产品
编 号：F762918
分子式：C30H25F3N6O2
分子量：558.55
分子式：C30H25F3N6O2
分子量：558.55
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CAS No: 3029240-84-1
产品详情
生物活性：
D6808 is a highly selective and potent c?Met inhibitor with an IC50 value of 2.9 nM. D6808 induces cell apoptosis and cell cycle arrest. D6808 can be used for the research of NSCLC and gastric cancers.
体内研究：
1.19Pharmacokinetic Properties of D6808 in Rats. RatsIV2.0 mg/kgRatsPO 10.0 mg/kgRatsIP 10.0 mg/kg
T1/2 (h)0.572.494.63
Tmax (h)0.080.250.25
Cmax (ng/mL)1071.2360.98282.12
AUC0-t (h×ng/mL)483.8448.89820.38
Vz (mL/kg)3470.78
CL (mL/h/kg)4207.06
MRT0-t (h)0.361.713.40
F (%)2.0233.91
体外研究：
D6808 shows c-Met biochemical kinase inhibitory activity with an IC50 value of 2.9 nM.D6808 (0.0001-10 μM; 5 d) shows cellular antiproliferative potency to Hs746T cancer cells with an IC50 value of 0.7 nM.D6808 displays extraordinary kinome selectivity with IC50 values of 401.3, 437.2, 1386 and 203.9 nM for Axl, TrkA, TrkB and TrkC kinase, respectively.D6808 (0-10 μM; 72 h) show antiproliferative potency to Tpr-Met fusion protein-transformed Ba/F3 cells with IC50 values of 4.3, 4.2, 3.2, 1.0, 39.0 and 33.4 nM for Ba/F3-Tpr-Met, Ba/F3-Tpr-MetF1200L, Ba/F3-Tpr-MetM1250T, Ba/F3-Tpr-MetH1094Y, Ba/F3-Tpr-MetF1200I, Ba/F3-Tpr-MetL1195V, respectively.D6808 (0-30 nM; 12 h) affects activation of MET and dose-dependently decreases the protein levels of CDK2, CDK4, CDK6, cyclin D2, and cyclin E1 and the cleave activation of PARP and caspase-9 in Ba/F3-Tpr-Met cells.D6808 (40 nM; 24 h) induces cell apoptosis and 87.37% G0/G1 phase arrest in Ba/F3-Tpr-Met cells.
D6808 is a highly selective and potent c?Met inhibitor with an IC50 value of 2.9 nM. D6808 induces cell apoptosis and cell cycle arrest. D6808 can be used for the research of NSCLC and gastric cancers.
体内研究：
1.19Pharmacokinetic Properties of D6808 in Rats. RatsIV2.0 mg/kgRatsPO 10.0 mg/kgRatsIP 10.0 mg/kg
T1/2 (h)0.572.494.63
Tmax (h)0.080.250.25
Cmax (ng/mL)1071.2360.98282.12
AUC0-t (h×ng/mL)483.8448.89820.38
Vz (mL/kg)3470.78
CL (mL/h/kg)4207.06
MRT0-t (h)0.361.713.40
F (%)2.0233.91
体外研究：
D6808 shows c-Met biochemical kinase inhibitory activity with an IC50 value of 2.9 nM.D6808 (0.0001-10 μM; 5 d) shows cellular antiproliferative potency to Hs746T cancer cells with an IC50 value of 0.7 nM.D6808 displays extraordinary kinome selectivity with IC50 values of 401.3, 437.2, 1386 and 203.9 nM for Axl, TrkA, TrkB and TrkC kinase, respectively.D6808 (0-10 μM; 72 h) show antiproliferative potency to Tpr-Met fusion protein-transformed Ba/F3 cells with IC50 values of 4.3, 4.2, 3.2, 1.0, 39.0 and 33.4 nM for Ba/F3-Tpr-Met, Ba/F3-Tpr-MetF1200L, Ba/F3-Tpr-MetM1250T, Ba/F3-Tpr-MetH1094Y, Ba/F3-Tpr-MetF1200I, Ba/F3-Tpr-MetL1195V, respectively.D6808 (0-30 nM; 12 h) affects activation of MET and dose-dependently decreases the protein levels of CDK2, CDK4, CDK6, cyclin D2, and cyclin E1 and the cleave activation of PARP and caspase-9 in Ba/F3-Tpr-Met cells.D6808 (40 nM; 24 h) induces cell apoptosis and 87.37% G0/G1 phase arrest in Ba/F3-Tpr-Met cells.
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