| CAS |
388082-78-8 |
| Chinese Name |
二对甲苯磺酸拉帕替尼 |
| English Name |
Lapatinib ditosylate |
| Synonyms |
Lapatinib ditoluenesulfonate monohydrate;二甲苯磺酸拉帕替尼单水合物;Lapatinib tosilate hydrate;Tykerb;Tyverb |
| Molecular Formula |
C43H44ClFN4O11S3 |
| Molecular Weight |
943.48 |
| Solubility |
Soluble in DMSO(Need ultrasonic) |
| Purity |
≥98% |
| Appearance |
Light yellow to yellow Solid |
| Storage |
Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| MDL |
MFCD18904381 |
| SMILES |
CC1=CC=C(C=C1)S(=O)(=O)O.CC1=CC=C(C=C1)S(=O)(=O)O.CS(=O)(=O)CCNCC1=CC=C(O1)C2=CC3=C(C=C2)N=CN=C3NC4=CC(=C(C=C4)OCC5=CC(=CC=C5)F)Cl.O |
| InChIKey |
XNRVGTHNYCNCFF-UHFFFAOYSA-N |
| InChI |
InChI=1S/C29H26ClFN4O4S.2C7H8O3S.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*1-6-2-4-7(5-3-6)11(8，9)10;/h2-10，13-15，18，32H，11-12，16-17H2，1H3，(H，33，34，35);2*2-5H，1H3，(H，8，9，10);1H2 |
| PubChem CID |
11557040 |
| Target Point |
ErbB-2;EGFR |
| Passage |
Angiogenesis;Protein Tyrosine Kinase/RTK |
| Background |
It is a potent inhibitor of ErbB-2 and EGFR tyrosine kinase domains. |
| Biological Activity |
Lapatinib ditosylate 是 ErbB-2 和表皮生长因子受体酪氨酸激酶结构域的强效抑制剂，对 EGFR 和 ErbB-2 的 IC50 值分别为 10.2 和 9.8 nM。[1] |
| IC50 |
EGFR: 10.2nM(IC50);ErbB2: 9.8nM(IC50)[1] |
| In Vitro |
After 3 days of lapatinib ditosylate exposure，average IC50 values for growth inhibition in the EGFR- and ErbB-2-overexpressing tumor cell lines were < 0.16 microM. The HN5 and BT474 cells were treated for 3 days in 1-10 μM concentrations of lapatinib ditosylate，and cell growth was monitored for an additional 12 days after removal of the compound. In each of these tumor cell lines，concentrations of lapatinib ditosylate were reached where outgrowth did not occur.[1] |
| In Vivo |
Lapatinib ditosylate treatment inhibited tumor xenograft growth of the HN5 and BT474 cells in a dose-responsive manner at 30 and 100 mg/kg orally，twice daily，with complete inhibition of tumor growth at the higher dose.[1] |
| Data Literature Source |
[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. |
| Unit |
Bottle |
| Specification |
25mg |
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