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324832 EGFR Inhibitor II, BIBX1382 - CAS 196612-93-8 - Calbiochem

The EGFR Inhibitor II, BIBX1382, also referenced under CAS 196612-93-8, controls the biological activity of EGFR. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: N⁸-(3-Chloro-4-fluorophenyl)-N²-(1-methylpiperidin-4-yl)-pyrimido[5,4-d]pyrimidine-2,8-diamine, 2HCl, BIBX1382BS

Primary Target: EGFR (ErbB-1, HER-1)
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Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
196612-93-8C₁₈H₁₉ClFN₇ • 2HCl • 2H₂O

Products

Catalogue NumberPackaging Qty/Pack
324832-5MGCN Plastic ampoule 5 mg
Description
OverviewA cell-permeable pyrimidopyrimidine compound that acts as a potent, reversible, ATP-competitive, and highly selective inhibitor of EGFR (ErbB-1, HER-1) both in cell-free enzymatic reactions (IC50 = 3 nM) and in culture (IC50 = 0.15, 1.82, and 3.2 µM in EGF-, HGF-, and FCS-dependent thymidine incorporation, respectively, in KB cells). It exhibits 1,000-fold greater selectivity over ErbB-2 (HER-2, neu; IC50 = 3.4 µM) and shows little activity towards IGF1R, β-InsRK, HGFR, c-src, and VEGFR-2 even at concentrations as high as 10 µM. Its antitumor efficacy has also been demonstrated in a murine xenograft model in vivo (10 mg/kg, daily, p.o.).
Catalogue Number324832
Brand Family Calbiochem®
SynonymsN⁸-(3-Chloro-4-fluorophenyl)-N²-(1-methylpiperidin-4-yl)-pyrimido[5,4-d]pyrimidine-2,8-diamine, 2HCl, BIBX1382BS
References
ReferencesSolca, F.F., et al. 2004. J. Pharm. Exp. Ther. 311, 502.
Egeblad, M., et al. 2001. Biochem. Biophys. Res. Commun. 281, 25.
Nuijen, B., et al. 2000. Int. J. Pharm. 194, 261.
Product Information
CAS number196612-93-8
ATP CompetitiveY
FormYellow solid
Hill FormulaC₁₈H₁₉ClFN₇ • 2HCl • 2H₂O
Chemical formulaC₁₈H₁₉ClFN₇ • 2HCl • 2H₂O
Hygroscopic Hygroscopic
ReversibleY
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Application CommentsTocris suggests 50 mM solution can be made in water or DMSO. Aliquot & store at -20*C; stable for 6 months.
Biological Information
Primary TargetEGFR (ErbB-1, HER-1)
Primary Target IC<sub>50</sub>3 nM against EGFR (ErbB-1, HER-1) in cell-free enzymatic reactions; 0.15, 1.82, and 3.2 µM in EGF-, HGF-, and FCS-dependent thymidine incorporation, respectively, in KB cells
Purity≥97% by HPLC
Physicochemical Information
Cell permeableY
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Ambient Temperature Only
Toxicity Irritant
Storage +2°C to +8°C
Protect from Light Protect from light
Hygroscopic Hygroscopic
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Packaging Information
Transport Information
Supplemental Information
Specifications
Global Trade Item Number
Catalogue Number GTIN
324832-5MGCN 04055977215717

Documentation

EGFR Inhibitor II, BIBX1382 - CAS 196612-93-8 - Calbiochem SDS

Title

Safety Data Sheet (SDS) 

EGFR Inhibitor II, BIBX1382 - CAS 196612-93-8 - Calbiochem Certificates of Analysis

TitleLot Number
324832

References

Reference overview
Solca, F.F., et al. 2004. J. Pharm. Exp. Ther. 311, 502.
Egeblad, M., et al. 2001. Biochem. Biophys. Res. Commun. 281, 25.
Nuijen, B., et al. 2000. Int. J. Pharm. 194, 261.
Data Sheet

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision21-April-2011 JSW
SynonymsN⁸-(3-Chloro-4-fluorophenyl)-N²-(1-methylpiperidin-4-yl)-pyrimido[5,4-d]pyrimidine-2,8-diamine, 2HCl, BIBX1382BS
DescriptionA cell-permeable pyrimidopyrimidine compound that acts as a potent, reversible, ATP-competitive, and highly selective inhibitor of EGFR (ErbB-1, HER-1) both in cell-free enzymatic reactions (IC50 = 3 nM) and in culture (IC50 = 0.15, 1.82, and 3.2 µM in EGF-, HGF-, and FCS-dependent thymidine incorporation, respectively, in KB cells). It exhibits 1,000-fold greater selectivity over ErbB-2 (HER-2, neu; IC50 = 3.4 µM) and shows little activity towards IGF1R, β-InsRK, HGFR, c-src, and VEGFR-2 even at concentrations as high as 10 µM. Its antitumor efficacy has also been demonstrated in a murine xenograft model in vivo (daily p.o. dose 10 mg/kg).
FormYellow solid
CAS number196612-93-8
Chemical formulaC₁₈H₁₉ClFN₇ • 2HCl • 2H₂O
Structure formulaStructure formula
Purity≥97% by HPLC
SolubilityDMSO (25 mg/ml) or H₂O (1 mg/ml)
CommentsTocris suggests 50 mM solution can be made in water or DMSO. Aliquot & store at -20*C; stable for 6 months.
Storage Protect from light
+2°C to +8°C
Hygroscopic
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity Irritant
ReferencesSolca, F.F., et al. 2004. J. Pharm. Exp. Ther. 311, 502.
Egeblad, M., et al. 2001. Biochem. Biophys. Res. Commun. 281, 25.
Nuijen, B., et al. 2000. Int. J. Pharm. 194, 261.