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BTK-IN-15
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
BTK-IN-15图片
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
BTK-IN-15 是一种新型的布鲁顿酪氨酸激酶 (BTK) 抑制剂,具有良好口服活性。BTK-IN-15 抑制BTKIC50为 0.7 nM,并具有良好的激酶选择性和抗肿瘤活性,能诱导癌细胞凋亡 (apoptosis)。
生物活性

BTK-IN-15 is a potentBruton's tyrosine kinase(BTK) inhibitor with highoralabsorption. BTK-IN-15 inhibitsBTKwith anIC50value of 0.7 nM. BTK-IN-15 displays excellent kinase selectivity, antitumor activity, and inducesapoptosis[1].

IC50& Target

IC50: 0.7 nM (BTK)[1]

体外研究
(In Vitro)

BTK inhibition is an effective approach against B-cell malignancies[1].
BTK-IN-15 (compound 42) demonstrates inhibitory against TMD8 with an IC50value 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 IC50value of 1.7 nM[1].
BTK-IN-15 (0-1 mM; 2 h) inhibits BTK auto-phosphorylation with an IC50value 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].

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 IC50value 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.
体内研究
(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]

RouteDose (mg/kg)Tmax(h)Cmax(ng/mL)AUC(0-t)(hong/mL)AUC(0-∞)(hong/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[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.
分子量

481.52

Formula

C28H24FN5O2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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