Niraparib tosylate

製品コードS7625 バッチS762507

化学情報

	Synonyms	MK 4827 tosylate	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₁₉H₂₀N₄O.C₇H₈O₃S
	分子量	492.59	CAS No.	1038915-73-9
Solubility (25°C)*	体外	DMSO	99 mg/mL (200.97 mM)
		Water	Insoluble
		Ethanol	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	Niraparib tosylate is a selective inhibitor of PARP1/PARP2 with IC50 of 3.8 nM/2.1 nM. Niraparib increases formation of PARP-DNA complexes resulting in DNA damage, apoptosis, and cell death.
in vitro	Micromolar concentrations of niraparib radiosensitizes tumor cell lines derived from lung, breast, and prostate cancers independently of their p53 status but not cell lines derived from normal tissues. Niraparib also sensitizes tumor cells to H2O2 and converts H2O2-induced single strand breaks (SSBs) into DSBs during DNA replication^[5].
in vivo	MK-4827 strongly enhances the effect of radiation on a variety of human tumor xenografts, both p53 wild type and p53 mutant. MK-4827 reduces PAR levels in tumors by 1 h after administration which persisted for up to 24 h^[1]. In vivo treatment with MK-4827 and radiation prolonged survival (p<0.01) compared to single modalities. In vivo superiority of MK-4827 plus radiation is further documented by significant elevations of cleaved caspase-3 and γ-H2AX in tumors from the combination group compared to single modality cohorts^[4].

プロトコル(参考用のみ)

細胞アッセイ	細胞株	V-C8 cells
	濃度	50 nM
	反応時間	24 h
	実験の流れ	V-C8 (BRCA2-negative) Chinese hamster cells are treated with the PARP inhibitor MK-4827 for 24 h, washed and incubated in drug-free medium for 5-7 days until colonies formed.
動物実験	動物モデル	Female nude mice (Ncr Nu/Nu)
	投薬量	25 or 50 mg/kg
	投与方法	p.o.

参考

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カスタマーフィードバック

: Data from [Data independently produced by , , Cell Death & Disease, 2017, 8: e3070]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Detection of senescence using machine learning algorithms based on nuclear features [ Nat Commun, 2024, 15(1):1041]	PubMed: 38310113
BRCA2 Germline Mutations Identify Gastric Cancers Responsive to PARP Inhibitors [ Cancer Res, 2023, 83(10):1699-1710]	PubMed: 37129948
OGG1 Inhibition Triggers Synthetic Lethality and Enhances The Effect of PARP Inhibitor Olaparib in BRCA1-Deficient TNBC Cells [ Front Oncol, 2022, 12:888810]	PubMed: 35619904
Novel Paired Normal Prostate and Prostate Cancer Model Cell Systems Derived from African American Patients [ Cancer Res Commun, 2022, 2(12):1617-1625]	PubMed: 36970725
Translational evidence for RRM2 as a prognostic biomarker and therapeutic target in Ewing sarcoma [ Mol Cancer, 2021, 20(1):97]	PubMed: 34315482
Targeting immunosuppressive macrophages overcomes PARP inhibitor resistance in BRCA1-associated triple-negative breast cancer [ Nat Cancer, 2021, 2(1):66-82]	PubMed: 33738458
Targeting immunosuppressive macrophages overcomes PARP inhibitor resistance in BRCA1-associated triple-negative breast cancer [ Nat Cancer, 2021, 2(1):66-82]	PubMed: 33738458
A subset of PARP inhibitors induces lethal telomere fusion in ALT-dependent tumor cells [ Sci Transl Med, 2021, 13(592)eabc7211]	PubMed: 33952676
Histone Parylation factor 1 contributes to the inhibition of PARP1 by cancer drugs [ Nat Commun, 2021, 12(1):736]	PubMed: 33531508
Replication catastrophe is responsible for intrinsic PAR glycohydrolase inhibitor-sensitivity in patient-derived ovarian cancer models [ J Exp Clin Cancer Res, 2021, 40(1):323]	PubMed: 34656146

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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