MK-4827 (tosylate)
- CAS No.
- 1038915-73-9
- Chemical Name:
- MK-4827 (tosylate)
- Synonyms
- Niraparib Tosylate;Niraparib TOS;Niraparib TsOH;MK-4827 (tosylate);Niraparib Tosilate;Nilapani methanesulfonate;Nilaparib toluenesulfonate;Niraparib(MK-4827) tosylate;MK-4827(Niraparib) tosylate;niraparib p-toluenesulfonate
- CBNumber:
- CB52682012
- Molecular Formula:
- C26H28N4O4S
- Molecular Weight:
- 492.58992
- MDL Number:
- MFCD28167748
- MOL File:
- 1038915-73-9.mol
- MSDS File:
- SDS
- TDS File:
- TDS
| Product description | Number | Pack Size | Price |
| MK-4827 (tosylate) ≥98% | 20842 | 5mg | $51 |
| MK-4827 (tosylate) ≥98% | 20842 | 10mg | $92 |
| MK-4827 (tosylate) ≥98% | 20842 | 25mg | $164 |
| MK-4827 (tosylate) ≥98% | 20842 | 50mg | $279 |
| MK-4827 (tosylate) ≥98% | 20842 | 5mg | $46 |
| More product size | |||
| 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| |
| FDA UNII | 75KE12AY9U |
SAFETY
Risk and Safety Statements
| Symbol(GHS) |  GHS07 |
|---|---|
| Signal word | Warning |
| Hazard statements | H302-H315-H319-H335 |
| Precautionary statements | P261-P305+P351+P338 |
MK-4827 (tosylate) price More Price(34)
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Cayman Chemical | 20842 | MK-4827 (tosylate) ≥98% | 1038915-73-9 | 5mg | $51 | 2026-04-30 | Buy |
| Cayman Chemical | 20842 | MK-4827 (tosylate) ≥98% | 1038915-73-9 | 10mg | $92 | 2026-04-30 | Buy |
| Cayman Chemical | 20842 | MK-4827 (tosylate) ≥98% | 1038915-73-9 | 25mg | $164 | 2026-04-30 | Buy |
| Cayman Chemical | 20842 | MK-4827 (tosylate) ≥98% | 1038915-73-9 | 50mg | $279 | 2026-04-30 | Buy |
| Cayman Chemical | 20842 | MK-4827 (tosylate) ≥98% | 1038915-73-9 | 5mg | $46 | 2024-03-01 | Buy |
MK-4827 (tosylate) Chemical Properties,Uses,Production
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)
References
[1] PHILIP JONES*. Discovery of 2-{4-[(3S)-Piperidin-3-yl]phenyl}-2H-indazole-7-carboxamide (MK-4827): A Novel Oral Poly(ADP-ribose)polymerase (PARP) Inhibitor Efficacious in BRCA-1 and -2 Mutant Tumors[J]. Journal of Medicinal Chemistry, 2009, 52 22: 7170-7185. DOI: 10.1021/jm901188v
[2] YUAN YUAN. Novel targeted therapeutics: inhibitors of MDM2, ALK and PARP.[J]. Journal of Hematology & Oncology, 2011, 4: 16. DOI: 10.1186/1756-8722-4-16
[3] LI WANG. MK-4827, a PARP-1/-2 inhibitor, strongly enhances response of human lung and breast cancer xenografts to radiation.[J]. Investigational New Drugs, 2012: 2113-2120. DOI: 10.1007/s10637-011-9770-x
[4] MIRZA M, MONK B, HERRSTEDT J, et al. Niraparib Maintenance Therapy in Platinum-Sensitive, Recurrent Ovarian Cancer.[J]. The New England Journal of Medicine, 2016, 75 1: 0. DOI: 10.1056/nejmoa1611310
MK-4827 (tosylate) Preparation Products And Raw materials
Raw materials
Preparation Products
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| Beijing Hope Pharmaceutical Co., Ltd. | +86-010-67886402 +8613611125266 | market@hopelife.cn | China | 72 | 58 |
| Zibo Hangyu Biotechnology Development Co., Ltd | +86-0533-2185556 +8615965530500 | nickzhang@hangyubiotech.com | China | 9880 | 58 |
| Beijing Cooperate Pharmaceutical Co.,Ltd | 010-60279497 | sales01@cooperate-pharm.com | CHINA | 1803 | 55 |
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 33024 | 60 |
| TianYuan Pharmaceutical CO.,LTD | +86-755-23284190 13684996853 | sales@tianpharm.com | CHINA | 304 | 58 |
| BOC Sciences | +1-631-485-4226 | inquiry@bocsci.com | United States | 19552 | 58 |
| Beijing Yibai Biotechnology Co., Ltd | 0086-182-6772-3597 | sales04@yibaibiotech.com | CHINA | 419 | 58 |
| CONIER CHEM AND PHARMA LIMITED | +8618523575427 | sales@conier.com | China | 49977 | 58 |
| career henan chemical co | +86-0371-86658258 +8613203830695 | factory@coreychem.com | China | 29794 | 58 |
| TargetMol Chemicals Inc. | +1-781-999-5354; +17819995354 | marketing@targetmol.com | United States | 32467 | 58 |
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
View Lastest Price from MK-4827 (tosylate) manufacturers
| Image | Update time | Product | Price | Min. Order | Purity | Supply Ability | Manufacturer | |
|---|---|---|---|---|---|---|---|---|
 |
2026-05-05 | MK-4827 (tosylate)
1038915-73-9
|
US $0.10-0.30 / kg | 1kg | 99% | 20n tons | Zibo Hangyu Biotechnology Development Co., Ltd | |
 |
2026-04-21 | Niraparib tosylate
1038915-73-9
|
US $61.00-119.00 / mg | 99.34% | 10g | TargetMol Chemicals Inc. | ||
 |
2025-04-04 | Niraparib tosylate
2191-20-5
|
US $0.00-0.00 / kg | 1kg | 98% | 1Ton | Henan Aochuang Chemical Co.,Ltd.
|
-
- MK-4827 (tosylate)
1038915-73-9
- US $0.10-0.30 / kg
- 99%
- Zibo Hangyu Biotechnology Development Co., Ltd
-
- Niraparib tosylate
1038915-73-9
- US $61.00-119.00 / mg
- 99.34%
- TargetMol Chemicals Inc.
-
- Niraparib tosylate
2191-20-5
- US $0.00-0.00 / kg
- 98%
- Henan Aochuang Chemical Co.,Ltd.
