产品
编 号：F082168
分子式：C32H31N5O3
分子量：533.62
分子式：C32H31N5O3
分子量：533.62
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
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1mg
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5mg
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10mg
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25mg
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结构图
CAS No: 1226549-49-0
产品详情
生物活性：
DBPR112 is an orally active furanopyrimidine-based EGFR inhibitor with IC50s of 15 nM and 48 nM for EGFRWT and EGFRL858R/T790M, respectively. DBPR112 can occupy the ATP-binding site. DBPR112 has significant antitumor efficacy.
体内研究：
DBPR112 (orally; 20-50 mg/kg; 5 days/week for 2 consecutive weeks) significantly reduces tumor growth in HCC827 tumor model. DBPR112 (orally; 50 mg/kg; once a day for 15 days) has a significant antitumor effect (mean tumor growth inhibition of 34%) in H1975 tumor model. DBPR112 (IV; 5 mg/kg) has a T1/2 of 2.3 hours, a CL of 55.6 mL/min?kg, and a Vss of 8.6 L/kg for rats. Animal Model:HCC827 tumor model (6- to 8-week-old athymic NU-Fox1nu nude mice)
Dosage:20, 50 mg/kg
Administration:Orally; 5 days/week for 2 consecutive weeks (days 1-5 and 8-12)
Result:Significantly reduced tumor growth.
Animal Model:Rats
Dosage:5 mg/kg for IV and 20 mg/kg for PO (Pharmacokinetic Analysis)
Administration:IV or PO
Result:Had a T1/2 of 2.3 hours, a CL of 55.6 mL/min?kg, and a Vss of 8.6 L/kg by IV. Had a T1/2 of 3.4 hours, a Cmax of 508 ng/mL and an AUC of 2978 ng/mL?h by PO.
体外研究：
DBPR112 (compound 78; 0.32-1000 nM; 16 hours) induces reduction of phosphorylated EGFR in a dose-dependent manner. DBPR112 shows the inhibitory activity against HCC827 (CC50=25 nM), H1975 (CC50=620 nM) and A431 Cell (CC50=1.02 μM) cell lines. DBPR112 occupies the ATP-binding site and interacts with surrounding residues by covalent bonding, hydrogen bonds, and hydrophobic interactions, which give it a potent inhibitory activity against WT EGFR.
DBPR112 is an orally active furanopyrimidine-based EGFR inhibitor with IC50s of 15 nM and 48 nM for EGFRWT and EGFRL858R/T790M, respectively. DBPR112 can occupy the ATP-binding site. DBPR112 has significant antitumor efficacy.
体内研究：
DBPR112 (orally; 20-50 mg/kg; 5 days/week for 2 consecutive weeks) significantly reduces tumor growth in HCC827 tumor model. DBPR112 (orally; 50 mg/kg; once a day for 15 days) has a significant antitumor effect (mean tumor growth inhibition of 34%) in H1975 tumor model. DBPR112 (IV; 5 mg/kg) has a T1/2 of 2.3 hours, a CL of 55.6 mL/min?kg, and a Vss of 8.6 L/kg for rats. Animal Model:HCC827 tumor model (6- to 8-week-old athymic NU-Fox1nu nude mice)
Dosage:20, 50 mg/kg
Administration:Orally; 5 days/week for 2 consecutive weeks (days 1-5 and 8-12)
Result:Significantly reduced tumor growth.
Animal Model:Rats
Dosage:5 mg/kg for IV and 20 mg/kg for PO (Pharmacokinetic Analysis)
Administration:IV or PO
Result:Had a T1/2 of 2.3 hours, a CL of 55.6 mL/min?kg, and a Vss of 8.6 L/kg by IV. Had a T1/2 of 3.4 hours, a Cmax of 508 ng/mL and an AUC of 2978 ng/mL?h by PO.
体外研究：
DBPR112 (compound 78; 0.32-1000 nM; 16 hours) induces reduction of phosphorylated EGFR in a dose-dependent manner. DBPR112 shows the inhibitory activity against HCC827 (CC50=25 nM), H1975 (CC50=620 nM) and A431 Cell (CC50=1.02 μM) cell lines. DBPR112 occupies the ATP-binding site and interacts with surrounding residues by covalent bonding, hydrogen bonds, and hydrophobic interactions, which give it a potent inhibitory activity against WT EGFR.
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