4,44喬,4喬(2,3,4,5-Thiophentetrayl)tetrakis-pyridine
中文名稱 | 4,44喬,4喬(2,3,4,5-Thiophentetrayl)tetrakis-pyridine |
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中文同義詞 | 4,4?4喬,4喬?(2,3,4,5-Thiophentetrayl)tetrakis-pyridine;2,3,4,5-四(4-吡啶基)噻吩;2,3,4,5-四-(4-吡啶)噻吩;2,3,4,5-四(4-吡啶基)噻吩(GANT58);化合物 GANT 58;GANT58,HH SIGNALING抑制劑;化合物GANT 58,10 MM DMSO 溶液 |
英文名稱 | 2,3,4,5-TETRA-(4-PYRIDYL) THIOPHENE |
英文同義詞 | ¥-(2,3,4,5-Thiophentetrayl)tetrakis-pyridine;,4¥4,4¥Nsc75503;Pyridine, 4,4',4'',4'''-(2,3,4,5-thiophenetetrayl)tetrakis-;GANT58;1,2,3,4-Tetrakis(4-pyridyl)thiophene |
CAS號(hào) | 64048-12-0 |
分子式 | C24H16N4S |
分子量 | 392.48 |
EINECS號(hào) | 200-258-5 |
相關(guān)類別 | 噻吩類衍生物;有機(jī)化合物 |
Mol文件 | 64048-12-0.mol |
結(jié)構(gòu)式 | ![]() |
4,44喬,4喬(2,3,4,5-Thiophentetrayl)tetrakis-pyridine 性質(zhì)
熔點(diǎn) | 252-253℃ |
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沸點(diǎn) | 414.1±40.0 °C(Predicted) |
密度 | 1.254 |
儲(chǔ)存條件 | Keep in dark place,Sealed in dry,2-8°C |
溶解度 | 二甲基亞砜:>10mg/mL |
形態(tài) | 黃色固體 |
酸度系數(shù)(pKa) | 4.50±0.10(Predicted) |
顏色 | 白色至淺黃色 |
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.
安全信息
WGK Germany | 3 |
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更新日期 | 產(chǎn)品編號(hào) | 產(chǎn)品名稱 | CAS號(hào) | 包裝 | 價(jià)格 |
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2025/05/22 | HY-13282 | 4,44喬,4喬(2,3,4,5-Thiophentetrayl)tetrakis-pyridine GANT 58 | 64048-12-0 | 5mg | 512元 |
2025/05/22 | HY-13282 | 4,44喬,4喬(2,3,4,5-Thiophentetrayl)tetrakis-pyridine GANT 58 | 64048-12-0 | 10mM * 1mLin DMSO | 563元 |