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  • 化合物 PND-1186|T1950

化合物 PND-1186|T1950

PND-1186
1061353-68-1
297 2mg 起订
492 5mg 起订
759 10mg 起订
上海 更新日期:2024-09-15

TargetMol中国(陶术生物)

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产品详情:

中文名称:
化合物 PND-1186
英文名称:
PND-1186
CAS号:
1061353-68-1
品牌:
TargetMol
产地:
美国
保存条件:
store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
纯度规格:
≥98%
产品类别:
抑制剂
货号:
T1950

Product Introduction

Bioactivity

名称PND-1186
描述PND-1186 (VS-4718) is a reversible and specific FAK inhibitor (IC50: 1.5 nM).
细胞实验For soft agar assays, 48-well plates are coated with a 1:4 mix of 2% agar (EM Science) in 0.2 mL growth media (bottom layer). 5×104 cells are plated per well (in triplicate) in a mixture of 0.3% agar in 0.2 mL growth media (top layer). After agar solidification, 0.2 mL growth media is added containing DMSO or PND-1186 (final concentration for 0.6 mL). In separate experiments, PND-1186 is added after 4 days. After 10 days, colonies are imaged in phase contrast, enumerated by counting 9 fields (3 fields per well), and total area determined using Image J. For all analyses, experimental points are performed in triplicate and repeated at least two times. (Only for Reference)
激酶实验In vitro kinase activity: GST-FAK in vitro kinase activity is measured and compared to His-tagged FAK 411–686 using the K-LISA screening kit and poly(Glu:Tyr) (4:1) copolymer as a substrate immobilized on microtiter plates. IC50 values are determined with various concentrations of test compounds in a buffer containing 50 μM ATP and 10 mM MnCl2, 50 mM HEPES (pH 7.5), 25 mM NaCl, 0.01% BSA, and 0.1 mM Na orthovanadate for 5 min at room temperature. Serial diluted compounds are tested in triplicate. Substrate phosphorylation is measured using horseradish peroxidase-conjugated anti-pTyr antibodies with spetrophotometric color quantitation. IC50 values are determined using the Hill-Slope Model. Kinase selectivity profiling is performed by using the KinaseProfiler service.
体外活性在负荷4T1肿瘤的小鼠体内,PND-1186(100 mg/kg,s.c.)可诱导细胞凋亡,对4T1皮下肿瘤生长产生抑制作用.在负荷ID8肿瘤的小鼠体内,PND-1186(0.5 mg/mL,p.o.)还会抑制卵巢癌肿瘤的生长.
体内活性在体外,PND-1186对4T1乳腺癌能动性有抑制作用,且可促进悬浮状态的4T1凋亡,并使4T1软琼脂集落数量和大小减少。在HEY 和 OVCAR8细胞中,PND-1186促使G0-G1细胞周期阻滞,从而使细胞死亡。
存储条件store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度H2O : < 1 mg/mL (insoluble or slightly soluble)
Ethanol : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 23 mg/mL (45.9 mM)
关键字tumor | integrin | PTK2 | inhibit | Apoptosis | growth | Focal adhesion kinase | FAK | PTK2 protein tyrosine kinase 2 | PND-1186 | VS4718 | SR2516 | SR 2516 | survival | Inhibitor | cell | VS 4718
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VS-4718|||SR-2516|||PND1186|||PND 1186|TargetMol

公司简介

上海陶术生物科技有限公司为美国Target Molecule Corp. ( Target Mol ) 在上海建立的全资子公司。我们与美国波士顿、德国慕尼黑的同事一起,为北美、欧洲和亚洲从事药物研发和生物学研究的科学家提供优质的产品和专业的服务。公司下设筛选事业部,化学事业部,生物事业部和新材料部。 从虚拟筛选到实体化合物分子供应;从商业化产品销售到个性化定制合成;从对明确靶点的分子筛选到对明确分子的多靶点筛选,从高通量筛选到化学结构优化,我们都可以满足您的科研用品及技术服务的需求。 经过在中国市场五年的精心耕耘,我们已成为筛选化合物领域优秀的供应商,为超过五百家学校和各类企业提供了品质卓越的小分子化合物和药物筛

成立日期 (12年)
注册资本 566.2651万人民币
员工人数 100-500人
年营业额 ¥ 1亿以上
经营模式 贸易,试剂,定制,服务
主营行业 化学试剂,生物活性小分子

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