1. Immunology/Inflammation
  2. IRAK
  3. IRAK4-IN-14

IRAK4-IN-14 

Cat. No.: HY-146112
Handling Instructions

IRAK4-IN-14 (compound 28) is a potent, selective and orally active IRAK4 inhibitor with an IC50 of 0.003 µM. IRAK4-IN-14 shows good PK parameters in rats and mouse. IRAK4-IN-14 shows synergistic in vitro activity against MyD88/CD79 double mutant ABC-DLBCL in combination with Acalabrutinib.

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

IRAK4-IN-14 Chemical Structure

IRAK4-IN-14 Chemical Structure

CAS No. : 2667681-71-0

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Description

IRAK4-IN-14 (compound 28) is a potent, selective and orally active IRAK4 inhibitor with an IC50 of 0.003 µM. IRAK4-IN-14 shows good PK parameters in rats and mouse. IRAK4-IN-14 shows synergistic in vitro activity against MyD88/CD79 double mutant ABC-DLBCL in combination with Acalabrutinib[1].

IC50 & Target[1]

IRAK4

0.003 μM (IC50)

In Vitro

IRAK4-IN-14 (compound 28) shows cell pIRAK4 potencies with an IC50 of 0.11 µM[1].
IRAK4-IN-14 (compound 28) shows selectivity with IC50s of 0.003,1.4, >8, >9, 0.053, 0.27, 0.76, 0.27 µM for IRAK4, IRAK1, BTK, Flt3, PI3Kδ, TRKa, TRKb, TRKc, respectively[1].

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

In Vivo

IRAK4-IN-14 (i.v. or p.o.) shows good PK parameters with oral bioavailability of 66% for mouse[1].
Pharmacokinetic Parameters of IRAK4-IN-14 in Male Han Wistar rats, male CD1 mice, male Cynomolgus monkeys[1].

parameter Value
A2B Papp 31
Efflux ratio 1.4
Solubility (µM) 800
Rat/mouse/monkey/human %free 21/16/33/21
Rat LM/H CLint 16/5.6
Mouse LM/H CLint 13/11
Minipig LM/H CLint 18/8.2
Dog LM/H CLint 21/4.5
Monkey LM/H CLint 35/4.7
Rat CL 15
Vdss 4.3
t1/2 5.2
F% 55%
Mouse CL 17
Vdss 4.1
t1/2 4.2
F% 66%
Monkey CL 68
Vdss 8.6
t1/2 1.4
Male Han Wistar rats; 1 mg/kg i.v.; 2 mg/kg p.o.; Male CD1 mice; 0.5 mg/kg i.v.; 1 mg/kg p.o.; Male Cynomolgus monkeys; 1 mg/kg i.v.[1].

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

Molecular Weight

489.55

Formula

C25H28FN9O

CAS No.
SMILES

CC1=NC=C(C2=NC3=C(OC4(C)CC4)N=C(NC5=CN(C6CCN(C)CC6)N=C5)N=C3C=C2F)C=N1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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