DC Chemicals Limited
China
Product Name: ALS-8112
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Purity: 98.0%
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1445379-92-9

1445379-92-9 structure

1445379-92-9 structure

Name: ALS-8112
Chemical Name: ALS-8112
CAS Number: 1445379-92-9
Molecular Formula: C₁₀H₁₃ClFN₃O₄
Molecular Weight: 293.679
Catalog: Signaling Pathways Anti-infection RSV
Create Date: 2018-03-22 12:31:49
Modify Date: 2024-01-10 22:47:41
ALS-8112 is a potent and selective respiratory syncytial virus (RSV) polymerase inhibitor. The 5'-triphosphate form of ALS-8112 inhibits RSV polymerase with an IC50 of 0.02 μM.

Name	ALS-8112
Synonyms	7795987MKM 2(1H)-Pyrimidinone, 4-amino-1-[5-chloro-2,5-dideoxy-2-fluoro-4-C-(hydroxymethyl)-α-L-lyxofuranosyl]- 4-Amino-1-[5-chloro-2,5-dideoxy-2-fluoro-4-(hydroxymethyl)-α-L-lyxofuranosyl]-2(1H)-pyrimidinone 4'-CHLOROMETHYL-2'-DEOXY-2'-FLUOROCYTIDINE

Description	ALS-8112 is a potent and selective respiratory syncytial virus (RSV) polymerase inhibitor. The 5'-triphosphate form of ALS-8112 inhibits RSV polymerase with an IC50 of 0.02 μM.
Related Catalog	Signaling Pathways >> Anti-infection >> RSV Research Areas >> Infection
Target	IC50: 0.02 μM (RSV)[1]
In Vitro	The 5'-triphosphate form of ALS-8112 (ALS-8112-TP) is the active form of the drug and selectively inhibits RSV polymerase through chain termination of RNA synthesis[2]. ALS-008112 enters various types of epithelial cells in the respiratory tract and is subsequently phosphorylated to form an intracellular nucleoside triphosphate with a half-life of approximately 29 hours. The nucleoside triphosphate analogue inhibits RSV replication by means of chain termination[3]. ALS-8112 is a pan-strain inhibitor of RSV replication in vitro. The RNA transcription activity of the RSV–RNP complex is dose-proportionally inhibited by ALS-8112-TP with an IC50 of 0.020 ± 0.008 μM[4].
Cell Assay	ALS-8112 and its prodrug ALS-8176 are stored at 4°C in dimethyl sulfoxide (DMSO), and diluted in water. HEp-2 cells per well are plated in a 96-well plate. Each compound is serially diluted (1:3) up to 9 distinct concentrations. Cells are pre-incubated with compounds for 24 hours at 37°C in a 5% CO2 atmosphere. After 24 hours of pre-incubation with compounds, RSV A2, Long, or B1 at a multiplicity of infection (MOI) of 0.5 is added to the cells, except for the background controls. The plate is then incubated for additional 4 days in the same conditions and at the end of the incubation 50 μL the supernatant from each well of the plate is collected[4].
References	[1]. Wang G, et al. Discovery of 4'-chloromethyl-2'-deoxy-3',5'-di-O-isobutyryl-2'-fluorocytidine (ALS-8176), a first-in-class RSV polymerase inhibitor for treatment of human respiratory syncytial virus infection. J Med Chem. 2015 Feb 26;58(4):1862-78. [2]. Jordan PC, et al. Activation Pathway of a Nucleoside Analog Inhibiting Respiratory Syncytial Virus Polymerase. ACS Chem Biol. 2017 Jan 20;12(1):83-91. [3]. DeVincenzo JP, et al. Activity of Oral ALS-008176 in a Respiratory Syncytial Virus Challenge Study. N Engl J Med. 2015 Nov 19;373(21):2048-58. [4]. Deval J, et al. Molecular Basis for the Selective Inhibition of Respiratory Syncytial Virus RNA Polymerase by 2'-Fluoro-4'-Chloromethyl-Cytidine Triphosphate. PLoS Pathog. 2015 Jun 22;11(6):e1004995.

Density	1.8±0.1 g/cm3
Boiling Point	532.8±60.0 °C at 760 mmHg
Molecular Formula	C₁₀H₁₃ClFN₃O₄
Molecular Weight	293.679
Flash Point	276.0±32.9 °C
Exact Mass	293.057861
LogP	-0.42
Vapour Pressure	0.0±3.2 mmHg at 25°C
Index of Refraction	1.668
Storage condition	2-8℃