化合物 PQ401 hydrochloride|T4324|TargetMol

PQ401 hydrochloride (196868-63-0(free base))

￥139 2mg 起订

￥277 5mg 起订

￥386 10mg 起订

上海更新日期：2025-11-17

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产品详情:

中文名称：: 化合物 PQ401 hydrochloride

英文名称：: PQ401 hydrochloride (196868-63-0(free base))

CAS号：

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/Shipping at ambient temperature.

产品类别：: 抑制剂

货号：: T4324

Product Introduction

Bioactivity

名称	PQ401 hydrochloride (196868-63-0(free base))
描述	PQ401 inhibits autophosphorylation of IGF-1R domain with IC50 of <1 μM.
细胞实验	Cell lines: MCF-7,MCNeuA. Concentrations: ~50 μM. Incubation Time: 3 days. Method: The inhibitory effects of diaryl urea on breast cancer cell growth are determined using a CyQuant cell proliferation assay kit.MCF-7 or MCNeuA cells are plated in 96-well plates (5×103 per well) in phenol red-free DMEM supplemented with 10% FCS.One plate isprepared for each harvest day.Cells are allowed to adhere overnight and are then treated with various concentrations of diaryl urea or DMSO as a vehicle control.Microplate cultures are harvested on days 0,1,2,and 3 by inverting the microplate onto paper towels with gentle blotting to remove growth medium without disrupting adherent cells.Each plate iskept at ?80 ℃ until the end of the experiment (day 3) when all of the plates are thawed and assayed together.After thawing,200 μL of CyQuant GR solution are added to each well and the plates are incubated in the dark for 2 to 5 minutes.Fluorescence ismeasured with a SpectraMax Gemini XS fluorescence microplate reader with 480-nm excitation and 520-nm emission.Proliferation index iscalculated as the percent of nucleotide content versus control cells at day 0.
激酶实验	IGF-IR Peptide Autophosphorylation:One microgram of constitutively active IGF-IR kinase domain peptide isincubated +/? varying concentrations of PQ 401 in 2% DMSO in 40 mM Tris (pH 7.4), 80 μMEGTA, 0.25% 2-mercaptoethanol, 80 μM Na3VO4, 10 mM MgCl2, and 2 mM MnCl2 for 20 minutes. ATP is then added at a final concentration of 20 μM. Autophosphorylation of the kinase domain peptide isallowed to occur for 20 minutes at 22℃. The reaction isstopped by the addition of SDS-reducing buffer and the samples are run on SDS-PAGE. Following transfer to nitrocellulose membrane, peptide autophosphorylation isdetermined by Western blotting employing an antibody against phosphotyrosine (PY20).
动物实验	Animal Models: FVB/N-TgN(MMTVneu)202 mouse injected with MCNeuA cells. Formulation: 8% polysorbate 80 and ethanol. Dosages: 50 or 100 mg/kg. Administration: i.p.
体外活性	PQ 401 是一种 IGF-1R 抑制剂，可在小于100 nM 的浓度下抑制 IGF-1R 激酶域的自磷酸化，IC50 值小于1 μM。PQ 401 显著降低了 MCF-7 细胞的增殖，IC50 为8 μM；同时，PQ 401 也能够抑制 MCNeuA 细胞的增长，IC50 为15 μM。此外，PQ 401 抑制了 MCF-7 细胞中 IGF-I介导的抗凋亡途径，并增加了 MCF-7 细胞中的 caspase 介导的凋亡活性。
体内活性	PQ 401（50 mg/Kg、100 mg/Kg）显著且剂量依赖性地抑制了MCNeuA肿瘤的生长。
存储条件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
溶解度	DMSO : 45 mg/mL (118.97 mM), Sonication is recommended.
关键字	PQ401 hydrochloride (196868-63-0(free base)) \| PQ-401 hydrochloride (196868-63-0(free base)) \| PQ401 hydrochloride (196868630(free base)) \| PQ401 hydrochloride (196868 63 0(free base)) \| IGF-1R \| IGF1R
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PQ401 hydrochloride (196868-63-0(free base))|TargetMol

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。

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