产品
编 号：F244411
分子式：C18H19ClFN7
分子量：387.84
分子式：C18H19ClFN7
分子量：387.84
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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50mg
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100mg
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结构图
CAS No: 196612-93-8
产品详情
生物活性：
Falnidamol (BIBX 1382) is an orally active, selective EGFR tyrosine kinase inhibitor with an IC50 of 3 nM. Falnidamol displays > 1000-fold lower potency against ErbB2 (IC50=3.4 μM) and a range of other related tyrosine kinases (IC50>10 μM). Falnidamol is a pyrimido-pyrimidine compound and has anti-cancer activity.
体内研究：
Falnidamol (BIBX 1382; p.o.; 10 mg/kg/day; 16 days) completely suppressed tumor growth of human A431 xenografts with respective a T/C value of 15% after 2 weeks of treatment. Falnidamol (50 mg/kg/day for 2 weeks) results in dephosphorylation of the EGF receptor in A431 xenograft-bearing mice. With Falnidamol (p.o.; 10 mg/kg/day; 16 days), the C4h is 2222 nM and the C24h is 244 nM. Animal Model:Five- to six-week-old athymic NMRI-nu/nu female mice (21-31 g) with A431, FaDu, or HN5 cells
Dosage:10 mg/kg
Administration:p.o.; daily; 16 days
Result:Completely suppressed tumor growth of human A431 xenografts with respective T/C values of 15 and 6% after 2 weeks of treatment.
Animal Model:Five- to six-week-old athymic NMRI-nu/nu female mice (21–31 g) with A431 cells
Dosage:10 mg/kg (Pharmacokinetic Analysis)
Administration:p.o.; daily; 16 days
Result:The C4h is 2222 nM and the C24h is 244 nM.
体外研究：
Falnidamol (BIBX 1382) demonstrates antiproliferative activity in mitogenic assays performed with KB cells.
Falnidamol (BIBX 1382) is an orally active, selective EGFR tyrosine kinase inhibitor with an IC50 of 3 nM. Falnidamol displays > 1000-fold lower potency against ErbB2 (IC50=3.4 μM) and a range of other related tyrosine kinases (IC50>10 μM). Falnidamol is a pyrimido-pyrimidine compound and has anti-cancer activity.
体内研究：
Falnidamol (BIBX 1382; p.o.; 10 mg/kg/day; 16 days) completely suppressed tumor growth of human A431 xenografts with respective a T/C value of 15% after 2 weeks of treatment. Falnidamol (50 mg/kg/day for 2 weeks) results in dephosphorylation of the EGF receptor in A431 xenograft-bearing mice. With Falnidamol (p.o.; 10 mg/kg/day; 16 days), the C4h is 2222 nM and the C24h is 244 nM. Animal Model:Five- to six-week-old athymic NMRI-nu/nu female mice (21-31 g) with A431, FaDu, or HN5 cells
Dosage:10 mg/kg
Administration:p.o.; daily; 16 days
Result:Completely suppressed tumor growth of human A431 xenografts with respective T/C values of 15 and 6% after 2 weeks of treatment.
Animal Model:Five- to six-week-old athymic NMRI-nu/nu female mice (21–31 g) with A431 cells
Dosage:10 mg/kg (Pharmacokinetic Analysis)
Administration:p.o.; daily; 16 days
Result:The C4h is 2222 nM and the C24h is 244 nM.
体外研究：
Falnidamol (BIBX 1382) demonstrates antiproliferative activity in mitogenic assays performed with KB cells.
产品资料
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