 =600 nM in HCT116 cells, IC 50 =850 nM in SW620 cells) [1]. ASR-490 (750 nM in HCT116 cells and 1.2 μM in SW620 cells, 24 h) shows apoptotic cell death and upregulation of the proapoptotic markers Bax and cleaved PARP Expression; inhibits the capability of colorectal cancer cells [1]. ASR-490 (HCT116 cells; 750 nM in 24 h, 600 nM in 48 h) overcomes Notch1 overexpression and inhibits the growth of HCT/Notch1 transfectants [1]. Cell Viability Assay [1] Cell Line: HCT116, SW620 cells Concentration: 0-1.6 μM Incubation Time: 24 h, 48 h Result: Reduced the viability of HCT116 and SW620 cells in 24h (IC 50 =750 nM in HCT116 cells, IC 50 =1.2 μM in SW620 cells) and 48h (IC 50 =600 nM in HCT116 cells, IC 50 =850 nM in SW620 cells). Apoptosis Analysis [1] Cell Line: HCT116, SW620 cells Concentration: 750 nM in HCT116 cells and 1.2 μM in SW620 cells Incubation Time: 24 h Result: Showed apoptotic cell death and upregulation the proapoptotic markers Bax and cleaved PARP Expression, inhibited the capability of colorectal cancer cells. Cell Proliferation Assay [1] Cell Line: HCT116 cells Concentration: 750 nM in 24 h, 600 nM in 48 h Incubation Time: 24 h, 48 h Result: Overcome Notch1 overexpression and inhibited the growth of HCT/Notch1 transfectants.

ASR-490 (5 mg/kg; i.p.; thrice a week for 4 weeks) inhibits the tumor growth in control (pCMV/HCT116) and Notch1/HCT116 in xenotransplanted mice [1]. Animal Model: Six- to 8-week-old BALB/c athymic nude mice (nu/nu) (pCMV/HCT116 and Notch1/HCT116 (C4) xenografts) [1]. Dosage: 5 mg/kg Administration: i.p., thrice a week for 4 weeks Result: Inhibited the tumor growth in control (pCMV/HCT116) and Notch1/HCT116 in xenotransplanted mice.

2690312-67-3

C34H41NO7

575.69

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years