[CAS NO. 1287665-60-4] AS2444697

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PRODUCTS SPECIFICATIONS [1287665-60-4]

Catalog

HY-18992

Brand

MCE

CAS

1287665-60-4

DESCRIPTION [1287665-60-4]

Overview

MDL	MFCD30182294
Molecular Weight	432.86
Molecular Formula	C19H21ClN6O4
SMILES	O=C(NC1=CN(C2CCOCC2)N=C1C(N)=O)C3=COC(C4=CC=NC(C)=C4)=N3.[H]Cl

For research use only. We do not sell to patients.

Summary

AS2444697 is an orally active IRAK-4 inhibitor with an IC ₅₀ of 21 nM ^[1] . AS2444697 potently inhibits human and rat IRAK-4 activity. AS2444697 exhibits renoprotective effects through anti-inflammatory action ^[2] .

IC50 & Target

IRAK4

21 nM (IC ₅₀ )

In Vivo

AS2444697 is efficacious in the rat adjuvant-induced arthritis (ED ₅₀ 2.7 mg/kg, BID, PO) and the rat collagen-induced arthritis (ED ₅₀ 1.6 mg/kg, BID, PO) disease models. Good bioavailability was seen in rat (F% 50) and dog (F% 78) pharmacokinetic studies ^[1] .
AS2444697 (0.3-3 mg/kg) significantly increases the plasma levels of IL-1β, IL-6, TNF-α, MCP-1, and aminotransferases (ALT and AST) in LPS/GalN-treated mice. Single administration of AS2444697 (0.3-3 mg/kg) dose-dependently decreases plasma levels of these all parameters, and these effects were significant at doses of 1 mg/kg or higher ^[2] .
After oral administration of AS2444697 (3 mg/kg) to 5/6 Nx rats, plasma, and tissue (liver and kidney) concentrations of the unchanged drug peaked at 1 h and then gradually decreased, with a terminal half-life of 2.7-2.9 h ^[2] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Male 6-week-old Wistar rats and Balb/c mice ^[2]
Dosage:	0.3-3 mg/kg
Administration:	Single administration; orally
Result:	The plasma levels of IL-1β, IL-6, TNF-α, MCP-1, and aminotransferases (ALT and AST) were significantly increased.

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : ≥ 12.5 mg/mL ( 28.88 mM )

* "≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.3102 mL	11.5511 mL	23.1022 mL
5 mM	0.4620 mL	2.3102 mL	4.6204 mL
10 mM	0.2310 mL	1.1551 mL	2.3102 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: 1.67 mg/mL (3.86 mM); Suspended solution; Need ultrasonic
2.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 1.67 mg/mL (3.86 mM); Clear solution

* All of the co-solvents are available by MCE.