ChemicalBook > CAS DataBase List > (S)-2-(4-(piperidin-3-yl)phenyl)-2H-indazole-7-carboxaMide

(S)-2-(4-(piperidin-3-yl)phenyl)-2H-indazole-7-carboxaMide

Product Name
(S)-2-(4-(piperidin-3-yl)phenyl)-2H-indazole-7-carboxaMide
CAS No.
1038915-64-8
Chemical Name
(S)-2-(4-(piperidin-3-yl)phenyl)-2H-indazole-7-carboxaMide
Synonyms
CS-787;Zejula;EOS-62286;MK-4827 (HCl);MK-4827 (hydrochloride);Niraparib hydrochloride;Niraparib HCl (MK-4827);MK-4827, Niraparib HCl salt;Niraparib Tosylate Monohydrate;Niraparib(MK4827) hydrochloride
CBNumber
CB42553458
Molecular Formula
C19H20N4O
Formula Weight
320.3883
MOL File
1038915-64-8.mol
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(S)-2-(4-(piperidin-3-yl)phenyl)-2H-indazole-7-carboxaMide Property

Melting point:
144 °C
storage temp. 
Store at -20°C
solubility 
Soluble in DMSO
form 
Solid
color 
White to light yellow
InChI
InChI=1/C19H20N4O/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/h1,3,5-9,12,14,21H,2,4,10-11H2,(H2,20,24)/t14-/s3
InChIKey
PCHKPVIQAHNQLW-WDHUHKLTNA-N
SMILES
N1=C2C(C=CC=C2C(N)=O)=CN1C1=CC=C([C@@H]2CCCNC2)C=C1 |&1:16,r|
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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.

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P270Do not eat, drink or smoke when using this product.

P271Use only outdoors or in a well-ventilated area.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P304+P340IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.

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

P312Call a POISON CENTER or doctor/physician if you feel unwell.

P321Specific treatment (see … on this label).

P330Rinse mouth.

P332+P313IF SKIN irritation occurs: Get medical advice/attention.

P337+P313IF eye irritation persists: Get medical advice/attention.

P362Take off contaminated clothing and wash before reuse.

P403+P233Store in a well-ventilated place. Keep container tightly closed.

P405Store locked up.

P501Dispose of contents/container to..…

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N-Bromosuccinimide Price

ChemScene
Product number
CS-2282
Product name
Niraparib(hydrochloride)
Purity
99.80%
Packaging
5mg
Price
$70
Updated
2021/12/16
ApexBio Technology
Product number
B1163
Product name
MK-4827hydrochloride
Packaging
5mg
Price
$95
Updated
2021/12/16
ChemScene
Product number
CS-2282
Product name
Niraparib(hydrochloride)
Purity
99.80%
Packaging
10mg
Price
$100
Updated
2021/12/16
ApexBio Technology
Product number
B1163
Product name
MK-4827hydrochloride
Packaging
10mg
Price
$168
Updated
2021/12/16
ChemScene
Product number
CS-2282
Product name
Niraparib(hydrochloride)
Purity
99.80%
Packaging
50mg
Price
$180
Updated
2021/12/16
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(S)-2-(4-(piperidin-3-yl)phenyl)-2H-indazole-7-carboxaMide Chemical Properties,Usage,Production

Uses

Niraparib hydrochloride (MK-4827 hydrochloride) is a highly potent and orally bioavailable PARP1 and PARP2 inhibitor with IC50s of 3.8 and 2.1 nM, respectively. Niraparib hydrochloride leads to inhibition of repair of DNA damage, activates apoptosis and shows anti-tumor activity[1][2][3].

in vivo

Niraparib is well tolerated and demonstrates efficacy as a single agent in a xenograft model of BRCA-1 deficient cancer. Niraparib is well tolerated in vivo and demonstrates efficacy as a single agent in a xenograft model of BRCA-1 deficient cancer. Niraparib 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 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] Jones P, et al. 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 Med Chem. 2009 Nov 26;52(22):7170-85. DOI:10.1021/jm901188v
[2] Bridges KA, et al. Niraparib (MK-4827), a novel poly(ADP-Ribose) polymerase inhibitor, radiosensitizes human lung and breast cancer cells. Oncotarget. 2014 Jul 15;5(13):5076-86. DOI:10.18632/oncotarget.2083
[3] Wang L, et al. MK-4827, a PARP-1/-2 inhibitor, strongly enhances response of human lung and breast cancer xenografts to radiation. Invest New Drugs. 2012 Dec;30(6):2113-20. DOI:10.1007/s10637-011-9770-x
[4] Mirza MR, et al. Niraparib Maintenance Therapy in Platinum-Sensitive, Recurrent Ovarian Cancer. N Engl J Med. 2016 Dec 1;375(22):2154-2164. DOI:10.1056/NEJMoa1611310

(S)-2-(4-(piperidin-3-yl)phenyl)-2H-indazole-7-carboxaMide Preparation Products And Raw materials

Raw materials

Preparation Products

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(S)-2-(4-(piperidin-3-yl)phenyl)-2H-indazole-7-carboxaMide Suppliers

China 99 United Kingdom 1 United States 9 Global 109
Jiangsu yize medical technology co. LTD
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18962082606
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Zhengzhou HongSheng Pharmaceutical Co., Ltd.
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LETOPHARM LIMITED
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Twochem Co.Ltd
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View Lastest Price from (S)-2-(4-(piperidin-3-yl)phenyl)-2H-indazole-7-carboxaMide manufacturers

Nanjing Fred Technology Co., Ltd
Product
Niraparib tosylate 1038915-64-8
Price
US $0.00-0.00/kg
Min. Order
1kg
Purity
99%, Single impurity＜0.1
Supply Ability
1 ton
Release date
2023-12-25
Zibo Hangyu Biotechnology Development Co., Ltd
Product
(S)-2-(4-(piperidin-3-yl)phenyl)-2H-indazole-7-carboxaMide 1038915-64-8
Price
US $0.10-0.30/kg
Min. Order
1kg
Purity
99%
Supply Ability
20 tons
Release date
2024-02-16
Career Henan Chemical Co
Product
Niraparib Tosylate Monohydrate 1038915-64-8
Price
US $200.00/KG
Min. Order
1KG
Purity
99%
Supply Ability
10kg
Release date
2018-08-02

1038915-64-8, (S)-2-(4-(piperidin-3-yl)phenyl)-2H-indazole-7-carboxaMideRelated Search:

Nintedanib (S)-tert-butyl 3-(4-aMinophenyl)piperidine-1-carboxylate 4-(3-PYRIDYL)ANILINE N-(tert-butyl)-1H-indazole-7-carboxamide 4-piperidin-3-ylaniline 4-(3-Piperidyl)aniline Dihydrochloride Methyl 3-formyl-2-nitrobenzoate tert-butyl (S)-3-(4-bromophenyl)piperidine-1-carboxylate Niraparib Niraparib tosylate MK-4827 (tosylate) 3-(4-Bromophenyl)piperidine-1-carboxylic acid tert-butyl ester Piperidine, 3-(4-bromophenyl)- tert-butyl (3S)-3-{4-[7-(aminocarbonyl)-2H-indazol-2-yl]phenyl}piperidine-1-carboxylate (S)-3-(4-Bromophenyl)piperidine 3-(4-AMINO-PHENYL)-PIPERIDINE-1-CARBOXYLIC ACID TERT-BUTYL ESTER (R)-tert-butyl 3-(4-aMinophenyl)piperidine-1-carboxylate MK-4827 (R-enantioMer)

  • MK-4827 (HCl)
  • MK-4827 (hydrochloride)
  • CS-787
  • Niraparib(MK4827) hydrochloride
  • 2-[4-[(3S)-piperidin-3-yl]phenyl]indazole-7-carboxamide,hydrochloride
  • Zejula
  • Niraparib hydrochloride
  • 2H-Indazole-7-carboxamide, 2-[4-(3S)-3-piperidinylphenyl]-, hydrochloride (1:1)
  • Niraparib Tosylate Monohydrate
  • EOS-62286
  • MK-4827, Niraparib HCl salt
  • (3S)-3-[4-[7-(aminocarbonyl)-2H-indazol-2-yl]phenyl]piperidinium chloride
  • (S)-2-(4-(piperidin-3-yl)phenyl)-2H-indazole-7-carboxamide dihydrochloride
  • Niraparib HCl (MK-4827)
  • 2-[4-(3S)-3-Piperidinylphenyl]-2H-indazole-7-carboxamide hydrochloride (1:1)
  • (S)-2-(4-(Piperidin-3-yl)phenyl)-2H-indazole-7-carboxamide hydrochloride
  • MK-4827 hydrochloride|||MK-4827 (hydrochloride)
  • Niraparib hydrochloride, 10 mM in DMSO
  • 2-[4-(3S)Piperidin-3-ylphenyl]-2H-indazol-7-carboxamide HCl
  • 1038915-64-8
  • API