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Chemical Structure| 1038915-64-8 Chemical Structure| 1038915-64-8

Structure of Niraparib HCl
CAS No.: 1038915-64-8

Chemical Structure| 1038915-64-8

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MK-4827 HCl is a selective inhibitor of PARP1/PARP2 with IC50 of 3.8 nM/2.1 nM, showing great activity in cancer cells with mutant BRCA-1 and BRCA-2, and is > 330-fold selective against PARP3, V-PARP and Tank1.

Synonyms: MK-4827 hydrochloride; Niraparib hydrochloride

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Product Details of Niraparib HCl

CAS No. :1038915-64-8
Formula : C19H21ClN4O
M.W : 356.85
SMILES Code : O=C(C1=CC=CC2=CN(C3=CC=C([C@H]4CNCCC4)C=C3)N=C12)N.[H]Cl
Synonyms :
MK-4827 hydrochloride; Niraparib hydrochloride
MDL No. :MFCD20502397

Safety of Niraparib HCl

GHS Pictogram:
Signal Word:Danger
Hazard Statements:H302-H340
Precautionary Statements:P260-P264-P270-P280-P281-P330-P301+P312-P405-P501

Related Pathways of Niraparib HCl

epigenetics
DNA

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
HT-1080 10 µM 4 h To evaluate the sensitivity of STS cell lines to Niraparib, results showed that STS cell lines were sensitive to Niraparib. PMC7449912
HT-1080 10 µM 48 h To evaluate the effect of Niraparib on cell cycle and apoptosis, results showed that Niraparib treatment caused cell cycle arrest and increased apoptosis. PMC7449912
ovarian and maμMary tumor cells 2 μM 12 hours Niraparib induced tumor cell death via the ATM-AMPK-ULK1 pathway, leading to mTOR inactivation and autophagosome formation PMC6154859
SKOV3 10 μM 48 h To investigate the effect of PARP inhibitors on PD-L1 protein expression, results showed that Niraparib upregulated PD-L1 expression. PMC8499579
UWB1.289 10 μM 48 h To investigate the effect of PARP inhibitors on PD-L1 protein expression, results showed that Niraparib upregulated PD-L1 expression. PMC8499579
MIA PaCa-2 26 µM 48 hours Niraparib showed stronger antitumor effects than Olaparib in MIA PaCa-2 cells with an IC50 of 26 µM. PMC9618811
PANC-1 50 µM 48 hours Niraparib showed stronger antitumor effects than Olaparib in PANC-1 cells with an IC50 of 50 µM. PMC9618811
Capan-1 15 µM 48 hours Niraparib showed stronger antitumor effects than Olaparib in Capan-1 cells with an IC50 of 15 µM. PMC9618811
OVCAR8 20 µM 48 hours Niraparib showed stronger antitumor effects than Olaparib in OVCAR8 cells with an IC50 of 20 µM. PMC9618811
PEO1 28 µM 48 hours Niraparib showed stronger antitumor effects than Olaparib in PEO1 cells with an IC50 of 28 µM. PMC9618811
Breast and ovarian cancer cell lines 10,000 nM to 0.3 nM 10 days To evaluate the anti-proliferative activity of the combination of PRMT5 and PARP inhibitors, the results showed significant growth inhibition and cytotoxicity in breast and ovarian cancer cell lines. PMC10436459
Breast and ovarian cancer cell lines 5000 nM to 8 nM 14 days To evaluate the anti-proliferative activity of the combination of PRMT5 and PARP inhibitors through long-term exposure, the results showed significant growth inhibition and cytotoxicity in breast and ovarian cancer cell lines. PMC10436459
breast cancer cell lines 10,000 nM to 0.3 nM 10 days To evaluate the anti-proliferative effects of the combination of Niraparib and PRMT5 inhibitor GSK3326595, synergistic effects were observed in breast cancer cell lines. PMC10436459
ovarian cancer cell lines 10,000 nM to 0.3 nM 10 days To evaluate the anti-proliferative effects of the combination of Niraparib and PRMT5 inhibitor GSK3326595, synergistic effects were observed in ovarian cancer cell lines. PMC10436459
Ovarian cancer cells 2 μM 12 hours Niraparib killed tumor cells via an ATM-AMPK-ULK1 pathway, resulting in mTOR inactivation and the formation of autophagosomes, followed by autolysosome formation. PMC6154859
Breast cancer cells 2 μM 12 hours Niraparib killed tumor cells via an ATM-AMPK-ULK1 pathway, resulting in mTOR inactivation and the formation of autophagosomes, followed by autolysosome formation. PMC6154859

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice CDX and PDX models Oral 50 mg/kg sulforaphane daily, 10 mg/kg docetaxel weekly daily sulforaphane, weekly docetaxel, continuous treatment To evaluate the effect of Niraparib and TMZ combination therapy, results showed that the combination significantly inhibited tumor growth. PMC7449912
athymic mice BT474 mammary tumor model oral 25 mg/kg or 50 mg/kg Every three days, for four weeks Niraparib significantly slowed the growth of BT474 tumors, but the growth delay was only approximately equivalent to the duration of drug exposure PMC6154859
mice ovarian cancer model oral Niraparib 50 mg/kg, Irinotecan 10 mg/kg Niraparib orally for 5 days a week, Irinotecan intraperitoneally for 2 days a week, for 4 weeks To investigate the effect of Niraparib on PD-L1 expression and its synergistic effect with PD-L1 blockade, results showed that Niraparib increased PD-L1 expression and combined with PD-L1 blockade could more effectively inhibit tumor growth. PMC8499579
C57BL/6 mice ID8 ovarian cancer model Intraperitoneal injection 25 mg/kg once daily for 5 days Evaluate the anti-tumor effects of Niraparib in combination with NRT PMC11380394
Mice MDA-MB-468 and OVCAR3 xenograft models Oral 25 mg/kg four times a week for 8 weeks To evaluate the anti-tumor activity of the combination of PRMT5 and PARP inhibitors in vivo, the results showed significant tumor growth inhibition and tumor stasis and regression in MDA-MB-468 and OVCAR3 xenograft models. PMC10436459
BALB/C nude mice CDX model oral 50 mg/kg/day Once daily for 3 days To evaluate the effect of Niraparib and TMZ combination therapy on tumor growth in CDX models, results showed that the combination significantly inhibited tumor growth PMC7449912
Mice C57BL/6 mice Oral GSK3326595: 50 mg/kg, Niraparib: 35 mg/kg GSK3326595: Twice daily, Niraparib: Once daily, until the end of the experiment To investigate the anti-tumor effect of Niraparib combined with PD-L1 blockade, results showed that the combination significantly inhibited tumor growth. PMC8499579
C57BL/6 mice ID8 ovarian cancer model Intraperitoneal injection 100 mg/kg once daily for 5 days/week Evaluate the anti-tumor effects of Niraparib in combination with NRT PMC11380394
mice MDA-MB-468 breast cancer and OVCAR-3 ovarian cancer xenograft models oral 25 mg/kg 4 times per week for 8 weeks To evaluate the tumor growth inhibition effects of the combination of Niraparib and PRMT5 inhibitor GSK3326595, tumor stasis was observed in the MDA-MB-468 model and tumor regression was observed in the OVCAR-3 model. PMC10436459
Athymic mice BT474 breast cancer model Oral 50 mg/kg/day Once daily for 3 days Niraparib significantly slowed the growth of BT474 tumors, but the growth delay caused by niraparib alone was only approximately equivalent to the prior duration of drug exposure. PMC6154859

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.80mL

0.56mL

0.28mL

14.01mL

2.80mL

1.40mL

28.02mL

5.60mL

2.80mL

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