BTK inhibitor 18
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.
- Formula: C29H25N5O4S2
- Molecular Weight:571.67
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
IC50: 142 nM (Btk)[1]
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:A rat collagen-induced arthritis (CIA) model[1]
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Dosage:1 mg/kg, 3 mg/kg, 10 mg/kg, 30 mg/kg
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Administration:Oral administration; once a day; for 7 days
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Result:Attenuated hind paw inflammation in a dose-dependent manner.
Chemical Information
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Molecular Weight 571.67
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Formula C29H25N5O4S2
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SMILES
CC1=CC(OC2=CC=CC=C2)=CC=C1N3C4=C5C(NC3=O)=C(C(N[C@H]6CN(C(C=C)=O)CC6)=O)SC5=NC=C4.[*S]
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)