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324832 Sigma-AldrichEGFR 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.

MSDS
分析证书
参考
Data Sheet

同义词: 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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概述

Replacement Information

重要规格表

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

价格及供货情况

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Description
Overview	A 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 Number	324832
Brand Family	Calbiochem®
Synonyms	N⁸-(3-Chloro-4-fluorophenyl)-N²-(1-methylpiperidin-4-yl)-pyrimido[5,4-d]pyrimidine-2,8-diamine, 2HCl, BIBX1382BS

References
References	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.

Product Information
CAS number	196612-93-8
ATP Competitive	Y
Form	Yellow solid
Hill Formula	C₁₈H₁₉ClFN₇ • 2HCl • 2H₂O
Chemical formula	C₁₈H₁₉ClFN₇ • 2HCl • 2H₂O
Hygroscopic	Hygroscopic
Reversible	Y
Structure formula Image
Quality Level	MQ100

Applications
Application Comments	Tocris suggests 50 mM solution can be made in water or DMSO. Aliquot & store at -20*C; stable for 6 months.

Biological Information
Primary Target	EGFR (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 permeable	Y

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 Instructions	Following 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
产品目录编号	GTIN
324832-5MGCN	04055977215717

Documentation

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

职位
物料安全数据表 (MSDS)

EGFR Inhibitor II, BIBX1382 - CAS 196612-93-8 - Calbiochem 分析证书

标题	批号
324832	输入批号

参考

参考信息概述
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.

数据表

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.

Revision	21-April-2011 JSW
Synonyms	N⁸-(3-Chloro-4-fluorophenyl)-N²-(1-methylpiperidin-4-yl)-pyrimido[5,4-d]pyrimidine-2,8-diamine, 2HCl, BIBX1382BS
Description	A 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).
Form	Yellow solid
CAS number	196612-93-8
Chemical formula	C₁₈H₁₉ClFN₇ • 2HCl • 2H₂O
Structure formula
Purity	≥97% by HPLC
Solubility	DMSO (25 mg/ml) or H₂O (1 mg/ml)
Comments	Tocris 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 Instructions	Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity	Irritant
References	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.

种类

Life Science Research > Inhibitors and Biochemicals > Small Molecules & Inhibitors > Protein Phosphorylation / Dephosphorylation > Protein Tyrosine Kinase (PTK) Inhibitors

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