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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
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.
Compound Libraries
BIBX 1382 dihydrochloride is also offered as part of the Tocriscreen Plus and Tocriscreen Kinase Inhibitor Toolbox I. Find out more about compound libraries available from Tocris.
Technical Data
| 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.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 19.39 | 50 | |
| DMSO | 19.39 | 50 |
Preparing Stock Solutions
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 |
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Product Datasheets
References
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.
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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
Do you know of a great paper that uses BIBX 1382 dihydrochloride from Tocris? Please let us know.
Reviews for BIBX 1382 dihydrochloride
Average Rating: 5 (Based on 1 Review.)
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In vitro culture: Excellent publishable, performed ideally.
By
Anonymous on 08/05/2018
Assay Type: In Vitro
Species: Mouse
Used in vitro to investigate ERG pathways
Literature in this Area
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Cancer Research Product Guide
A collection of over 750 products for cancer research, the guide includes research tools for the study of:
- Cancer Metabolism
- Epigenetics in Cancer
- Receptor Signaling
- Cell Cycle and DNA Damage Repair
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- Invasion and Metastasis
Kinases Product Listing
A collection of over 400 products for kinase research, the listing includes inhibitors of:
- Receptor Tyrosine Kinases
- Protein Kinases A, C, D and G
- PI-3 Kinase, Akt and mTOR
- MAPK Signaling
- Receptor Serine/Threonine Kinases
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