BIBX 1382 DIHYDROCHLORIDE Chemical Properties

Melting point:

>217°C (dec.)

Boiling point:

552.0±60.0 °C(Predicted)

Density 

1.427

storage temp. 

Keep in dark place,Inert atmosphere,2-8°C

solubility 

DMSO (Slightly), Methanol (Slightly)

pka

8?+-.0.10(Predicted)

form 

Solid

color 

Pale Yellow to Yellow

Water Solubility 

water: 1mg/mL
DMSO: 25mg/mL

BIBX 1382 DIHYDROCHLORIDE Usage And Synthesis

Uses

Falnidamol is a novel ErbB receptor kinase inhibitor that is more potent at inhibiting signaling induced by TGF-α than that induced by neuregulin1-β1 or anti-ErbB2 agonist antibodies.

Uses

BIBX 1382 Dihydrochloride, is a potent, selective inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase (IC50 = 3 nM).

Definition

ChEBI: N4-(3-chloro-4-fluorophenyl)-N6-(1-methyl-4-piperidinyl)pyrimido[5,4-d]pyrimidine-4,6-diamine is a substituted aniline.

Biological Activity

Potent, selective inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase (IC 50 = 3 nM). Displays > 1000-fold lower potency against ErbB2 (IC 50 = 3.4 μ M) and a range of other related tyrosine kinases (IC 50 > 10 μ M). Oral administration inhibits growth of established human xenografts in athymic mice.

References

1. f. f. solca, a. baum, e. langkopf, g. dahmann, k. h. heider, f. himmelsbach and j. c. van meel, j pharmacol exp ther 2004, 311, 502-509.

BIBX 1382 DIHYDROCHLORIDE(196612-93-8)Related Product Information

• Piperidin-4-yl-pyrimidin-2-yl-amine dihydrochloride
• BIBX 1382 DIHYDROCHLORIDE