O6-Benzylguanine
O6-Benzylguanine structure
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Common Name | O6-Benzylguanine | ||
|---|---|---|---|---|
| CAS Number | 19916-73-5 | Molecular Weight | 241.249 | |
| Density | 1.4±0.1 g/cm3 | Boiling Point | 621.4±63.0 °C at 760 mmHg | |
| Molecular Formula | C12H11N5O | Melting Point | 193(dec.) | |
| MSDS | Chinese USA | Flash Point | 329.6±33.7 °C | |
| Symbol |
GHS07 |
Signal Word | Warning | |
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Differential expression of miR200a-3p and miR21 in grade II-III and grade IV gliomas: evidence that miR200a-3p is regulated by O⁶-methylguanine methyltransferase and promotes temozolomide responsiveness.
Cancer Biol. Ther. 15(7) , 938-50, (2014) Glioblastoma multiforme (GBM) is the most common primary brain tumor and is among the deadliest of human cancers. Dysregulation of microRNAs (miRNAs) expression is an important step in tumor progression as miRNAs can act as tumor suppressors or oncogenes and ... |
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Formation and repair of pyridyloxobutyl DNA adducts and their relationship to tumor yield in A/J mice.
Chem. Res. Toxicol. 25(10) , 2167-78, (2012) The nitrosamine 4-(methylnitrosamino)-1-(3-pyridyl)-1-butanone (NNK) is a known human carcinogen. It generates methyl and pyridyloxobutyl DNA adducts. The role of the methyl DNA adducts has been well-established in the tumorigenic properties of NNK. However, ... |
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Evaluation of novel imidazotetrazine analogues designed to overcome temozolomide resistance and glioblastoma regrowth.
Mol. Cancer Ther. 14(1) , 111-9, (2015) The cellular responses to two new temozolomide (TMZ) analogues, DP68 and DP86, acting against glioblastoma multiforme (GBM) cell lines and primary culture models are reported. Dose-response analysis of cultured GBM cells revealed that DP68 is more potent than... |
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4-nitrobenzyloxycarbonyl derivatives of O(6)-benzylguanine as hypoxia-activated prodrug inhibitors of O(6)-alkylguanine-DNA alkyltransferase (AGT), which produces resistance to agents targeting the O-6 position of DNA guanine.
J. Med. Chem. 54(21) , 7720-8, (2011) A series of 4-nitrobenzyloxycarbonyl prodrug derivatives of O(6)-benzylguanine (O(6)-BG), conceived as prodrugs of O(6)-BG, an inhibitor of the resistance protein O(6)-alkylguanine-DNA alkyltransferase (AGT), were synthesized and evaluated for their ability t... |
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Phase I clinical trial of O6-benzylguanine and topical carmustine in the treatment of cutaneous T-cell lymphoma, mycosis fungoides type.
Arch. Dermatol. 148(5) , 613-20, (2012) To evaluate the toxic effects and maximum tolerated dose of topical carmustine [1,3-bis(2-chloroethyl)-1-nitrosourea] following intravenous O6-benzylguanine in the treatment of cutaneous T-cell lymphoma (CTCL), and to determine pharmacodynamics of O6-alkylgua... |
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MGMT inhibition restores ERα functional sensitivity to antiestrogen therapy.
Mol. Med. 18 , 913-29, (2012) Antiestrogen therapy resistance remains a huge stumbling block in the treatment of breast cancer. We have found significant elevation of O(6) methylguanine DNA methyl transferase (MGMT) expression in a small sample of consecutive patients who have failed tamo... |
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Blockade of MGMT expression by O6 benzyl guanine leads to inhibition of pancreatic cancer growth and induction of apoptosis.
Clin. Cancer Res. 15(19) , 6087-95, (2009) We sought to determine whether administration of a MGMT blocker, O(6)-benzyl guanine (O(6)BG), at an optimal biological dose alone or in combination with gemcitabine inhibits human pancreatic cancer cell growth.Human pancreatic cancer L3.6pl and PANC1 cells w... |
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Humanized bone marrow mouse model as a preclinical tool to assess therapy-mediated hematotoxicity.
Clin. Cancer Res. 17(8) , 2195-206, (2011) Preclinical in vivo studies can help guide the selection of agents and regimens for clinical testing. However, one of the challenges in screening anticancer therapies is the assessment of off-target human toxicity. There is a need for in vivo models that can ... |
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Pharmacokinetics of temozolomide administered in combination with O6-benzylguanine in children and adolescents with refractory solid tumors.
Cancer Chemother. Pharmacol. 65(1) , 137-42, (2009) Temozolomide pharmacokinetics were evaluated in children receiving concurrent O(6)-benzylguanine (O(6)BG), which enhanced the hematological toxicity of temozolomide.Temozolomide was administered orally, daily for 5 days starting at 28 mg/m(2) per day with esc... |
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A phase II study of O6-benzylguanine and temozolomide in pediatric patients with recurrent or progressive high-grade gliomas and brainstem gliomas: a Pediatric Brain Tumor Consortium study.
J. Neurooncol. 106(3) , 643-9, (2012) To estimate the sustained (≥8 weeks) objective response rate in pediatric patients with recurrent or progressive high-grade gliomas (HGG, Stratum A) or brainstem gliomas (BSG, Stratum B) treated with the combination of O6-benzylguanine (O6BG) and temozolomide... |