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Rucaparib phosphate

CAS No. : 459868-92-9

MCE 站：Rucaparib phosphate

产品活性：Rucaparib phosphate (AG-014699 phosphate) 是一种具有口服活性的、有效的 PARP 抑制剂，结合 PARP1 的 K_i 为 1.4 nM，对其他八种 PARP 结构域也有亲和性。

研究领域：Cell Cycle/DNA Damage  |  Epigenetics

作用靶点：PARP

In Vitro: Rucaparib is the most potent PARP inhibitor in enzyme assays (K_i, 1.4 nM), and a possible?N-demethylation metabolite of AG14644. The radio-sensitization by Rucaparib is due to downstream inhibition of activation of NF-κB, and is independent of SSB repair inhibition. Rucaparib could target NF-κB activated by DNA damage and overcome toxicity observed with classical NF-κB inhibitors without compromising other vital inflammatory functions. Rucaparib inhibits PARP-1 activity by 97.1% at a concentration of 1 μM in permeabilised D283Med cells.

In Vivo: Rucaparib and AG14584 significantly (P < 0.05) increases temozolomide toxicity. Rucaparib (1 mg/kg) significantly increases temozolomide-induced body weight loss.?Rucaparib (0.1 mg/kg) results in a 50% increase in the temozolomide-induced tumor growth delay. Rucaparib is not toxic but significantly enhances temozolomide-induced TGD in the DNA repair protein-competent D384Med xenografts. Pharmacokinetics studies also show that Rucaparib is detected in the brain tissue, which indicates that Rucaparib has potential in intra-cranial malignancy therapy. Rucaparib significantly potentiates the cytotoxicity of topotecan and temozolomide in NB-1691, SH-SY-5Y, and SKNBE (2c) cells. Rucaparib enhances the antitumor activity of temozolomide and indicates complete and sustained tumor regression in NB1691 and SHSY5Y xenografts.

相关产品：Drug Repurposing Compound Library Plus  |  FDA-Approved Drug Library Plus  |  FDA-Approved Drug Library Mini  |  Bioactive Compound Library Plus  |  Cell Cycle/DNA Damage Compound Library  |  Epigenetics Compound Library  |  FDA-Approved Drug Library  |  Anti-Cancer Compound Library  |  Anti-Aging Compound Library  |  Drug Repurposing Compound Library  |  Diabetes Related Compound Library  |  Anti-COVID-19 Compound Library  |  Orally Active Compound Library  |  FDA Approved & Pharmacopeial Drug Library  |  Anti-Breast Cancer Compound Library  |  Anti-Pancreatic Cancer Compound Library  |  XAV-939  |  Rucaparib  |  PJ34  |  3-Aminobenzamide  |  G007-LK  |  Dehydrocorydaline chloride  |  AG14361  |  Iniparib  |  AZD-2461  |  BGP-15  |  Fucosterol  |  JW 55  |  EB-47 dihydrochloride  |  UPF 1069  |  AZ6102  |  iRucaparib-AP6  |  ME0328  |  MN-64  |  5,?7,?4'-?Trimethoxyflavone  |  Benzamide  |  GeA-69  |  Paris saponin VII  |  PARP14 inhibitor H10  |  BYK204165  |  NU1025  |  Oroxin A  |  2-Methylquinazolin-4-ol

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