FALNIDAMOL

生物活性靶点体外研究体内研究 FALNIDAMOL 试剂级价格

FALNIDAMOL

CAS号:196612-93-8
英文名:BIBX 1382 DIHYDROCHLORIDE
中文名:FALNIDAMOL
CBNumber:CB6842590
分子式:C18H19ClFN7
分子量:387.84
MOL File:196612-93-8.mol

FALNIDAMOL化学性质

熔点 :>217°C (dec.)
沸点 :552.0±60.0 °C(Predicted)
密度 :1.427
储存条件 :Keep in dark place,Inert atmosphere,2-8°C
溶解度 :DMSO (Slightly), Methanol (Slightly)
酸度系数(pKa) :8?+-.0.10(Predicted)
形态 :Solid
颜色 :Pale Yellow to Yellow

FALNIDAMOL性质、用途与生产工艺

生物活性 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。
靶点

EGFR

3 nM (IC ₅₀ )

ErbB2

3.4 μM (IC ₅₀ )
体外研究

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

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 C _4h is 2222 nM and the C _24h 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 C _4h is 2222 nM and the C _24h is 244 nM.