CAS 850140-73-7

Afatinib dimaleate

Description:

Afatinib dimaleate is a potent, irreversible inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase, primarily used in the treatment of non-small cell lung cancer (NSCLC) with specific EGFR mutations. It is characterized by its ability to bind covalently to the active site of the EGFR, thereby blocking downstream signaling pathways that promote tumor growth and survival. The substance is typically administered orally and is known for its selectivity towards EGFR, which minimizes effects on other kinases. Afatinib dimaleate is a white to off-white solid, and its solubility profile allows for effective absorption in the gastrointestinal tract. The compound's pharmacokinetics indicate a relatively long half-life, which supports once-daily dosing. Common side effects associated with its use include diarrhea, rash, and stomatitis, reflecting its mechanism of action on epithelial tissues. Overall, Afatinib dimaleate represents a significant advancement in targeted cancer therapy, offering a tailored approach to treatment based on genetic profiling of tumors.

Formula: C₂₄H₂₅ClFN₅O₃

InChI: 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

SMILES: N(C=1C2=C(C=C(O[C@H]3CCOC3)C(NC(/C=C/CN(C)C)=O)=C2)N=CN1)C4=CC(Cl)=C(F)C=C4.C(=C\C(O)=O)\C(O)=O

Synonyms:

• 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)
• BIBW2992 DiMaleate
• Bibw 2992Ma2
• Bibw2992-Ma2
• BIBW 2992 dimaleate
• Afatinib dimaleate
• Afatinib (diMaleate), BIBW2992
• Afatinib dimaleate BIBW 2992MA2
• Afatinib double Maleate
• 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 (BIBW2992) Dimaleate
• (S,E)-N-(4-((3-Chloro-4-fluorophenyl)amino)-7-((tetrahydrofuran-3-yl)oxy)quinazolin-6-yl)-4-(d
• (2E)-N-(4-[(3-chloro-4-fluorophenyl)aMino]-7-{[(3S)
• Afatinib dimaleate, >=99%

Afatinib (Dimaleate)

CAS: 850140-73-7

Afatinib (Dimaleate)

Formula: C₃₂H₃₃ClFN₅O₁₁

Purity: 98%

Molecular weight: 718.08

Ref: 54-PC109115

Afatinib Dimaleate

CAS: 850140-73-7

Formula: C₂₄H₂₅ClFN₅O₃·2C₄H₄O₄

Molecular weight: 485.94 2*116.07

Ref: 4Z-A-111063

Afatinib Dimaleate

CAS: 850140-73-7

Afatinib Dimaleate

Formula: C₃₂H₃₃ClFN₅O₁₁

Purity: ≥98%

Molecular weight: 718.08

Ref: 54-BUP17135

Afatinib-d6 dimaleate(N,N-dimethyl-d6)

CAS: 850140-73-7

Purity: 98 atom % D

Molecular weight: 724.13

Ref: 3U-D7675

Afatinib Dimaleate

Controlled Product

CAS: 850140-73-7

Formula: C₂₄H₂₅ClFN₅O₃·2C₄H₄O₄

Color and Shape: Neat

Molecular weight: 718.08

Ref: 86-MM3700.00

Afatinib Dimaleate

CAS: 850140-73-7

Afatinib Dimaleate (BIBW 2992MA2) is an orally bioavailable anilino-quinazoline derivative and inhibitor of the EGFR family, with antineoplastic activity.

Formula: C₃₂H₃₃ClFN₅O₁₁

Purity: 98.11% - 99.87%

Color and Shape: White Solid

Molecular weight: 718.083

Ref: TM-T1773

Afatinib dimaleate

CAS: 850140-73-7

(S,E)-N-(4-((3-Chloro-4-fluorophenyl)amino)-7-((tetrahydrofuran-3-yl)oxy)quinazolin-6-yl)-4-(dimethylamino)but-2-enamide dimaleate

Formula: C₃₂H₃₃ClFN₅O₁₁

Purity: 98%

Molecular weight: 718.08

Ref: IN-DG305999

Afatinib dimaleate

CAS: 850140-73-7

Irreversible blocker of three members of the ErbB family (ErbB1, ErbB2/HER2, and ErbB4) with IC50 in nanomolar range. The compound binds covalently to cysteine 797 residue in HER2 and blocks downstream cellular signalling, inhibits cellular growth and promotes apoptosis. Afatinib has been used for the treatment of tyrosine kinase inhibitor-resistant tumours with mutations in ErbB genes, especially for deletions in exon 19 and single nucleotide substitutions in exon 21. It has been used for treatment of non-small cell lung cancer (NSCLC), breast cancer, pancreatic cancer, colorectal cancer, etc.

Formula: C₂₄H₂₅ClFN₅O₃·C₈H₈O₈

Purity: Min. 95%

Color and Shape: Solid

Molecular weight: 718.08 g/mol

Ref: 3D-BA162012

Afatinib Dimaleate

CAS: 850140-73-7

Formula: C₃₂H₃₃ClFN₅O₁₁

Molecular weight: 718.1

Ref: BE-RMCA078062

Afatinib Dimaleate

CAS: 850140-73-7

Purity: 98%

Color and Shape: Solid

Molecular weight: 718.0900269

Ref: 10-F798908

Afatinib-d6 Dimaleate

Controlled Product

CAS: 850140-73-7

Applications Afatinib-d6 Dimaleate is deuterium labelled Afatinib Dimaleate, which is a salt of Afatinib (BIBW 2992) (B377000). BIBW 2992 is 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.
References D, Li. et al.: Oncogene., 27, 4702 (2008); Wang, X. et al.: Cancer Res., 74, 4431 (2014)

Formula: C₂₄D₆H₁₉ClFN₅O₃·C₄H₄O₄

Color and Shape: Neat

Molecular weight: 608.048

Ref: TR-A355317

Afatinib Dimaleate

Controlled Product

CAS: 850140-73-7

Applications Afatinib Dimaleate is a salt of Afatinib {BIBW 2992) (B377000), 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.
References D, Li. et al.: Oncogene., 27, 4702 (2008); Wang, X. et al.: Cancer Res., 74, 4431 (2014);

Formula: C₂₄H₂₅ClFN₅O₃·2C₄H₄O₄

Color and Shape: Neat

Molecular weight: 718.08

Ref: TR-A355315

Afatinib Dimaleate

CAS: 850140-73-7

Formula: C₂₄H₂₅ClFN₅O₃(C₄H₄O₄)

Molecular weight: 485.9 : 2(116.1)

Ref: ST-EA-CP-A50034

afatinib dimaleate

CAS: 850140-73-7

Formula: C₃₂H₃₃ClFN₅O₁₁

Purity: 98%

Color and Shape: Solid

Molecular weight: 718.0827

Ref: IN-DA00391H