BIBX 1382 dihydrochloride

Discontinued Product

BIBX 1382 dihydrochloride (Cat. No. 2416) has been withdrawn from sale for commercial reasons.
Description: Highly selective EGFR-kinase inhibitor
Chemical Name: N8-(3-Chloro-4-fluorophenyl)-N2-(1-methyl-4-piperidinyl)-pyrimido[5,4-d]pyrimidine-2,8-diamine dihydrochloride
Purity: ≥97% (HPLC)
Citations (1)
Reviews (2)
Literature (1)

Biological Activity for BIBX 1382 dihydrochloride

BIBX 1382 dihydrochloride is a potent, selective inhibitor of epidermal growth factor receptor (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). Oral administration inhibits growth of established human xenografts in athymic mice.

Technical Data for BIBX 1382 dihydrochloride

M. Wt 460.77
Formula C18H19ClFN7.2HCl
Storage Desiccate at +4°C
Purity ≥97% (HPLC)
CAS Number 1216920-18-1
PubChem ID 46861540
Smiles Cl.Cl.CN1CCC(CC1)NC1=NC=C2N=CN=C(NC3=CC(Cl)=C(F)C=C3)C2=N1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Product Datasheets for BIBX 1382 dihydrochloride

References for BIBX 1382 dihydrochloride

References are publications that support the biological activity of the product.

Dittrich et al (2002) Phase I and pharmacokinetic study of BIBX1382 BS, an epidermal growth factor receptor (EGFR) inhibitor, given in a continuous daily oral administration. Eur.J.Cancer 38 1072 PMID: 12008195

Solca et al (2004) Inhibition of epidermal growth factor receptor activity by two pyrimidopyrimidine derivatives. J.Pharmacol.Exp.Ther. 311 502 PMID: 15199094

View Related Products by Product Action

View all EGFR Inhibitors

Keywords: BIBX 1382 dihydrochloride, BIBX 1382 dihydrochloride supplier, selective, EGFR-kinases, inhibitors, inhibits, Epidermal, Growth, Factors, Receptors, ErbB, Her, Receptor, Tyrosine, Kinases, RTKs, BIBX1382, dihydrochloride, EGFR, 2416, Tocris Bioscience

1 Citation for BIBX 1382 dihydrochloride

Citations are publications that use Tocris products. Selected citations for BIBX 1382 dihydrochloride include:

Xia et al (2013) Identification of repurposed small molecule drugs for chordoma therapy. Cancer Biol Ther 14 638 PMID: 23792643

Reviews for BIBX 1382 dihydrochloride

Average Rating: 5 (Based on 2 Reviews.)

5 Star
4 Star
3 Star
2 Star
1 Star

Have you used BIBX 1382 dihydrochloride?

Submit a review and receive an Amazon gift card.

$50/€35/£30/$50CAN/¥300 Yuan/¥5000 Yen for first to review with an image

$25/€18/£15/$25CAN/¥75 Yuan/¥1250 Yen for a review with an image

$10/€7/£6/$10 CAD/¥70 Yuan/¥1110 Yen for a review without an image

Submit a Review

Filter by:

Blockage of EGFR signaling.
Assay Type: In Vitro
Species: Human

BIBX 1382 dihydrochloride was used to block EGFR signaling and determine the pathway of a chemotherapeutic in glioblastoma lines. The inhibitor worked nicely, and the results were consistent.

In vitro culture.
By Anonymous on 08/05/2018
Assay Type: In Vitro
Species: Mouse

Used in vitro to investigate ERG pathways

Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.

Angiogenesis in Cancer Poster

Angiogenesis in Cancer Poster

This poster summarizes the pathogenesis of angiogenesis in cancer, as well as some of the main angiogenesis therapeutic targets.