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

BTK-IN-17 (compound 36R) is a selective and orally activeBTK inhibitor with an IC50 value of 13.7 nM. BTK-IN-17 decreases the expression of p-BTKY223 and p-PLCγ2Y1217. BTK-IN-17 shows anti-inflammatory effects.

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BTK-IN-17 Chemical Structure

BTK-IN-17 Chemical Structure

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Description

BTK-IN-17 (compound 36R) is a selective and orally activeBTK inhibitor with an IC50 value of 13.7 nM. BTK-IN-17 decreases the expression of p-BTKY223 and p-PLCγ2Y1217. BTK-IN-17 shows anti-inflammatory effects[1].

IC50 & Target

IC50: 13.7 nM (BTK)[1]

In Vitro

BTK-IN-17 (compound 36R) shows hERG channel inhibition with an IC50 value of 8.6 µM[1].
BTK-IN-17 (0-10000 nM) decreases the expression of p-BTKY223 and p-PLCγ2Y1217 in Ramos cells[1].

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

Western Blot Analysis[1]

Cell Line: Ramos cells
Concentration: 0-10000 nM
Incubation Time:
Result: Inhibited phosphorylation of downstream BTK (p-BTKY223) and phosphorylation of PLCγ2 (p-PLCγ2Y1217).
In Vivo

BTK-IN-17 (1 mg/kg for i.v.; 10 mg/kg for p.o.) shows the plasma concentrations rapidly reached 125 nM and BTK occupancy reached 79%one hour after oral administration, target occupancy of roughly 62% was maintained after 24 h in rats[1].
BTK-IN-17 (10, 30, 50 mg/kg; p.o.; once daily for 10 days) shows good anti-inflammatory effects in rats[1].
Pharmacokinetic Parameters of BTK-IN-17 in Male Sprague-Dawley rats[1].

iv (1 mg/kg) po (10 mg/kg)
C0 (ng·mL-1) 786±121 -
C max (ng·mL-1) - 52.5±11.3
T1/2 (h) 0.73±0.05 1.67±0.27
Tmax (h) - 1.00±0.5
AUC(ng·h·mL-1) 454±25 164±18
CL (mL·kg-1·min-1) 36.8±2.0 -
Vdss (L·kg-1) 1.67±0.04 -
F (%) - 3.6±0.4
Sprague-Dawley rats, 1 mg/kg for i.v.; 10 mg/kg p.o.[1].

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

Molecular Weight

465.51

Formula

C26H23N7O2

SMILES

C=CC(N1CC[C@H](C1)N2N=C(C3=CNC4=NC=NC2=C34)NC5=CC=C(C=C5)OC6=CC=CC=C6)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation
References
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BTK-IN-17 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
BTK-IN-17
Cat. No.:
HY-151920
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