1. Protein Tyrosine Kinase/RTK
  2. Btk
  3. BTK inhibitor 18

BTK inhibitor 18 

Cat. No.: HY-132196
Handling Instructions

BTK inhibitor 18 is a potent, selective,orally active and covalent Btk inhibitor with a IC50 of 142 nM. BTK inhibitor 18 has anti-inflammatory activities.

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

BTK inhibitor 18 Chemical Structure

BTK inhibitor 18 Chemical Structure

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Description

BTK inhibitor 18 is a potent, selective,orally active and covalent Btk inhibitor with a IC50 of 142 nM. BTK inhibitor 18 has anti-inflammatory activities[1].

IC50 & Target

IC50: 142 nM (Btk)[1]

In Vitro

BTK inhibitor 18 (Compound 27) irreversibly inhibits BTK by targeting a noncatalytic cysteine residue (Cys481) for covalent bond formation[1].
BTK inhibitor 18 (Compound 27) inhibits anti-IgM-induced activation of B cells in human whole blood with an IC50 of 84 nM[1].
BTK inhibitor 18 (Compound 27) also inhibits BMX, LCK, ErbB4, TEC, and TXK kinases with IC50 values of 129 nM, 130 nM, 377 nM, 409 nM, 1770 nM, respectively[1].

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

In Vivo

BTK inhibitor 18 (Compound 27; 1-30 mg/kg; oral administration; once a day; for 7 days) treatment shows dose-dependent efficacy at reducing joint inflammation in a rat collagen-induced arthritis model[1].
The IV and PO pharmacokinetics of BTK inhibitor 18 (Compound 27) are investigated in nonfasted rats (1 and 5 mg/kg IV and PO) and fasted dogs (0.5 and 2.5 mg/kg IV and PO). IV pharmacokinetics are characterized by moderate clearance in rat and low clearance in dog, a moderate volume of distribution, and a short plasma half-life across both species (T1/2 of 0.3 h and 1.9 h for rat and dog, respectively). The oral bioavailability is 30% and 68% in rat and dog, respectively[1].

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

Animal Model: A rat collagen-induced arthritis (CIA) model[1]
Dosage: 1 mg/kg, 3 mg/kg, 10 mg/kg, 30 mg/kg
Administration: Oral administration; once a day; for 7 days
Result: Attenuated hind paw inflammation in a dose-dependent manner.
Molecular Weight

571.67

Formula

C₂₉H₂₅N₅O₄S₂

SMILES

CC1=CC(OC2=CC=CC=C2)=CC=C1N3C4=C5C(NC3=O)=C(C(N[[email protected]]6CN(C(C=C)=O)CC6)=O)SC5=NC=C4.[*S]

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

References
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Keywords:

BTK inhibitor 18BTK inhibitor18BTK inhibitor-18BtkBruton tyrosine kinaseirreversiblecovalentautoimmuneanti-inflammatoryoralInhibitorinhibitorinhibit

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BTK inhibitor 18
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HY-132196
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