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BIBW2992 (Afatinib)

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EGFR inhibitor

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Catalog No. A10141

Availability:Stock in USAIn stock

Product Name Catalog No. Price Qty
BIBW2992 5mg A10141-5

Regular Price: €38.00

Special Price: €34.20

BIBW2992 10mg A10141-10

Regular Price: €47.50

Special Price: €42.75

BIBW2992 25mg A10141-25

Regular Price: €66.50

Special Price: €59.85

BIBW2992 100mg A10141-100

Regular Price: €180.50

Special Price: €162.45

BIBW2992 (Afatinib) 10mM * 1mL in DMSO A10141-10mM-D

Regular Price: €47.50

Special Price: €42.75

Products are for laboratory research use only. Not for human use. We do not sell to patients.

Quick Overview

BIBW2992 (Afatinib) is tyrosine kinase inhibitor (TKI) that irreversibly inhibits human epidermal growth factor receptor 2 (Her2) and epidermal growth factor receptor (EGFR) kinases.

BIBW2992 (Afatinib)

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Publications citing Adooq Products
BIBW2992 (Afatinib) Citations (1)
  • Fujita KI, .et al. Involvement of the Transporters P-Glycoprotein and Breast Cancer Resistance Protein in Dermal Distribution of the Multikinase Inhibitor Regorafenib and Its Active Metabolites, J Pharm Sci, 2017, Sep;106(9):2632-2641 PMID: 28479358

Chemical Information

Catalog Num A10141
Actions Inhibitor
M. Wt 485.9
Formula C24H25ClFN5O3
Solubility DMSO
Purity >98%
Storage at -20°C 3 years Powder
CAS No. 439081-18-2
Synonyms Tomtovok,Afatinib
SMILES code CN(C)C/C=C/C(=O)NC1=C(C=C2C(=C1)C(=NC=N2)NC3=CC(=C(C=C3)F)Cl)O[[email protected]]4CCOC4
Chemical Name N-[4-[(3-Chloro-4-fluorophenyl)amino]-7-[[(3S)-tetrahydro-3-furanyl]oxy]-6-quinazolinyl]-4(dimethylamino)-2-butenamide

Biological Activity

Description
 BIBW2992 (Afatinib) is tyrosine kinase inhibitor (TKI) that irreversibly inhibits human epidermal growth factor receptor 2 (Her2) and epidermal growth factor receptor (EGFR) kinases.
Targets
EGFR (L858R) (Cell-free assay) EGFR (wt) (Cell-free assay) EGFR (L858R/T790M) (Cell-free assay) HER2 (Cell-free assay)
0.4 nM0.5 nM10 nM14 nM

Solubility

Solubility (25°C) * In vitro DMSO 97 mg/mL (199.61 mM)
Water <1 mg/mL (<1 mM)
Ethanol 15 mg/mL (30.86 mM)
In vivo 0.5% methylcellulose/0.2% Tween 80 30 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Adooq tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Preparing Stock Solutions

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.1 mM 20.58 mL 102.9 mL 205.8mL
0.5 mM 4.12 mL 20.58 mL 41.16 mL
1 mM 2.06 mL 10.29 mL 20.58 mL
5 mM 0.41 mL 2.06 mL 4.12 mL

*The above data is based on the productmolecular weight 485.9. 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.

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WaterDMSOEthanol
A10043 AEE788 <1 mg/mL 88 mg/mL <1 mg/mL
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A11027 ARRY-380 <1 mg/mL 114 mg/mL <1 mg/mL
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A10743 BMS 599626 (AC480) <1 mg/mL 55 mg/mL <1 mg/mL
A10211 Canertinib (CI-1033) <1 mg/mL 2 mg/mL 9 mg/mL
A10210 Chrysophanic acid (Chrysophanol) <1 mg/mL <1 mg/mL <1 mg/mL
A10242 CP-724714 <1 mg/mL 94 mg/mL 94 mg/mL
A10362 Erlotinib hydrochloride <1 mg/mL 3 mg/mL <1 mg/mL
A10422 Gefitinib (Iressa) <1 mg/mL 89 mg/mL 4 mg/mL
A10514 Lapatinib Ditosylate <1 mg/mL 185 mg/mL <1 mg/mL
A10612 Mubritinib (TAK 165) 13 mg/mL <1 mg/mL <1 mg/mL
A10638 Neratinib (HKI-272) 2 mg/mL <1 mg/mL <1 mg/mL
A10678 OSI-420 83 mg/mL 2 mg/mL <1 mg/mL
A10702 PD153035 (HCl salt) <1 mg/mL <1 mg/mL <1 mg/mL
A10706 Pelitinib (EKB-569) <1 mg/mL 13 mg/mL <1 mg/mL
A11051 PF299804 <1 mg/mL 19 mg/mL <1 mg/mL
A11236 TAK-285 <1 mg/mL 110 mg/mL 54 mg/mL
A10053 Tyrphostin AG 879 36 mg/mLtd <1 mg/mL 3 mg/mL
A10990 WZ3146 <1 mg/mL 93 mg/mL <1 mg/mL
A10991 WZ4002 13 mg/mL <1 mg/mL <1 mg/mL
A10992 WZ8040 96 mg/mL <1 mg/mL 3 mg/mL

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