生物活性
Pazopanib HCl (GW786034)是VEGFR-1，VEGFR-2，VEGFR-3，PDGFR-a/β和c-kit的有效且选择性的多靶点酪氨酸激酶抑制剂，可阻止肿瘤生长并抑制血管生成。
Targets
| Target | Value |
| VEGFR1 | IC50: 10nM |
| VEGFR2 | IC50: 30nM |
| VEGFR3 | IC50: 47nM |
| FGFR | IC50: 74nM |
| PDGFR | IC50: 84nM |
| c-Kit | IC50: 140nM |
| c-Fms | IC50: 146nM |
化学数据
| 目录号 | A10699 |
| 作用机制 | Inhibitor (抑制剂) |
| M. Wt | 474.0 |
| Formula | C21H23N7O2S.HCl |
| 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. | 635702-64-6 |
| Synonyms | GW786034, GW-786034 |
| SMILES | CC1=C(C=C(C=C1)NC2=NC=CC(=N2)N(C)C3=CC4=NN(C(=C4C=C3)C)C)S(=O)(=O)N.Cl |
溶解度
| In vitro (25°C) | DMSO | 15 mg/mL (31.64 mM) |
| Water | Insoluble |
| Ethanol | Insoluble |
| In vivo | 30% PEG400+0.5% Tween80+5% propylene glycol | 28 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 | 21.1 mL | 105.49 mL | 210.97 mL |
| 0.5 mM | 4.22 mL | 21.1 mL | 42.19 mL |
| 1 mM | 2.11 mL | 10.55 mL | 21.1 mL |
| 5 mM | 0.42 mL | 2.11 mL | 4.22 mL |
*The above data is based on the productmolecular weight 474.0 . 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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