2. Cell Cycle/DNA Damage Epigenetics
  3. PARP
  4. Rucaparib hydrochloride

Rucaparib hydrochloride  (Synonyms: AG014699 hydrochloride; PF-01367338 hydrochloride)

目录号: HY-10617B
产品使用指南

摩尔计算器

Rucaparib (AG014699) hydrochloride 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 Ki 为 1.4 nM。Rucaparib hydrochloride 是六磷酸己糖脱氢酶 (H6PD) 抑制剂。Rucaparib hydrochloride 具有用于去势抵抗性前列腺癌 (CRPC) 研究的潜力。

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Rucaparib hydrochloride Chemical Structure

Rucaparib hydrochloride Chemical Structure

CAS No. : 773059-19-1

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Rucaparib hydrochloride 的其他形式现货产品:

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Other Forms of Rucaparib hydrochloride:

Rucaparib hydrochloride 相关抗体

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PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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

IC50 & Target

PARP-1

1.4 nM (Ki)

PARP-2

 

PARP-3

 

体外研究
(In Vitro)

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 LC50 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].

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

Rucaparib hydrochloride 相关抗体:
体内研究
(In Vivo)

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].

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

Animal Model: Female athymic nude mice, implanted SW620 colorectal tumor cells (1 × 107 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.
Clinical Trial
分子量

359.83

Formula

C19H19ClFN3O
CAS 号
中文名称

瑞卡帕布盐酸盐；鲁卡帕尼盐酸盐
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

Rucaparib hydrochloride 相关分类

  • 摩尔计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Rucaparib773059-19-1AG014699PF-01367338瑞卡帕布盐酸盐鲁卡帕尼盐酸盐AG 014699AG-014699PF01367338PF 01367338PARPpoly ADP ribose polymeraseorallyPARP-1PARP-2PARP-3hexose-6-phosphate dehydrogenaseH6PDcastration-resistant prostate cancerCRPCInhibitorinhibitorinhibit

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