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)
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.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 19.39 50
water 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.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.17 mL 10.85 mL 21.7 mL
5 mM 0.43 mL 2.17 mL 4.34 mL
10 mM 0.22 mL 1.09 mL 2.17 mL
50 mM 0.04 mL 0.22 mL 0.43 mL

Molarity Calculator

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Reconstitution Calculator

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Dilution Calculator

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Product Datasheets

Safety Datasheet

References

References are publications that support the products' biological activity.

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, supplier, selective, EGFR-kinases, inhibitors, inhibits, Epidermal, Growth, Factors, Receptors, ErbB, Her, Receptor, Tyrosine, Kinases, RTKs, BIBX1382, dihydrochloride, EGFR, 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? If so please let us know.

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Literature in this Area

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Kinases Product Listing

A collection of over 400 products for kinase research, the listing includes inhibitors of:

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Pathways for BIBX 1382 dihydrochloride

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