- Spautin-1
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- $48.00
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2026-05-11
- CAS:1262888-28-7
- Purity: 99.78%
- Supply Ability: 10g
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| | 6-fluoro-N-(4-fluorobenzyl)quinazolin-4-aMine Basic information |
| Product Name: | 6-fluoro-N-(4-fluorobenzyl)quinazolin-4-aMine | | Synonyms: | 6-fluoro-N-(4-fluorobenzyl)quinazolin-4-aMine;6-Fluoro-N-[(4-fluorophenyl)methyl]-4-quinazolinamine;4-((4-Fluorobenzyl)amino)-6-fluoroquinazoline;Spautin-1;6-Fluoro-N-(4-fluorobenzyl)-4-quinazolinamine;6-Fluoro-N-[(4-fluorophenyl)methyl]quinazolin-4-amine;Spautin 1 - MBCQ derivative C43;CS-1649 | | CAS: | 1262888-28-7 | | MF: | C15H11F2N3 | | MW: | 271.26 | | EINECS: | | | Product Categories: | Inhibitors | | Mol File: | 1262888-28-7.mol |  |
| | 6-fluoro-N-(4-fluorobenzyl)quinazolin-4-aMine Chemical Properties |
| Melting point | 211 °C | | Boiling point | 419.6±40.0 °C(Predicted) | | density | 1.366±0.06 g/cm3(Predicted) | | storage temp. | 2-8°C | | solubility | DMSO: soluble15mg/mL (clear solution) | | pka | 5.75±0.50(Predicted) | | form | powder | | color | white to beige | | Stability: | Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 3 months. | | InChI | 1S/C15H11F2N3/c16-11-3-1-10(2-4-11)8-18-15-13-7-12(17)5-6-14(13)19-9-20-15/h1-7,9H,8H2,(H,18,19,20) | | InChIKey | AWIVHRPYFSSVOG-UHFFFAOYSA-N | | SMILES | FC1=CC=C(C=C1)CNC2=C3C=C(F)C=CC3=NC=N2 |
| Hazard Codes | Xi | | Risk Statements | 22-41 | | Safety Statements | 26-39 | | WGK Germany | 3 | | HS Code | 2922390090 | | Storage Class | 11 - Combustible Solids | | Hazard Classifications | Acute Tox. 4 Oral
Eye Dam. 1 |
| | 6-fluoro-N-(4-fluorobenzyl)quinazolin-4-aMine Usage And Synthesis |
| Description | Spautin-1 (1262888-28-7) is a specific and potent autophagy inhibitor. Spautin-1 promotes the degradation of Vps34 PI3 kinase complexes by inhibiting two ubiquitin-specific proteases USP10 and USP13 which target the Beclin-1 subunit of Vps34 complexes.1Deranges dengue virion maturation.2Spautin-1 inhibits autophagy in a Beclin-1 independent manner in primary epithelial ovarian cancer cells.3Selectively induces cell death of mutant p53-expressing cancer cell lines under confluency.4Cell permeable. | | Uses | Spautin-1 is a potent pharmacological autophagy inhibitor that promotes UVB-induced tumorigenesis. It is also a small-molecule drug that modulate autophagic pathways in different types of cancer. | | Uses | Spautin-1 has been used as an autophagy inhibitor:
- to study its effects on vascular, glial, and neuronal alterations in the oxygen-induced retinopathy mouse model
- to evaluate its pre-treatment effect on the response of canine osteosarcoma cells to doxorubicin
- to study its effects on the production of interleukin (IL)-6 by oxidatively stressed dendritic cells (OS-DCs) in Luminex assay
| | Biochem/physiol Actions | Spautin-1 inhibits the activity of two ubiquitin-specific peptidases, USP10 and USP13, causing an increase in proteasomal degradation of class III PI3 kinase complexes, which have been shown to regulate autophagy. | | Synthesis | GENERAL METHOD: 4-Chloro-6-fluoroquinazoline (1.84 g, 10 mmol), trimethylamine (1.06 g, 10 mmol) were mixed with p-fluorobenzylamine (10 mmol) in 5 mL N,N-dimethylformamide (DMF). The reaction mixture was heated to reflux for 4 h, subsequently cooled to room temperature and decanted into crushed ice. The precipitated solid was collected by filtration and purified by recrystallization with ethanol. The melting points of the resulting 6-fluoro-N-(4-fluorobenzyl)quinazolin-4-amines were all above 300 °C. | | in vitro | spautin-1 promotes the degradation of vps34 pi3 kinase complexes via inhibiting two ubiquitinspecific peptidases, usp10 and usp13, that target the beclin1 subunit of vps34 complexes. spautin-1 had no effect on the growth and survival of bcap-37 cells under normal culture conditions but dramatically enhanced cell death in glucose-free media. under glucose-free conditions, western blotting for lc3 further confirmed that autophagy was induced, which was inhibited by spautin-1. similar results were obtained with mcf-7 and bt549 cells. therefore, spautin-1 can sensitize tumor cells to apoptosis under nutritional deprived conditions [1]. | | IC 50 | 0.6 and 0.7 μm for usp10 and usp13 activity, respectively | | storage | Store at +4°C | | References | [1] JUNLI LIU. Beclin1 controls the levels of p53 by regulating the deubiquitination activity of USP10 and USP13.[J]. Cell, 2011, 147 1: 223-234. DOI:10.1016/j.cell.2011.08.037
[2] ROBERTO MATEO. Inhibition of cellular autophagy deranges dengue virion maturation.[J]. Journal of Virology, 2013, 87 3: 1312-1321. DOI:10.1128/jvi.02177-12
[3] ROHANN J M CORREA. Combination of AKT inhibition with autophagy blockade effectively reduces ascites-derived ovarian cancer cell viability.[J]. Carcinogenesis, 2014, 35 9: 1951-1961. DOI:10.1093/carcin/bgu049
[4] HELIN VAKIFAHMETOGLU-NORBERG. Chaperone-mediated autophagy degrades mutant p53.[J]. Genes & development, 2013, 27 15: 1718-1730. DOI:10.1101/gad.220897.113 |
| | 6-fluoro-N-(4-fluorobenzyl)quinazolin-4-aMine Preparation Products And Raw materials |
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