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RH1 (NSC 697726) Sale

(Synonyms: 2,5-二(1-氮丙啶基)-3-(羟甲基)-6-甲基-2,5-环己二烯-1,4-二酮,NSC 697726) 目录号 : GC33393

RH1 (NSC 697726) (NSC 697726) 是一种有效的生物还原剂,具有显着的体外和体内抗癌活性。

RH1 (NSC 697726) Chemical Structure

Cas No.:221635-42-3

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1mg
¥1,782.00
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5mg
¥3,915.00
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10mg
¥6,300.00
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Sample solution is provided at 25 µL, 10mM.

Description

RH1 (NSC 697726) is a potent bioreductive agent with profound anti-cancer activity in vitro and in vivo.

Treatment of NQ16 cells with RH1 (50 and 100 nM) for 60 and 120 min results in a significant increase (p< 0.05) in cross-linked DNA. RH1 induces apoptosis in a time- and concentration-dependent manner in NQ16 cells [1].

RH1 exhibits antitumor activity in a dose-dependent manner against NQ16 tumors growing in athymic mice. RH1 treatment (0.4 mg/kg and 0.2 mg/kg) of mice bearing NQ16 tumors results in a significant reduction in tumor volume between treated groups and controls as early as 5 days after the treatment period ended. Low-dose RH1 (0.1 mg/kg) also results in a significant reduction in tumor volume between treated mice and controls[2].

[1]. Park MT, et al. The anti-tumour compound, RH1, causes mitochondria-mediated apoptosis by activating c-Jun N-terminal kinase. Br J Pharmacol. 2011 Jun;163(3):567-85. [2]. Dehn DL, et al. Development of a new isogenic cell-xenograft system for evaluation of NAD(P)H:quinone oxidoreductase-directed antitumor quinones: evaluation of the activity of RH1. Clin Cancer Res. 2004 May 1;10(9):3147-55.

实验参考方法

Cell experiment:

MDA468 and NQ16 cells are treated with RH1 at 50, 100, and 500 nM or 10, 50, and 100 nM, respectively, in unsupplemented media for 30, 60, or 120 min, after which the dosing medium is aspirated, rinsed with PBS, and then harvested[1].

Animal experiment:

Mice[2]Female athymic nude mice bearing bilateral tumors are randomized into a control and three drug-treatment groups of seven to eight animals per cell line. RH1 (0.1 mg/kg, 0.2 mg/kg, or 0.4 mg/kg) is injected into mice daily for five consecutive days (every day for 5 days)[2].

References:

[1]. Park MT, et al. The anti-tumour compound, RH1, causes mitochondria-mediated apoptosis by activating c-Jun N-terminal kinase. Br J Pharmacol. 2011 Jun;163(3):567-85.
[2]. Dehn DL, et al. Development of a new isogenic cell-xenograft system for evaluation of NAD(P)H:quinone oxidoreductase-directed antitumor quinones: evaluation of the activity of RH1. Clin Cancer Res. 2004 May 1;10(9):3147-55.

化学性质

Cas No. 221635-42-3 SDF
别名 2,5-二(1-氮丙啶基)-3-(羟甲基)-6-甲基-2,5-环己二烯-1,4-二酮,NSC 697726
Canonical SMILES O=C1C(N2CC2)=C(CO)C(C(N3CC3)=C1C)=O
分子式 C12H14N2O3 分子量 234.25
溶解度 Soluble in DMSO 储存条件 Store at -20°C
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溶解性数据

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1 mg 5 mg 10 mg
1 mM 4.2689 mL 21.3447 mL 42.6894 mL
5 mM 0.8538 mL 4.2689 mL 8.5379 mL
10 mM 0.4269 mL 2.1345 mL 4.2689 mL
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