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  • 化合物 SAR125844|T5467|TargetMol

化合物 SAR125844|T5467|TargetMol

SAR125844
1116743-46-4
315 1mg 起订
745 5mg 起订
1180 10mg 起订
上海 更新日期:2024-12-12

TargetMol中国(陶术生物)

VIP3年
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 SAR125844
英文名称:
SAR125844
CAS号:
1116743-46-4
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:
98.39%
产品类别:
抑制剂
货号:
T5467

Product Introduction

Bioactivity

名称SAR125844
描述SAR125844, a potent and highly selective inhibitor of the MET receptor tyrosine kinase (RTK), for intravenous administration. (IC50 value of 4.2 nmol/L)
细胞实验MKN-45, Hs 746T, and SNU-5 cells were seeded in poly d-lysine 96-well plates in complete medium.?Plates were incubated with increasing SAR125844 concentrations for 1 hour, cell lysates were generated using standard procedures and pMETY1230/1234/1235 level evaluated.?IC50 values were calculated using the Biost@t-SPEED internal software and a 4-parameter logistic model
激酶实验SAR125844 was preincubated at room temperature with each enzyme for 30 minutes in a buffer containing 10 mmol/L MOPS-NaOH pH 7.0, 0.01% Tween 20, and 1 mmol/L dithiothreitol. The enzymatic reactions were initiated by the addition of a mix of 1 ng/μL of a biotinylated poly(glutamate-alanine-tyrosine) peptide ATP and MgCl2. After 5-minute incubation at room temperature, the reactions were stopped by the addition of anti-phosphotyrosine monoclonal antibody (mAb) PT-66 -Europium cryptate and streptavidin 61SAXLB. After two hours at room temperature, the emission signals at 620 and 665 nm were recorded with a GENios reader, with an excitation wavelength of 320 nm. The percentage of inhibition versus nontreated sample was estimated using the emission ratios at 665/620 nm.
动物实验Long duration of MET kinase inhibition up to 7 days was achieved with a nanosuspension formulation of SAR125844.?Daily or every-2-days intravenous treatment of SAR125844 promoted a dose-dependent tumor regression in MET-amplified human gastric cancer models at tolerated doses without treatment-related body weight loss.
体外活性SAR125844在纳摩尔范围内,通过细胞实验抑制MET自磷酸化作用,并且在具有MET基因扩增或路径依赖的细胞系中,以低纳摩尔浓度选择性促进凋亡和抗增殖活性。
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 : 45 mg/mL (81.72 mM)
关键字Inhibitor | SAR-125844 | SAR-125884 | c-Met/HGFR | inhibit | Apoptosis | SAR 125884 | SAR 125844 | SAR125844
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SAR125884|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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