O6-Benzylguanine|19916-73-5|-陌孚医药/Medlife

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O6-Benzylguanine

目录号: PC15114 纯度: ≥98%

CAS No. :19916-73-5

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PC15114-10mM (in 1mL DMSO)	10mM (in 1mL DMSO)	¥490.00	请登录

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中文名称	O6-Benzylguanine
中文别名	苄基鸟嘌呤;2-氨基-6-(苄氧基)嘌呤;O-6-苄基鸟嘌呤;6-氧苄基鸟嘌呤;2-氨基-6-苄氧基嘌呤;6-苄基鸟嘌呤;O6-苄基鸟嘌呤;氘代十八烷酸(2,2-D2);6-苄氧基鸟嘌呤;6-O-苄基鸟嘌呤;2-氨基-6-苄氧基鸟嘌呤;O-6-苄基鸟嘌呤,MGMT 的抑制剂;O-6-苄基鸟嘌呤,2-氨基-6-(苄氧基)嘌呤;O-6-苄基鸟嘌呤 10G
英文名称	O6-Benzylguanine
英文别名	6-(Benzyloxy)-7H-purin-2-amine;6-Benzyloxy Guanine;2-amino-6-benzyloxypurine;O-6-Benzylguanine;6-o-Benzylguanine;6-phenylmethoxy-7H-purin-2-amine;O6-Benzylguanine;: 6-O-Benzylguanine;2-Amino-6-(benzyloxy)purine;2-amino-6-(phenylmethoxy)-9H-purine;2-Amino-6-benzyloxy-9H-purine;6-(benzyloxy)guanine;6-(phenylmethoxy)-9H-purin-2-amine;amino-6-(phenylmethoxy)-9H-purine;O(6)-Benzylguanine;O(6)-Bgua;NSC 637037;6-benzylguanine;6-oxo -benzylguanine;4 6-Benzyloxyguanine;6-O-Benzylguanine(O6BG);O(sup 6)benzylguanidine;O6-Benzylguanine ,98%
Cas No.	19916-73-5
分子式	C₁₂H₁₁N₅O
分子量	241.25
包装储存	4°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

生物活性

O6-Benzylguanine, a guanine analog, is the DNA repair enzyme O6-alkylguanine-DNA alkyltransferase (MGMT/AGT) inhibitor. O6-Benzylguanine acts as an AGT substrate, which transfers its benzyl group to the AGT cysteine residue, thereby irreversibly inactivating AGT and preventing DNA repair. O6-Benzylguanine induces tumor cell apoptosis. Antineoplastic activity.

性状

Solid

体外研究(In Vitro)

The L3.6pl cells are relatively sensitive to O6-Benzylguanine (24-72 hours) in a dose- and time-dependent manner. The IC₅₀ 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.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

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(In Vivo)

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.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

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.

运输条件

Room temperature or refrigerated transportation.

储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

ClinicalTrial

参考文献

[1]. Rabik CA, Njoku MC, Dolan ME. Inactivation of O6-alkylguanine DNA alkyltransferase as a means to enhance chemotherapy. Cancer Treat Rev. 2006;32(4):261‐276. [Information]

[2]. Konduri, Santhi D et al. Blockade of MGMT expression by O6 benzyl guanine leads to inhibition of pancreatic cancer growth and induction of apoptosis. Clinical cancer research : an official journal of the American Association for Cancer Research vol. 15,19 [Information]

溶解度数据

体外研究:

DMSO : 110 mg/mL (455.96 mM; Need ultrasonic)

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	4.1451 mL	20.7254 mL	41.4508 mL
5 mM	0.8290 mL	4.1451 mL	8.2902 mL
10 mM	0.4145 mL	2.0725 mL	4.1451 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

建议依照次序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.75 mg/mL (11.40 mM); Clear solution

此方案可获得 ≥ 2.75 mg/mL (11.40 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 27.5 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH?O 中，得到澄清透明的生理盐水溶液
2.

建议依照次序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.75 mg/mL (11.40 mM); Clear solution

此方案可获得 ≥ 2.75 mg/mL (11.40 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 27.5 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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