化合物 PF-03814735|T6936|TargetMol

PF-03814735
942487-16-3

￥678 2mg 起订

上海更新日期：2024-12-02

TargetMol中国（陶术生物）

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产品详情:

中文名称：: 化合物 PF-03814735

英文名称：: PF-03814735

CAS号：: 942487-16-3

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.

产品类别：: 抑制剂

货号：: T6936

Product Introduction

Bioactivity

名称	PF-03814735
描述	PF-03814735 is a novel, potent and reversible inhibitor of Aurora A/B with IC50of 0.8 nM/5 nM, is less potent to Flt3, FAK, TrkA, and minimally active to Met and FGFR1. Phase 1.
细胞实验	Cell lines are grown in appropriate media and evaluated after 48 h of exposure to either PF-03814735 or vehicle, followed by cell number determination in a Coulter Counter. Proliferation (as measured by an increase in cell number) is expressed as a percent of untreated controls. To evaluate the PF-03814735 exposure time required for antiproliferative activity, HL-60 cell cultures are cultured in RPMI medium supplemented with 15% heat-inactivated fetal bovine serum and exposed to various PF-03814735 concentrations for 4, 8, 12, 24, and 48 hours, followed by a washout step and incubation with growth media without PF-03814735 for the remainder of the 72-h assay period. Continuous exposure to PF-03814735 for 72 hours is also evaluated. Cell counts are determined by a Coulter Counter.(Only for Reference)
激酶实验	Recombinant Kinase Assays: Aurora1 and Aurora2 proteins are produced as full-length His-tag recombinant proteins expressed in insect cells. For the Aurora2 kinase assay, phosphorylation of the substrate peptide by recombinant Aurora2 protein is assessed by a Z'-LYTE assay at 3 to 300 μM ATP and various concentrations of PF-03814735 over 60 minutes, at a substrate peptide concentration of 2 μM (biotinylated LRRWSLG, ×4). Phosphorylation is linear over this time for all conditions. For the Aurora1 kinase assay, phosphorylation of the substrate peptide by recombinant Aurora1 protein is assessed by a scintillation proximity assay in a 96-well plate format in which the incorporation of 33P into the peptide substrate (biotinylated LRRWSLG, ×4) is measured by capturing the peptide on a streptavidin scintillation proximity assay bead.
体外活性	在完整细胞中，PF-03814735对Aurora1和Aurora2激酶的抑制作用降低了磷酸化Aurora1（Thr 232，Aurora1活性的敏感标志，IC50约为20 nM）、磷酸化组蛋白H3（IC50约为50 nM）和磷酸化Aurora2（IC50约为150 nM）的水平。PF-03814735引发细胞分裂阻塞，导致细胞增殖受抑和多倍体多核细胞的形成。[1] 最近的研究表明，小细胞肺癌（SCLC）和在较小程度上的结肠癌细胞线对PF-03814735特别敏感。Myc基因家族的状态和视网膜母细胞瘤途径成员的表达与PF-03814735的效力显著相关。[1]
体内活性	每日一次口服PF-03814735，剂量≥20 mg/kg，连续10天给予携带HCT-116异种移植瘤的小鼠治疗，能够与对照组（车辆处理的小鼠）相比，显著并且剂量依赖性地抑制肿瘤生长≥50%。这种抑制与磷酸化组蛋白H3水平的降低相关。在包括A2780卵巢癌、MDA-MB-231乳腺癌、colo-205和SW620结直肠癌、以及HL-60急性早幼粒细胞性白血病等五种额外的异种移植瘤模型中观察到显著的单药抗肿瘤效果。[1] 两种SCLC异种移植模型的体内实验确认了Myc基因驱动模型对PF-03814735的敏感性以及MYC/c-Myc驱动肿瘤可能的时间依赖性。[1]
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	DMSO : 47.5 mg/mL (100 mM) Ethanol : 9.5 mg/mL (20 mM)
关键字	PF03814735 \| inhibit \| PF-03814735 \| VEGFR \| Inhibitor \| Vascular endothelial growth factor receptor \| PF 03814735 \| Aurora Kinase
相关产品	Gilteritinib \| Amitriptyline hydrochloride \| Ribociclib \| Axitinib \| Sorafenib tosylate \| Lenvatinib mesylate \| Regorafenib \| Pazopanib \| Nintedanib \| Sorafenib \| Pexidartinib \| Regorafenib monohydrate

PF-03814735|TargetMol

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