1. Protein Tyrosine Kinase/RTK
  2. Btk
  3. BTK inhibitor 17

BTK inhibitor 17 

Cat. No.: HY-131705
Handling Instructions

BTK inhibitor 17 is a potent and orally active irreversible BTK inhibitor with an IC50 of 2.1 nM. BTK inhibitor 17 can be used for rheumatoid arthritis research.

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

BTK inhibitor 17 Chemical Structure

BTK inhibitor 17 Chemical Structure

CAS No. : 1858206-76-4

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Description

BTK inhibitor 17 is a potent and orally active irreversible BTK inhibitor with an IC50 of 2.1 nM. BTK inhibitor 17 can be used for rheumatoid arthritis research[1].

IC50 & Target

IC50: 2.1 nM (BTK)[1]

In Vitro

BTK inhibitor 17 (compound 8) could covalently bind to Cys481 and formed an HB network with hinge key residues Met477, Glu475, and gatekeeper Thr474[1].

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

In Vivo

BTK inhibitor 17 (compound 8; 3-10 mg/kg; oral gavage; daily; for 28 days) treatment inhibits the significant progression of the disease and exhibits a clear dose-dependent reduction per paw clinical scores, and no significant body weight loss is observed for all different dosages[1].
BTK inhibitor 17 (compound 8) shows >95% plasma protein binding across three species of human, rat, and mouse. After an intravenous injection, the half-life (rat, 0.32 h; mice, 0.42 h), clearance (rat, 54.6 mL/min/kg; mice, 31.3 mL/min/kg), volume of distribution (rat, 1.55 L/kg; mice, 0.82 L/kg), and AUC exposure (rat, 604 ng.h/mL; mice, 576 ng.h/mL) are observed in two species. After oral administration, BTK inhibitor 17 exhibits higher Cmax (rat, 466 ng/mL; mice, 252 ng/mL) and plasma exposure (rat, 642 ng.h/mL; mice, 128 ng.h/mL) with a favorable oral bioavailability (rat, 23.7%; mice, 11.2%)[1].

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

Animal Model: Male Balb/C mice injected with collagen[1]
Dosage: 3 mg/kg or 10 mg/kg
Administration: Oral gavage; daily; for 28 days
Result: Inhibited the significant progression of the disease and exhibited a clear dose-dependent reduction per paw clinical scores.
Molecular Weight

456.50

Formula

C₂₅H₂₄N₆O₃

CAS No.

1858206-76-4

SMILES

O=C1C(N([[email protected]]2CN(C(C=C)=O)CCC2)N=C3C4=CC=C(OC5=CC=CC=C5)C=C4)=C3C(N)=NN1

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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Keywords:

BTK inhibitor 17BTK inhibitor17BTK inhibitor-17BtkBruton tyrosine kinaseCys481oralrheumatoidarthritisInhibitorinhibitorinhibit

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BTK inhibitor 17
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