Lapatinib
231277-92-2
99%
Yes
2026-11-15
Coenzymes,Inhibito,Enzymes,Zymogens,Substrates,Native Microorganism Creatine Amidinohydrolase
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Product Description
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Seller Information
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Description
ProductName Lapatinib Cat No CEI-0018 Description Lapatinib Alias GW572016 CAS No 231277-92-2 Molecular Weight 581.06 Purity >99% Storage 2 years -20centigrade Powder Synonyms GW572016 Targets EGFR Molecular Formula C29H26ClFN4O4S Chemical Name N-(4-(3-fluorobenzyloxy)-3-chlorophenyl)-6-(5-((2-(methylsulfonyl)ethylamino)methyl)furan-2-yl)quinazolin-4-amine,di4-methylbenzenesulfonate Solubility DMSO 100 mg/mL, Water In vitro Lapatinib can inihbit Epidermal growth factor receptor (erbB1) with IC50 of 2.9 nM.[1] Lapatinib also inhibit receptor protein-tyrosine kinase(erbB-2) with IC50 around 3 nM.[1] Overexpression of ABC subfamily B member 1 (ABCB1) and ABC subfamily G member 2 (ABCG2) transporters would result in tumor multidrug resistance (MDR). Lapatinib significantly enhanced the sensitivity to ABCB1 or ABCG2 substrates in cells by stimulating the ATPase activity of both ABCB1 and ABCG2. And lapatinib reverses ABCB1- and ABCG2-mediated MDR by directly inhibiting their transport function so that lapatinib (Tykerb, GW572016) may combinate with other inhibitors to block proliferation of cancer cells and get better results. Lapatinib can inhibit SK-OV-3, an Ovarian carcinoma cell line which overexpress HER2, with IC50 from 3 to 4.5 nM. category Antineoplastic Agents(c1417) cas_num 231277-92-2 ECHEMI Editorial ReferenceLapatinib (GW572016) is a potent EGFR and ErbB2 inhibitor with IC50s of 10.2 and 9.8 nM, respectively.
Solid
Lapatinib is an organofluorine compound, an organochlorine compound, a member of quinazolines and a member of furans. It has a role as an antineoplastic agent and a tyrosine kinase inhibitor. It derives from a monofluorobenzene.|Lapatinib is an anti-cancer drug developed by GlaxoSmithKline (GSK) as a treatment for solid tumours such as breast and lung cancer. It was approved by the FDA on March 13, 2007, for use in patients with advanced metastatic breast cancer in conjunction with the chemotherapy drug Capecitabine. Lapatinib is human epidermal growth factor receptor type 2 (HER2/ERBB2) and epidermal growth factor receptor (HER1/EGFR/ERBB1) tyrosine kinases inhibitor. It binds to the intracellular phosphorylation domain to prevent receptor autophosphorylation upon ligand binding.|Lapatinib is a Kinase Inhibitor. The mechanism of action of lapatinib is as a Protein Kinase Inhibitor.|Lapatinib is a small molecule inhibitor of several tyrosine kinase receptors involved in tumor cell growth that is used in the therapy of advanced breast cancer and other solid tumors. Lapatinib therapy is associated with transient elevations in serum aminotransferase levels and rare instances of clinically apparent acute liver injury.|Lapatinib is a synthetic, orally-active quinazoline with potential antineoplastic properties. Lapatinib reversibly blocks phosphorylation of the epidermal growth factor receptor (EGFR), ErbB2, and the Erk-1 and-2 and AKT kinases; it also inhibits cyclin D protein levels in human tumor cell lines and xenografts. EGFR and ErbB2 have been implicated in the growth of various tumor types.|A quinazoline derivative that inhibits EPIDERMAL GROWTH FACTOR RECEPTOR and HER2 (RECEPTOR, ERBB-2) tyrosine kinases. It is used for the treatment of advanced or metastatic breast cancer, where tumors overexpress HER2.Basic Info-
Product Name:
Lapatinib
Other Name:4-Quinazolinamine,N-[3-chloro-4-[(3-fluorophenyl)methoxy]phenyl]-6-[5-[[[2-(methylsulfonyl)ethyl]amino]methyl]-2-furanyl]-;N-[3-Chloro-4-[(3-fluorophenyl)methoxy]phenyl]-6-[5-[[[2-(methylsulfonyl)ethyl]amino]methyl]-2-furanyl]-4-quinazolinamine;GW 572016;Lapatinib;4-[[3-Chloro-4-(3-fluorobenzyloxy)phenyl]amino]-6-[5-[[(2-methanesulfonylethyl)amino]methyl]furan-2-yl]quinazoline;GSK 572016;N-[3-Chloro-4-[(3-fluorobenzyl)oxy]phenyl]-6-[5-[[[2-(methylsulfonyl)ethyl]amino]methyl]-2-furyl]-4-quinazolinamine;GW 572016X;N-[3-Chloro-4-[(3-fluorobenzyl)oxy]phenyl]-6-[5-[[[2-(methanesulfonyl)ethyl]amino]methyl]-2-furyl]-4-quinazolinamine;Tyverb;N-[3-Chloro-4-[(3-fluorophenyl)methoxy]phenyl]-6-[5-[(2-methylsulfonylethylamino)methyl]furan-2-yl]quinazolin-4-amine;N-[4-(3-Fluorobenzyloxy)-3-chlorophenyl]-6-[5-[[2-(methylsulfonyl)ethylamino]methyl]furan-2-yl]quinazolin-4-amine;GD 2016;Tycerb
CAS No.:231277-92-2
Molecular Formula:C29H26ClFN4O4S
InChIKeys:InChIKey=BCFGMOOMADDAQU-UHFFFAOYSA-N
Molecular Weight:581.0575432
Exact Mass:581.06
EC Number:1806241-263-5
UNII:0VUA21238F
NSC Number:745750
DSSTox ID:DTXSID7046675
NCI Thesaurus Code:C26653
ATC Code:L01XE07|L - Antineoplastic and immunomodulating agents
HScode:2934999090
Categories:
Characteristics-
PSA:
115
XLogP3:5.1
Appearance:Solid
Density:1.4±0.1 g/cm3
Boiling Point:750.7°C at 760 mmHg
Flash Point:407.8±32.9 °C
Refractive Index:1.645
Water Solubility:2.23e-02 g/L
Storage Conditions:Store at 25 deg C (77 deg F); excursions permitted to 15 deg to 30 deg C (59 deg to 86 deg F).
Vapor Pressure:1.63X10-17 mm Hg at 25 deg C (est)
Henrys Law Constant:Henry's Law constant = 4.93X10-22 atm-cu m/mol at 25 °C (est)
Dissociation Constants:pKa1 = 3.80 (amine); pKa2 = 7.20 (amine)
Experimental Properties:Hydroxyl radical reaction rate constant = 3.04X10-10 cu cm/molec-sec at 25 °C (est)
Hazard IdentificationClassification of the substance or mixture
no data available
GHS label elements, including precautionary statements
Pictogram(s) no data available Signal word no data available
Hazard statement(s) no data available
Precautionary statement(s) Prevention no data available
Response no data available
Storage no data available
Disposal no data available
Other hazards which do not result in classification
no data available
Handling and StoragePrecautions for safe handling
Handling in a well ventilated place. Wear suitable protective clothing. Avoid contact with skin and eyes. Avoid formation of dust and aerosols. Use non-sparking tools. Prevent fire caused by electrostatic discharge steam.
Conditions for safe storage, including any incompatibilities
Store the container tightly closed in a dry, cool and well-ventilated place. Store apart from foodstuff containers or incompatible materials.
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Seller Information
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Business Type:
Manufactory
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Main Products:
Coenzymes,Inhibito,Enzymes,Zymogens,Substrates,Native Microorganism Creatine Amidinohydrolase
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Location:
Shirley, New York 11967, USA
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Payment Terms:
TT against copy of documents,D/P
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Average lead Time:
15 days
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Total Annual Revenue:
$1 million-$2.5 million
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Year of Establishment:
2004
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