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  • 化合物 ASP-5878|T5473|TargetMol

化合物 ASP-5878|T5473|TargetMol

ASP5878
1453208-66-6
619 1mg 起订
1650 5mg 起订
2480 10mg 起订
上海 更新日期:2024-09-29

TargetMol中国(陶术生物)

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联系人:邵小姐
手机:4008200310 拨打
邮箱:marketing@tsbiochem.com

产品详情:

中文名称:
化合物 ASP-5878
英文名称:
ASP5878
CAS号:
1453208-66-6
品牌:
TargetMol
产地:
美国
保存条件:
Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
纯度规格:
99.86%
产品类别:
抑制剂
货号:
T5473

Product Introduction

Bioactivity

名称ASP5878
描述ASP5878 potently inhibited the tyrosine kinase activities of recombinant FGFR1, 2, 3, and 4 with IC50 values of 0.47, 0.60, 0.74, and 3.5 nmol/L.
细胞实验The human HCC cell lines,?The experiments were conducted using low-passage cultures of these stocks.?The cells were seeded in 96-well plates and incubated overnight.?The cells were treated with ASP5878 for 5 days.?Cell viability was measured using CellTiter-Glo.
激酶实验Inhibitory activities of 128 serine/threonine kinases were measured using the Mobility Shift Assay Kit.?IC50 values were determined for kinases that were inhibited by more than 50% by 200 nmol/L of ASP5878.
动物实验HuH-7-Luc cells were inoculated into hepatic parenchyma at 3×10^5 cells/0.01 mL (Matrigel 100%)/mouse.?One week after inoculation, the mice were divided into three groups (n = 5 per group) on day 0 on the basis of bioluminescent imaging.?Vehicle (Cremophor EL/ethanol or 0.5% MC), sorafenib (30 mg/kg), or ASP5878 (3 mg/kg) was administered as a once-daily oral dose for 91 days.?Tumor growth was monitored by in vivo bioluminescent imaging of the abdomen after intraperitoneally injecting luciferin using IVIS-Lumina2.?During the study period (181 days), the survival of mice bearing hepatic tumors was recorded.?The condition of the mice was monitored daily.?The mice were scored as dead if any of the following signs of suffering were observed: cachexia, weakening, and difficulty in moving or eating.?Mice that were scored as dead were euthanized.
体内活性sorafenib administration for 14 days caused 40% tumor growth inhibition in the Hep3B2.1-7 xenograft model. Even after continuous sorafenib treatment, the Hep3B2.1-7 tumor gradually enlarged, and 47% tumor growth inhibition was observed by day 31. In contrast, the switch from sorafenib to ASP5878 on day 14 induced 83% tumor regression on day 52 relative to the tumor size observed on day 14. This indicates the therapeutic potential of ASP5878 for FGF19-overexpressing HCC patients who previously received sorafenib treatment.
存储条件Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度DMSO : 250 mg/mL (613.69 mM)
关键字ASP5878 | Inhibitor | FGFR | ASP 5878 | Fibroblast growth factor receptor | inhibit
相关产品Ponatinib | AZD4547 | Amlexanox | Lenvatinib | Formononetin | Lenvatinib mesylate | Ferulic Acid | Pazopanib | Nintedanib | Pemigatinib | Erdafitinib | Nintedanib esylate
相关库抑制剂库 | 抗癌活性化合物库 | 经典已知活性库 | 已知活性化合物库 | 激酶抑制剂库 | 膜蛋白靶向化合物库 | 药物功能重定位化合物库 | 酪氨酸激酶分子库 | 抗癌临床化合物库 | 抗癌药物库
ASP-5878|TargetMol

公司简介

TargetMol Chemicals Inc. 总部位于马萨诸塞州波士顿,致力于为全球生化领域科学家的研究提供专业的产品和服务。TargetMol?品牌的客户群分布于40多个国家和地区,已发展成为全球知名的化合物库和小分子化合物研究供应商。 TargetMol?可提供160多种满足不同需求的化合物库,以及多种类型的生化试剂产品,包括12000多种抑制剂、16000多种天然产物和各类多肽、抗体、生命科学试剂盒等,此外,我们还建设有CADD(计算机辅助药物设计)研究中心、药理实验室、药化合成平台三大技术中心,全方位满足客户的定制需求。 凭借我们优质的产品和服务、快速高效的全球供应链和专业的技术支持,我们将有效帮助您缩短研发周期,取得更成功的结果。

成立日期 (12年)
注册资本 566.265100万人民币
员工人数 100-500人
年营业额 ¥ 1亿以上
经营模式 贸易,工厂,试剂,定制,服务
主营行业 天然产物,生化试剂,分子生物学,分子砌块,生物技术服务

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