CAS 388082-77-7

Lapatinib ditosylate

Description:

Lapatinib ditosylate is a small molecule tyrosine kinase inhibitor primarily used in the treatment of certain types of breast cancer, particularly those that are HER2-positive. It functions by inhibiting the activity of the epidermal growth factor receptor (EGFR) and HER2, which are involved in the proliferation and survival of cancer cells. The compound is characterized by its molecular formula, which reflects its complex structure, including a dichloroaniline moiety and a sulfonate group that enhances its solubility. Lapatinib ditosylate is typically administered orally and is known for its ability to penetrate the blood-brain barrier, making it a potential option for treating brain metastases. Its pharmacokinetics include moderate absorption and a half-life that allows for once-daily dosing. Common side effects may include diarrhea, rash, and nausea. As with any targeted therapy, its use is often accompanied by monitoring for efficacy and adverse reactions, emphasizing the importance of personalized medicine in oncology.

Formula: C₄₃H₄₂ClFN₄O₁₀S₃

InChI: InChI=1/C29H26ClFN4O4S.2C6H6O3S.H2O/c1-40(36,37)12-11-32-16-23-7-10-27(39-23)20-5-8-26-24(14-20)29(34-18-33-26)35-22-6-9-28(25(30)15-22)38-17-19-3-2-4-21(31)13-19;2*7-10(8,9)6-4-2-1-3-5-6;/h2-10,13-15,18,32H,11-12,16-17H2,1H3,(H,33,34,35);2*1-5H,(H,7,8,9);1H2

InChI key: InChIKey=OZDXXJABMOYNGY-UHFFFAOYSA-N

SMILES: N(C=1C2=C(C=CC(=C2)C=3OC(CNCCS(C)(=O)=O)=CC3)N=CN1)C4=CC(Cl)=C(OCC5=CC(F)=CC=C5)C=C4.S(=O)(=O)(O)C1=CC=C(C)C=C1

Synonyms:

• 4-Quinazolinamine, N-[3-chloro-4-[(3-fluorophenyl)methoxy]phenyl]-6-[5-[[[2-(methylsulfonyl)ethyl]amino]methyl]-2-furanyl]-, 4-methylbenzenesulfonate (1:2)
• 4-Quinazolinamine, N-[3-chloro-4-[(3-fluorophenyl)methoxy]phenyl]-6-[5-[[[2-(methylsulfonyl)ethyl]amino]methyl]-2-furanyl]-, bis(4-methylbenzenesulfonate)
• Benzenesulfonic Acid
• Gw 572016F
• Hydrate
• Lapatinib Ditoyslate
• Lapatinib ditosylate anhydrous
• Lapatinib, Tykerb, GW572016
• N-(3-Chloro-4-((3-fluorophenyl)methoxy)phenyl)-6-(5-(((2-(methylsulfonyl)ethyl)amino)methyl)-2-furanyl)-4-quinazolinamine bis(4-methylbenzenesulfonate)
• N-[3-chloro-4-[(3-fluorophenyl)methoxy]phenyl]-6 -[5-[(2-methylsulfonylethylamino)methyl]-2-furyl]quinazolin-4-amine h ydrate
• N-[3-chloro-4-[(3-fluorophenyl)methoxy]phenyl]-6-[5-[(2-methylsulfonylethylamino)methyl]furan-2-yl]quinazolin-4-amine
• N-{3-chloro-4-[(3-fluorobenzyl)oxy]phenyl}-6-[5-({[2-(methylsulfonyl)ethyl]amino}methyl)furan-2-yl]quinazolin-4-amine benzenesulfonate hydrate (1:2:1)
• N-{3-chloro-4-[(3-fluorobenzyl)oxy]phenyl}-6-[5-({[2-(methylsulfonyl)ethyl]amino}methyl)furan-2-yl]quinazolin-4-amine bis(4-methylbenzenesulfonate)
• Tykerb
• Tykerb N-{3-Chloro-4-[(3-fluorophenyl)-methoxy]-phenyl}-6-{5-{(2-methylsulfonylethy amino)-methyl]-2-furyl}-quinazolin-4-amine-benzenesulfonic acid
• Lapatinib ditosylate
• GW-572016 ditosylate
• Lapatinib (GW-572016) Ditosylate
• GW 572016 ditosylate
• N-{3-chloro-4-[(3-fluorobenzyl)oxyl]phenyl}-6-[5-({[2-(methylsulfonyl)ethyl]amino}methyl)furan-2-yl]quinazolin-4-amine bis(4-methylBenzenesulfonate)
• Lapatinib Ditosylate (Tykerb)
• N-{3-Chloro-4-[(3-fluorobenzyl)oxy]phenyl}-6-[5-({[2-(Methylsulfonyl)ethyl]aMino}Methyl)-2-furyl]-4-quinazolinaMine 4-Methylbenzenesulfonate (1:2)
• GW-572016F Ditosylate
• Tykerb Ditosylat
• Lapatinib ditasylate
• N-(4-(3-fluorobenzyloxy)-3-chlorophenyl)-6-(5-((2-(methylsulfonyl)ethylamino)methyl)furan-2-yl)quinazolin-4-amine,di4-methylbenzenesulfonate
• Tykerb(lapatinib)
• Tykerb Ditosylate

Lapatinib Ditosylate

CAS: 388082-77-7

Lapatinib Ditosylate (Tykerb ditosylate) is an effective EGFR and ErbB2 inhibitor (IC50: 10.8/9.2 nM for EGFR/ErbB2).

Formula: C₂₉H₂₆ClFN₄O₄S·2C₇H₈O₃S

Purity: 99.41%

Color and Shape: Yellow Solid

Molecular weight: 925.46

Ref: TM-T6235

Lapatinib ditosylate

CAS: 388082-77-7

Formula: C₄₃H₄₂ClFN₄O₁₀S₃

Purity: 98%

Color and Shape: Solid

Molecular weight: 925.4608

Ref: IN-DA00C6B6

Lapatinib Ditosylate

CAS: 388082-77-7

Lapatinib Ditosylate

Purity: ≥98%

Molecular weight: 925.46g/mol

Ref: 54-BUP15047

Lapatinib Ditosylate

CAS: 388082-77-7

Formula: C₂₉H₂₆ClFN₄O₄S·2C₇H₈O₃S

Color and Shape: Yellow Solid

Molecular weight: 581.06 2*172.20

Ref: 4Z-L-255

Lapatinib-d4 Ditosylate

CAS: 388082-77-7

Formula: C₂₉H₂₂D₄ClFN₄O₄S·2C₇H₈O₃S

Color and Shape: Light Yellow Solid

Molecular weight: 585.08 2 172.20

Ref: 4Z-L-253

N-(3-Chloro-4-((3-Fluorobenzyl)Oxy)Phenyl)-6-(5-(((2-(Methylsulfonyl)Ethyl)Amino)Methyl)Furan-2-Yl)Quinazolin-4-Amine Bis(4-Methylbenzenesulfonate)

CAS: 388082-77-7

N-(3-Chloro-4-((3-Fluorobenzyl)Oxy)Phenyl)-6-(5-(((2-(Methylsulfonyl)Ethyl)Amino)Methyl)Furan-2-Yl)Quinazolin-4-Amine Bis(4-Methylbenzenesulfonate)

Purity: 98%

Molecular weight: 925.46g/mol

Ref: 54-PC109179

Lapatinib Ditosylate

CAS: 388082-77-7

Formula: C₂₉H₂₆ClFN₄O₄S·2C₇H₈O₃S

Purity: >98.0%(T)(HPLC)

Color and Shape: White to Light yellow powder to crystal

Molecular weight: 925.46

Ref: 3B-L0467

Lapatinib Ditosylate

Controlled Product

CAS: 388082-77-7

Applications Reversible dual inhibitor of ErbB1 and ErbB2 tyrosine kinases. Antineoplastic.
References Kim, T.E., et al.: Drugs, 6, 886 (2003), Wood, E.R., et al.: Cancer Res., 64, 6652 (2004), Spector, N.L., et al.: J. Clin. Oncol., 23, 2502 (2005),

Formula: C₂₉H₂₆ClFN₄O₄S·2C₇H₈O₃S

Color and Shape: Yellow

Molecular weight: 925.46

Ref: TR-L175800

Lapatinib tosylate anhydrous

CAS: 388082-77-7

Inhibitor of EGFR (ErbB1) and HER2 (ErbB2) receptor tyrosine kinases. Used for sensitization of HER2-overexpressing cancer cells to radiation as well as chemotherapy to tamoxifen- and trastuzumab-resistant cell lines. The compound blocks signalling via Akt and mitogen-activated protein kinase (MAPK) pathways leading to reduced cell survival. In trastuzumab resistant cancer cells, it inhibits HER2 phosphorylation, prevents receptor ubiquitination and causes accumulation of inactive HER2 dimers on the cell surface.

Formula: C₂₉H₂₆ClFN₄O₄S•(C₇H₈O₃S)₂

Purity: Min. 95%

Color and Shape: Off-White Powder

Molecular weight: 925.46 g/mol

Ref: 3D-FL65053