BIBX 1382 | CAS:196612-93-8

Chemscene社は、高品質な低分子化合物を提供しているメーカーです。
Chemscene社のBIBX 1382(CAS:196612-93-8)をご紹介します。

※本製品は研究用です。研究用以外には使用できません。

Name:BIBX 1382; Falnidamol
Cat. No. :CS-0691
CAS No. :196612-93-8
Formula:C18H19ClFN7
M. Wt. : 387.84
Solubility:DMSO: ≥ 41 mg/mL

BIBX 1382 is a potent, selective inhibitor of EGFR tyrosine kinase (IC50 = 3 nM); displays > 1000-fold lower potency against ErbB2 (IC50 = 3.4 μM) and a range of other related tyrosine kinases (IC50 > 10 μM). IC50 value: 3 nM [1]Target: EGFRin vitro: BIBX1382 and BIBU1361 are both potent and selective submicromolar inhibitors of the EGFR kinase activity. An IC50 value of 3 nM was determined for both compounds. The potency of these two compounds compares with the one obtained with Iressa, which is a leading EGFR inhibitor in the field. Inhibition of the closest family member, HER2, was 100- to 1000-fold less potent. Furthermore, BIBX1382 and BIBU1361 did not inhibit a number of other related tyrosine kinases [1].in vivo: In nude mice, oral once daily dosing at 10 mg/kg with either BIBX1382 or BIBU1361 completely suppressed tumor growth of human A431 xenografts with respective T/C values of 15 and 6% after 2 weeks of treatment [1].

Solca FF, et al. Inhibition of epidermal growth factor receptor activity by two pyrimidopyrimidine derivatives. J Pharmacol Exp Ther. 2004 Nov;311(2):502-9.