IITZ-01
| 中文名称 | IITZ-01 |
|---|---|
| 中文同义词 | N2-(4-(1H-苯并[D]咪唑-2-基)苯基)-N4-(4-氟苯基)-6-吗啉代-1,3,5-三嗪-2,4-二胺;化合物IITZ-01 |
| 英文名称 | IITZ-01 |
| 英文同义词 | IITZ-01;AUTOPHAGY INHIBITOR;IITZ 01;IITZ01;Autophagy inhibitor IITZ-01;AUTOPHAGY INHIBITOR IITZ-01;IITZ 01;IITZ01;CS-2857;1,3,5-Triazine-2,4-diamine, N2-[4-(1H-benzimidazol-2-yl)phenyl]-N4-(4-fluorophenyl)-6-(4-morpholinyl)-;N-[4-(1H-Benzimidazol-2-yl)phenyl]-N'-(4-fluorophenyl)-6-(4-morpholinyl)-1,3,5-triazine-2,4-diamine;Phosphoinositide 3-kinase,IITZ 01,IITZ01,Apoptosis,IITZ-01,Autophagy,inhibit,Inhibitor,PI3K |
| CAS号 | 1807988-47-1 |
| 分子式 | C26H23FN8O |
| 分子量 | 482.51 |
| EINECS号 | |
| 相关类别 | API |
| Mol文件 | 1807988-47-1.mol |
| 结构式 |  |
IITZ-01 性质
| 沸点 | 747.0±70.0 °C(Predicted) |
|---|---|
| 密度 | 1.420±0.06 g/cm3(Predicted) |
| 储存条件 | under inert gas (nitrogen or Argon) at 2–8 °C |
| 溶解度 | DMSO:100.0(最大浓度 mg/mL);207.24(最大浓度 mM) |
| 酸度系数(pKa) | 11.55±0.10(Predicted) |
| 形态 | 固体 |
| 颜色 | 白色至米白色 |
IITZ-01 是一个具有抗肿瘤活性的、有效的亲溶酶体的自噬抑制剂，其对 PI3Kγ 的 IC50 值为 2.62 μM。
|
PI3Kγ 2.62 μM (IC 50 ) |
Autophagy
|
IITZ-01 (0-2 μM, 24 h) enhances autophagosomes formation as indicated by increased expression of LC3-II levels time- and dose-dependently in triple-negative breast cancer (TNBC) cell lines (MDA-MB-231 and MDA-MB-453). IITZ-01 also demonstrates potent autophagy inhibitory activity in other breast, lung, and colon cancer cells.
Western Blot Analysis
| Cell Line: | Triple-negative breast cancer (TNBC) cell lines (MDA-MB-231 and MDA-MB-453). |
| Concentration: | 0-2 μM. |
| Incubation Time: | 24 hours. |
| Result: | Enhanced autophagosomes formation as indicated by increased expression of LC3-II levels. |
IITZ-01 (45 mg/kg, i.p. every alternate day for 4 weeks) inhibits average breast tumor growth when compared with control from third day of treatment in triple-negative breast tumor models in mice.
| Animal Model: | MDA-MB-231 (TNBC)/green fluorescent protein (GFP) orthotropic breast cancer xenografts were developed in CrTac:NCr-Foxn nu BALB/c female nude mice. |
| Dosage: | 45 mg/kg. |
| Administration: | Intraperitoneal every alternate day for 4 weeks. |
| Result: | Inhibited average breast tumor growth when compared with control from third day of treatment. |
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/04/30 | HY-112897 | IITZ-01 IITZ-01 | 1807988-47-1 | 5mg | 700元 |
| 2024/04/30 | HY-112897 | IITZ-01 IITZ-01 | 1807988-47-1 | 10mM * 1mLin DMSO | 740元 |