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Submit ReviewBIBX 1382 dihydrochloride
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)
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 |
| InChI Key | RFXGEKWBTCMDAW-UHFFFAOYSA-N |
| 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
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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.)
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Blockage of EGFR signaling.
By
MARINA KOUTSIOUMPA on 10/13/2022
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
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Angiogenesis in Cancer Poster
This poster summarizes the pathogenesis of angiogenesis in cancer, as well as some of the main angiogenesis therapeutic targets.