Home / Pharmacology / Enzyme-Linked Receptors / Receptor Tyrosine Kinases (RTKs) / EGFR / EGFR Inhibitors / BIBX 1382 dihydrochloride

BIBX 1382 dihydrochloride

Cat. No. 2416 1 Citation Datasheet / COA / SDS
Pricing Availability Delivery Time Qty
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
Literature
Biological Activity Technical Data Solubility Calculators Datasheets References

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
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
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

Calculate the mass, volume, or concentration required for a solution.
=
x
x
g/mol

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / CoA (available online).

Reconstitution Calculator

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

=
÷

Dilution Calculator

Calculate the dilution required to prepare a stock solution.
x
=
x

Product Datasheets

Certificate of Analysis / Product Datasheet
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

If you know of a relevant reference for BIBX 1382 dihydrochloride, please let us know.

View Related Products by Target

View Related Products by Product Action

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, 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.

Reviews for BIBX 1382 dihydrochloride

There are currently no reviews for this product. Be the first to review BIBX 1382 dihydrochloride and earn rewards!

Have you used BIBX 1382 dihydrochloride?

Submit a review and receive an Amazon gift card.

$10US/$10CAN/€7/£6 gift card for a review without an image

$25US/$25CAN/€18/£15 gift card for a review with an image

*Offer only valid in the USA / Canada, UK and Europe

Submit a Review

Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* or download your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.

Cancer

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
  • Angiogenesis
  • Invasion and Metastasis
Kinases

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
Angiogenesis in Cancer

Angiogenesis in Cancer Poster

Adapted from the 2015 Cancer Product Guide, Edition 3, this poster summarizes the pathogenesis of angiogenesis in cancer, as well as some of the main angiogenesis therapeutic targets.

Schizophrenia

Schizophrenia Poster

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.