Pamiparib

製品コードS8592 バッチS859202

化学情報

	Synonyms	BGB-290	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₁₆H₁₅FN₄O
	分子量	298.31	CAS No.	1446261-44-4
Solubility (25°C)*	体外	DMSO	60 mg/mL (201.13 mM)
		Ethanol	15 mg/mL (50.28 mM)
		Water	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	Pamiparib is a potent and selective inhibitor of PARP1 and PARP2 with IC50 values of 0.83 and 0.11 nM, respectively in biochemical assays. It shows high selectivity over other PARP enzymes.
in vitro	BGB-290 shows potent DNA-trapping activity with IC50 of 13 nM. In the cellular assays, BGB-290 inhibits intracellular PAR formation with an IC50 of 0.24 nM^[1].
in vivo	Oral administration of BGB-290 results in time-dependent and dose-dependent inhibition of PARylation in MDA-MB-436 (BRCA1 mutant) breast cancer xenograft, correlating well with the tumor drug concentrations. BGB-290 has also demonstrated good combination activity with chemotherapeutics in patient biopsy derived SCLC models^[1]. BGB-290 has significant brain penetration in C57 mice. The drug exposure in brain vs. that in plasma was close to 20% after oral administration of BGB-290^[2].

製品説明

Pamiparib is a potent and selective inhibitor of PARP1 and PARP2 with IC50 values of 0.83 and 0.11 nM, respectively in biochemical assays. It shows high selectivity over other PARP enzymes.

in vitro

BGB-290 shows potent DNA-trapping activity with IC50 of 13 nM. In the cellular assays, BGB-290 inhibits intracellular PAR formation with an IC50 of 0.24 nM^[1].

in vivo

Oral administration of BGB-290 results in time-dependent and dose-dependent inhibition of PARylation in MDA-MB-436 (BRCA1 mutant) breast cancer xenograft, correlating well with the tumor drug concentrations. BGB-290 has also demonstrated good combination activity with chemotherapeutics in patient biopsy derived SCLC models^[1].

BGB-290 has significant brain penetration in C57 mice. The drug exposure in brain vs. that in plasma was close to 20% after oral administration of BGB-290^[2].

プロトコル(参考用のみ)

細胞アッセイ	細胞株	U251 cells
	濃度	0.1 μM
	反応時間
	実験の流れ
動物実験	動物モデル	Orthotopic GBM12 xenograft model
	投薬量	3 mg/kg
	投与方法

参考

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：

Aggregability of the SQSTM1/p62-based aggresome-like induced structures determines the sensitivity to parthanatos [ Cell Death Discov, 2024, 10(1):74]	PubMed: 38346947
Zinc Finger MYND-Type Containing 8 (ZMYND8) Is Epigenetically Regulated in Mutant Isocitrate Dehydrogenase 1 (IDH1) Glioma to Promote Radioresistance [ Clin Cancer Res, 2023, 29(9):1763-1782]	PubMed: 36692427
Class I HDAC inhibition reduces DNA damage repair capacity of MYC-amplified medulloblastoma cells [ J Neurooncol, 2023, 164(3):617-632]	PubMed: 37783879
Class I HDAC inhibition reduces DNA damage repair capacity of MYC-amplified medulloblastoma cells [ J Neurooncol, 2023, 164(3):617-632]	PubMed: 37783879
PARP-mediated PARylation of MGMT is critical to promote repair of temozolomide-induced O6-methylguanine DNA damage in glioblastoma [ Neuro Oncol, 2021, 23(6):920-931]	PubMed: 33433610
A pan-cancer organoid platform for precision medicine [ Cell Rep, 2021, 36(4):109429]	PubMed: 34320344
Pharmacological Poly (ADP-Ribose) Polymerase Inhibitors Decrease Mycobacterium tuberculosis Survival in Human Macrophages [ Front Immunol, 2021, 12:712021]	PubMed: 34899683
Pharmacological Poly (ADP-Ribose) Polymerase Inhibitors Decrease Mycobacterium tuberculosis Survival in Human Macrophages [ Front Immunol, 2021, 12:712021]	PubMed: 34899683
EGFR Amplification Induces Increased DNA Damage Response and Renders Selective Sensitivity to Talazoparib (PARP Inhibitor) in Glioblastoma [ Clin Cancer Res, 2020, 26(6):1395-1407]	PubMed: 31852834
EGFR amplification induces increased DNA damage response and renders selective sensitivity to Talazoparib (PARP inhibitor) in glioblastoma. [ Clin Cancer Res, 2019, 10.1158/1078-0432.CCR-19-2549]	PubMed: 31852834

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。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。