ASR-490

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。

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10mg

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货号: ajcf19110
CAS: 2690312-67-3
别名:
分子式: C34H41NO7
分子量: 575.69
纯度: >98%
溶解度: DMSO : 25 mg/mL (43.43 mM; Need ultrasonic)
储存: Store at -20°C
库存: 现货

Background

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 (IC₅₀ =750 nM in HCT116 cells, IC₅₀ =1.2 µM in SW620 cells) and 48h (IC₅₀ =600 nM in HCT116 cells, IC₅₀ =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 (IC₅₀ =750 nM in HCT116 cells, IC₅₀ =1.2 µM in SW620 cells) and 48h (IC₅₀ =600 nM in HCT116 cells, IC₅₀ =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 PARPExpression, 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 atmic nude mice (nu/nu) (pCMV/HCT116and 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.