|3-(4-氯苯基)-N-(吡啶-4-基甲基)金刚烷-1-甲酰胺|CsnPharm

CAS No.: 915385-81-8

奥帕尼布 Catalog No. CSN16869

Synonyms: ABC294640

ABC294640 markedly alters the ratio of ceramide/S1P consistent with inhibition of SK activity in MDA-MB-231 cells.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 SPHK2

IC50:60μM
描述Sphingosine is an intermediate of sphingolipids that can be rapidly phosphorylated by sphingosine kinase (SK1 and SK2) to produce sphingosine 1-phosphate, which is a mitogenic compound. ABC294640 is a selective inhibitor of SK2 with a K_i value of 9.8 μM. ABC294640 dose-dependently inhibited recombinant human SK2 with an IC₅₀ value of 60μM, while the activity of SK1 was not affected by ABC294640 at the concentration up to 100μM. In MDA-MB-231 cells, ABC294640 decreased [³H]S1P formation in a dose-dependent manner with an IC₅₀ value of 26μM. ABC294640 also inhibited the proliferation of human tumor cell lines (1025LU, A-498, Caco-2, HT-29, DU145, SK-OV-3) with IC₅₀ values ranging from 10.5-48.1μM^[2]. In a mouse model of tri-nitrobenzene sulfonic acid (TNBS)-induced colitis, oral administration of ABC294640 (50mg/kg, twice daily) decreased TNBS-induced increase in mucosal myeloperoxidase activity by 60%. The histological analysis on colon sections revealed that the inflammation and damage caused by TNBS was reduced or negated by ABC294640 treatment^[3].
动物研究
剂量
Mice^[2] (p.o.): min = 50 mg/kg, max = 100 mg/kg

给药途径
p.o.
临床研究

动物研究
剂量	Mice^[2] (p.o.): min = 50 mg/kg, max = 100 mg/kg
给药途径	p.o.

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT02757326	Multiple Myeloma	Phase 1 Phase 2	Recruiting	December 2021	United States, North Carolina ... more >> Duke University Medical Center Recruiting Durham, North Carolina, United States, 27705 Contact: Jackie McIntyre, RN 919-668-6524 jackie.mcintyre@duke.edu Contact: Peggy Alton, RN 919-681-4769 peggy.alton@duke.edu Collapse <<
NCT03414489	-	-	-	-	-
NCT01488513	Pancreatic Cancer ... more >> Unspecified Adult Solid Tumor, Protocol Specific Collapse <<	Phase 1	Completed	-	United States, South Carolina ... more >> Medical University of South Carolina Charleston, South Carolina, United States, 29425 Collapse <<

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参考文献

[3] Maines LW, Fitzpatrick LR, Green CL, Zhuang Y, Smith CD. Efficacy of a novel sphingosine kinase inhibitor in experimental Crohn's disease. Inflammopharmacology. 2010 Apr;18(2):73-85. doi: 10.1007/s10787-010-0032-x. Epub 2010 Feb 12. PMID: 20151210.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.6253 mL
- 13.1265 mL
- 26.2529 mL
- 5 mM
- 0.5251 mL
- 2.6253 mL
- 5.2506 mL
- 10 mM
- 0.2625 mL
- 1.3126 mL
- 2.6253 mL

技术信息

CAS号

915385-81-8

储存条件

粉末: Inert atmosphere,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C23H25ClN2O

运输

蓝冰

分子量

380.91

别名

ABC294640

溶解度

DMSO	115.0 mg/mL (301.9 mM)
Water	insoluble

动物实验配方

2% DMSO+30% PEG 300+5% Tween 80+water

5 mg/mL

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NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点

NCT02757326	Multiple Myeloma	Phase 1 Phase 2	Recruiting	December 2021	United States, North Carolina ... more >> Duke University Medical Center Recruiting Durham, North Carolina, United States, 27705 Contact: Jackie McIntyre, RN 919-668-6524 jackie.mcintyre@duke.edu Contact: Peggy Alton, RN 919-681-4769 peggy.alton@duke.edu Collapse <<
NCT03414489	-	-	-	-	-
NCT01488513	Pancreatic Cancer ... more >> Unspecified Adult Solid Tumor, Protocol Specific Collapse <<	Phase 1	Completed	-	United States, South Carolina ... more >> Medical University of South Carolina Charleston, South Carolina, United States, 29425 Collapse <<
NCT02229981	Diffuse Large B Cell Lymphoma ... more >> Kaposi Sarcoma Collapse <<	Phase 1 Phase 2	Withdrawn(Study was discontinu... more >>ed due to lack of recruitment.) Collapse <<	December 2019	United States, Louisiana ... more >> Louisiana State University Health Sciences Center New Orleans, Louisiana, United States, 70112 Collapse <<
NCT02939807	Carcinoma, Hepatocellular	Phase 2	Recruiting	May 2021	United States, South Carolina ... more >> Medical University of South Carolina Recruiting Charleston, South Carolina, United States, 29425 Contact: Lindsay Hunt 843-792-9321 hcc-clinical-trials@musc.edu Principal Investigator: Carolyn Britten, MD Collapse <<
NCT03377179	Cholangiocarcinoma ... more >> Cholangiocarcinoma Non-resectable Cholangiocarcinoma, Perihilar Cholangiocarcinoma, Extrahepatic Cholangiocarcinoma, Intrahepatic Collapse <<	Phase 2	Recruiting	January 2021	United States, Arizona ... more >> Mayo Clinic Cancer Center Recruiting Phoenix, Arizona, United States, 85054 Contact: Clinical Trials Office 855-776-0015 Principal Investigator: Daniel Ahn, MD United States, Georgia Emory University Recruiting Atlanta, Georgia, United States, 30322 Contact: Tyra Gaines 404-712-3308 tgaine3@emory.edu United States, Minnesota Mayo Clinic Cancer Center Recruiting Rochester, Minnesota, United States, 55905 Contact: Clinical Trials Office 855-776-0015 Principal Investigator: Amit Mahipal, MD United States, Texas MD Anderson Cancer Center Recruiting Houston, Texas, United States, 77030 Contact: Michelle Escano 713-794-1776 MEscano@mdanderson.org Principal Investigator: Shubham Pant, MD United States, Utah Huntsman Cancer Institute, University of Utah Recruiting Salt Lake City, Utah, United States, 84103 Contact: Cherie Peterson 801-587-5598 Cherie.peterson@hci.utah.edu Contact: Ignacio Garrido-Laguna, MD 801-585-0255 Ignacio.garrido-laguna@hci.utah.edu Principal Investigator: Ignacio Garrido-Laguna, MD Collapse <<

奥帕尼布 Catalog No. CSN16869

靶点选择性

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