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Afatinib dimaleate

Afatinib dimaleate Structure
Afatinib dimaleate structure
CAS No.
850140-73-7
Chemical Name:
Afatinib dimaleate
Synonyms
Alfatinib maleate;BAY-2416964;BIBW2992 DiMaleate;Afatinib (diMaleate);BIBW2992-MA2;Afatinib DimaL;Aftinib maleate;Afatinib diMalea;Afatinib DIMELATE;Afatinib (maleate)
CBNumber:
CB22630067
Molecular Formula:
C28H29ClFN5O7
Molecular Weight:
602.02
MDL Number:
MFCD28969755
MOL File:
850140-73-7.mol
MSDS File:
SDS
TDS File:
TDS
Last updated:2026-07-27 17:00:41
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Afatinib dimaleate Properties

Melting point >237oC (dec.)
storage temp. Refrigerator
solubility DMSO (Slightly), Methanol (Slightly)
form Solid
color White to Pale Yellow
Water Solubility H2O: 2mg/mL, clear
InChIKey LIENDGDDWJRJLO-LBXKZPGENA-N
SMILES C(/C(=O)O)=C/C(=O)O.N(C1C=CC(F)=C(Cl)C=1)C1=NC=NC2C=C(O[C@@H]3COCC3)C(NC(=O)/C=C/CN(C)C)=CC1=2 |&1:25,r|
NCI Dictionary of Cancer Terms afatinib dimaleate
FDA UNII V1T5K7RZ0B
NCI Drug Dictionary afatinib dimaleate
UNSPSC Code 12352200
NACRES NA.77

SAFETY

Risk and Safety Statements

Symbol(GHS)  Exclamation Mark (GHS07)Health Hazard (GHS08)
GHS07,GHS08
Signal word  Warning
Hazard statements  H362-H319-H302-H372-H361
Precautionary statements  P201-P260-P263-P264-P270-P308+P313-P264-P280-P305+P351+P338-P337+P313P-P264-P270-P301+P312-P330-P501-P260-P264-P270-P314-P501-P201-P202-P281-P308+P313-P405-P501
target organs Kidney,Skin
WGK Germany  WGK 3
HS Code  29339900
Storage Class 11 - Combustible Solids
Hazard Classifications Acute Tox. 4 Oral
Eye Irrit. 2
STOT RE 2
NFPA 704
0
2 0

Afatinib dimaleate price More Price(63)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Cayman Chemical 21567 Afatinib (maleate) ≥95% 850140-73-7 100mg $54 2026-04-30 Buy
Cayman Chemical 21567 Afatinib (maleate) ≥95% 850140-73-7 250mg $108 2026-04-30 Buy
Cayman Chemical 21567 Afatinib (maleate) ≥95% 850140-73-7 500mg $203 2026-04-30 Buy
Cayman Chemical 21567 Afatinib (maleate) ≥95% 850140-73-7 1g $378 2026-04-30 Buy
ChemScene CS-1329 Afatinib (dimaleate) 99.74% 850140-73-7 5mg $41 2026-06-04 Buy
Product number Packaging Price Buy
21567 100mg $54 Buy
21567 250mg $108 Buy
21567 500mg $203 Buy
21567 1g $378 Buy
CS-1329 5mg $41 Buy

Afatinib dimaleate Chemical Properties, Uses, Production

Description

Afatinib dimaleate (Tovok; BIBW2992; Gilotrif) is a salt form of Afatinib. Afatinib is a second-generation, orally administered, irreversible inhibitor of the ErbB family of tyrosine kinases.

Mechanism of Action

Afatinib (850140-73-7) downregulates ErbB signalling by covalently binding to the kinase domains of epidermal growth factor receptor (EGFR), human epidermal growth factor receptor (HER) 2 and HER4, resulting in irreversible inhibition of tyrosine kinase autophosphorylation; it also inhibits transphosphorylation of HER3. Afatinib is approved as monotherapy for the treatment of EGFR tyrosine kinase inhibitor (TKI)-na?ve adults with locally advanced or metastatic non-small cell lung cancer (NSCLC) with activating EGFR mutations in the EU, and for the first-line treatment of patients with metastatic NSCLC whose tumours have EGFR exon 19 deletions or exon 21 (L858R) substitution mutations as detected by a US FDA-approved test in the US.

Description

Afatinib dimaleate was approved by the U.S. Food and Drug Administration (FDA) in 2013 for the treatment of non-small cell lung cancer (NSCLC). Specifically, it was approved for patients presenting with metastatic NSCLC tumors which contain epidermal growth factor receptor (EGFR) exon deletions or exon 21 mutations. Afatinib dimaleate is a covalent inhibitor of ErbB tyrosine kinases (tyk), which downregulates ErbB signaling by irreversible binding of EGFR tyk binding sites. While no manufacturing route has been disclosed to date, the most scalable published route likely derives from two Boehringer Ingelheim patents.

Uses

Afatinib Dimaleate is a salt of Afatinib {BIBW 2992), an aminocrotonylamino-substituted quinazoline derivative used for treating cancer and diseases of the respiratory tract, lungs, gastrointestinal tract, bile duct, and gallbladder. An anilino-quinazoline that irreversibly inhibits EGFR and HER2 kinase activity.

Definition

ChEBI: Afatinib dimaleate is a maleate salt obtained by combining afatinib with two molar equivalents of maleic acid. Used for the first-line treatment of patients with metastatic non-small cell lung cancer. It has a role as a tyrosine kinase inhibitor and an antineoplastic agent. It contains an afatinib.

General Description

Afatinib dimaleate is the dimaleate form of afatinib. It is a tyrosine kinase inhibitor of epidermal growth factor receptors (ERBB RECEPTORS) and an anti-angiogenic agent. Afatinib dimaleate has anti-tumour activity and is mainly used for the treatment of patients with metastatic non-small cell lung cancer (which has metastasised or spread to other parts of the body), or certain tumours with mutations in the EGFR gene and patients whose disease has worsened after platinum-based chemotherapy. It is also used for the treatment of esophageal squamous cell carcinoma (ESCC) and gastric cancer.

Biological Activity

Afatinib dimaleate is an orally bioavailable and irreversible dual-specific inhibitor of the ErbB family (EGFR and HER2). IC50 are 0.4, 0.5, 10, 14, 1 nM for EGFRL858R, EGFRwt, EGFR L858R/T790M, ErbB2 (HER2) and ErbB4 (HER4), respectively. Afatinib dimaleate is available for cancer (esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC) and gastric cancer) studies.

Side effects

Afatinib dimaleate is similar to afatinib in terms of side effects. Common side effects include: diarrhoea, fever, difficulty urinating, burning or pain, redness, swelling or pain in the skin, discharge or excessive tearing, burning, dryness or itching of the eyes, and skin ulcers. Occasional symptoms of coughing and difficulty breathing. A very small number of patients may have bloody stools, black stools or tarry stools, indigestion, nausea, severe abdominal pain, cramping or burning sensation, and vomiting of a substance that looks like coffee grounds. Please contact your doctor promptly if any serious adverse reactions occur.

Synthesis

Nitroquinazolinone (6), which is commercially available, was first chlorinated with phosphorous oxychloride (POCl3) followed by treatment with commercial 3-chloro-4-fluoroaniline (7) to afford SNAr adduct 8 in 90% yield over two steps. Sulfonylation to afford 9 (86%) and subsequent displacement with (S)-tetrahydrofuran- 3-ol gave 10 in 90% yield. Raney¨CNickel reduction of the nitro group delivered 11 in 97% yield, which set the stage for the final side-chain functionalization. 2-(Diethoxyphosphoryl) acetic acid and N,N0-carbonyldiimidazole (CDI) were pre-mixed and added to aniline 11 to afford 12 in 70% isolated yield. Next, a Horner¨CWadsworth¨CEmmons homologation gave the (E)-olefin 13 in quantitative yield, followed by maleate salt formation (92%) to deliver the final API. The final five steps of this synthesis have been successfully demonstrated on multi-kilogram scale.

Synthesis_850140-73-7

storage

Store at -20°C

Afatinib dimaleate Preparation Products And Raw materials

Raw materials

Preparation Products

Afatinib dimaleate Suppliers

Global Suppliers ( 408)
Supplier Tel Email Country ProdList Advantage
Nanjing EnMing Pharmaceutical Technology Co., Ltd. 13305188663 njempt@163.com China 16 58
ZHEJIANG ZETIAN FINE CHEMICALS CO.,LTD 0571-87322520 18957127338 sales@zetchem.com China 466 55
HANGZHOU KELAI BIOMEDICAL TECHNOLOGY Co., Ltd. 18957050573 752803249@qq.com China 240 58
Shandong Mingfeng Pharmaceutical and Technology Co. Ltd 053155551677 15315114555 1345456643@qq.com China 299 58
Shanghai Boyle Chemical Co., Ltd. sales@boylechem.com China 2915 55
Chembest Research Laboratories Limited 021-20908456 sales@BioChemBest.com China 5996 61
Adamas Reagent, Ltd. 400-6009262 15618770481 yhx@titansci.com China 14098 59
Nanjing Chemlin Chemical Co., Ltd 025-83697070 13770331960 info@chemlin.com.cn China 16306 64
Jinan Trio PharmaTech Co., Ltd. 0531-88811783 sales@trio-pharmatech.com China 1856 62
Shanghai Sphchem Co., Ltd. 021-56491756 13512199871 2819742715@qq.com China 3994 55
Supplier Advantage
Nanjing EnMing Pharmaceutical Technology Co., Ltd. 58
ZHEJIANG ZETIAN FINE CHEMICALS CO.,LTD 55
HANGZHOU KELAI BIOMEDICAL TECHNOLOGY Co., Ltd. 58
Shandong Mingfeng Pharmaceutical and Technology Co. Ltd 58
Shanghai Boyle Chemical Co., Ltd. 55
Chembest Research Laboratories Limited 61
Adamas Reagent, Ltd. 59
Nanjing Chemlin Chemical Co., Ltd 64
Jinan Trio PharmaTech Co., Ltd. 62
Shanghai Sphchem Co., Ltd. 55

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View Latest Price from Afatinib dimaleate manufacturers

Image Update time Product Price Min. Order Purity Supply Ability Manufacturer
Afatinib dimaleate pictures 2026-09-18 Afatinib dimaleate
850140-73-7
 1g 99%min 1000g WUHAN FORTUNA CHEMICAL CO., LTD
Afatinib Dimaleate pictures 2026-09-18 Afatinib Dimaleate
850140-73-7
 $1.00 1g More Than 99% 50kg/Month BEIJING SJAR TECHNOLOGY DEVELOPMENT CO., LTD.
Afatinib Dimaleate. pictures 2026-09-18 Afatinib Dimaleate.
850140-73-7
 $1.00 1g More Than 99% 50kg/Month BEIJING SJAR TECHNOLOGY DEVELOPMENT CO., LTD.
  • Afatinib Dimaleate pictures
  • Afatinib Dimaleate
    850140-73-7
  • $1.00
  • More Than 99%
  • BEIJING SJAR TECHNOLOGY DEVELOPMENT CO., LTD.

Afatinib dimaleate Spectrum

Afatinib dimaleate(850140-73-7)1HNMR

850140-73-7 (Afatinib dimaleate) Related Search:

Alectinib Hydrochloride Nintedanib esylate Olaparib trans-4-Dimethylaminocrotonic acid hydrochloride (S)-N4-(3-chloro-4-fluorophenyl)-7-(tetrahydrofuran-3-yloxy)quinazoline-4,6-diaMine
Afatinib 4-Quinazolinamine, N-(3-chloro-4-fluorophenyl)-7-fluoro-6-nitro- (S)-(+)-3-Hydroxytetrahydrofuran Afatinib (BIBW 2992) 7-Fluoro-6-nitro-4-hydroxyquinazoline
4-QuinazolinaMine, N-(3-chloro-4-fluorophenyl)-6-nitro-7-[[(3S)-tetrahydro-3-furanyl]oxy]- PLX4032 Cabozantinib Malate Crizotinib PLERIXAFOR
201530-41-8 918504-65-1 1110813-31-4

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BIBW2992-MA2 Afatinib (diMaleate) Afatinib (diMaleate), BIBW2992 2-ButenaMide, N-[4-[(3-chloro-4-fluorophenyl)aMino]-7-[[(3S)-tetrahydro-3-furanyl]oxy]-6-quinazolinyl]-4-(diMethylaMino)-, (2E)-, (2Z)-2-butenedioate (1:2) (2E)-N-(4-[(3-chloro-4-fluorophenyl)aMino]-7-{[(3S) Afatinib double Maleate Afatinib (BIBW2992) Dimaleate N-[4-[(3-chloro-4-fluorophenyl)amino]-7-[[(3S)-tetrahydro-3-furanyl]oxy]-6-quinazolinyl]-4-(dimethylamino)-(2E)-2-butenamide,(2Z)-2-butenedioate (1:2) Afatinib dimaleate BIBW 2992MA2 Afatinib dimaleate, >=99% (S,Z)-N-(4-((3-chloro-4-fluorophenyl)amino)-7-((tetrahydrofuran-3-yl)oxy)quinazolin-6-yl)-4-(dimethylamino)but-2-enamide dimaleate (2E)-N-[4-[(3-Chloro-4-fluorophenyl)amino]-7-[[(3S)-tetrahydro-3-furanyl]oxy]-6-quinazolinyl]-4-(dimethylamino)-2-butenamide dimaleate BIBW2992-MA2 (Afatinib dimaleate) (E)-N-[4-[(3-Chloro-4-fluorophenyl)amino]-7-[[(S)-tetrahydrofuran-3-yl]oxy]-6-quinazolinyl]-4-(dimethylamino)-2-butenamide Dimaleate (S,E)-N-(4-((3-Chloro-4-fluorophenyl)amino)-7-((tetrahydrofuran-3-yl)oxy)quinazolin-6-yl)-4-(d Afatinib (maleate) Afatinib dimaleate(BIBW2992,Gilotrif) Afatinib dimaleate hcl Afatinib DimaL BIBW2993 DiMaleate (2E)-N-[4-[(3-Chloro-4-fluorophenyl)amino]-7-[[(3S)-tetrahydro-3-furanyl]oxy]-6-quinazolinyl]-4-(dimethylamino)-2-butenamide (2Z)-2-butenedioate Afatinib double Maleat BIBW2992 DiMaleate USP/EP/BP AfatinibdimaleateQ: What is Afatinibdimaleate Q: What is the CAS Number of Afatinibdimaleate Q: What is the storage condition of Afatinibdimaleate Q: What are the applications of Afatinibdimaleate Afatiniβ-d6 Dimaleate Alfatinib maleate Aftinib maleate (S,E)-N-(4-((3-Chloro-4-fluorophenyl)amino)-7-((tetrahydrofuran-3-yl)oxy)quinazolin-6-yl)-4-(dimethylamino)but-2-enamide dimaleate Malate afatinib impurities Afatinib Dimaleate CRS Afatinib DIMELATE Afatinib Dimaleate, 10 mM in DMSO Afatinib diMalea BAY-2416964 BIBW2992 DiMaleate 850140-73-7 850140-73-8 C24H25ClFN5O32C4H4O4 C28H29ClFN5O7 C32H33ClFN5O11 C24H25ClFN5O3C8H8O8 Inhibitors tyrosine kinase receptor inhibitor 850140-73-7