10074-G5

製品コードS8426 バッチS842601

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	C₁₈H₁₂N₄O₃
	分子量	332.31	CAS No.	413611-93-5
Solubility (25°C)*	体外	DMSO	66 mg/mL (198.6 mM)
		Ethanol	10 mg/mL warmed with 50ºC water bath (30.09 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	10074-G5 is a c-Myc inhibitor that binds to and distorts the bHLH-ZIP domain of c-Myc (Kd = 2.8 µM), thereby inhibiting c-Myc/Max heterodimer formation and inhibiting its transcriptional activity (IC50 = 146 µM).
in vitro	10074-G5 binds to and distorts the bHLH-ZIP domain of c-Myc, thereby inhibiting c-Myc/Max heterodimer formation and inhibiting its transcriptional activity. In vitro, 10074-G5 inhibits the growth of Daudi Burkitt's lymphoma cells and disrupts c-Myc/Max dimerization. Daudi cells accumulates 10074-G5, and the highest intracellular concentration is observed at 6 h. 10074-G5 inhibits c-Myc/Max dimerization in Daudi cells by approximately 75% at 4 h, and this inhibition is maintained through 24 h of incubation. Total c-Myc protein expression also decreases, and after 24 h exposure to 10 μM 10074-G5, c-Myc protein expression decreases approximately 40% compared with vehicle-treated control. 10074-G5 is cytotoxic in vitro against Daudi and HL-60 cells, which overexpress c-Myc ^[2].
in vivo	The plasma half-life of 10074-G5 in mice treated with 20 mg/kg i.v. is 37 min, and peak plasma concentration is 58 μM, which is 10-fold higher than peak tumor concentration. The lack of antitumor activity probably is caused by the rapid metabolism of 10074-G5 to inactive metabolites, resulting in tumor concentrations of 10074-G5 insufficient to inhibit c-Myc/Max dimerization. Plasma 10074-G5 peak concentration (Cmax) of 58.5 ± 2.7 nmol/ml is observed at 5 min after intravenous administration of 20 mg/kg to mice bearing Daudi xenografts, 10074-G5 concentration in plasma declines rapidly. Except for lung, liver, and fat, tissue concentrations of 10074-G5 are lower than those of plasma at all time points^[2].

プロトコル(参考用のみ)

細胞アッセイ	細胞株	Daudi cells
	濃度	10 μM
	反応時間	0, 1, 3, 6, or 24 h
	実験の流れ	Daudi cells (3 × 10⁸ cells in logarithmic growth) are incubated for 0, 1, 3, 6, or 24 h in 3 ml of complete medium containing 10 μM 10074-G5. After incubation, cells are harvested, split into two samples of 1.5 ml each, and overlaid in microcentrifuge tubes containing 0.5 ml of silicon oil. The tubes are centrifuged at 12,000g for 4 min. After centrifugation, the top 1 ml of medium is removed and stored in cryovials at −70°C until analysis. The remaining medium and silicon oil are carefully removed without disturbing the cell pellets. The sides of the tubes are cleaned with cotton-tipped applicators, and the cell pellets are stored at −70°C until analysis.
動物実験	動物モデル	Specific-pathogen-free, female C.B-17 SCID mice
	投薬量	20 mg/kg
	投与方法	i.v.

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：

SLC39A10 promotes malignant phenotypes of gastric cancer cells by activating the CK2-mediated MAPK/ERK and PI3K/AKT pathways [ Exp Mol Med, 2023, 10.1038/s12276-023-01062-5]	PubMed: 37524874
Inhibiting the glycerophosphodiesterase EDI3 in ER-HER2+ breast cancer cells resistant to HER2-targeted therapy reduces viability and tumour growth [ J Exp Clin Cancer Res, 2023, 42(1):25]	PubMed: 36670508
The calcium channel TRPC6 promotes chemotherapy-induced persistence by regulating integrin α6 mRNA splicing [ Cell Rep, 2023, 10.1016/j.celrep.2023.113347]	PubMed: 37910503
The ABL-MYC axis controls WIPI1-enhanced autophagy in lifespan extension [ Commun Biol, 2023, 6(1):872]	PubMed: 37620393
The ABL-MYC axis controls WIPI1-enhanced autophagy in lifespan extension [ Commun Biol, 2023, 6(1):872]	PubMed: 37620393
The ABL-MYC axis controls WIPI1-enhanced autophagy in lifespan extension [ Commun Biol, 2023, 6(1):872]	PubMed: 37620393
c-MYC-mediated TRIB3/P62+ aggresomes accumulation triggers paraptosis upon the combination of everolimus and ginsenoside Rh2 [ Acta Pharm Sin B, 2022, 12(3):1240-1253]	PubMed: 35530150
The insulin and IGF signaling pathway sustains breast cancer stem cells by IRS2/PI3K-mediated regulation of MYC [ Cell Rep, 2022, 41(10):111759]	PubMed: 36476848
c-Myc-PD-L1 Axis Sustained Gemcitabine-Resistance in Pancreatic Cancer [ Front Pharmacol, 2022, 13:851512]	PubMed: 35586061
c-Myc Represses Transcription of Epstein-Barr Virus Latent Membrane Protein 1 Early after Primary B Cell Infection. [ J Virol, 2018, 92(2)]	PubMed: 29118124

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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