ChemicalBook > CAS DataBase List > MK-4827 (tosylate)

MK-4827 (tosylate)

Product Name
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
Formula Weight
492.58992
MOL File
1038915-73-9.mol
More
Less

MK-4827 (tosylate) Property

Melting point:
>142oC (dec.)
storage temp. 
-20°C Freezer
solubility 
Methanol (Slightly)
form 
Solid
color 
Off-White to Pale Yellow
InChI
InChI=1/C19H20N4O.C7H8O3S/c20-19(24)17-5-1-3-15-12-23(22-18(15)17)16-8-6-13(7-9-16)14-4-2-10-21-11-14;1-6-2-4-7(5-3-6)11(8,9)10/h1,3,5-9,12,14,21H,2,4,10-11H2,(H2,20,24);2-5H,1H3,(H,8,9,10)/t14-;/s3
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|
More
Less

Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

More
Less

N-Bromosuccinimide Price

Cayman Chemical
Product number
20842
Product name
MK-4827 (tosylate)
Purity
≥98%
Packaging
5mg
Price
$46
Updated
2024/03/01
Cayman Chemical
Product number
20842
Product name
MK-4827 (tosylate)
Purity
≥98%
Packaging
50 mg
Price
$253
Updated
2024/03/01
Cayman Chemical
Product number
20842
Product name
MK-4827 (tosylate)
Purity
≥98%
Packaging
1mg
Price
$32
Updated
2023/01/06
Cayman Chemical
Product number
20842
Product name
MK-4827 (tosylate)
Purity
≥98%
Packaging
10mg
Price
$83
Updated
2024/03/01
Cayman Chemical
Product number
20842
Product name
MK-4827 (tosylate)
Purity
≥98%
Packaging
25mg
Price
$149
Updated
2024/03/01
More
Less

MK-4827 (tosylate) Chemical Properties,Usage,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

More
Less

MK-4827 (tosylate) Suppliers

China 146 India 3 United States 11 Global 160
Kaixin Chemical (Hong Kong) Limited
Tel
010-88886666-01 13112345678
Fax
CDXH21@126.com
Email
loyson@tcypharm.com
Country
China
ProdList
597
Advantage
55
Chembest Research Laboratories Limited
Tel
+86-21-20908456
Fax
021-58180499
Email
sales@BioChemBest.com
Country
China
ProdList
6003
Advantage
61
Haoyuan Chemexpress Co., Ltd.
Tel
021-58950125
Fax
(86) 21-58955996
Email
info@chemexpress.com
Country
China
ProdList
7552
Advantage
61
TargetMol Chemicals Inc.
Tel
021-021-33632979 15002134094
Fax
021-33632979
Email
marketing@targetmol.com
Country
China
ProdList
7783
Advantage
58
LETOPHARM LIMITED
Tel
+86-21-5821 5861
Fax
+86-21-5106 2861
Email
sales@letopharm.com
Country
China
ProdList
2384
Advantage
58
SPIRO PHARMA
Tel
Fax
-
Email
eric_feng1954@126.com
Country
China
ProdList
9248
Advantage
55
BOC Sciences
Tel
16314854226
Email
info@bocsci.com
Country
United States
ProdList
9923
Advantage
65
Twochem Co.Ltd
Tel
021-021-58111628 15800915896
Fax
QQ 3285589261
Email
sales@twochem.com
Country
China
ProdList
304
Advantage
55
TaiChem Taizhou Limited
Tel
052386810091
Email
zcwy9518@yeah.net
Country
China
ProdList
3912
Advantage
58
Guangzhou QiYun Biotechnology Co., Ltd.
Tel
020-61288194 61288195
Fax
020-61288700
Email
505721671@qq.com
Country
China
ProdList
3866
Advantage
58
More
Less

View Lastest Price from MK-4827 (tosylate) manufacturers

Henan Aochuang Chemical Co.,Ltd.
Product
Niraparib tosylate 2191-20-5
Price
US $0.00-0.00/kg
Min. Order
1kg
Purity
98%
Supply Ability
1Ton
Release date
2022-09-22
Zibo Hangyu Biotechnology Development Co., Ltd
Product
MK-4827 (tosylate) 1038915-73-9
Price
US $0.10-0.30/kg
Min. Order
1kg
Purity
99%
Supply Ability
20n tons
Release date
2024-02-16
Beijing Yibai Biotechnology Co., Ltd
Product
Niraparib Tosylate 1038915-73-9
Price
US $0.00-0.00/KG
Min. Order
1g
Purity
99%
Supply Ability
50kg/month
Release date
2019-08-16

1038915-73-9, MK-4827 (tosylate)Related Search:

(S)-2-(4-(piperidin-3-yl)phenyl)-2H-indazole-7-carboxaMide Ruxolitinib phosphate Nintedanib Triethyl orthoformate Tosyl azide EGF816 (mesylate) Epacadostat (INCB024360) Nintedanib Ethanesulfonate Salt MK-4827 (R-enantioMer) AnaMorelin hydrochloride BKM120 (NVP-BKM120, Buparlisib) tert-butyl (S)-3-(4-bromophenyl)piperidine-1-carboxylate Niraparib Niraparib tosylate 3-(4-Bromophenyl)piperidine-1-carboxylic acid tert-butyl ester

  • 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
  • NIRAPARIB TOSYLATE;MK 4827 TOSYLATE;MK4827 TOSYLATE
  • 2H-Indazole-7-carboxamide,2-[4-[(3S)-3-piperidinyl]phenyl]-,4-methylbenzenesulfonate(1:1)
  • Niraparib TOS
  • MK-4827 (tosylate) ISO 9001：2015 REACH
  • Niraparib Tosylate (MK-4827)
  • (S)-2-(4-(piperidin-3-yl)phenyl)-2H-indazole-7-carboxamide 4-methylbenzenesulfonate
  • Niraparib tosylate monohydrate (S)-2-(4-(piperidin-3-yl)phenyl)-2H-isoindole-4-carboxamide compound with 1-methyl-4-(methylsulfonyl)benzene (1:1) hydrate
  • Niraparib Tosilate
  • Niraparib tosylate, 10 mM in DMSO
  • Nilaparib toluenesulfonate
  • Nilapani methanesulfonate
  • Nilapani toluene sulfonic acid salt hydrate
  • 1038915-73-9
  • C19H20N4OC7H8O3S