产品
编 号：F756575
分子式：C35H47BrN9O4PS
分子量：800.75
分子式：C35H47BrN9O4PS
分子量：800.75
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CAS No: 2882851-77-4
产品详情
生物活性：
EGFR-IN-48 is a potent and orally active EGFR inhibitor with IC50s of 0.193 nM, 0.251 nM, 10.4 nM for EGFRd19/TM/CS, EGFRLR/TM/CS, EGFRWT, respectively. EGFR-IN-48 inhibits the proliferation of BaF3EGFR del19/T790M/C797S and PC-9EGFR del19/T790M/C797S cells with IC50s of 1.526, 66.7 nM, respectively.
体内研究：
EGFR-IN-48 (2 mg/kg for i.v.; 10 mg/kg for o.p.) shows good oral bioavailability and high plasma exposure in CD-1 mouse.Pharmacokinetic Parameters of EGFR-IN-48 in CD-1 mouse.RouteDose (mg/kg) Vdss (L/kg) T1/2 (h)CL (L/h/kg)AUC0-last (h*ng/mL)Cmax (ng/mL)Tmax (h)F (%)
i.v.20.73.32.413820.0
p.o.1033811.06600.00.548.9
CD-1 mouse; 2 mg/kg for i.v.; 10 mg/kg for o.p..Animal Model:CD-1 mouse
Dosage:
Administration:2 mg/kg for i.v.; 10 mg/kg for o.p.
Result:Showed good oral bioavailability and high plasma exposure.
体外研究：
EGFR-IN-48 (compound 23) (10 nM) shows anti-proliferative activities against BaF3EGFR del19/T790M/C797S and PC-9EGFR del19/T790M/C797S cells with IC50s of 1.526, 66.7 nM, respectively.EGFR-IN-48 exhibits potent inhibitory activities against various clinically relevant EGFR mutants with IC50s of 10.4, 3.1, 0.9, 0.1, 0.2, 0.3, 0.2 nM for EGFRWT, EGFRLR, EGFRdel19, EGFRdel19/TM, EGFRLR/TM, EGFRLR/TM/CS, EGFRdrl19/TM/CS, respectively.
EGFR-IN-48 is a potent and orally active EGFR inhibitor with IC50s of 0.193 nM, 0.251 nM, 10.4 nM for EGFRd19/TM/CS, EGFRLR/TM/CS, EGFRWT, respectively. EGFR-IN-48 inhibits the proliferation of BaF3EGFR del19/T790M/C797S and PC-9EGFR del19/T790M/C797S cells with IC50s of 1.526, 66.7 nM, respectively.
体内研究：
EGFR-IN-48 (2 mg/kg for i.v.; 10 mg/kg for o.p.) shows good oral bioavailability and high plasma exposure in CD-1 mouse.Pharmacokinetic Parameters of EGFR-IN-48 in CD-1 mouse.RouteDose (mg/kg) Vdss (L/kg) T1/2 (h)CL (L/h/kg)AUC0-last (h*ng/mL)Cmax (ng/mL)Tmax (h)F (%)
i.v.20.73.32.413820.0
p.o.1033811.06600.00.548.9
CD-1 mouse; 2 mg/kg for i.v.; 10 mg/kg for o.p..Animal Model:CD-1 mouse
Dosage:
Administration:2 mg/kg for i.v.; 10 mg/kg for o.p.
Result:Showed good oral bioavailability and high plasma exposure.
体外研究：
EGFR-IN-48 (compound 23) (10 nM) shows anti-proliferative activities against BaF3EGFR del19/T790M/C797S and PC-9EGFR del19/T790M/C797S cells with IC50s of 1.526, 66.7 nM, respectively.EGFR-IN-48 exhibits potent inhibitory activities against various clinically relevant EGFR mutants with IC50s of 10.4, 3.1, 0.9, 0.1, 0.2, 0.3, 0.2 nM for EGFRWT, EGFRLR, EGFRdel19, EGFRdel19/TM, EGFRLR/TM, EGFRLR/TM/CS, EGFRdrl19/TM/CS, respectively.
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