- GSK2879552
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- $9.80 / 1KG
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2020-01-10
- CAS:1401966-69-5
- Min. Order: 1KG
- Purity: ≥98%
- Supply Ability: 20 tons
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| | GSK2879552 Basic information |
| Product Name: | GSK2879552 | | Synonyms: | GSK2879552;GSK2879522;4-[[4-[[((1R,2S)-2-Phenylcyclopropyl)amino]methyl]piperidin-1-yl]methyl]benzoic acid;GSK2879552 DIHYDROCHLORIDE;CS-1621;LSD1 inhibiror GS2879552;GSK-2879552;GSK 2879552;Benzoic acid, 4-[[4-[[[(1R,2S)-2-phenylcyclopropyl]amino]methyl]-1-piperidinyl]methyl]- | | CAS: | 1401966-69-5 | | MF: | C23H28N2O2 | | MW: | 364.48 | | EINECS: | | | Product Categories: | | | Mol File: | 1401966-69-5.mol |  |
| | GSK2879552 Chemical Properties |
| Boiling point | 534.2±50.0 °C(Predicted) | | density | 1.20±0.1 g/cm3(Predicted) | | storage temp. | -20°C | | solubility | Soluble in DMSO (up to 25 mg/ml) or in Water (up to at least 25 mg/ml) | | pka | 4.03±0.10(Predicted) | | form | solid | | color | White | | Stability: | Stable for 1 year from date of purchase as supplied. Solutions in DMSO or distilled water may be stored at -20°C for up to 3 months. |
| | GSK2879552 Usage And Synthesis |
| Description | GSK2879552 (1401966-65-5, free base) is potent, selective, and irreversible inhibitor of Lysine Demethylase 1 (LSD1) via covalent modification of the LSD1 cofactor FAD (Ki = 1.7 μM). It is selective for LSD1 over the closely related LSD2, MAO-A, MAO-B, and the FAD dependent enzymes D-amino acid oxidase and glutathione reductase. Tested against a panel of 165 cancer cell lines, GSK2879552 inhibited the proliferation of 9 small cell lung carcinoma lines and 20 AML cell lines. | | Definition | ChEBI: GSK2879552 is a member of the class of piperidines that is piperidine substituted by (4-carboxyphenyl)methyl and {[(1R,2S)-2-phenylcyclopropyl]amino}methyl groups at positions 1 and 4, respectively. It is a potent and irreversible inhibitor of lysine specific demethylase 1 (LSD1, also known as KDM1A). It was under clinical investigation for the treatment of acute myeloid leukaemia and small cell lung carcinoma. It has a role as an EC 1.14.99.66 (lysine-specific histone demethylase 1A) inhibitor and an antineoplastic agent. It is a member of benzoic acids, a monocarboxylic acid, a member of piperidines, a member of cyclopropanes, a tertiary amino compound, a secondary amino compound and a member of benzenes. | | in vitro | six days of gsk2879552 treatment resulted in potent anti-proliferative growth effects in 19 of 25 aml cell lines representing a range of aml subtypes. treating for longer time periods revealed sensitivity in all aml cell lines. aml blast colony forming ability was also inhibited in 4 of 5 bone marrow samples derived from primary aml patient samples [1]. | | in vivo | after 17 days of gsk2879552 treatment, control mice had 80% gfp+ cells in the bone marrow whereas treated mice had only 2.8% gfp positive cells, and the treated animals survived weeks beyond control mice [1]. | | References | 1) Mohammad?et al.?(2015),?A DNA Hypomethylation Signature Predicts Antitumor Activity of LSD1 Inhibitors in SCLC; Cancer Cell?28?57 |
| | GSK2879552 Preparation Products And Raw materials |
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