Rucaparib monocamsylate 瑞卡帕布樟脑磺酸盐; AG014699 monocamsylate; PF-01367338 monocamsylate|cas:1859053-21-6|西域试剂

Rucaparib monocamsylate 瑞卡帕布樟脑磺酸盐; AG014699 monocamsylate; PF-01367338 monocamsylate,99.82%

产品编号：Bellancom-102003| CAS NO：1859053-21-6| 分子式：C₂₉H₃₄FN₃O₅S| 分子量：555.66

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货号	价格	库存与货期
Bellancom-102003	￥700.00	杭州北京（现货）
Bellancom-102003	￥1200.00	杭州北京（现货）
Bellancom-102003	￥3000.00	杭州北京（现货）
Bellancom-102003	￥4500.00	杭州北京（现货）

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Rucaparib monocamsylate 瑞卡帕布樟脑磺酸盐; AG014699 monocamsylate; PF-01367338 monocamsylate

产品介绍

Rucaparib (AG014699) monocamsylate 是一种口服有效的 PARP 蛋白 (PARP-1, PARP-2 and PARP-3) 抑制剂，对 PARP-1 的 K_i 为 1.4 nM。Rucaparib monocamsylate 是六磷酸己糖脱氢酶 (H6PD) 抑制剂。Rucaparib monocamsylate 具有用于去势抵抗性前列腺癌 (CRPC) 研究的潜力。

生物活性

Rucaparib (AG014699) monocamsylate is an orally active, potent inhibitor of PARP proteins (PARP-1, PARP-2 and PARP-3) with a K_i of 1.4 nM for PARP1. Rucaparib monocamsylate is a modest hexose-6-phosphate dehydrogenase (H6PD) inhibitor. Rucaparib monocamsylate has the potential for castration-resistant prostate cancer (CRPC) research^[4].

体外研究

Rucaparib (AG014699) monocamsylate is a possible N-demethylation metabolite of AG14644.
Rucaparib (0.1, 1, 10, 100 μM; 24 hours) monocamsylate is cytotoxic and has the LC₅₀ being 5 μM in Capan-1 (BRCA2 mutant) cells and only 100 nM in MX-1 (BRCA1 mutant) cells.
The radio-sensitization by Rucaparib monocamsylate is due to downstream inhibition of activation of NF-κB, and is independent of SSB repair inhibition. Rucaparib monocamsylate can target NF-κB activated by DNA damage and overcome toxicity observed with classical NF-κB inhibitors without compromising other vital inflammatory functions^[5].
Rucaparib monocamsylate inhibits PARP-1 activity by 97.1% at a concentration of 1 μM in permeabilised D283Med cells^[6].

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

体内研究

Rucaparib (AG014699) monocamsylate and AG14584 significantly increase Temozolomide toxicity. Rucaparib (1 mg/kg) monocamsylate significantly increases Temozolomide-induced body weight loss. Rucaparib (0.1 mg/kg) monocamsylate results in a 50% increase in the temozolomide-induced tumor growth delay.
Rucaparib (10 mg/kg for i.p. or 50, 150 mg/kg for p.o.; daily for 5 days per week for 6 weeks) monocamsylate significantly inhibits the growth of the tumor, and there is one complete tumor regression and two persistent partial regressions.
Rucaparib (150 mg/kg; p.o.; once per week for 6 weeks or three times per week for 6 weeks) monocamsylate has greatest antitumor effect with three complete regressions.
Rucaparib monocamsylate enhances the antitumor activity of temozolomide and indicates complete and sustained tumor regression in NB1691 and SHSY5Y xenografts^[6].

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

Animal Model:	Female CD-1 nude mice aged 10-12 weeks with Capan-1 cells
Dosage:	10 mg/kg or 50, 150 mg/kg
Administration:	10 mg/kg for i.p. or 50, 150 mg/kg for p.o.
Result:	Significantly inhibited the growth of the tumor.

体内研究

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

Animal Model:	Female CD-1 nude mice aged 10-12 weeks with Capan-1 cells
Dosage:	10 mg/kg or 50, 150 mg/kg
Administration:	10 mg/kg for i.p. or 50, 150 mg/kg for p.o.
Result:	Significantly inhibited the growth of the tumor.

性状

Solid

溶解性数据

In Vitro:

DMSO : 83.33 mg/mL (149.97 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.7997 mL	8.9983 mL	17.9966 mL
5 mM	0.3599 mL	1.7997 mL	3.5993 mL
10 mM	0.1800 mL	0.8998 mL	1.7997 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，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 (sealed storage, away from moisture)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 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.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (3.74 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.74 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 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 ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (3.74 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.74 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (3.74 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.74 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 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。