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388082-78-8

388082-78-8 structure
388082-78-8 structure
  • Name: Lapatinib ditosylate hydrate
  • Chemical Name: Lapatinib ditosylate
  • CAS Number: 388082-78-8
  • Molecular Formula: C86H86Cl2F2N8O21S6
  • Molecular Weight: 943.476
  • Catalog: Organic raw materials Amino compound Sulfonic acid amino compound
  • Create Date: 2018-07-23 20:18:09
  • Modify Date: 2024-01-02 18:53:29
  • 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].
Name Lapatinib ditosylate
Synonyms 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
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
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.
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.)

Chemsrc provides CAS#:388082-78-8 MSDS, density, melting point, boiling point, structure, formula, molecular weight, synthetic route, etc.
title: CAS No. 388082-78-8 | Chemsrc address: https://www.chemsrc.com/en/baike/123928.html

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