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Submit ReviewBIBX 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.
BIBX 1382 dihydrochloride is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Kinase Inhibitor Library. Find out more about compound libraries available from Tocris.
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.
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
water | 19.39 | 50 | |
DMSO | 19.39 | 50 |
The following data is based on the product molecular weight 460.77. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
0.5 mM | 4.34 mL | 21.7 mL | 43.41 mL |
2.5 mM | 0.87 mL | 4.34 mL | 8.68 mL |
5 mM | 0.43 mL | 2.17 mL | 4.34 mL |
25 mM | 0.09 mL | 0.43 mL | 0.87 mL |
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
If you know of a relevant reference for BIBX 1382 dihydrochloride, please let us know.
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
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
Do you know of a great paper that uses BIBX 1382 dihydrochloride from Tocris? Please let us know.
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Used in vitro to investigate ERG pathways
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Schizophrenia is a debilitating psychiatric disorder that affects 1% of the worldwide population. This poster describes the neurobiology of Schizophrenia, as well as highlighting the genetic and environmental factors that play a fundamental role in the etiology of the disease. The current and emerging drug targets are also discussed.