产品
编 号：F755914
分子式：C36H34N8O8
分子量：706.7
分子式：C36H34N8O8
分子量：706.7
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CAS No: 2770263-77-7
产品详情
生物活性：
SZUH280 is a potent and selective PROTAC HDAC8 degrader with a DC50 of 0.58 μM in A549 cells. SZUH280 induces cancer cell apoptosis. SZUH280 hampers DNA damage repair in cancer cells, promoting cellular radiosensitization.
体内研究：
SZUH280 (5 mg/kg; i.p.; every 5 days for 6 weeks) shows antitumor activity in an A549 nude mouse model.Animal Model:NOD/SCID mice (severe combined immunodeficient mice), A549 model
Dosage:5 mg/kg
Administration:Intraperitoneal injection, every 5 days for 6 weeks
Result:Exhibited a significantly greater anti-lung cancer activity in vivo than the control group. When in combination with 3 Gy irradiation, achieved a much stronger antitumor activity.
体外研究：
HDAC8 degradation induced by SZUH280 (5 μM; 20 h) is mediated by the CRBN E3 ubiquitin ligase.SZUH280 (0.1-10 μM; 20 h) can regulate the oncogenic protein expression and suppress cancer metastasis, potentially improving the efficacy of chemotherapy in various types of cancers.SZUH280 (0-20 μM; 72 h) inhibits A549 cell proliferation in a concentration-dependent manner and shows stronger antiproliferative effect with irradiation.SZUH280 (0-20 μM; 72 h) induces apoptosis and arrests cell cycle at G2/M phase in A549 cells.SZUH280 (5 μM; 24 h) hampers DNA damage repair in cancer cells when in combination with irradiation.
SZUH280 is a potent and selective PROTAC HDAC8 degrader with a DC50 of 0.58 μM in A549 cells. SZUH280 induces cancer cell apoptosis. SZUH280 hampers DNA damage repair in cancer cells, promoting cellular radiosensitization.
体内研究：
SZUH280 (5 mg/kg; i.p.; every 5 days for 6 weeks) shows antitumor activity in an A549 nude mouse model.Animal Model:NOD/SCID mice (severe combined immunodeficient mice), A549 model
Dosage:5 mg/kg
Administration:Intraperitoneal injection, every 5 days for 6 weeks
Result:Exhibited a significantly greater anti-lung cancer activity in vivo than the control group. When in combination with 3 Gy irradiation, achieved a much stronger antitumor activity.
体外研究：
HDAC8 degradation induced by SZUH280 (5 μM; 20 h) is mediated by the CRBN E3 ubiquitin ligase.SZUH280 (0.1-10 μM; 20 h) can regulate the oncogenic protein expression and suppress cancer metastasis, potentially improving the efficacy of chemotherapy in various types of cancers.SZUH280 (0-20 μM; 72 h) inhibits A549 cell proliferation in a concentration-dependent manner and shows stronger antiproliferative effect with irradiation.SZUH280 (0-20 μM; 72 h) induces apoptosis and arrests cell cycle at G2/M phase in A549 cells.SZUH280 (5 μM; 24 h) hampers DNA damage repair in cancer cells when in combination with irradiation.
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