生物活性
Lapatinib (free base)是一种双重酪氨酸激酶抑制剂，是一种有效的EGFR和ErbB2抑制剂，在无细胞试验中IC50分别为10.2和9.8 nM。可阻断HER2生长受体途径。
Targets
| Target | Value |
| ErbB2 | IC50: 9.2nM |
| EGFR | IC50: 10.8nM |
| ErbB4 | IC50: 367nM |
| c-Src | IC50: 3.5μM |
| C-Raf-1 | IC50: >10μM |
| MEK | IC50: >10μM |
| ERK | IC50: >10μM |
| c-Fms | IC50: >10μM |
| CDK1 | IC50: >10μM |
| CDK2 | IC50: >10μM |
| p38 | IC50: >10μM |
| Tie-2 | IC50: >10μM |
| VEGFR2 | IC50: >10μM |
化学数据
| 目录号 | A11752 |
| M. Wt | 581.1 |
| Formula | C29H26ClFN4O4S |
| Purity | >99% |
| Storage | Store lyophilized at -20ºC, keep desiccated.
In lyophilized form, the chemical is stable for36 months.
In solution, store at -20ºC and use within3 monthsto prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles. |
| CAS No. | 231277-92-2 |
| SMILES | 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 |
溶解度
| In vitro (25°C) | DMSO | 99 mg/mL (170.37 mM) |
| Water | Insoluble |
| Ethanol | Insoluble |
| In vivo | 2% DMSO+30% PEG 300+5% Tween 80+ddH2O | 9 mg/mL |
*<1 mg/ml means slightly soluble or insoluble.
*Please note that Adooq tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
储备液配制
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
| 0.1 mM | 17.21 mL | 86.04 mL | 172.09 mL |
| 0.5 mM | 3.44 mL | 17.21 mL | 34.42 mL |
| 1 mM | 1.72 mL | 8.6 mL | 17.21 mL |
| 5 mM | 0.34 mL | 1.72 mL | 3.44 mL |
*The above data is based on the productmolecular weight 581.1 . Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
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