O-6-苄基鸟嘌呤

简介药理活性靶点体外研究体内研究 O-6-苄基鸟嘌呤试剂级价格

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

O-6-苄基鸟嘌呤化学性质

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)

安全信息

危险品标志 :Xi
危险类别码 :36/37/38
安全说明 :26-36
WGK Germany :3
Hazard Note :Irritant
海关编码 :29339900

O-6-苄基鸟嘌呤性质、用途与生产工艺

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。
靶点
Target Value
AGT
()

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.