|1-(3,4-二氯苄基)吲哚啉-2,3-二酮|CsnPharm

CAS No.: 79183-19-0

1-(3,4-二氯苄基)-1H-吲哚-2,3-二酮 Catalog No. CSN17056

Synonyms: AAII;N-(3,4-dichlorobenzyl) Isatin;MDK83190

Apoptosis activator 2 is a potent apoptosis activator which increases procaspase-9 processing and subsequent caspase-3 activation.

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技术信息

生物活性

描述Apoptosis is an evolutionarily conserved process that regulates development and homeostasis, and defects in this pathway are implicated in both tumorigenesis and multidrug resistance. Apoptosis activator 2 is a potent apoptosis Inducer in cells, strongly inducing caspase-3 activation, PARP cleavage, and DNA fragmentation, and finally killing cells with an IC₅₀ of ≈4 μM. Of the five normal cell lines tested, apoptosis activator 2 had no effect except at the highest concentration (50 μM) when tested against HMEC, PREC, or MCF-10A cells. Apoptosis activator 2 exerted a cytostatic effect on the majority of tumor cell lines tested, inhibiting cell growth by 50–100% at 10 μM in 40 of 48 tumor cell lines tested^[3]. TUNEL test in gastric adenocarcinoma cell line (AGS) cells treated with 10 μM of apoptosis activator 2 showed a significant increase in apoptosis in comparison with non-treated AGS cells^[4].
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
NCT02314156	BRCA1 Mutation Carrier ... more >> BRCA2 Mutation Carrier Ductal Breast Carcinoma In Situ Lobular Breast Carcinoma In Situ Stage 0 Breast Cancer Stage IA Breast Cancer Stage IB Breast Cancer Stage IIA Breast Cancer Stage IIB Breast Cancer Collapse <<	Phase 2	Active, not recruiting	March 2021	United States, California ... more >> Cedars-Sinai Medical Center West Hollywood, California, United States, 90048 United States, Illinois Northwestern University Chicago, Illinois, United States, 60611 United States, New York Memorial Sloan-Kettering Cancer Center New York, New York, United States, 10065 Collapse <<
NCT02862652	Acute Lymphoblastic Leukemia	Not Applicable	Completed	-	France ... more >> Chu de Reims Reims, France, 51092 Collapse <<
NCT01281722	-	-	Recruiting	July 2019	Taiwan ... more >> Department of Dermatology, National Taiwan University Hospital. Recruiting Taipei, Taiwan, 100 Contact: Shiou-Hwa Jee, M.D., Ph.D. 886-9-72651116 shiouhwa@gmail.com; shiouhwa@ntu.edu.tw Sub-Investigator: Jung-Ting Kao, M.D. Collapse <<

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参考文献

[1] Alavian KN, Sgadò P, et al. Elevated P75NTR expression causes death of engrailed-deficient midbrain dopaminergic neurons by Erk1/2 suppression. Neural Dev. 2009 Mar 16;4:11.
[2] Nguyen JT, Wells JA. Direct activation of the apoptosis machinery as a mechanism to target cancer cells. Proc Natl Acad Sci U S A. 2003 Jun 24;100(13):7533-8. Epub 2003 Jun 13.
[3] Nguyen JT, Wells JA. Direct activation of the apoptosis machinery as a mechanism to target cancer cells. Proc Natl Acad Sci U S A. 2003 Jun 24;100(13):7533-8. doi: 10.1073/pnas.1031631100. Epub 2003 Jun 13. PMID: 12808146; PMCID: PMC164621.
[4] Farivar TN, Najafipour R, Johari P. Nano - drug Delivery of Apoptosis Activator 2 to AGS Cells by Liposomes Conjugated with Anti-TROP2 Antibody. N Am J Med Sci. 2012 Nov;4(11):582-5. doi: 10.4103/1947-2714.103319. PMID: 23181231; PMCID: PMC3503378.

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
- 3.2664 mL
- 16.3322 mL
- 32.6644 mL
- 5 mM
- 0.6533 mL
- 3.2664 mL
- 6.5329 mL
- 10 mM
- 0.3266 mL
- 1.6332 mL
- 3.2664 mL

技术信息

CAS号

79183-19-0

储存条件

粉末: Sealed in dry,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C15H9Cl2NO2

运输

蓝冰

分子量

306.14

别名

AAII;N-(3,4-dichlorobenzyl) Isatin;MDK83190;N-(3,4-dichlorobenzyl) Isatin. MDK83190

溶解度

DMSO	98.0 mg/mL (320.1 mM)
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

NCT02314156	BRCA1 Mutation Carrier ... more >> BRCA2 Mutation Carrier Ductal Breast Carcinoma In Situ Lobular Breast Carcinoma In Situ Stage 0 Breast Cancer Stage IA Breast Cancer Stage IB Breast Cancer Stage IIA Breast Cancer Stage IIB Breast Cancer Collapse <<	Phase 2	Active, not recruiting	March 2021	United States, California ... more >> Cedars-Sinai Medical Center West Hollywood, California, United States, 90048 United States, Illinois Northwestern University Chicago, Illinois, United States, 60611 United States, New York Memorial Sloan-Kettering Cancer Center New York, New York, United States, 10065 Collapse <<
NCT02862652	Acute Lymphoblastic Leukemia	Not Applicable	Completed	-	France ... more >> Chu de Reims Reims, France, 51092 Collapse <<
NCT01281722	-	-	Recruiting	July 2019	Taiwan ... more >> Department of Dermatology, National Taiwan University Hospital. Recruiting Taipei, Taiwan, 100 Contact: Shiou-Hwa Jee, M.D., Ph.D. 886-9-72651116 shiouhwa@gmail.com; shiouhwa@ntu.edu.tw Sub-Investigator: Jung-Ting Kao, M.D. Collapse <<
NCT03167268	Colorectal Cancer Metastatic ... more >> Skin Toxicity Collapse <<	Phase 2	Recruiting	November 30, 2019	Italy ... more >> Marco Pirovano Recruiting Milano, Italy, 20153 Contact: Marco Pirovano, MD +390240222108 marco.pirovano@asst-santipaolocarlo.it Collapse <<
NCT00322140	Solid Tumors ... more >>Lymphoma Collapse <<	Phase 1	Completed	-	United States, Maryland ... more >> National Institutes of Health Clinical Center, 9000 Rockville Pike Bethesda, Maryland, United States, 20892 Collapse <<
NCT03042702	Ovarian Cancer	Phase 2	Completed	-	United States, New Hampshire ... more >> Cancer Research Lebanon, New Hampshire, United States, 03766 United States, Texas Cancer Research Dallas, Texas, United States, 75230 Collapse <<

1-(3,4-二氯苄基)-1H-吲哚-2,3-二酮 Catalog No. CSN17056

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