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Niraparib Tosylate Monohydrate

CAS No. 1613220-15-7

Niraparib Tosylate Monohydrate( —— )

Catalog No. M21829 CAS No. 1613220-15-7

Niraparib is an orally active small molecule PARP inhibitor developed by Tesaro to treat ovarian cancer.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
Size Price / USD Stock Quantity
5MG 50 Get Quote
10MG 71 Get Quote
25MG 107 Get Quote
50MG 132 Get Quote
100MG 205 Get Quote
200MG 309 Get Quote
500MG 516 Get Quote
1G Get Quote Get Quote

Biological Information

  • Product Name
    Niraparib Tosylate Monohydrate
  • Note
    Research use only, not for human use.
  • Brief Description
    Niraparib is an orally active small molecule PARP inhibitor developed by Tesaro to treat ovarian cancer.
  • Description
    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.
  • In Vitro
    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.
  • In Vivo
    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.
  • Synonyms
    ——
  • Pathway
    Others
  • Target
    Other Targets
  • Recptor
    ——
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    1613220-15-7
  • Formula Weight
    510.61
  • Molecular Formula
    C26H30N4O5S
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : 50 mg/mL (97.92 mM)
  • SMILES
    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
  • Chemical Name
    2-{4-[(3S)-piperidin-3-yl]phenyl}-2H-indazole-7-carboximidic acid 4-methylbenzene-1-sulfonic acid hydrate

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

molnova catalog
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