Key Documents

Afatinib dimaleate

Name: Afatinib dimaleate
Brand: SIGMA

≥98% (HPLC)

Synonym(s):

(2E)-N-[4-[(3-Chloro-4-fluorophenyl)amino]-7-[[(3S)-tetrahydro-3-furanyl]oxy]-6-quinazolinyl]-4-(dimethylamino)-2-butenamide, (2Z)-2-butenedioate (1:2), (S,E)-N-(4-(3-Chloro-4-fluorophenylamino)-7-(tetrahydrofuran-3-yloxy)quinazolin-6-yl)-4-(dimethylamino)but-2-enamide dimaleate, BIBW 2992 dimaleate, BIBW-2992 dimaleate, BIBW2992 dimaleate

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About This Item

Empirical Formula (Hill Notation):

C₃₂H₃₃ClFN₅O₁₁

CAS Number:

850140-73-7

Molecular Weight:

718.08

UNSPSC Code:

12352200

NACRES:

NA.77

MDL number:

MFCD25974239

Assay:

≥98% (HPLC)

Form:

powder

Pricing and availability is not currently available.

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Properties

Quality Segment

100

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

H₂O: 2 mg/mL, clear

storage temp.

2-8°C

SMILES string

OC(/C=C\C(O)=O)=O.OC(/C=C\C(O)=O)=O.CN(C)C/C=C/C(NC1=CC(C(NC2=CC=C(F)C(Cl)=C2)=NC=N3)=C3C=C1O[C@H]4CCOC4)=O

InChI

1S/C24H25ClFN5O3.2C4H4O4/c1-31(2)8-3-4-23(32)30-21-11-17-20(12-22(21)34-16-7-9-33-13-16)27-14-28-24(17)29-15-5-6-19(26)18(25)10-15;2*5-3(6)1-2-4(7)8/h3-6,10-12,14,16H,7-9,13H2,1-2H3,(H,30,32)(H,27,28,29);2*1-2H,(H,5,6)(H,7,8)/b4-3+;2*2-1-/t16-;;/m0../s1

InChI key

USNRYVNRPYXCSP-JUGPPOIOSA-N

Description

Biochem/physiol Actions

Afatinib (BIBW2992) is an orally active, irreversible, potent and selective EGFR/HER2 (ErbB2) dual inhibitor (EGFR IC50 = 0.5 nM (Wt), 0.4 nM (L858R), 10 nM (L858R/T790M); HER2 IC50 = 14 nM) that covalently targets EGFR Cys773 and HER2 Cys805 residues. BIBW2992 suppresses 100 ng/mL EGF-induced EGFR/HER2 tyrosin phosphorylation (IC50 = 13-71 nM; A431, NIH-3T3-HER2, BT-474, NCI-N87), inhibits cancer cells survival in cultures and induces tumor regression in xenograft and transgenic lung cancer models in vivo (20 mg/kg/day p.o.).

Orally active, irreversible, potent and selective EGFR/HER2 (ErbB2) dual inhibitor with in vitro and in vivo anti-cancer efficacy.

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This Item	SML3109	PZ0330	SML3195
Sigma-Aldrich SML3073 Afatinib dimaleate	Sigma-Aldrich SML3109 Afatinib	Sigma-Aldrich PZ0330 Dacomitinib	Sigma-Aldrich SML3195 AZD0530
assay ≥98% (HPLC)	assay ≥98% (HPLC)	assay ≥98% (HPLC)	assay ≥98% (HPLC)
form powder	form powder	form powder	form powder
Quality Level 100	Quality Level 100	Quality Level 100	Quality Level 100
storage temp. 2-8°C	storage temp. 2-8°C	storage temp. room temp	storage temp. 2-8°C
solubility H₂O: 2 mg/mL, clear	solubility DMSO: 2 mg/mL, clear	solubility DMSO: 2 mg/mL, clear	solubility DMSO: 2 mg/mL, clear
color white to beige	color white to beige	color white to beige	color white to beige