GMB-475

製品コードS8888 バッチS888801

化学情報

	Synonyms	N/A	Storage (From the date of receipt)	3 years -20°C powder
	化学式	C₄₃H₄₆F₃N₇O₇S
	分子量	861.93	CAS No.	2490599-18-1
Solubility (25°C)*	体外	DMSO	100 mg/mL (116.01 mM)
		Ethanol	50 mg/mL (58.0 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	GMB-475 is a proteolysis-targeting chimera (PROTAC) that allosterically targets BCR-ABL1 protein and recruit the E3 ligase Von Hippel-Lindau (VHL), resulting in ubiquitination and subsequent degradation of the oncogenic fusion protein.
in vitro	GMB-475 induces rapid proteasomal degradation and inhibition of downstream biomarkers, such as STAT5 in both human CML K562 cells and murine Ba/F3 cells expressing BCR-ABL1. GMB-475 inhibits the proliferation of certain clinically relevant BCR-ABL1 kinase domain point mutants and further sensitizes Ba/F3 BCR-ABL1 cells to inhibition by imatinib, while demonstrating no toxicity toward Ba/F3 parental cells.^[1]

製品説明

GMB-475 is a proteolysis-targeting chimera (PROTAC) that allosterically targets BCR-ABL1 protein and recruit the E3 ligase Von Hippel-Lindau (VHL), resulting in ubiquitination and subsequent degradation of the oncogenic fusion protein.

in vitro

GMB-475 induces rapid proteasomal degradation and inhibition of downstream biomarkers, such as STAT5 in both human CML K562 cells and murine Ba/F3 cells expressing BCR-ABL1. GMB-475 inhibits the proliferation of certain clinically relevant BCR-ABL1 kinase domain point mutants and further sensitizes Ba/F3 BCR-ABL1 cells to inhibition by imatinib, while demonstrating no toxicity toward Ba/F3 parental cells.^[1]

プロトコル(参考用のみ)

細胞アッセイ	細胞株	K562 cell line, Ba/F3 murine cell lines (Ba/F3 BCR-ABL1 cells, Ba/F3 parental cells)
	濃度	0.001-0.300 μM, 5 μM
	反応時間	3 days, 8 h
	実験の流れ	Cell viability assay: Cell lines and patient samples are exposed to dose ranges of GMB-475 (0.001-0.300 μM) and incubated for 3 days at 37°C, 5% CO2 and subjected to a CellTiter 96 AQueous One solution cell proliferation assay. Reverse phase protein arrays (RPPA): K562 cells are treated with DMSO, GMB-475 (5 μM) for 8 h in duplicate, washed twice with PBS and lysed in RPPA lysis buffer.

参考

[1] Burslem GM, et al. Cancer Res. 2019 Sep 15;79(18):4744-4753.

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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