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

BTK inhibitor 17 

Cat. No.: HY-131705 Purity: 98.98%
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

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 452 In-stock
Estimated Time of Arrival: December 31
5 mg USD 450 In-stock
Estimated Time of Arrival: December 31
10 mg USD 800 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1650 In-stock
Estimated Time of Arrival: December 31
50 mg USD 2550 In-stock
Estimated Time of Arrival: December 31
100 mg USD 3800 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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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.
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
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (219.06 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1906 mL 10.9529 mL 21.9058 mL
5 mM 0.4381 mL 2.1906 mL 4.3812 mL
10 mM 0.2191 mL 1.0953 mL 2.1906 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.48 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.5 mg/mL (5.48 mM); Clear solution

  • 3.

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

    Solubility: ≥ 2.5 mg/mL (5.48 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

BTK inhibitor 17BTK inhibitor17BTK inhibitor-17BtkBruton tyrosine kinaseCys481oralrheumatoidarthritisInhibitorinhibitorinhibit

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BTK inhibitor 17
Cat. No.:
HY-131705
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