IITZ-01
| 中文名稱 | IITZ-01 |
|---|---|
| 中文同義詞 | N2-(4-(1H-苯并[D]咪唑-2-基)苯基)-N4-(4-氟苯基)-6-嗎啉代-1,3,5-三嗪-2,4-二胺;化合物IITZ-01;化合物IITZ-01,10 MM DMSO 溶液;IITZ-01 ,S8764 |
| 英文名稱 | IITZ-01 |
| 英文同義詞 | 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號 | 1807988-47-1 |
| 分子式 | C26H23FN8O |
| 分子量 | 482.51 |
| EINECS號 | |
| 相關(guān)類別 | API |
| Mol文件 | 1807988-47-1.mol |
| 結(jié)構(gòu)式 |  |
IITZ-01 性質(zhì)
| 沸點(diǎn) | 747.0±70.0 °C(Predicted) |
|---|---|
| 密度 | 1.420±0.06 g/cm3(Predicted) |
| 儲存條件 | under inert gas (nitrogen or Argon) at 2–8 °C |
| 溶解度 | DMSO:100.0(最大濃度 mg/mL);207.24(最大濃度 mM) |
| 酸度系數(shù)(pKa) | 11.55±0.10(Predicted) |
| 形態(tài) | 固體 |
| 顏色 | 白色至米白色 |
| InChIKey | XGEDDGLPNSLBFE-UHFFFAOYSA-N |
| SMILES | Fc1ccc(cc1)Nc2nc(nc(n2)Nc4ccc(cc4)c5[nH]c6c(n5)cccc6)N3CCOCC3 |
IITZ-01 是一個具有抗腫瘤活性的、有效的親溶酶體的自噬抑制劑，其對 PI3Kγ 的 IC50 值為 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
| WGK Germany | WGK 3 |
|---|---|
| 存儲類別 | 11 - 可燃固體 |
| 更新日期 | 產(chǎn)品編號 | 產(chǎn)品名稱 | CAS號 | 包裝 | 價格 |
|---|---|---|---|---|---|
| 2026/06/05 | HY-112897 | IITZ-01 IITZ-01 | 1807988-47-1 | 5mg | 433元 |
| 2026/06/05 | HY-112897 | IITZ-01 IITZ-01 | 1807988-47-1 | 10mM * 1mLin DMSO | 460元 |