19916-73-5
19916-73-5 結(jié)構(gòu)式
基本信息
O-6-芐基鳥(niǎo)嘌呤
6-芐基鳥(niǎo)嘌呤
2-amino-6-(phenylmethoxy)-9h-purine
6-BENZYLOXY-9H-PURIN-2-AMINE
6-BENZYLOXY GUANINE
6-O-BENZYLGUANINE
O6-BENZYLGUANINE
4 6-Benzyloxyguanine
6-BENZYLOXY GUANINE2-AMINO-6-BENZYLOXYPURINE
O(sup 6)benzylguanidine
2-Amino-6-(benzyloxy)-9H-purine
6-(Benzyloxy)-1H-purin-2-amine
物理化學(xué)性質(zhì)
安全數(shù)據(jù)
常見(jiàn)問(wèn)題列表
O6-Benzylguanine 是鳥(niǎo)嘌呤類似物，是 DNA 修復(fù)酶 O6 烷基鳥(niǎo)嘌呤DNA烷基轉(zhuǎn)移酶 (MGMT/AGT) 抑制劑。
| Target | Value |
|
AGT
() |
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. |
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. |