Molecular structure of BIBX 1382, CAS Number: 196612-93-8
BIBX 1382 (CAS 196612-93-8)
See product citations (2)
Application:
BIBX 1382 is a potent, reversible, selective inhibitor of EGFR
CAS Number:
196612-93-8
Purity:
≥97%
Molecular Weight:
496.80
Molecular Formula:
C18H19ClFN7 2HCl 2H2O
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.
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SDS & Certificate of Analysis
BIBX 1382 is a cell-permeable pyrimidopyrimidine compound that acts as a potent, reversible, ATP-competitive, and highly selective inhibitor of EGFR (ErbB-1, HER-1) both in cell-free enzymatic reactions (IC50 = 3 nM) and in culture (IC50 = 0.15, 1.82, and 3.2 μM in EGF-, HGF-, and FCS-dependent thymidine incorporation, respectively, in KB cells). BIBX 1382 has been shown to exhibit a 1,000-fold greater selectivity over ErbB-2 (HER-2, neu; IC50 = 3.4 μM) and shows little activity towards IGF1R, b-InsRK, HGFR, c-src, and VEGFR-2 even at concentrations as high as 10 μM.
BIBX 1382 (CAS 196612-93-8) References
- In vitro biocompatibility studies with the experimental anticancer agent BIBX1382BS. | Nuijen, B., et al. 2000. Int J Pharm. 194: 261-7. PMID: 10692650
- BIBX1382BS, but not AG1478 or PD153035, inhibits the ErbB kinases at different concentrations in intact cells. | Egeblad, M., et al. 2001. Biochem Biophys Res Commun. 281: 25-31. PMID: 11178955
- Phase I and pharmacokinetic study of BIBX 1382 BS, an epidermal growth factor receptor (EGFR) inhibitor, given in a continuous daily oral administration. | Dittrich, Ch., et al. 2002. Eur J Cancer. 38: 1072-80. PMID: 12008195
- Inhibition of epidermal growth factor receptor activity by two pyrimidopyrimidine derivatives. | Solca, FF., et al. 2004. J Pharmacol Exp Ther. 311: 502-9. PMID: 15199094
- Ultrafine carbon black particles stimulate proliferation of human airway epithelium via EGF receptor-mediated signaling pathway. | Tamaoki, J., et al. 2004. Am J Physiol Lung Cell Mol Physiol. 287: L1127-33. PMID: 15298855
- Tamoxifen-induced rapid death of MCF-7 breast cancer cells is mediated via extracellularly signal-regulated kinase signaling and can be abrogated by estrogen. | Zheng, A., et al. 2007. Endocrinology. 148: 2764-77. PMID: 17363451
- Inhibitors of cellular kinases with broad-spectrum antiviral activity for hemorrhagic fever viruses. | Mohr, EL., et al. 2015. Antiviral Res. 120: 40-7. PMID: 25986249
- Troglitazone Stimulates Cancer Cell Uptake of 18F-FDG by Suppressing Mitochondrial Respiration and Augments Sensitivity to Glucose Restriction. | Moon, SH., et al. 2016. J Nucl Med. 57: 129-35. PMID: 26449833
- 25-Hydroxycholesterol Inhibition of Lassa Virus Infection through Aberrant GP1 Glycosylation. | Shrivastava-Ranjan, P., et al. 2016. mBio. 7: PMID: 27999160
- EGF receptor stimulation shifts breast cancer cell glucose metabolism toward glycolytic flux through PI3 kinase signaling. | Jung, KH., et al. 2019. PLoS One. 14: e0221294. PMID: 31532771
Inhibitor of:
EGFR.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
BIBX 1382, 5 mg | sc-202497 | 5 mg | $180.00 |