BIBX 1382 dihydrochloride

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Cat.No. 2416 - BIBX 1382 dihydrochloride | C18H19ClFN7.2HCl | CAS No. 1216920-18-1
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)
Datasheet
Citations (1)
Reviews (1)
Literature

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 solvent 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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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


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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


Do you know of a great paper that uses BIBX 1382 dihydrochloride from Tocris? Please let us know.

Reviews for BIBX 1382 dihydrochloride

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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

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