|7-苄基-4-(2-甲基苄基)-1,2,6,7,8,9-六氢咪唑并[1,2-a]吡啶并[3,4-e]嘧啶-5(4H)-酮|CsnPharm

CAS No.: 1616632-77-9

7-Benzyl-4-(2-methylbenzyl)-1,2,6,7,8,9-hexahydroimidazo[1,2-a]pyrido[3,4-e]pyrimidin-5(4H)-one Catalog No. CSN15801

Synonyms: ONC-201;NSC-350625;TRAIL inducing compound 10

TIC10 is a brain-permeable and pharmacokinetics-improved Akt inhibitor, also inactivates ERK.

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实验方案

技术信息

生物活性

描述TRAIL is an endogenous protein that induces fulminant tumor-specific apoptosis through binding to death receptors DR4 or DR5 expressed in human tumor cells^[2]. TIC10 is a novel small molecule inducer of the human TRAIL gene that improves efficacy-limiting properties of recombinant TRAIL. TIC10, which is the most potent inducer of cell death, exclusively activate Foxo3a through inactivation of Akt/ERK to upregulate TRAIL and its pro-apoptotic death receptor DR5^[2]. In a vivo experiment, TIC10 induced a delayed and modest amount of cell death that was apparent at 72 hours post-treatment with a 1 μM dose. TIC10 can synergistically inhibit Panc-1 xenograft growth in SCID mice. TIC10 at 5-25 μM significantly decreased viability of Panc-1 cells^[2].
动物研究
剂量
Mice: 25 mg/kg - 100 mg/kg^[1] (i.v.); 25 mg/kg^[1] (p.o.); 100 mg/kg^[1] (i.p.)

给药途径
i.v., p.o., i.p.
临床研究

动物研究
剂量	Mice: 25 mg/kg - 100 mg/kg^[1] (i.v.); 25 mg/kg^[1] (p.o.); 100 mg/kg^[1] (i.p.)
给药途径	i.v., p.o., i.p.

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT01669915	Cognitive Decline	Not Applicable	Active, not recruiting	December 2020	United States, Massachusetts ... more >> Boston, Massachusetts, United States Collapse <<
NCT02525692	Glioblastoma ... more >>Diffuse Midline Glioma H3 K27M Glioma Thalamic Glioma Infratentorial Glioma Basal Ganglia Glioma Collapse <<	Phase 2	Recruiting	December 2019	United States, Florida ... more >> Miami Cancer Institute Recruiting Miami, Florida, United States, 33176 Contact: Danieska Sandino danieskas@baptisthealth.net Principal Investigator: Yazmin Odia, MD, MS United States, Massachusetts Massachusetts General Hospital Recruiting Boston, Massachusetts, United States, 02114 Contact: Isabel Arrillaga, MD, PhD 617-726-2000 iarrillaga@mgh.harvard.edu Dana-Farber Cancer Institute Recruiting Boston, Massachusetts, United States, 02115 Contact: Patrick Wen, MD 617-632-2166 Dana-FarberContactUs@dfci.harvard.edu Collapse <<
NCT03134131	-	-	-	-	United States, Pennsylvania ... more >> Oncoceutics Philadelphia, Pennsylvania, United States, 19104 Collapse <<

更多
参考文献

[1] Allen JE, Krigsfeld G, et al. Dual inactivation of Akt and ERK by TIC10 signals Foxo3a nuclear translocation, TRAIL gene induction, and potent antitumor effects. Sci Transl Med. 2013 Feb 6;5(171):171ra17.
[2] Allen JE, Krigsfeld G, Patel L, Mayes PA, Dicker DT, Wu GS, El-Deiry WS. Identification of TRAIL-inducing compounds highlights small molecule ONC201/TIC10 as a unique anti-cancer agent that activates the TRAIL pathway. Mol Cancer. 2015 May 1;14:99. doi: 10.1186/s12943-015-0346-9. PMID: 25927855; PMCID: PMC4428111.

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
- 2.5874 mL
- 12.9370 mL
- 25.8739 mL
- 5 mM
- 0.5175 mL
- 2.5874 mL
- 5.1748 mL
- 10 mM
- 0.2587 mL
- 1.2937 mL
- 2.5874 mL

技术信息

CAS号

1616632-77-9

储存条件

粉末: Sealed in dry,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C24H26N4O

运输

蓝冰

分子量

386.49

别名

ONC-201;NSC-350625;TRAIL inducing compound 10;imipridone

溶解度

DMSO	50.0 mg/mL (129.4 mM) warming
Water	insoluble

动物实验配方

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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

NCT01669915	Cognitive Decline	Not Applicable	Active, not recruiting	December 2020	United States, Massachusetts ... more >> Boston, Massachusetts, United States Collapse <<
NCT02525692	Glioblastoma ... more >>Diffuse Midline Glioma H3 K27M Glioma Thalamic Glioma Infratentorial Glioma Basal Ganglia Glioma Collapse <<	Phase 2	Recruiting	December 2019	United States, Florida ... more >> Miami Cancer Institute Recruiting Miami, Florida, United States, 33176 Contact: Danieska Sandino danieskas@baptisthealth.net Principal Investigator: Yazmin Odia, MD, MS United States, Massachusetts Massachusetts General Hospital Recruiting Boston, Massachusetts, United States, 02114 Contact: Isabel Arrillaga, MD, PhD 617-726-2000 iarrillaga@mgh.harvard.edu Dana-Farber Cancer Institute Recruiting Boston, Massachusetts, United States, 02115 Contact: Patrick Wen, MD 617-632-2166 Dana-FarberContactUs@dfci.harvard.edu Collapse <<
NCT03134131	-	-	-	-	United States, Pennsylvania ... more >> Oncoceutics Philadelphia, Pennsylvania, United States, 19104 Collapse <<
NCT03485729	Endometrial Cancer Recurrent	Phase 2	Recruiting	March 21, 2021	United States, New Jersey ... more >> Rutgers, The State University of New Jersey Recruiting New Brunswick, New Jersey, United States, 08903 Contact: Lorna Rodriguez, MD PhD 732-235-2465 rodriglo@cinj.rutgers.edu United States, North Carolina UNC Lineberger Comprehensive Cancer Center Recruiting Chapel Hill, North Carolina, United States, 27599 Contact: Jennifer Gruhn, MS 919-445-4212 jennifer_gruhn@med.unc.edu Principal Investigator: Victoria L Bae-Jump, MD, PhD United States, Pennsylvania Fox Chase Cancer Center Recruiting Philadelphia, Pennsylvania, United States, 19111 Contact: Gina Mantia-Smaldone, MD Principal Investigator: Gina Mantia-Smaldone, MD Collapse <<
NCT03295396	Glioma	Phase 2	Recruiting	November 1, 2020	United States, California ... more >> University of California, San Francisco Recruiting San Francisco, California, United States, 94143-0112 Contact: Nicholas Butowski, MD Butowski@neurosurg.ucsf.edu Principal Investigator: Nicholas Butowski, MD United States, New York New York University School of Medicine Recruiting New York, New York, United States, 10016 Contact: Amy Patel, RN 212-731-6267 amie.patel@nyumc.org United States, North Carolina Levine Cancer Institute Recruiting Charlotte, North Carolina, United States, 28204 Contact: Sylvia Rushing 980-442-2358 Sylvia.Rushing@atriumhealth.org United States, Texas MD Anderson Cancer Center Recruiting Houston, Texas, United States, 77030 Contact: Kathy Wagner kuhunter@mdanderson.org Principal Investigator: Rebecca Harrison, MD Collapse <<
NCT02190721	Neutropenia	Phase 2	Completed	-	-
NCT02392572	Leukemia	Phase 1 Phase 2	Recruiting	November 2023	United States, Texas ... more >> University of Texas MD Anderson Cancer Center Recruiting Houston, Texas, United States, 77030 Collapse <<
NCT03394027	Triple Negative Breast Cancer ... more >> Endometrial Cancer Hormone Receptor Positive, HER2 Negative Breast Cancer Collapse <<	Phase 2	Recruiting	December 30, 2027	United States, Maryland ... more >> National Institutes of Health Clinical Center Recruiting Bethesda, Maryland, United States, 20892 Contact: For more information at the NIH Clinical Center contact National Cancer Institute Referral Office 888-624-1937 Collapse <<
NCT02609230	Advanced Solid Tumors ... more >> Multiple Myeloma Collapse <<	Phase 1	Recruiting	January 2020	United States, Pennsylvania ... more >> Fox Chase Cancer Center - Philadelphia Recruiting Philadelphia, Pennsylvania, United States, 19111-2497 Contact: Anthony Olszanski, MD 215-728-6900 Anthony.Olszanski@fccc.edu Collapse <<
NCT02190721	-	-	Completed	-	-
NCT03416530	Diffuse Intrinsic Pontine Glio... more >>ma Glioma, Malignant Collapse <<	Phase 1	Recruiting	July 24, 2020	United States, Florida ... more >> Miami Cancer Institute Recruiting Miami, Florida, United States, 33176 Contact: Danieska Sandino danieskas@baptisthealth.net Principal Investigator: Yazmin Odia, MD, MS United States, Michigan University of Michigan Cancer Center Recruiting Ann Arbor, Michigan, United States, 48109 Contact: Carl Koschmann, MD 734-936-9814 ckoschma@umich.edu Principal Investigator: Carl Koschmann, MD United States, New York New York University Recruiting New York, New York, United States, 10016 Contact: Sharon Gardner, MD 646-929-7870 Sharon.Gardner@nyumc.org Principal Investigator: Sharon Gardner, MD United States, Texas MD Anderson Cancer Center Recruiting Houston, Texas, United States, 77030 Contact: Soumen Khatua, MD 713-792-2121 SKhatua@mdanderson.org Principal Investigator: Wafik Zaky, MD Principal Investigator: Soumen Kahtua, MD Collapse <<
NCT02863991	Multiple Myeloma	Phase 1 Phase 2	Recruiting	December 31, 2020	United States, New York ... more >> The Mount Sinai Medical Center Recruiting New York, New York, United States, 10029-6574 Contact: Lisa La, MS, CCRP 212-241-8615 Lisa.La@mssm.edu Principal Investigator: Ajai Chari, MD United States, Pennsylvania Fox Chase Cancer Center Recruiting Philadelphia, Pennsylvania, United States, 19111 Contact: Carlyn Tan, MD 888-369-2427 Principal Investigator: Carlyn Tan, MD Collapse <<
NCT03492138	Multiple Myeloma	Phase 1 Phase 2	Recruiting	March 15, 2023	United States, New York ... more >> Icahn School of Medicine at Mount Sinai Recruiting New York, New York, United States, 10029 Contact: Lisa La, MS 212-241-7873 Lisa.La@mssm.edu Collapse <<
NCT03099499	Endometrial Cancer	Phase 2	Recruiting	October 1, 2020	United States, Pennsylvania ... more >> Fox Chase Cancer Center Recruiting Philadelphia, Pennsylvania, United States, 19111 Contact: Gina Mantia-Smaldone, MD 215-214-1515 Gina.Mantia-Smaldone@fccc.edu Collapse <<
NCT03034200	Recurrent Neuroendocrine Tumor... more >> Metastatic Neuroendocrine Tumor Collapse <<	Phase 2	Recruiting	February 2019	United States, Ohio ... more >> Cleveland Clinic Taussig Cancer Institute, Case Comprehensive Cancer Center Recruiting Cleveland, Ohio, United States, 44195 Contact: Peter M Anderson, MD, PhD 216-445-4007 andersp@ccf.org Principal Investigator: Peter M Anderson, MD, PhD Collapse <<
NCT02324621	Unspecified Adult Solid Tumor	Phase 1	Recruiting	March 2019	United States, New Jersey ... more >> Rutgers Cancer Institute of New Jersey Recruiting New Brunswick, New Jersey, United States, 08903 Contact: Jyoti Malhotra 732-235-7521 jyoti.malhotra@rutgers.edu Principal Investigator: Jyoti Malhotra Collapse <<
NCT02420795	Lymphoma	Phase 1 Phase 2	Recruiting	November 2021	United States, Texas ... more >> University of Texas MD Anderson Cancer Center Recruiting Houston, Texas, United States, 77030 Contact: MD Anderson Health Information Specialist 877-632-6789 Collapse <<
NCT02038699	Advanced Glioblastoma ... more >> Advanced Colorectal Cancer Advanced Triple-negative Breast Cancer Advanced Non-small Cell Lung Cancer Collapse <<	Phase 1 Phase 2	Withdrawn(Protocol not activat... more >>ed.) Collapse <<	-	United States, Massachusetts ... more >> Massachusetts General Hospital Boston, Massachusetts, United States, 02114 Collapse <<
NCT03733119	Triple Negative Breast Cancer	Phase 2	Recruiting	October 1, 2021	United States, Wisconsin ... more >> University of Wisconsin Carbone Cancer Center Recruiting Madison, Wisconsin, United States, 53792 Contact: Renae Quale 608-265-2789 rmq@medicine.wisc.edu Principal Investigator: Ruth O'Regan Collapse <<
NCT02250781	Solid Tumors	Phase 1	Suspended(funding unavailable)	January 2019	United States, New Jersey ... more >> Rutgers Cancer Institute of New Jersey New Brunswick, New Jersey, United States, 08903 Collapse <<

7-Benzyl-4-(2-methylbenzyl)-1,2,6,7,8,9-hexahydroimidazo[1,2-a]pyrido[3,4-e]pyrimidin-5(4H)-one Catalog No. CSN15801

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