产品
编 号：F756067
分子式：C20H19FN6O3
分子量：410.4
分子式：C20H19FN6O3
分子量：410.4
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CAS No: 2803679-07-2
产品详情
生物活性：
LPM4870108 is a potent and orally active pan-Trk (WT and MT) inhibitor, with IC50s of 0.2 nM, 2.4 nM, 3.5 nM and 2.3 nM for TrkC, TrkA, TrkAG595R and TrkAG667C, respectively. LPM4870108 shows selectivity for Trk over ALK (IC50=182 nM). LPM4870108 exhibits anti-tumor activity.
体内研究：
LPM4870108 (compound 10) (5-20 mg/kg; p.o. once daily for 21 days) inhibits tumor growth in BaF3-NTRK xenograft tumor models.LPM4870108 (2 mg/kg; a single i.v.) exhibits terminal half-life (t1/2) (male 0.87 h, 2.21 h), the Cl (male 19.3 mL/kg/min, female 8.19 mL/kg/min), and the AUC0-t (male 4191 nM?h, female 10282 nM?h) in rats.LPM4870108 (10 mg/kg; a single p.o.) exhibits oral bioavailability (male 56.0%, female 61.9%), Cmax (male 6384 nM, female 6628 nM) and Tmax (male 0.667 h, female 0.667 h) in rats.Animal Model:Mice bearing 100-200 mm3 BaF3-NTRK tumors
Dosage:5, 10, 20 mg/kg
Administration:P.o. once daily for 21 days
Result:Showed slight weight loss and all animals survived at the highest dose.
Animal Model:Sprague-Dawley rats (six males and six females)
Dosage:2 mg/kg for i.v.; 10 mg/kg for oral (Pharmacokinetic Analysis)
Administration:Intravenous administration and oral administration
Result:I.v.: t1/2 (male 0.87 h, 2.21 h), Cl (male 19.3 mL/kg/min, female 8.19 mL/kg/min), AUC0-t (male 4191 nM?h, female 10282 nM?h).P.o.: F (male 56.0%, female 61.9%), Cmax (male 6384 nM, female 6628 nM), Tmax (male 0.667 h, female 0.667 h).
体外研究：
LPM4870108 (compound 10) inhibits the activities of TrkA, TrkB, and TRC with high selectivity at 0.5 μM (kinase activity remaining, LPM4870108 相关抗体:
LPM4870108 is a potent and orally active pan-Trk (WT and MT) inhibitor, with IC50s of 0.2 nM, 2.4 nM, 3.5 nM and 2.3 nM for TrkC, TrkA, TrkAG595R and TrkAG667C, respectively. LPM4870108 shows selectivity for Trk over ALK (IC50=182 nM). LPM4870108 exhibits anti-tumor activity.
体内研究：
LPM4870108 (compound 10) (5-20 mg/kg; p.o. once daily for 21 days) inhibits tumor growth in BaF3-NTRK xenograft tumor models.LPM4870108 (2 mg/kg; a single i.v.) exhibits terminal half-life (t1/2) (male 0.87 h, 2.21 h), the Cl (male 19.3 mL/kg/min, female 8.19 mL/kg/min), and the AUC0-t (male 4191 nM?h, female 10282 nM?h) in rats.LPM4870108 (10 mg/kg; a single p.o.) exhibits oral bioavailability (male 56.0%, female 61.9%), Cmax (male 6384 nM, female 6628 nM) and Tmax (male 0.667 h, female 0.667 h) in rats.Animal Model:Mice bearing 100-200 mm3 BaF3-NTRK tumors
Dosage:5, 10, 20 mg/kg
Administration:P.o. once daily for 21 days
Result:Showed slight weight loss and all animals survived at the highest dose.
Animal Model:Sprague-Dawley rats (six males and six females)
Dosage:2 mg/kg for i.v.; 10 mg/kg for oral (Pharmacokinetic Analysis)
Administration:Intravenous administration and oral administration
Result:I.v.: t1/2 (male 0.87 h, 2.21 h), Cl (male 19.3 mL/kg/min, female 8.19 mL/kg/min), AUC0-t (male 4191 nM?h, female 10282 nM?h).P.o.: F (male 56.0%, female 61.9%), Cmax (male 6384 nM, female 6628 nM), Tmax (male 0.667 h, female 0.667 h).
体外研究：
LPM4870108 (compound 10) inhibits the activities of TrkA, TrkB, and TRC with high selectivity at 0.5 μM (kinase activity remaining, LPM4870108 相关抗体:
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