2. Protein Tyrosine Kinase/RTK Immunology/Inflammation Apoptosis
  3. Btk Pyroptosis
  4. BTK-IN-15

BTK-IN-15 (compound 42) is a potent Bruton's tyrosine kinase (BTK) inhibitor with high oral absorption. BTK-IN-15 inhibits BTK with an IC50 value of 0.7 nM. BTK-IN-15 displays excellent kinase selectivity, antitumor activity, and induces apoptosis.

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BTK-IN-15 Chemical Structure

BTK-IN-15 Chemical Structure

CAS No. : 2820426-92-2

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BTK-IN-15 Related Antibodies

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Description

BTK-IN-15 (compound 42) is a potent Bruton's tyrosine kinase (BTK) inhibitor with high oral absorption. BTK-IN-15 inhibits BTK with an IC50 value of 0.7 nM. BTK-IN-15 displays excellent kinase selectivity, antitumor activity, and induces apoptosis[1].

IC50 & Target

IC50: 0.7 nM (BTK)[1]
In Vitro

BTK inhibition is an effective approach against B-cell malignancies[1].
BTK-IN-15 (compound 42) demonstrates inhibitory against TMD8 with an IC50 value of 2.6 nM[1].
BTK-IN-15 (1 μM; 1 h) displays significant selectivity to BTK over EGFR kinase with 0.05% and 44% of the control, respectively[1].
BTK-IN-15 (0-1 mM; 72 h) exerts potent anti-proliferative activity against a human mantle cell lymphoma cell line (REC-1) with an IC50 value of 1.7 nM[1].
BTK-IN-15 (0-1 mM; 2 h) inhibits BTK auto-phosphorylation with an IC50 value of 1.49 nM[1].
BTK-IN-15 (0-100 nM; 48 h) arrests cell cycle at G1 phase and (0-1 mM; 72 h) induces apoptosis in TMD8[1].
BTK-IN-15 shows low hERG channel activity (IC50=4.38 μM), indicating low cardiotoxicity[1].

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

BTK-IN-15 Related Antibodies

Western Blot Analysis[1]

Cell Line: B-cell lymphoma (DLBCL) TMD8 cancer cells
Concentration: 0, 0.15, 0.46, 1.37, 4.12, 12.35, 37.04, 111, 333, 1000 nM
Incubation Time: 2 hours
Result: Inhibited BTK auto-phosphorylation at the Tyr223 site with an IC50 value of 1.49 nM.

Cell Cycle Analysis[1]

Cell Line: B-cell lymphoma (DLBCL) TMD8 cancer cells
Concentration: 0, 10, 100 nM
Incubation Time: 48 hours
Result: Arrested cell cycle progression at G1 phase in a dose-dependent manner, the percentage of cells in the G0/G1 phase increased from 33.0 to 63.0% with a dose range of 1-100 nM.

Apoptosis Analysis[1]

Cell Line: B-cell lymphoma (DLBCL) TMD8 cancer cells
Concentration: 0, 10, 100, 1000 nM
Incubation Time: 72 hours
Result: Induced apoptosis of TMD8 cells in a weakly triggered concentration-dependent manner, with the apoptosis cell values of 19% (10 nM), 25.2% (100 nM), and 31.4% (1000 nM), respectively.
In Vivo

BTK-IN-15 (compound 42) (12.5-50 mg/kg; p.o.; twice daily; 21 d) inhibits tumor growth (TGI = 104%) at a dosage of 50 mg/kg in mice[1].
BTK-IN-15 (300, 400, 500 mg/kg; p.o.; twice daily; 14 d) has biological safety and displays no affect against body weight in mice compared with control[1].
BTK-IN-15 (10 mg/kg; p.o.) shows a high oral bioavailability of 40.98% in mice[1].
Pharmacokinetics of BTK-IN-15 in Mice[1]

Route Dose (mg/kg) Tmax (h) Cmax (ng/mL) AUC(0-t) (h•ng/mL) AUC(0-∞) (h•ng/mL) T1/2 (h) Vz (L/kg) CL (L/h/kg) F (%)
i.v. 2 0.03 2245.39 1471.35 718.33 0.67 2.79 2.87 40.98
p.o. 10 0.39 1441.59 718.33 1472.06 0.59

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

Animal Model: Female CB-17 SCID nude mice with TMD8 xenograft model[1]
Dosage: 12.5 mg/kg, 25 mg/kg, and 50 mg/kg
Administration: Oral gavage; twice daily; 21 days
Result: Inhibited tumor growth at a dosage of 50 mg/kg and reduced tumor volume after 21 days with a TGI of 104%.
Reduced the content of white blood cells, lymphocytes and monocytes, while showed no effect on red blood cell and platelets.
Animal Model: ICR mice (acclimation for 5 days, 18-20 g)[1]
Dosage: 300, 400, 500 mg/kg
Administration: Oral gavage; 14 days
Result: Demonstrated no affect against body weight in mice compared with control.
Molecular Weight

481.52

Formula

C28H24FN5O2
CAS No.
SMILES

O=C(C=C)N1CCC(C2=CNC3=NC=NC(C4=CC=C(CNC(C5=CC=CC=C5)=O)C(F)=C4)=C23)=CC1
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-15 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.

Keywords:

BTK-IN-152820426-92-2BtkPyroptosisBruton tyrosine kinasekinase selectivityB-celllymphomaspyrrolopyrimidinelow toxicityantitumor activityoral absorptionantiproliferativeInhibitorinhibitorinhibit

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