Niraparib Tosylate Monohydrate

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Niraparib 是 Tesaro 开发的一种口服活性小分子 PARP 抑制剂，用于治疗卵巢癌。

Niraparib is an orally active small molecule PARP inhibitor developed by Tesaro to treat ovarian cancer.It is used for the maintenance treatment of adult patients with recurrent epithelial ovarian, fallopian tube, or primary peritoneal cancer who are in complete or partial response to platinum-based chemotherapy.Niraparib is an orally active small molecule PARP inhibitor developed by Tesaro to treat ovarian cancer.

Niraparib (MK-4827) tosylate hydrate inhibits PARP activity with EC50=4 nM and EC90=45 nM in a whole cell assay. Niraparib tosylate hydrate inhibits proliferation of cancer cells with mutant BRCA-1 and BRCA-2 with CC50 in the 10-100 nM range. Niraparib tosylate hydrate displays excellent PARP 1 and 2 inhibition with IC50=3.8 and 2.1 nM, respectively, and in a whole cell assay. Niraparib tosylate hydrate inhibits PARP within 15 minutes of treatment reaching about 85% inhibition in the A549 cells at 1 h and about 55% inhibition at 1 h for the H1299 cells.

Niraparib (MK-4827) tosylate hydrate is well tolerated and demonstrates efficacy as a single agent in a xenograft model of BRCA-1 deficient cancer. Niraparib (MK-4827) tosylate hydrate is well tolerated in vivo and demonstrates efficacy as a single agent in a xenograft model of BRCA-1 deficient cancer.Niraparib (MK-4827) tosylate hydrate is characterized by acceptable pharmacokinetics in rats with plasma clearance of 28 (mL/min)/kg, very high volume of distribution (Vdss=6.9 L/kg), long terminal half-life (t1/2=3.4 h), and excellent bioavailability, F=65%. Niraparib (MK-4827) tosylate hydrate enhances radiation response of p53 mutant Calu-6 tumor in both cases, with the single daily dose of 50 mg/kg being more effective than 25 mg/kg given twice daily. Animal Model:Female nude mice (Ncr Nu/Nu) with solitary tumor xenografts Dosage:25 mg/kg or 50 mg/kg Administration:Gavage, 25 mg/kg twice a day with 6 h between doses or 50 mg/kg once daily for 21 consecutive days Result:Enhanced radiation response.

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1613220-15-7

510.61

C26H30N4O5S

>98% (HPLC)

In Vitro:?DMSO : 50 mg/mL (97.92 mM)

O.CC1=CC=C(C=C1)S(O)(=O)=O.[H][C@]1(CCCNC1)C1=CC=C(C=C1)N1C=C2C=CC=C(C(O)=N)C2=N1

2-{4-[(3S)-piperidin-3-yl]phenyl}-2H-indazole-7-carboximidic acid 4-methylbenzene-1-sulfonic acid hydrate

(-20℃)

With Ice Pack

≥ 2 years