Niraparib NEW
| Price | $8 | $2 | $0.8 |
| Package | 1kg | 25kg | 100kg |
| Min. Order: | 1kg |
| Supply Ability: | g-kg-tons, free sample is available |
| Update Time: | 2024-04-08 |
Product Details
| Product Name: Niraparib | CAS No.: 1038915-60-4 |
| Min. Order: 1kg | Purity: 99% |
| Supply Ability: g-kg-tons, free sample is available | Release date: 2024/04/08 |
| Lead time: In stock, ready for shipment | In stock: bag/bottle/drum/IBC |
| COA, MSDS: Available, contact us for details | Origin: Manufacturer, advantage product |
| Delivery : By express, by air, by sea | NAME: Sun |
1. Materials information
| Name | 2-[4-[(3S)-piperidin-3-yl]phenyl]indazole-7-carboxamide |
|---|---|
| Synonym | More Synonyms |
| Description | Niraparib (MK-4827) is a highly potent PARP1 and PARP2 inhibitor with IC50s of 3.8 and 2.1 nM, respectively. |
|---|---|
| Related Catalog | Signaling Pathways >> Cell Cycle/DNA Damage >> PARP Signaling Pathways >> Epigenetics >> PARP Research Areas >> Cancer |
| Target | 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) |
| In Vitro | Niraparib (MK-4827) inhibits PARP activity with EC50=4 nM and EC90=45 nM in a whole cell assay. MK-4827 inhibits proliferation of cancer cells with mutant BRCA-1 and BRCA-2 with CC50 in the 10-100 nM range. MK-4827 displays excellent PARP 1 and 2 inhibition with IC50=3.8 and 2.1 nM, respectively, and in a whole cell assay[1]. To validate that Niraparib (MK-4827) inhibits PARP in these cell lines, A549 and H1299 cells are treated with 1 μM MK-4827 for various times and measured PARP enzymatic activity using a chemiluminescent assay. The results show that Niraparib (MK-4827) 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[2]. |
| 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]. |
| Cell Assay | The inhibition of PARP is analyzed in A549 and H1299 cells using the HT Universal Chemiluminescent PARP Assay Kit. Briefly, cells are treated with DMSO or 1 μM Niraparib (MK-4827) for 15, 30, 60, or 120 minutes, trypsinized, and transferred to a pre-chilled tube. The cells are washed twice with ice cold PBS and resuspended in cold PARP extraction buffer. The cell suspensions are incubated on ice for 30 minutes with periodic vortexing to disrupt the cell membrane. The suspensions are centrifuged and the supernatant transferred to a pre-chilled tube on ice. The histone coated wells of the 96-well plate are rehydrated with 1X PARP buffer and incubated at room temperature for 30 minutes. The PARP buffer is removed and 20 μg of protein as determined by the Bio-Rad Protein Assay is added to each well followed by diluted PARP-HSA enzyme and 1X PARP buffer. The strip wells are then incubated at room temperature for 60 minutes, washed twice with PBS containing 0.1% Triton X-100, and then washed with PBS. Diluted Strep-HRP is added to the strip wells and incubated for 60 minutes at room temperature. The wells are washed again as before. Equal volumes of PeroxyGlow A and B are combined and added to the wells and chemiluminescent readings are obtained immediately using a plate-reader[2]. |
| Animal Admin | Mice[3] Female nude mice (Ncr Nu/Nu) are randomly assigned to treatment groups consisting of 5 to 8 mice each when tumors grew to 6.0 mm in diameter at which time treatment with Niraparib (MK-4827) is initiated. Niraparib (MK-4827) is given at a dose of 25 mg/kg twice daily or 50 mg/kg once daily for either 21 days or is discontinued at 9 days from the time tumors reached 8 mm in diameter. Fractionated local tumor irradiation (XRT) is given when tumors reach 8.0 mm in diameter (7.7-8.2 mm). Radiation (2 Gy per fraction) is delivered to the tumor-bearing leg of mice once daily for 14 consecutive days or twice daily for 7 consecutive days using a small-animal irradiator consisting of two parallel-opposed 137Cs sources, at a dose rate of 5 Gy/min. During irradiation un-anesthetized mice are mechanically immobilized in a jig so that the tumor is centered within a 3.0 cm diameter radiation field and the animal’s body shielded from radiation exposure. On the day when both Niraparib and radiation are given, drug is administered 1 h before the first radiation dose of the day. |
| 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. [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. [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. |
| Density | 1.3±0.1 g/cm3 |
|---|---|
| Boiling Point | 463.6±45.0 °C at 760 mmHg |
| Molecular Formula | C19H20N4O |
| Molecular Weight | 320.388 |
| Flash Point | 234.2±28.7 °C |
| Exact Mass | 320.163696 |
| PSA | 73.93000 |
| LogP | 2.85 |
| Vapour Pressure | 0.0±1.1 mmHg at 25°C |
| Index of Refraction | 1.705 |
| Storage condition | -20°C |
| HS Code | 2933990090 |
|---|
 3-{4-[7-(aminoc... CAS#:1038915-56-8 ~%  MK-4827(Niraparib) CAS#:1038915-60-4  MK-4827 (R-enan... CAS#:1038915-58-0 |
| Literature: WO2009/87381 A1, ; Page/Page column 37-38 ; |
| Precursor 1 | |
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| |
| DownStream 0 | |
| HS Code | 2933990090 |
|---|---|
| Summary | 2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0% |
| pound notMK4827 pound not MK 4827 |
| 2H-Indazole-7-carboxamide, 2-[4-[(3S)-3-piperidinyl]phenyl]- |
| 2-{4-[(3S)-piperidin-3-yl]phenyl}-2H-indazole-7-carboxamide |
| Niraparib |
| MK4827 |
| 2-{4-[(3S)-3-Piperidinyl]phenyl}-2H-indazole-7-carboxamide |
| UNII:HMC2H89N35 |
| MK-4827 |
2. Packaging of materials
For powders: normal is 25kgs/Drum or bag, or larger/smaller package as request.
For liquids: normal 25kgs/drum, 180-300kgs/bucket, or IBC, determined by the nature of the product.
Or smaller package 1kg/bottle, 10kgs/bottle as request.
3. Shipping & Delivery
By Express
Provide door to door service
Suitable for goods under 50kg
Delivery: 3-7 days
Cost: low cost
By Air
Provide airport to airport service
Suitable for goods over 50kg
Delivery: 3-14 days
Cost: high cost
By Sea
Provide seaport to seaport service
Suitable for goods over 100kg
Delivery: 2-45 days
Cost: low cost
4. Contact information
For more details, pls contact us freely.
Email address: sun@fdachem.com
Mob: 86 13526505137
WhatsApp/Skype/Wechat/LINE: 8613526505137
Company Profile Introduction
Henan Fengda Chemical Co., Ltd. is located in the High-tech Development Zone of Henan Province. Specializing in the production and sales of various fine chemical products required for industrial production, including chemical raw materials, organic raw materials, petrochemicals, chemical reagents, solvents, catalysts, and additives, etc.
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China
- Since: 2023-02-10
- Address: Room 01, 2288 E05, Building 14, East Henan University, Science and Technology Park, 279 Xisanhuan Ro
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