Rucaparib Camsylate

目录号: GC32793纯度: >99.50%同义词: 瑞卡帕布樟脑磺酸盐,AG014699 camsylate; PF-01367338 camsylate

A PARP1 inhibitor

Cas No.: 1859053-21-6

规格	价格	库存	数量
5mg	¥670.00	现货	1
10mg	¥1,160.00	现货	1
50mg	¥2,700.00	现货	1
100mg	¥4,050.00	现货	1
10mM (in 1mL DMSO)	¥707.00	现货	1

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产品描述 Description

Poly(ADP-ribose) polymerases (PARPs) are activated by DNA single- and double-strand breaks and promote repair of DNA damage through the relaxation of chromatin and recruitment of other repair proteins.^1,2,3 Inhibition of PARP activity has been linked to synthetic lethality in cells with mutations in BRCA1 or BRCA2 and is used as a therapeutic strategy to selectively target cancers.^4,5 Rucaparib is a potent, cell-permeable inhibitor of PARP1 (K_i = <5 nM) that is used in clinical therapy to sensitize cancer cells to chemotherapy.^6,7 Rucaparib inactivates PARP activity in cells with homologous recombination DNA repair pathway mutations at LC₅₀ values ranging from 1.3-5.5 μM.⁷ At 25 mg/kg, rucaparib arrests tumor growth in mice bearing epigenetically silenced BRCA1 UACC3199 xenograft tumors.⁷ It has been shown to increase efficacy of temozolomide in medulloblastoma cells and xenografts.⁶

1.Yuan, Y., Liao, Y.M., Hsueh, C.T., et al.Novel targeted therapeutics: Inhibitors of MDM2, ALK and PARPJ. Hematol. Oncol.4(16)1-14(2011) 2.Javle, M., and Curtin, N.J.The potential for poly (ADP-ribose) polymerase inhibitors in cancer therapyTher. Adv. Med. Oncol.3(6)257-267(2011) 3.Plummer, R.Poly(ADP-ribose) polymerase inhibition: A new direction for BRCA and triple-negative breast cancer?Breast Cancer Res.13(4)1-6(2011) 4.Johnson, N., Li, Y.C., Walton, Z.E., et al.Compromised CDK1 activity sensitizes BRCA-proficient cancers to PARP inhibitionNat. Med.17(7)875-882(2011) 5.Rowe, B.P., and Glazer, P.M.Emergence of rationally designed therapeutic strategies for breast cancer targeting DNA repair mechanismsBreast Cancer Res.12(2)1-11(2010) 6.Daniel, R.A., Rozanska, A.L., Mulligan, E.A., et al.Central nervous system penetration and enhancement of temozolomide activity in childhood medulloblastoma models by poly(ADP-ribose) polymerase inhibitor AG-014699Br. J. Cancer103(10)1588-1596(2010) 7.Drew, Y., Mulligan, E.A., Vong, W.T., et al.Therapeutic potential of poly(ADP-ribose) polymerase inhibitor AG014699 in human cancers with mutated or methylated BRCA1 or BRCA2JNCI103(4)334-346(2011)

实验参考方法 Experimental Reference Method

Kinase experiment:	Inhibition of PARP activity in 5×103 D283Med cells is measured using various concentrations of Rucaparib (0-1 μM), compared with DMSO-only. Maximally stimulated PARP activity is measured in samples of permeabilised cells by immunologica[1].
Cell experiment:	Medulloblastoma cell lines are seeded in 96-well plates at a density of 1×103, 3×103 and 3×103, respectively. At 24 hours (D384Med) or 48 hours (D283Med and D425Med) after seeding, the cells are exposed to various concentrations of temozolomide in the presence or absence of 0.4 μM Rucaparib. After 3 days (D425Med and D384Med) or 5 days (D283Med) of culture, cell viability is evaluated by a XTT cell proliferation kit assay. Cell growth is expressed as a percentage in relation to DMSO or 0.4 μM Rucaparib-alone controls. The concentration of temozolomide, alone or in combination with Rucaparib that inhibited growth by 50% (GI50) is calculated. The potentiation factor 50 (PF50) is defined as the ratio of the GI50 of temozolomide in the presence of Rucaparib to the GI50 of temozolomide alone[1].
Animal experiment:	A single dose of temozolomide is administrated p.o. as a suspension in saline at 200 mg/kg either alone or in combination with a single i.p. administration of PARP inhibitor administered at 0.1 [Rucaparib and MS-AG14644 (equivalent to 0.078 mg/kg free AG14644 only)], 1.0, and 10 mg/kg (for the mesylate salts equivalent to 0.79 and 7.9 mg/kg free AG14451 and AG14452 and 0.78 and 7.8 free AG14531 and AG14644). Control animals are treated with either normal saline p.o. and i.p or normal saline p.o and PARP inhibitor 10 mg/kg i.p[1].
References: [1]. Thomas HD, et al. Preclinical selection of a novel poly(ADP-ribose) polymerase inhibitor for clinical trial. Mol Cancer Ther, 2007, 6(3), 945-956. [2]. Hunter JE, et al. NF-κB mediates radio-sensitization by the PARP-1 inhibitor, AG-014699. Oncogene, 2012, 31(2), 251-264. [3]. Daniel RA, et al. Central nervous system penetration and enhancement of temozolomide activity in childhood medulloblastoma models by poly(ADP-ribose) polymerase inhibitor AG-014699. Br J Cancer, 2010, 103(10), 1588-1596. [4]. Daniel RA, et al. Inhibition of poly(ADP-ribose) polymerase-1 enhances temozolomide and topotecan activity against childhood neuroblastoma. Clin Cancer Res, 2009, 15(4), 1241-1249.

产品文档 Product Documents

Purity:>99.50%

化学性质Chemical Properties

CAS 号

1859053-21-6

同义词

瑞卡帕布樟脑磺酸盐,AG014699 camsylate; PF-01367338 camsylate

SMILES

FC1=CC2=C3C(CCNC2=O)=C(C4=CC=C(CNC)C=C4)NC3=C1.O=S(C[C@@]5(C6(C)C)C(C[C@@]6([H])CC5)=O)(O)=O

分子式

C₂₉H₃₄FN₃O₅S

分子量

555.66 g/mol

溶解性

DMSO : 83.33 mg/mL (149.97 mM)

保存条件

Store at -20°C

General tips

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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
为了提高溶解度，请将管子加热至 37°C，然后在超声波浴中震荡一段时间。

Shipping Condition

评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备 RT，或根据请求配备蓝冰。

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