NEO2734 (EP31670)

製品コードS9648 バッチS964802

化学情報

	Synonyms	EP31670	Storage (From the date of receipt)	3 years -20°C powder
	化学式	C₂₂H₂₄F₃N₃O₃
	分子量	435.44	CAS No.	2081072-29-7
Solubility (25°C)*	体外	DMSO	87 mg/mL (199.79 mM)
		Ethanol	87 mg/mL (199.79 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	NEO2734 (EP31670)は、IC50が両方とも<30 nMである、新規の経口活性選択的p300/CBPおよびBETブロモドメイン二重阻害剤です。
in vitro	Treatment of NMC cells with the novel dual p300/CBP and BET bromodomain–selective inhibitor, NEO2734, potently inhibits growth and induces differentiation of NMC cells in vitro; findings that correspond with potentiated transcriptional effects from combined BET and p300 bromodomain inhibition.
in vivo	In three disseminated NMC xenograft models, NEO2734 provides greater growth inhibition, with tumor regression and significant survival benefit seen in two of three models, compared with a lead clinical BET inhibitor or “standard” chemotherapy.

プロトコル(参考用のみ)

細胞アッセイ	細胞株	NUT carcinoma patient cell lines (TC-797, 14169, 10-15, PER-403)
	濃度	1 μM
	反応時間	24 h
	実験の流れ	NUT carcinoma patient cell lines (TC-797, 14169, 10-15, and PER-403) are plated in T-25 flasks and grown in DMEM (797) containing 10 % fetal bovine serum and 1 % penicillin/streptomycin. Cells are treated with either 500 nM OTX-015, 1 μM GNE-781, combination of 62.5 nM GNE-781 and 62.5 nM OTX-015, 1 μM NEO2734, or the equivalent volume of DMSO (0.025 %). At 24H, 2 × 10⁶ cells are spun at 500 × g for 5 minutes at 4 ℃ and washed twice with PBS. Pellets are resuspended in 1 ml of cold PBS and added dropwise while gently vortexing to 9 ml 70 % ethanol in a 15 ml polypropylene centrifuge tube. Fixed cells are then frozen at –20 ℃ overnight. The next day, cells are centrifuged at 500 × g for 10 minutes at 4 ℃ and washed twice with 3 ml of cold PBS. Cells are resuspended in 400 μl of propidium iodide staining solution (0.2 mg/ml RNAse A, 0.02 mg/ml propidium iodide, 0.1 % Triton-X in PBS) and incubated for 15 minutes at 37 ℃.
動物実験	動物モデル	tumor bearing NSG mice
	投薬量	8 mg/kg
	投与方法	Oral gavage

参考

https://pubmed.ncbi.nlm.nih.gov/32371576/

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：

Targeting of vulnerabilities of drug-tolerant persisters identified through functional genetics delays tumor relapse [ Cell Rep Med, 2024, 5(3):101471]	PubMed: 38508142
PD-1 instructs a tumor-suppressive metabolic program that restricts glycolysis and restrains AP-1 activity in T cell lymphoma [ Nat Cancer, 2023, 4(10):1508-1525]	PubMed: 37723306
Characterization of molecular mechanisms driving Merkel cell polyomavirus oncogene transcription and tumorigenic potential [ PLoS Pathog, 2023, 19(8):e1011598]	PubMed: 37647312
PD-1 instructs a tumor-suppressive metabolic program that restricts glycolysis and restrains AP-1 activity in T cell lymphoma [ Nat Cancer, 2023, 10.1038/s43018-023-00635-7]	PubMed: 37723306
Therapeutic impact of BET inhibitor BI 894999 treatment: backtranslation from the clinic [ Br J Cancer, 2022, 10.1038/s41416-022-01815-5]	PubMed: 35444289

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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