BTK-IN-51
BTK-IN-51 is an orally active, selective, and reversible BTK inhibitor with IC50s of 5.3 nM and 39 nM for BTKWT and BTKC481S, respectively. BTK-IN-51 shows >30-fold selectivity for BTK over most TEC/SRC family kinases, except for BLK (28-fold). BTK-IN-51 can be used for the study of rheumatoid arthritis.
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- CAS No.: 2375071-58-0
- Formule: C18H14FN5O2
- Masse moléculaire:351.33
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
IC50 & Target
[1]|
BTK 5.3 nM (IC50) |
BTKC481S 39 nM (IC50) |
BLK 150.2 nM (IC50) |
FYN 165.2 nM (IC50) |
TEC 227.0 nM (IC50) |
ITK 306.9 nM (IC50) |
SRC 902.5 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Ramos | EC50 |
42.7 nM
Compound: 25
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Reversible inhibition of sodium orthovanadate-stimulated BTK autophosphorylation at Tyr223 residues in human Ramos cells preincubated for 2 hrs followed by sodium orthovanadate addition and measured after 15 mins by Western blot analysis
Reversible inhibition of sodium orthovanadate-stimulated BTK autophosphorylation at Tyr223 residues in human Ramos cells preincubated for 2 hrs followed by sodium orthovanadate addition and measured after 15 mins by Western blot analysis
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[PMID: 31260299] |
| Sf21 | IC50 |
39 nM
Compound: 25
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Reversible inhibition of FAM-labeled peptide binding to full-length human N-terminal GST-tagged BTK C481S mutant (2 to 659 residues) expressed in baculovirus infected Sf21 insect cells preincubated for 10 mins followed by FAM-labeled peptide addition and
Reversible inhibition of FAM-labeled peptide binding to full-length human N-terminal GST-tagged BTK C481S mutant (2 to 659 residues) expressed in baculovirus infected Sf21 insect cells preincubated for 10 mins followed by FAM-labeled peptide addition and
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[PMID: 31260299] |
| Sf21 | IC50 |
5.3 nM
Compound: 25
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Reversible inhibition of FAM-labeled peptide binding to full-length human N-terminal GST-tagged BTK (2 to 659 residues) expressed in baculovirus infected Sf21 insect cells at preincubated for 10 mins followed by FAM-labeled peptide addition and measured b
Reversible inhibition of FAM-labeled peptide binding to full-length human N-terminal GST-tagged BTK (2 to 659 residues) expressed in baculovirus infected Sf21 insect cells at preincubated for 10 mins followed by FAM-labeled peptide addition and measured b
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[PMID: 31260299] |
In Vitro
BTK-IN-51 (compound 25) (0.03-1 μM; 2 h) dose-dependently inhibits the autophosphorylation of BTK at Tyr223 in Ramos cells[1].
BTK-IN-51 (compound 25) (1 μM; 2 h) exhibits excellent plasma stability at 37 °C, with ≥ 88% of the parent compound remaining in plasma from humans, dogs, rats, mice, and monkeys and no significant interspecies differences observed[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Ramos cells
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Concentration:0.03 μM, 0.1 μM, 0.3 μM, 1 μM
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Incubation Time:2 h
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Result:Exhibited dose-dependent inhibition and efficiently blocked Tyr223 autophosphorylation at a concentration of 1 μM (EC50 = 42.7 nM).
Parmacokinetics
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male DBA/1 mice received intradermal injections at the base of the tail containing bovine collagen type II emulsified in Complete Freund's Adjuvant (CFA) on day 0, and were challenged with collagen type II in Incomplete Freund's Adjuvant (IFA) on day 20[1].
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Dosage:10 mg/kg
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Administration:Oral gavage (p.o.); once a day; 14 days
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Result:Effectively inhibited the progression of arthritis and significantly decreased paw volumes.
Exhibited comparable efficacy to Dexamethasone (HY-14648) (0.2 mg/kg; p.o.; once a day; 14 days).
Chemical Information
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CAS No. 2375071-58-0
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Masse moléculaire 351.33
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Formule C18H14FN5O2
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SMILES
FC1=C2C(N=CC(C(N)=O)=C2N)=C(C3=C(OC)C=C(C=NN4)C4=C3)C=C1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
BTK-IN-51 Related Classifications
HY-128725 Related Classifications
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