AZD2461

製品コードS7029 バッチS702901

化学情報

	Synonyms	N/A	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₂₂H₂₂FN₃O₃
	分子量	395.43	CAS No.	1174043-16-3
Solubility (25°C)*	体外	DMSO	79 mg/mL (199.78 mM)
		Ethanol	31 mg/mL (78.39 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	AZD2461 is a novel PARP inhibitor with low affinity for Pgp than Olaparib. Phase 1.
in vitro	AZD2461 has lower affinity for Pgp than does Olaparib. ^[1]
in vivo	AZD2461 has an 80-fold increased Mdr1b expression on Olaparib-resistant KB1P tumor T6-28, without inhibition of Pgp. AZD2461 induces loss of 53BP1 expression in mice with KB1P tumors with short-term treatment. Long-term AZD2461 treatment is well tolerated and doubled the median relapse-free survival. ^[1]

プロトコル(参考用のみ)

動物実験	動物モデル	Olaparib-resistant tumors from KB1PM1, KB1PM3, and KB1PM4 in female mice
	投薬量	100 mg/kg
	投与方法	p.o.

参考

[1] Jaspers JE, et al. Cancer Discov, 2013, 3(1), 68-81.

カスタマーフィードバック

: Data from [Data independently produced by , , Cell Death Differ, 2017, 24(6):1091-1099]

: Data from [Data independently produced by , , J Cancer Res Clin Oncol, 2019, 145(1):137-152]

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：

Histone Parylation factor 1 contributes to the inhibition of PARP1 by cancer drugs [ Nat Commun, 2021, 12(1):736]	PubMed: 33531508
A small-molecule inhibitor of the BRCA2-RAD51 interaction modulates RAD51 assembly and potentiates DNA damage-induced cell death [ Cell Chem Biol, 2021, S2451-9456(21)00058-1]	PubMed: 33662256
Illuminating NAD+ Metabolism in Live Cells and In Vivo Using a Genetically Encoded Fluorescent Sensor [ Dev Cell, 2020, 53(2):240-252.e7]	PubMed: 32197067
Illuminating NAD+ Metabolism in Live Cells and In Vivo Using a Genetically Encoded Fluorescent Sensor. [ Dev Cell, 2020, 20;53(2):240-252]	PubMed: 32197067
Response of Breast Cancer Cells to PARP Inhibitors Is Independent of BRCA Status. [ J Clin Med, 2020, 30;9(4)]	PubMed: 32235451
PARP inhibitors affect growth, survival and radiation susceptibility of human alveolar and embryonal rhabdomyosarcoma cell lines [Camero S, et al. J Cancer Res Clin Oncol, 2019, 145(1):137-152.]	PubMed: 30357520
Neuroprotectin D1 upregulates Iduna expression and provides protection in cellular uncompensated oxidative stress and in experimental ischemic stroke. [Belayev L, et al. Cell Death Differ, 2017, 24(6):1091-1099]	PubMed: 28430183
TOPBP1Dpb11 plays a conserved role in homologous recombination DNA repair through the coordinated recruitment of 53BP1Rad9. [ J Cell Biol, 2017, 216(3):623-639]	PubMed: 28228534

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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