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中文名称:

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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

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

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

沸点 

747.0±70.0 °C(Predicted)

密度 

1.420±0.06 g/cm3(Predicted)

储存条件 

Keep in dark place,Inert atmosphere,2-8°C

酸度系数(pKa)

11.55±0.10(Predicted)

生物活性

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。

靶点

PI3Kγ 2.62 μM (IC 50 ) Autophagy

PI3Kγ 2.62 μM (IC 50 )

Autophagy

体外研究

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.

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.

体内研究

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.

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.