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Lapatinib ditosylate hydrate

Names

[ CAS No. ]:
388082-78-8

[ Name ]:
Lapatinib ditosylate hydrate

[Synonym ]:
N-{3-Chloro-4-[(3-fluorobenzyl)oxy]phenyl}-6-[5-({[2-(methylsulfonyl)ethyl]amino}methyl)-2-furyl]quinazolin-4-amine bis(4-methylbenzenesulfonate) hydrate
N-{3-Chloro-4-[(3-fluorobenzyl)oxy]phenyl}-6-[5-({[2-(methylsulfonyl)ethyl]amino}methyl)-2-furyl]-4-quinazolinamine 4-methylbenzenesulfonate hydrate (1:2:1)
Lapatinib ditosylate (USAN)
N-[3-Chloro-4-[(3-fluorophenyl)methoxy]phenyl]-6-[5-[[[2-(methylsulfonyl)ethyl]amino]methyl]-2-furanyl]-4-quinazolinamine, 4-methylbenzenesulfonate, hydrate (1:2:1)
T66 BN DNJ EMR CG DO1R CF&& H- BT5OJ E1M2SW1 &&2 p-Tosoh H2O
Lapatinib Ditosilate
4-Quinazolinamine, N-[3-chloro-4-[(3-fluorophenyl)methoxy]phenyl]-6-[5-[[[2-(methylsulfonyl)ethyl]amino]methyl]-2-furanyl]-, 4-methylbenzenesulfonate, hydrate (1:2:1)
Lapatinib ditosylate monohydrate
Lapatinib Ditosylate

Biological Activity

[Description]:

Lapatinib ditosylate monohydrate (GW572016 ditosylate monohydrate) is a potent inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively[1].

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> JAK/STAT Signaling >> EGFR
Signaling Pathways >> Protein Tyrosine Kinase/RTK >> EGFR
Signaling Pathways >> Autophagy >> Autophagy

[Target]

EGFR:10.8 nM (IC50)

ErbB2:9.2 nM (IC50)


[In Vitro]

Lapatinib (GW2016; 0.03-10 µM; 6 hours; BT474 and HN5 cells) treatment inhibits receptor autophosphorylation of EGFR and ErbB-2 in a dose-responsive manner. Phosphorylation of serine 473 of AKT was inhibited by GW2016 in a dose-dependent manner[1]. Lapatinib (GW2016; 72 hours; HN5, A-43, BT474, N87, and CaLu-3 cells) treatment has a selective inhibition of the proliferation of human tumor cell lines[1]. Lapatinib (GW2016; 1-10 µM; 72 hours; HN5 cells) treatment results in induces G1 arrest[1]. Western Blot Analysis[1] Cell Line: BT474 and HN5 cells Concentration: 0.03 µM, 0.1 µM, 0.3 µM, 1 µM, 3 µM, or 10 µM Incubation Time: 6 hours Result: Inhibited receptor autophosphorylation of EGFR and ErbB-2 in a dose-responsive manner. Phosphorylation of serine 473 of AKT was also inhibited in a dose-dependent manner. Cell Proliferation Assay[1] Cell Line: HN5, A-43, BT474, N87, and CaLu-3 cells Concentration: Incubation Time: 72 hours Result: Inhibited the growth of tumor cells overexpressing EGFR or ErbB-2. Cell Cycle Analysis[1] Cell Line: HN5 cells Concentration: 1 µM, or 10 µM Incubation Time: 72 hours Result: Resulted in induction of G1 arrest.

[In Vivo]

Lapatinib (GW2016; 30-100 mg/kg; oral administration; twice daily; for 21 days; CD-1 nude female mice) treatment inhibits tumor xenograft growth of the HN5 cells in a dose-responsive manner at 30 and 100 mg/kg, with complete inhibition of tumor growth at the higher dose[1]. Animal Model: CD-1 nude female mice (4-6 weeks old) with HN5 cells[1] Dosage: 30 mg/kg, 100 mg/kg Administration: Oral administration; twice daily; for 21 days Result: Inhibited tumor xenograft growth of the HN5 cells in a dose-responsive manner.

[References]

[1]. Rusnak DW, et al. The effects of the novel, reversible epidermal growth factor receptor/ErbB-2 tyrosine kinase inhibitor, GW2016, on the growth of human normal and tumor-derived cell lines in vitro and in vivo. Mol Cancer Ther. 2001 Dec;1(2):85-94.

Chemical & Physical Properties

[ Density]:
1.403 g/mL (20.84 °C)

[ Boiling Point ]:
750.7ºC at 760 mmHg

[ Melting Point ]:
237 - 239 °C

[ Molecular Formula ]:
C86H86Cl2F2N8O21S6

[ Molecular Weight ]:
943.476

[ Flash Point ]:
68 °F

[ Exact Mass ]:
942.184143

[ PSA ]:
249.46000

[ LogP ]:
12.26450

[ Index of Refraction ]:
n20/D 1.5520(lit.)

Safety Information

[ Hazard Codes ]:
Xi,N

[ Risk Phrases ]:
R43:May cause sensitization by skin contact. R51/53:Toxic to aquatic organisms, may cause long-term adverse effects in the aquatic environment .

[ Safety Phrases ]:
S24-S37-S61

Precursor & DownStream

Precursor

DownStream

Related Compounds