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GANT58
产品纠错
CAS号:64048-12-0 | 英文名称:GANT58
分子式 C24H16N4S
分子量 392
EINECS号 200-258-5
MDL MFCD01103196
Smiles
InChIKey
乙二醇化学百科
基本信息
中文名称 4,44乔,4乔(2,3,4,5-Thiophentetrayl)tetrakis-pyridine
英文名称 2,3,4,5-TETRA-(4-PYRIDYL) THIOPHENE
CAS号 64048-12-0
分子式 C24H16N4S
分子量 392.48
EINECS号 200-258-5
物化性质
熔点 252-253℃
沸点 414.1±40.0 °C(Predicted)
密度 1.254
溶解度 二甲基亚砜:>10mg/mL
形态 黄色固体
酸度系数(pKa) 4.50±0.10(Predicted)
颜色 白色至浅黄色
安全信息
WGK Germany 3
生产及用途
GANT 58 是一种有效的 Gli 拮抗剂,抑制 GLI1 诱导的转录,IC50 为 5 μM。

IC50: 5 μM (Gli)

GANT58 is a downstream inhibitor of Hh signaling. GANT58 is an indeed inhibitor of Hh signaling downstream of Smo and Sufu. GANT58 mainly acts at the nuclear level because transcription induced by GLI1 with a mutated nuclear export signal is still blocked. GANT58 efficiently inhibits in vitro tumor cell proliferation in a GLI-dependent manner and successfully blocks cell growth using human prostate cancer cells harboring downstream activation of the Hh pathway. GANT58 (NSC75503) has been shown to inhibit transcriptional activation by GLI1 (as well as by the other GLI species). GANT58 has been shown to inhibit GLI transactivation.

Nude mice are injected s.c. with GLI1-positive 22Rv1 prostate cancer cells, and tumors are established (median size ≈250 mm 3 ). Nude mice are treated with daily s.c. injections at a concentration of 50 mg/kg of cyclopamine, GANT61, GANT58, or solvent only (n=4-5 for each group). However, after 3 days, cyclopamine-treated animals presented with severe ulcerations at the injection sites. Therefore, changing the treatment regimen to injections only every second day. To be able to compare all compounds, this protocol is also introduced for the GANTs, although mice treated with these compounds showed no such signs of toxicity. All injections are done 2-3 cm away from the tumors. During an 18-day treatment period, suppression of tumor cell growth is observed for all compounds. Treatment with cyclopamine or GANT58 results in the inhibition of additional xenograft growth and limited the increase in tumor size.

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