- Niraparib tosylate
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- $38.00 / 2mg
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2025-05-19
- CAS:1038915-73-9
- Min. Order:
- Purity: 98.69%
- Supply Ability: 10g
- MK-4827 (tosylate)
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- $0.10 / 1kg
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2025-04-22
- CAS:1038915-73-9
- Min. Order: 1kg
- Purity: 99%
- Supply Ability: 20n tons
- Niraparib tosylate
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- $0.00 / 1kg
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2025-04-04
- CAS:2191-20-5
- Min. Order: 1kg
- Purity: 98%
- Supply Ability: 1Ton
Related articles - MK-4827 (tosylate)
- To validate that MK-4827 (Niraparib) inhibits PARP in these cell lines, A549 and H1299 cells are treated with 1 μM MK-4827 for....
- Aug 26，2019
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| | MK-4827 (tosylate) Basic information |
| Product Name: | MK-4827 (tosylate) | | Synonyms: | Niraparib TsOH;niraparib p-toluenesulfonate;MK-4827(Niraparib) tosylate;Niraparib Tosylate;MK-4827 (tosylate);(3S)-3-[4-[7-(Aminocarbonyl)-2H-indazol-2-yl]phenyl]piperidine tosylate;MK-4827, Niraparib TsOH salt;Niraparib(MK-4827) tosylate | | CAS: | 1038915-73-9 | | MF: | C26H28N4O4S | | MW: | 492.58992 | | EINECS: | | | Product Categories: | | | Mol File: | 1038915-73-9.mol |  |
| | MK-4827 (tosylate) Chemical Properties |
| Melting point | >142oC (dec.) | | storage temp. | -20°C Freezer | | solubility | Methanol (Slightly) | | form | Solid | | color | Off-White to Pale Yellow | | InChIKey | LCPFHXWLJMNKNC-XOIICWPPNA-N | | SMILES | S(C1C=CC(C)=CC=1)(O)(=O)=O.C(C1=CC=CC2=CN(C3C=CC([C@H]4CNCCC4)=CC=3)N=C12)(=O)N |&1:23,r| |
| | MK-4827 (tosylate) Usage And Synthesis |
| Description | Niraparib tosylate (MK-4827 tosylate) is a highly potent and orally bioavailable PARP1 and PARP2 inhibitor with an IC50 of 3.8 and 2.1 nM, respectively; with significant activity in cancer cells with mutant BRCA-1 and BRCA-2; >330-fold selective against PARP3, V-PARP, and Tank1. Niraparib tosylate leads to inhibition of repair of DNA damage, activates apoptosis, and shows anti-tumor activity. | | Uses | Niraparib is a novel oral poly(ADP-ribose)polymerase (PARP) inhibitor efficacious in BRCA-1 and -2 mutant tumors. | | in vitro | In a whole-cell assay, Niraparib (MK-4827) tosylate hydrate inhibits PARP activity with EC50=4 nM and EC90=45 nM. Niraparib tosylate hydrate inhibits the 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) is well tolerated and demonstrates efficacy as a single agent in a xenograft model of BRCA-1 deficient cancer. Niraparib (MK-4827) is well tolerated in vivo and demonstrates efficacy as a single agent in a xenograft model of BRCA-1 deficient cancer. Niraparib (MK-4827) 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%[1].
Niraparib (MK-4827) 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[3].
| | IC 50 | PARP-2: 2.1 nM (IC50); PARP-1: 3.8 nM (IC50); V-PARP: 330 nM (IC50); TANK-1: 570 nM (IC50); PARP-3: 1300 nM (IC50) |
| | MK-4827 (tosylate) Preparation Products And Raw materials |
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