Spautin-1

Modify Date: 2024-01-08 11:54:48

Spautin-1 Structure
Spautin-1 structure
Common Name Spautin-1
CAS Number 1262888-28-7 Molecular Weight 271.265
Density 1.4±0.1 g/cm3 Boiling Point 419.6±40.0 °C at 760 mmHg
Molecular Formula C15H11F2N3 Melting Point N/A
MSDS Chinese USA Flash Point 207.6±27.3 °C
Symbol GHS05 GHS07
GHS05, GHS07
Signal Word Danger

 Use of Spautin-1


Spautin-1 is a specific and potent autophagy inhibitor-1.

 Names

Name spautin-1
Synonym More Synonyms

 Spautin-1 Biological Activity

Description Spautin-1 is a specific and potent autophagy inhibitor-1.
Related Catalog
In Vitro Spautin-1 enhances imatinib mesylate (IM)-induced CmL cell apoptosis by reducing the expression of the anti-apoptotic proteins Mcl-1 and Bcl-2. The pro-apoptotic activity of spautin-1 is associated with activation of GSK3β, an important downstream effector of PI3K/AKT. Spautin-1 enhances IM-induced cytotoxicity in CmL cell line K562, decreasing the IC50 from 1 to 0.5 μM[1]. The mechanism of spautin-1 acting on acute pancreatitis is associated with impaired autophagy inhibition[2].
In Vivo Spautin-1 ameliorates the pathogenesis of acute pancreatitis induced by cerulein or L-arginine. Spautin-1 pretreatment significantly diminishes the elevation of serum amylase and lipase levels, which are indicative of trypsin activity. Increasing levels of serum TNFα caused by cerulein are inhibited in the presence of spautin-1. Spautin-1 treatment can ameliorate the inflammation damage induced by cerulein, such as edema, degeneration, coagulative necrosis and infiltration of inflammatory cells[2].
Cell Assay Spautin-1 is dissolved in DMSO. Cell proliferation is evaluated using CCK-8 kit. K562 cells (1x105/mL) are seeded into 96-well plates in triplicate and then treated with 125 to 4,000 nM IM alone or in combi¬nation with spautin-1 (10 μM). After 48 h of incubation, 10 μL of CCK-8 reagent is added to each well. Four hours later, the absorbance is read at 450 nm using a microplate reader[1].
Animal Admin Mice: In this study, mice models with acute pancreatitis, including cerulein- and L-arginine-induced models, are constructed. For the cerulein-induced model, four intraperitoneal injections of cerulein (50 μg/kg body weight) are given consecutively at hourly intervals; The L-arginine-induced model received hourly intraperitoneal injections of 1.4 g/kg (optimal dosage for this study) L-arginine three times[2].
References

[1]. Shao S, et al. Spautin-1, a novel autophagy inhibitor, enhances imatinib-induced apoptosis in chronic myeloid leukemia. Int J Oncol. 2014 May;44(5):1661-1668.

[2]. Xiao J, et al. Spautin-1 Ameliorates Acute Pancreatitis via Inhibiting Impaired Autophagy and Alleviating Calcium Overload. Mol Med. 2016 Aug 18;22.

 Chemical & Physical Properties

Density 1.4±0.1 g/cm3
Boiling Point 419.6±40.0 °C at 760 mmHg
Molecular Formula C15H11F2N3
Molecular Weight 271.265
Flash Point 207.6±27.3 °C
Exact Mass 271.092102
PSA 37.81000
LogP 3.40
Vapour Pressure 0.0±1.0 mmHg at 25°C
Index of Refraction 1.672

 Safety Information

Symbol GHS05 GHS07
GHS05, GHS07
Signal Word Danger
Hazard Statements H302-H318
Precautionary Statements P280-P305 + P351 + P338
Hazard Codes Xi
Risk Phrases 22-41
Safety Phrases 26-39
RIDADR NONH for all modes of transport
HS Code 2933990090

 Customs

HS Code 2933990090
Summary 2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

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 Synonyms

spautin-1, autophagy inhibitor (6-fluoro-n-(4-fluorobenzyl)quinozaline-4-amine)
6-fluoro-n-(4-fluorobenzyl)quinazolin-4-amine
4-Quinazolinamine, 6-fluoro-N-[(4-fluorophenyl)methyl]-
6-Fluoro-N-(4-fluorobenzyl)-4-quinazolinamine
Spautin 1