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网站主页 化工产品目录 生物化工 抑制剂 细胞骨架(Cytoskeletal Signaling) PAK 抑制剂 PF-3758309 化合物 PF3758309
  • 化合物 PF3758309|T6626|TargetMol

化合物 PF3758309|T6626|TargetMol

PF-3758309
898044-15-0
193 1mg 起订
412 5mg 起订
663 10mg 起订
上海 更新日期:2024-12-12

TargetMol中国(陶术生物)

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联系人:邵小姐
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邮箱:marketing@tsbiochem.com

产品详情:

中文名称:
化合物 PF3758309
英文名称:
PF-3758309
CAS号:
898044-15-0
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:
99.37%
产品类别:
抑制剂
货号:
T6626

Product Introduction

Bioactivity

名称PF-3758309
描述PF-3758309 (PF-03758309) (IC50=1.3 nM), a pyrrolopyrazole inhibitor of PAK4, has effective ATP-competition.
细胞实验HEK293T, HCT116, and SKOV3 cells are plated on 384-well plates for 24 hours culture. PF-3758309( ~1 μM) is added to the cell culture incubating 72 hours. After drug treatment,cell proliferation and other indicators of metabolism are measured.
激酶实验In phospho-GEF-H1 cellular assay, TR-293-KDG cells are incubated for 3 hours with PF-3758309. TR-293-KDG cells were captured on an anti-HA antibody-coated plate, which is detected with an anti-phospho-S810-GEF-H1 antibody, and quantified with a horseradish peroxidase-goat anti-rabbit antibody conjugate. TR-293-KDG cells are constructed from HEK293 cells, which is transfected with tetracycline-inducible PAK4-kinase domain (amino acids 291-591) and expressed HA-tagged GEFH1ΔDH (amino acids 210-921).
动物实验Nude mice with Xenograft tumors were orally fed with PF-3758309(7.5-30 mg/kg BID)dissolved in 0.5% methylcellulose.
体外活性PF-3758309 (Kd = 2.7 nM), an effective inhibitor of PAK4 (Ki=18.7 nM), has ATP competition. PF-3758309 (IC50 = 1.3 nM) inhibits phosphorylation of the PAK4 substrate GEF-H1 in cells. In the tumor cell, PF-3758309(IC50 = 4.7 nM) grows in a linesanchorage-independent manner. In HCT116 cells, PF-3758309 inhibits endogenous pGEF-H1 accumulation. In A549 cells, PF-3758309 effectively inhibits cellular proliferation in IC50 of 20 nM and anchorage-independent growth in IC50 of 27 nM.
体内活性In the HCT116 tumor model, PF-3758309 act as an antiproliferative inducing apoptosis. In the sensitive model, PF-3758309 (EC50=0.4 nM) blocks the growth of multiple human tumor xenografts.
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 : 91 mg/mL (185.5 mM)
Ethanol : 91 mg/mL (185.5 mM)
H2O : < 1 mg/mL (insoluble or slightly soluble)
关键字PF-3758309 | proliferation | tumor | oncogenic | survival | PF03758309 | inhibit | p21 activated kinases | signaling | Apoptosis | ATP-competitive | PF 309 | PF 03758309 | Inhibitor | PF3758309 | growth | PF309 | PAK
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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 | 抗衰老化合物库 | NO PAINS 化合物库 | 药物功能重定位化合物库 | 抗癌临床化合物库 | 抗癌药物库
PF-309|||PF-03758309|||PF 3758309|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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