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编 号：F756163
分子式：C28H24FN5O2
分子量：481.52
分子式：C28H24FN5O2
分子量：481.52
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CAS No: 2820426-92-2
产品详情
生物活性：
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.
体内研究：
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.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.BTK-IN-15 (10 mg/kg; p.o.) shows a high oral bioavailability of 40.98% in mice.Pharmacokinetics of BTK-IN-15 in MiceRouteDose (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.20.032245.391471.35718.330.672.792.8740.98
p.o.100.391441.59718.331472.060.59
Animal Model:Female CB-17 SCID nude mice with TMD8 xenograft model
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)
Dosage:300, 400, 500 mg/kg
Administration:Oral gavage; 14 days
Result:Demonstrated no affect against body weight in mice compared with control.
体外研究：
BTK inhibition is an effective approach against B-cell malignancies.BTK-IN-15 (compound 42) demonstrates inhibitory against TMD8 with an IC50 value of 2.6 nM.BTK-IN-15 (1 μM; 1 h) displays significant selectivity to BTK over EGFR kinase with 0.05% and 44% of the control, respectively.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.BTK-IN-15 (0-1 mM; 2 h) inhibits BTK auto-phosphorylation with an IC50 value of 1.49 nM.BTK-IN-15 (0-100 nM; 48 h) arrests cell cycle at G1 phase and (0-1 mM; 72 h) induces apoptosis in TMD8. BTK-IN-15 shows low hERG channel activity (IC50=4.38 μM), indicating low cardiotoxicity.
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.
体内研究：
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.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.BTK-IN-15 (10 mg/kg; p.o.) shows a high oral bioavailability of 40.98% in mice.Pharmacokinetics of BTK-IN-15 in MiceRouteDose (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.20.032245.391471.35718.330.672.792.8740.98
p.o.100.391441.59718.331472.060.59
Animal Model:Female CB-17 SCID nude mice with TMD8 xenograft model
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)
Dosage:300, 400, 500 mg/kg
Administration:Oral gavage; 14 days
Result:Demonstrated no affect against body weight in mice compared with control.
体外研究：
BTK inhibition is an effective approach against B-cell malignancies.BTK-IN-15 (compound 42) demonstrates inhibitory against TMD8 with an IC50 value of 2.6 nM.BTK-IN-15 (1 μM; 1 h) displays significant selectivity to BTK over EGFR kinase with 0.05% and 44% of the control, respectively.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.BTK-IN-15 (0-1 mM; 2 h) inhibits BTK auto-phosphorylation with an IC50 value of 1.49 nM.BTK-IN-15 (0-100 nM; 48 h) arrests cell cycle at G1 phase and (0-1 mM; 72 h) induces apoptosis in TMD8. BTK-IN-15 shows low hERG channel activity (IC50=4.38 μM), indicating low cardiotoxicity.
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