IITZ-01

生物活性靶点体外研究体内研究 IITZ-01 试剂级价格

IITZ-01

CAS号:1807988-47-1
英文名:IITZ-01
中文名:IITZ-01
CBNumber:CB04668033
分子式:C26H23FN8O
分子量:482.51
MOL File:1807988-47-1.mol

IITZ-01化学性质

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(Max Conc. mg/mL);207.24(Max Conc. mM)
酸度系数(pKa) :11.55±0.10(Predicted)
形态 :Solid
颜色 :White to off-white

IITZ-01性质、用途与生产工艺

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

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.

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.