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CAS No.: 1570496-34-2

IACS-010759 Catalog No. CSN21365

Synonyms: IACS-10759

IACS-010759 is a potent and selective inhibits oxidative phosphorylation with IC50 < 10 nM. It also binds to and inhibits complex I of the electron transport chain (NADH ubiquinone oxidoreductase), selectively depriving tumor cells of nutrients and energy, inhibiting nucleotide and amino acid production, and induces autophagy.

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技术信息

生物活性

描述OxPhos (oxidative phosphorylation) is an energy-efficient way of synthesizing ATP in the mitochondria which is a predominant pathway in CLL (chronic lymphocytic leukemia) for energy production and is further augmented in the presence of the stromal microenvironment. IACS-010759, currently in clinical development, is a small-molecule, orally bioavailable OxPhos inhibitor that targets mitochondrial complex I at low nanomolar levels. Treatment of primary CLL cells with 100 nM IACS-010759 greatly inhibited OxPhos but caused only minor cell death at 24 and 48 h. In 100 nM IACS-010759-treated CLL cells, basal OCR (oxygen consumption rate, a measure of OxPhos) was greatly inhibited followed by a drastic decrease in spare respiratory capacity (after addition of FCCP, a kind of uncoupler) compared with the untreated control. CLL cells were incubated with 100 nM IACS-010759 for 24 h (n = 19) and 48 h (n = 6). The ribonucleotide pools decreased at both time points upon drug treatment. ATP concentrations in CLL cells from these patients ranged from 693 to 5267 μM with a mean of 2775 μM. This mean value decreased to 1652 μM after 24 h. At 48 h, the levels further decreased from 2124 to 943 μM. In CLL cells incubated with the combination of 100 nM IACS-010759 and 2-dG, the OCR was further and significantly reduced compared with controls and even compared with cells treated with IACS-010759 alone^[1].
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
NCT03291938	Malignant Neoplasm of Breast ... more >> Malignant Neoplasms of Bone and Articular Cartilage Malignant Neoplasms of Digestive Organs Malignant Neoplasms of Female Genital Organs Malignant Neoplasms of Lip Oral Cavity and Pharynx Malignant Neoplasms of Male Genital Organs Malignant Neoplasms of Mesothelial and Soft Tissue Malignant Neoplasms of Respiratory and Intrathoracic Organs Malignant Neoplasms of Thyroid and Other Endocrine Glands Malignant Neoplasms of Urinary Tract Malignant Neoplasms Stated as Primary Lymphoid Haematopoietic Collapse <<	Phase 1	Recruiting	November 2023	United States, Texas ... more >> University of Texas MD Anderson Cancer Center Recruiting Houston, Texas, United States, 77030 Contact tyap@mdanderson.org Collapse <<
NCT02882321	Acute Myeloid Leukemia	Phase 1	Recruiting	September 2022	United States, Texas ... more >> University of Texas MD Anderson Cancer Center Recruiting Houston, Texas, United States, 77030 Collapse <<

参考文献

[1] Biological and metabolic effects of IACS-010759, an OxPhos inhibitor, on chronic lymphocytic leukemia cells

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
- 1.7776 mL
- 8.8879 mL
- 17.7758 mL
- 5 mM
- 0.3555 mL
- 1.7776 mL
- 3.5552 mL
- 10 mM
- 0.1778 mL
- 0.8888 mL
- 1.7776 mL

技术信息

CAS号

1570496-34-2

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

C25H25F3N6O4S

运输

蓝冰

分子量

562.56

别名

IACS-10759

溶解度

DMSO	31.0 mg/mL (55.1 mM) warming
Water	insoluble

动物实验配方

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