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HomeProduct name listSaracatinib

Saracatinib

  • CAS NO.:379231-04-6
  • Empirical Formula: C27H32ClN5O5
  • Molecular Weight: 542.03
  • MDL number: MFCD09832698
  • EINECS: 1592732-453-0
  • SAFETY DATA SHEET (SDS)
  • Update Date: 2024-11-05 19:05:58
Saracatinib Structural

What is Saracatinib?

Description

Saracatinib is a dual inhibitor of the tyrosine kinases c-Src and Abl (IC50 = 2.7 and 30 nM, respectively). It less effectively inhibits other receptor and non-receptor tyrosine kinases as well as assorted serine/threonine kinases. Saracatinib is orally available and blocks cell motility, migration, adhesion, invasion, proliferation, differentiation, and survival. Through its effects on c-Src, it reduces osteoclast bone resorption. Saracatinib also blocks denque virus RNA replication through its effect on Fyn kinase.

Chemical properties

White Solid

The Uses of Saracatinib

An oral, selective dual inhibitor of Src and ABL kinase. It is a COVID19-related research product.

The Uses of Saracatinib

An oral, selective dual inhibitor of Src and ABL kinase.

Definition

ChEBI: Saracatinib is a member of the class of quinazolines that is quinazoline substituted by (5-chloro-2H-1,3-benzodioxol-4-yl)amino, (oxan-4-yl)oxy and 2-(4-methylpiperazin-1-yl)ethoxy groups at positions 4, 5 and 7, respectively. It is a dual inhibitor of the tyrosine kinases c-Src and Abl (IC50 = 2.7 and 30 nM, respectively). Saracatinib was originally developed by AstraZeneca for the treatment of cancer but in 2019 it was granted orphan drug designation by the US Food and Drug Administration for the treatment of idiopathic pulmonary fibrosis (IPF), a type of lung disease that results in scarring (fibrosis) of the lungs. It has a role as an antineoplastic agent, an EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor, a radiosensitizing agent, an autophagy inducer, an apoptosis inducer and an anticoronaviral agent. It is a member of quinazolines, a secondary amino compound, a N-methylpiperazine, an aromatic ether, a member of oxanes, a member of benzodioxoles, an organochlorine compound and a diether.

What are the applications of Application

Saracatinib is a diverse Src inhibitor

storage

Store at -20°C

References

Hennequin et al. (2006), N-(5-chloro-1,3-benzodioxol-4-yl)-7-[2-(4-methylpiperazin-1-yl)ethoxy]-5-(tetrahydro-2H-pyran-4-yloxy)quinazolin-4-amine, a novel, highly selective, orally available, dual-specific c-Src/Abl kinase inhibitor; J. Med. Chem., 49 6465 Green et al. (2009), Preclinical anticancer activity of the potent, oral Src inhibitor AZD0530; Oncol., 3 248 de Wispelaere et al. (2013), The small molecules AZD0530 and Dasatinib inhibit dengue virus RNA replication via Fyn kinase; Virol., 87 7367 Shin et al. (2018), Saracatinib Inhibits Middle East Respiratory Syndrome-Coronavirus Replication In Vitro; Viruses, 10 283 Tang et al. (2020), Fyn kinase inhibition reduces protein aggregation, increases synapse density and improves memory in transgenic mice and traumatic Tauopathy; Acta Neuropathol. Commun., 8 96 Kaufman et al. (2015), Fyn inhibition rescues established memory and synapse loss in Alzheimer mice; Neurol., 77 953

Properties of Saracatinib

Melting point: 84-89°C
Boiling point: 671.2±55.0 °C(Predicted)
Density  1.348
storage temp.  -20°C
solubility  Soluble in DMSO (50 mg/ml) and ethanol (54 mg/mL with warming)
form  solid
pka 7.55±0.10(Predicted)
color  White
Stability: Stable for 2 years from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months.

Safety information for Saracatinib

Signal word Warning
Pictogram(s)
ghs
Exclamation Mark
Irritant
GHS07
GHS Hazard Statements H317:Sensitisation, Skin
H319:Serious eye damage/eye irritation
Precautionary Statement Codes P280:Wear protective gloves/protective clothing/eye protection/face protection.
P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

Computed Descriptors for Saracatinib

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