化合物 Rucaparib hydrochloride,Rucaparib hydrochloride

化合物 Rucaparib hydrochloride|T61335|TargetMol

价格	￥24625	￥19420	￥14900
包装	100mg	50mg	25mg

最小起订量	1mg
发货地	上海
更新日期	2024-09-29

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产品详情

中文名称:化合物 Rucaparib hydrochloride	英文名称:Rucaparib hydrochloride
CAS:773059-19-1	品牌: TargetMol
产地: 美国	保存条件: Shipping with blue ice.
产品类别: 抑制剂
货号: T61335

Product Introduction

Bioactivity

名称	Rucaparib hydrochloride
描述	Rucaparib hydrochloride, also known as AG014699, is a powerful and orally active compound that inhibits PARP proteins including PARP-1, PARP-2, and PARP-3 with a Ki value of 1.4 nM for PARP1. Additionally, Rucaparib hydrochloride acts as a modest inhibitor of hexose-6-phosphate dehydrogenase (H6PD). This compound shows potential in research for castration-resistant prostate cancer (CRPC) [1] [2] [3] [4].
体外活性	Rucaparib (AG014699) hydrochloride is a possible N-demethylation metabolite of AG14644 [1]. Rucaparib (0.1, 1, 10, 100 μM; 24 hours) hydrochloride is cytotoxic and has the LC 50 being 5 μM in Capan-1 (BRCA2 mutant) cells and only 100 nM in MX-1 (BRCA1 mutant) cells [2]. The radio-sensitization by Rucaparib hydrochloride is due to downstream inhibition of activation of NF-κB, and is independent of SSB repair inhibition. Rucaparib hydrochloride 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 hydrochloride inhibits PARP-1 activity by 97.1% at a concentration of 1 μM in permeabilised D283Med cells [6].
体内活性	Rucaparib (AG014699) hydrochloride and AG14584 significantly increase Temozolomide toxicity. Rucaparib (1 mg/kg) hydrochloride significantly increases Temozolomide-induced body weight loss. Rucaparib (0.1 mg/kg) hydrochloride results in a 50% increase in the temozolomide-induced tumor growth delay [1]. Rucaparib (10 mg/kg for i.p. or 50, 150 mg/kg for p.o.; daily for 5 days per week for 6 weeks) hydrochloride significantly inhibits the growth of the tumor, and there is one complete tumor regression and two persistent partial regressions [2]. Rucaparib (150 mg/kg; p.o.; once per week for 6 weeks or three times per week for 6 weeks) hydrochloride has greatest antitumor effect with three complete regressions [2]. Rucaparib (1 mg/kg; i.p.; daily for 5d) hydrochloride enhances the antitumor activity of temozolomide and indicates complete and sustained tumor regression in NB1691 and SHSY5Y xenografts [6]. Animal Model: Female athymic nude mice, implanted SW620 colorectal tumor cells (1 × 10 7 cells per animal) s.c. [1] Dosage: 0.1 mg/kg in combination with Temozolomide (p.o., 200 mg/kg), 0.05, 0.15, and 0.5 mg/kg in combination with Temozolomide (p.o., 68 mg/kg) or 10 mg/kg Administration: IP, single dose for 0.1 mg/kg and 10 mg/kg, five daily doses for 0-0.5 mg/kg Result: Significantly increased Temozolomide toxicity, showed outstanding chemosensitization potency and caused enhancement of Temozolomide-induced tumor growth delay. Animal Model: CD-1 nude mice bearing established Capan-1 xenografts [2] Dosage: 10 mg/kg or 50, 100 and 150 mg/kg Administration: IP for 10 mg/kg; PO for 50, 100 and 150 mg/kg, single dose (Pharmacokinetics) Result: Parent drug was detectable in the plasma only at 30 min after 10 mg/kg i.p and up to 4 h for 50–150 mg/kg p.o.. Was still detectable in most mice receiving oral rucaparib at 3 days. Does not easily cross the plasma membrane. Animal Model: CD-1 nude mice bearing established Capan-1 xenografts [2] Dosage: 10 mg/kg i.p. daily for 5 days per week for 6 weeks, 50 or 150 mg/kg p.o. daily × five weekly × six, 150 mg/kg p.o. once per week for 6 weeks or three times per week for 6 weeks, or 150 mg/kg p.o. daily for five days every 3 weeks Administration: IP or PO Result: 10 mg/kg i.p. significantly inhibited the growth of the tumor, daily oral administration at 150 mg/kg had an equivalent effect on tumor growth to 10 mg/kg i.p.. The schedule with the greatest antitumor effect was oral administration of 150 mg/kg on a once weekly schedule with three complete regressions. Animal Model: CD-1 nude mice, NB1691 and SHSY5Y xenografts [6] Dosage: 1 mg/kg Administration: IP, daily for 5 d in combination with Temozolomide (orally daily ×5 at a dose of 68 mg/kg) Result: Enhanced the antitumor activity of Temozolomide and indicated complete and sustained tumor regression.
存储条件	Shipping with blue ice.

关键字： Rucaparib hydrochloride|TargetMol

公司简介

TargetMol Chemicals Inc. 总部位于马萨诸塞州波士顿，致力于为全球生化领域科学家的研究提供专业的产品和服务。TargetMol?品牌的客户群分布于40多个国家和地区，已发展成为全球知名的化合物库和小分子化合物研究供应商。 TargetMol?可提供160多种满足不同需求的化合物库，以及多种类型的生化试剂产品，包括12000多种抑制剂、16000多种天然产物和各类多肽、抗体、生命科学试剂盒等，此外，我们还建设有CADD（计算机辅助药物设计）研究中心、药理实验室、药化合成平台三大技术中心，全方位满足客户的定制需求。凭借我们优质的产品和服务、快速高效的全球供应链和专业的技术支持，我们将有效帮助您缩短研发周期，取得更成功的结果。

成立日期	2013-04-18 （12年）	注册资本	566.265100万人民币
员工人数	100-500人	年营业额	￥ 1亿以上
主营行业	天然产物,生化试剂,分子生物学,分子砌块,生物技术服务	经营模式	贸易,工厂,试剂,定制,服务

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公司成立：12年
注册资本：566.265100万人民币
企业类型：有限责任公司(自然人投资或控股)
主营产品：小分子抑制剂、药物筛选化合物库、药物筛选等
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Rucaparib phosphate; AG014699; PF01367388	询价	VIP9年	上海芮晖化工科技有限公司	2024-11-08
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