GPI-15427
CAS 805242-85-7 MFCD05242857
化学结构图
SMILES: CN1CCN(Cc2ccc3oc4cccc5c(=O)[nH]nc(c3c2)c45)CC1
化学属性
| Mol. Weight | 348.4 |
|---|---|
| Appearance | Solid powder |
| Solubility | Soluble in DMSO, not in water |
别名和识别编码
| Chemical Name | GPI-15427 |
|---|---|
| Formula | C20H20N4O2 |
| Synonym | GPI15427; GPI 15427; GPI-15427. |
| IUPAC Name | 10-((4-methylpiperazin-1-yl)methyl)chromeno[4,3,2-de]phthalazin-3(2H)-one. |
| InChIKey | DZRLVSOGARUEGQ-UHFFFAOYSA-N |
| InChI | InChI=1S/C20H20N4O2/c1-23-7-9-24(10-8-23)12-13-5-6-16-15(11-13)19-18-14(20(25)22-21-19)3-2-4-17(18)26-16/h2-6,11H,7-10,12H2,1H3,(H,22,25) |
| Canonical SMILES | O=C1NN=C2C3=C1C=CC=C3OC4=C2C=C(CN5CCN(C)CC5)C=C4 |
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产品应用
- GPI-15427 is a potent PARP-1 inhibitor capable of crossing the blood-brain barrier, which can significantly increased the antitumor activity of the methylating agent TMZ against malignant melanoma, glioblastoma multiforme, or lymphoma growing at the CNS site. GPI-15427 acts as a potent inhibitor of the enzyme, being capable of inhibiting the activity of purified PARP-1 at nanomolar concentrations. GPI-15427 induced significant sensitization to radiotherapy, representing a promising new treatment in the management of HNSCC.
