化合物 T11896
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- CAS号:
- 2449093-46-1
- 英文名:
- Propanoic acid, 3-[[[4-[2-(7-chloro-4-quinolinyl)ethenyl]phenyl][(2-phenylethyl)thio]methyl]thio]-
- 英文别名:
- Propanoic acid, 3-[[[4-[2-(7-chloro-4-quinolinyl)ethenyl]phenyl][(2-phenylethyl)thio]methyl]thio]-
- 中文名:
- 化合物 T11896
- 中文别名:
- 化合物 T11896
- CBNumber:
- CB88250483
- 分子式:
- C29H26ClNO2S2
- 分子量:
- 520.11
- MOL File:
- 2449093-46-1.mol
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化合物 T11896化学性质
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沸点:
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718.4±60.0 °C(Predicted)
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密度:
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1.317±0.06 g/cm3(Predicted)
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储存条件:
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Store at -20°C
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溶解度:
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DMSO : 135 mg/mL (259.56 mM; Need ultrasonic)
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酸度系数(pKa):
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4.28±0.10(Predicted)
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形态:
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Solid
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颜色:
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Light yellow to yellow
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化合物 T11896性质、用途与生产工艺
LV-320 是一种有效且非竞争性的 ATG4B 抑制剂，其 IC50 值为 24.5 μM，Kd 值为 16 μM。 LV-320 抑制 ATG4B 的酶促活性，阻断细胞自噬，并且在体内稳定，无毒且有活性。
IC50: 24.5 µM (ATG4B); Kd: 16 μM (ATG4B)
LV-320 (0-120 µM; SKBR3, MCF7, JIMT1, and MDA-MB-231 cells) treatment results in a dose-dependent increase in endogenous LC3B-II and protein p62 levels in all four cell lines.
LV-320 (120 µM; 48 hours; MDA-MB-231 cells) treatment results in an increase in LC3B-II, indicating that LV-320 blocks autophagic flux.
Western Blot Analysis
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Cell Line:
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SKBR3, MCF7, JIMT1, and MDA-MB-231 cells
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Concentration:
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0 µM, 25 µM, 50 µM, 75 µM, 100 µM, or 120 µM
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Incubation Time:
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Result:
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Resulted in a dose-dependent increase in endogenous LC3B-II and protein p62 levels in all four cell lines.
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Cell Autophagy Assay
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Cell Line:
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MDA-MB-231 cells
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Concentration:
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120 µM
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Incubation Time:
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48 hours
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Result:
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Blocked autophagic flux.
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LV-320 (100-200 mg/kg; oral gavage; three times over two days; GFP-LC3 mice) treatment results in a terminal blood level of 169 µM and a liver level of 104 µM. The expression of GFP-LC3 puncta is significantly greater accumulation in LV-320 treated animals compared to controls. LC3B-II protein is also increased in LV-320-treated animals. The treatment do not cause significant toxicity in mice at either dose.
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Animal Model:
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GFP-LC3 mice (females, 9-14 weeks)
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Dosage:
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100 mg/kg or 200 mg/kg
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Administration:
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Oral gavage; three times over two days (Pharmacokinetic study)
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Result:
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Terminal blood levels were 169 µM and liver levels were 104 µM. LC3B-II protein level was also increased.
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化合物 T11896
上下游产品信息
上游原料
下游产品
2449093-46-1, 化合物 T11896 相关搜索:
- C29H26ClNO2S2
- 化合物 T11896
- 2449093-46-1
- Propanoic acid, 3-[[[4-[2-(7-chloro-4-quinolinyl)ethenyl]phenyl][(2-phenylethyl)thio]methyl]thio]-