Falnidamol

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Falnidamol (BIBX 1382) 是一种具有口服活性的，选择性的 EGFR 酪氨酸激酶抑制剂，IC50 为3 nM。Falnidamol 对 ErbB2 (IC50=3.4 μM) 和其他一系列相关酪氨酸激酶 (IC50>10 μM) 的选择性 >1000倍。Falnidamol 是嘧啶-嘧啶化合物，具有抗癌活性。

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.

Falnidamol (BIBX 1382) demonstrates antiproliferative activity in mitogenic assays performed with KB cells.

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.

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Angiogenesis

EGFR

EGFR

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196612-93-8

387.84

C18H19ClFN7

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 31.25 mg/mL (80.57 mM; 超声助溶 (<60°C)

CN1CCC(CC1)Nc1ncc2ncnc(Nc3ccc(F)c(Cl)c3)c2n1

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(-20℃)

With Ice Pack

≥ 2 years