O-6-苄基鸟嘌呤
- CAS号:19916-73-5
- 英文名:6-O-Benzylguanine
- 中文名:O-6-苄基鸟嘌呤
- CBNumber:CB9263934
- 分子式:C12H11N5O
- 分子量:241.25
- MOL File:19916-73-5.mol
- 熔点 :193(dec.)
- 沸点 :459.3±55.0 °C(Predicted)
- 密度 :1.48±0.1 g/cm3(Predicted)
- 储存条件 :room temp
- 溶解度 :methanol: 20 mg/mL
- 形态 :solid
- 酸度系数(pKa) :7.47±0.20(Predicted)
- 颜色 :Off-White to Light Yellow
- CAS 数据库 :19916-73-5(CAS DataBase Reference)
O-6-苄基鸟嘌呤性质、用途与生产工艺
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简介
O6-Benzylguanine 是鸟嘌呤类似物，是 DNA 修复酶 O6 烷基鸟嘌呤DNA烷基转移酶 (MGMT/AGT) 抑制剂。
- 药理活性 O6-Benzylguanine 作为 AGT 底物，将其苄基转移到 AGT 半胱氨酸残基上，从而不可逆地灭活 AGT 并阻止 DNA 修复。O6-Benzylguanine 诱导肿瘤细胞凋亡，具有抗肿瘤活性。
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靶点
Target Value AGT
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体外研究
The L3.6pl cells are relatively sensitive to O6-Benzylguanine (24-72 hours) in a dose- and time-dependent manner. The IC 50 is 50 μg (at 48 hours).
O6-Benzylguanine (50 μg; 48 hours) modulates p53 downstream target protein expression, induces apoptosis, and decreases cell proliferation.
O6-Benzylguanine (50 μg; 48 hours) significantly decreases the MGMT transcriptional activity in L3.6pl.Western Blot Analysis
Cell Line: L3.6pl and PANC1 cells Concentration: 50 μg Incubation Time: 48 hours Result: Expressions of O6 methyl guanine DNA methyl transferase (MGMT), cyclin B1, cyclin B2, cyclin A, p53, and ki-67 were decreased, whereas p21 was increased. The levels of cyto C and caspase 9 were increased, whereas the levels of PARP1 protein were decreased. RT-PCR
Cell Line: L3.6pl cells Concentration: 50 μg Incubation Time: 48 hours Result: Decreased the MGMT transcriptional activity in L3.6pl. -
体内研究
O6-Benzylguanine (100 μg; i.p.; daily for 35 days) inhibits pancreatic cancer cell growth and increases pancreatic cell sensitivity to Gemcitabine (100 mg/kg).
O6-Benzylguanine inhibits pancreatic cancer cell proliferation and induces tumor cell apoptosis in vivo.Animal Model: Male athymic nude mice (NCI-nu) (bearing human pancreatic cancer L3.6pl cells) Dosage: 100 μg Administration: i.p; daily for 35 days Result: Significantly decreased median tumor volume and weight. - 用途 用于各种DNA修复机制研究。
- 更新日期：2024/11/11
- 产品编号：XW199167352
- 产品名称：O-6-苄基鸟嘌呤
- CAS编号：19916-73-5
- 包装：500MG
- 价格：32元
- 更新日期：2024/11/08
- 产品编号：H60274
- 产品名称：O6-苄基鸟嘌呤, 98% O6-Benzylguanine, 98%
- CAS编号：19916-73-5
- 包装：250mg
- 价格：418元
- 公司名称：CAYMAN PHARMA SRO
- 联系电话：--
- 电子邮件：sales@caymanpharma.com
- 国家：捷克共和国
- 产品数：8
- 优势度：58
