6-fluoro-N-(4-fluorobenzyl)quinazolin-4-aMine

6-fluoro-N-(4-fluorobenzyl)quinazolin-4-aMine
  • CAS No.:1262888-28-7

Important Notice

  1. This product is a chemical product/pharmaceutical intermediate. It is not a drug, an active pharmaceutical ingredient (API), or a pharmaceutical-grade material. It has not been granted a drug approval number or a Chemical Drug Substance Approval Notice, has not passed drug-related review and approval, and is not manufactured, tested, or released in accordance with pharmaceutical GMP.
  2. This product is intended solely for non-clinical research, process development, quality studies, further chemical processing, or chemical synthesis. It must not be used in drug-product manufacturing, clinical trials, clinical diagnosis, or administration to humans or animals, or be sold, used as an input, submitted for regulatory filing, or released as an API or pharmaceutical material.
  3. The purchaser must not use this product, or supply it to another party, for personal consumption, sports or fitness, weight loss, health supplements, food, or animal feed.
Other grades of this product :
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;C43;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
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)
pka5.75±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.
Safety Information
Hazard Codes Xi
Risk Statements 22-41
Safety Statements 26-39
WGK Germany 3
HS Code 2922390090
MSDS Information
6-fluoro-N-(4-fluorobenzyl)quinazolin-4-aMine Usage And Synthesis
DescriptionSpautin-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.1?Deranges dengue virion maturation.2?Spautin-1 inhibits autophagy in a Beclin-1 independent manner in primary epithelial ovarian cancer cells.3?Selectively induces cell death of mutant p53-expressing cancer cell lines under confluency.4?Cell permeable.
UsesSpautin-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.
UsesSpautin-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 ActionsSpautin-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.
in vitrospautin-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 500.6 and 0.7 μm for usp10 and usp13 activity, respectively
References1) Liu et al. (2011), Beclin1 controls the levels of p53 by regulating the deubiquitination activity of USP10 and USP13; Cell, 147 223 2) Mateo et al. (2013), Inhibition of cellular autophagy deranges dengue virion maturation; J. Virol., 87 1312 3) Correa et al. (2014), Combination of AKT inhibition with autophagy blockade effectively reduces ascites-derived ovarian cancer cell viability; Carcinogenesis,?35 1951 4) Vakifahmetoglu-Norburg et al. (1987), Chaperone-mediated autophagy degrades mutant p53; Genes Dev., 27 1718
6-fluoro-N-(4-fluorobenzyl)quinazolin-4-aMine Preparation Products And Raw materials
Raw materials2-Amino-5-fluorobenzoic acid-->6-FLUOROQUINAZOLIN-4-ONE-->2-AMINO-5-FLUOROBENZAMIDE-->4-CHLORO-6-FLUOROQUINAZOLINE-->4-Fluorobenzylamine

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