Apilimod | 阿吡莫德 | STA 5326 | IL-12/IL-23 Inhibitor

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阿匹莫德 /Apilimod {[allProObj[0].p_purity_real_show]}

货号：A149227 同义名： 阿吡莫德 / STA 5326;LAM-002A free base

Apilimod（STA 5326）是一种有效的IL-12/IL-23抑制剂，在IFN-γ/SAC刺激的人PBMCs和SAC处理的猴PBMCs中，IL-12的IC50值分别为1 nM和2 nM。它还作为PIKfyve的有效且高度选择性的抑制剂。

Apilimod 化学结构
CAS号：541550-19-0

Apilimod 3D分子结构
CAS号：541550-19-0

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Apilimod 纯度/质量文件产品仅供科研

货号：A149227 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

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Apilimod 生物活性

描述

Phosphatidylinositol-3-phosphate 5-kinase (PIKfyve) is a lipid kinase that synthesizes two phosphoinositides (PIs), regulating degradative and recycling endosomal trafficking, cytoskeletal rearrangement and autophagy. Apilimod is a 1,3,5-triazine derivative that binds to and inhibits PIKfyve kinase activity with an IC50 value of 14 nM. Treatment of apilimod (10 nM and 1 μM) for 120min decreased PI(3,5)P₂ in HeLa cells at a dose-dependent manner. RAW264.7 cells treated with 10 nM Apilimod for 3h showed enlarged vacuoles due to the disruption of PIKfyve activity. In A549 cells, overexpression of wild-type PIKfyve resulted in the disappearance of vacuoles induced by 10 nM apilimod. Bone-marrow-derived dendritic cells from mutant mice demonstrated extensive vacuole formation with the treatment of 1 μM apilimod^[3]. Apilimod showed selective antiproliferative activity in B-NHL cells with an IC50 value of 142 nM. After the treatment of 200 nM apilimod for 3 days, increased apoptosis was shown in SU-DHL-10 B-NHL cells. In a subcutaneous daudi burkitt lymphoma xenograft model, apilimod (50 - 150 mg/kg free base; p.o., once a day) displayed tumor growth inhibition at a dose-dependent manner. The growth inhibition was also observed in SU-DHL-6 DLBCL model treated with both apilimod (41 mg/kg free base, p.o., twice a day) and rituximab (7 mg/kg, i.p.)^[4].

作用机制

Apilimod is a potent, highly selective PIKfyve inhibitor that binds to the PIKfyve domain (amino acids 1522 to 2098) to block the phosphotransferase activity of PIKfyve, thereby inhibiting IL-12/23p40^[3].

Apilimod 动物研究

Dose	Mice: 41 mg/kg^[1] (p.o.)
Administration	p.o.

Apilimod 临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT02594384	Lymphoma, Non-Hodgkin; Leukema... 展开 >>i, Chronic Lymphocytic 收起 <<	Phase 1	Recruiting	December 2019	United States, Alabama ... 展开 >> Clearview Cancer Institute Recruiting Huntsville, Alabama, United States, 35805 Contact: Avitra Bone, RN 256-705-4283 studycoordinator@ccihsv.com Principal Investigator: Marshall Schreeder, MD United States, Florida Mayo Clinic Recruiting Jacksonville, Florida, United States, 32224 Contact: Lisa Melfi 904-953-3320 melfi.lisa@mayo.edu Principal Investigator: Taimur Sher, MD United States, Georgia Winship Cancer Institute at Emory University Recruiting Atlanta, Georgia, United States, 30322 Contact: Kaylan Dixon 404-778-4449 kaylan.dixon@emory.edu Principal Investigator: Jonathan Cohen, MD United States, Indiana Horizon Oncology Research, Inc. Recruiting Lafayette, Indiana, United States, 47905 Contact: Wael A Harb, MD 765-446-5111 wharb@horizonbioadvance.com Principal Investigator: Wael A Harb, MD United States, Massachusetts Massachusetts General Hospital Recruiting Boston, Massachusetts, United States, 02114 Contact: Lauren Ramos 617-643-9607 lramos7@mgh.harvard.edu Principal Investigator: Jeremy Abramson, MD United States, Minnesota Mayo Clinic Recruiting Rochester, Minnesota, United States, 55905 Contact: Corinne Parker 507-266-3784 parker.corinne@mayo.edu Principal Investigator: Stephen Ansell, MD United States, New York New York University School of Medicine Recruiting New York, New York, United States, 10016 Contact: Ion Marinescu 646-501-7920 Ion.Marinescu@nyumc.org Principal Investigator: Catherine Diefenbach, MD Weill Cornell Medical College Recruiting New York, New York, United States, 10021 Contact: Rita Gazivoda 212-746-0702 rig9021@med.cornell.edu Principal Investigator: Sarah Rutherford, MD United States, Texas University of Texas MD Anderson Cancer Center Recruiting Houston, Texas, United States, 77030 Contact: Linda Claret 713-792-1044 lcclaret@mdanderson.org Principal Investigator: Loretta Nastoupil, MD United States, Virginia Virginia Cancer Specialists Recruiting Fairfax, Virginia, United States, 22031 Contact: VCS Phase 1 Team 703-208-3192 Karin.Choquette@usoncology.com Principal Investigator: Dipti Patel-Donnelly, MD United States, Washington Virginia Mason Medical Center Recruiting Seattle, Washington, United States, 98101 Contact: Anas Najjar 206-287-5671 Anas.Najjar@virginiamason.org Principal Investigator: David Aboulafia, MD 收起 <<

Apilimod 参考文献

[1]Gayle S, Landrette S, et al. Identification of apilimod as a first-in-class PIKfyve kinase inhibitor for treatment of B-cell non-Hodgkin lymphoma. Blood. 2017 Mar 30;129(13):1768-1778.

[2]Wada Y, Lu R, et al. Selective abrogation of Th1 response by STA-5326, a potent IL-12/IL-23 inhibitor. Blood. 2007;109(3):1156-64

[3]Cai X, Xu Y, Cheung AK, Tomlinson RC, Alcázar-Román A, Murphy L, Billich A, Zhang B, Feng Y, Klumpp M, Rondeau JM, Fazal AN, Wilson CJ, Myer V, Joberty G, Bouwmeester T, Labow MA, Finan PM, Porter JA, Ploegh HL, Baird D, De Camilli P, Tallarico JA, Huang Q. PIKfyve, a class III PI kinase, is the target of the small molecular IL-12/IL-23 inhibitor apilimod and a player in Toll-like receptor signaling. Chem Biol. 2013 Jul 25;20(7):912-21.

[4]Gayle S, Landrette S, Beeharry N, Conrad C, Hernandez M, Beckett P, Ferguson SM, Mandelkern T, Zheng M, Xu T, Rothberg J, Lichenstein H. Identification of apilimod as a first-in-class PIKfyve kinase inhibitor for treatment of B-cell non-Hodgkin lymphoma. Blood. 2017 Mar 30;129(13):1768-1778.

Apilimod 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.39mL

0.48mL

0.24mL

11.95mL

2.39mL

1.19mL

23.90mL

4.78mL

2.39mL

Apilimod 技术信息

CAS号	541550-19-0
分子式	C₂₃H₂₆N₆O₂
分子量	418.491

别名	阿吡莫德 ;STA 5326;LAM-002A free base;AIT-101
运输	蓝冰

存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Inert atmosphere,2-8°C

溶解度

DMSO: 105 mg/mL(250.9 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

动物实验配方

临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点

NCT02594384

Lymphoma, Non-Hodgkin; Leukema... 展开 >>i, Chronic Lymphocytic 收起 <<

Phase 1

Recruiting

December 2019

United States, Alabama ... 展开 >> Clearview Cancer Institute Recruiting Huntsville, Alabama, United States, 35805 Contact: Avitra Bone, RN 256-705-4283 studycoordinator@ccihsv.com Principal Investigator: Marshall Schreeder, MD United States, Florida Mayo Clinic Recruiting Jacksonville, Florida, United States, 32224 Contact: Lisa Melfi 904-953-3320 melfi.lisa@mayo.edu Principal Investigator: Taimur Sher, MD United States, Georgia Winship Cancer Institute at Emory University Recruiting Atlanta, Georgia, United States, 30322 Contact: Kaylan Dixon 404-778-4449 kaylan.dixon@emory.edu Principal Investigator: Jonathan Cohen, MD United States, Indiana Horizon Oncology Research, Inc. Recruiting Lafayette, Indiana, United States, 47905 Contact: Wael A Harb, MD 765-446-5111 wharb@horizonbioadvance.com Principal Investigator: Wael A Harb, MD United States, Massachusetts Massachusetts General Hospital Recruiting Boston, Massachusetts, United States, 02114 Contact: Lauren Ramos 617-643-9607 lramos7@mgh.harvard.edu Principal Investigator: Jeremy Abramson, MD United States, Minnesota Mayo Clinic Recruiting Rochester, Minnesota, United States, 55905 Contact: Corinne Parker 507-266-3784 parker.corinne@mayo.edu Principal Investigator: Stephen Ansell, MD United States, New York New York University School of Medicine Recruiting New York, New York, United States, 10016 Contact: Ion Marinescu 646-501-7920 Ion.Marinescu@nyumc.org Principal Investigator: Catherine Diefenbach, MD Weill Cornell Medical College Recruiting New York, New York, United States, 10021 Contact: Rita Gazivoda 212-746-0702 rig9021@med.cornell.edu Principal Investigator: Sarah Rutherford, MD United States, Texas University of Texas MD Anderson Cancer Center Recruiting Houston, Texas, United States, 77030 Contact: Linda Claret 713-792-1044 lcclaret@mdanderson.org Principal Investigator: Loretta Nastoupil, MD United States, Virginia Virginia Cancer Specialists Recruiting Fairfax, Virginia, United States, 22031 Contact: VCS Phase 1 Team 703-208-3192 Karin.Choquette@usoncology.com Principal Investigator: Dipti Patel-Donnelly, MD United States, Washington Virginia Mason Medical Center Recruiting Seattle, Washington, United States, 98101 Contact: Anas Najjar 206-287-5671 Anas.Najjar@virginiamason.org Principal Investigator: David Aboulafia, MD 收起 <<

阿匹莫德 /Apilimod {[allProObj[0].p_purity_real_show]}

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Apilimod 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

Apilimod 质控信息

Apilimod 生物活性

Apilimod 动物研究

Apilimod 临床研究

Apilimod 参考文献

Apilimod 实验方案

Apilimod 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

确认信息

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