Bexarotene

製品コードS2098 バッチS209805

化学情報

	Synonyms	LGD1069	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₂₄H₂₈O₂
	分子量	348	CAS No.	153559-49-0
Solubility (25°C)*	体外	DMSO	69 mg/mL (198.27 mM)
		Water	Insoluble
		Ethanol	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	Bexarotene is a retinoid specifically selective for retinoid X receptors, used as an oral antineoplastic agent in the treatment of cutaneous T-cell lymphoma.
in vitro	Bexarotene treatment at 1 mM and 10 mM for 96 h increases the number of cells with sub-G1 populations and annexin V binding in a dose-dependent manner compared with vehicle controls (DMSO) in well-established CTCL cell lines (MJ, Hut78, and HH), respectively. Bexarotene treatment suppresses the expression of retinoid X receptor alpha and retinoic acid receptor alpha proteins in all three lines compared with untreated controls. Bexarotene treatment decreases the protein levels of survivin, activates caspase-3, and cleaved poly(ADP-Ribose) polymerase, but has no obvious effect on expression of Fas/Fas ligand and bcl-2 proteins in all three CTCL lines. ^[1] Bexarotene induces a loss of viability and more pronounced inhibition of clonogenic proliferation in HH and Hut-78 cells, whereas the MJ line exhibits resistance. Bexarotene upregulates and activates Bax in sensitive lines, although not enough to signal significant apoptosis. Bexarotene signals both G(1) and G(2)/M arrest by the modulation of critical checkpoint proteins. Bexarotene activates p53 by phosphorylation at Ser15, which influences the binding of p53 to promoters for cell cycle arrest, induces p73 upregulation, and, in concordance, also modulates some p53/p73 downstream target genes, such as p21, Bax, survivin and cdc2. ^[2]
in vivo	Bexarotene significantly prevents ER-negative mammary tumorigenesis with less toxicity than naturally occurring retinoids in animal models. Bexarotene inhibits the development of preinvasive mammary lesions such as hyperplasias and carcinoma-in-situ in MMTV-erbB2 mice. ^[3]

プロトコル(参考用のみ)

参考

カスタマーフィードバック

: Data from [Data independently produced by , , Neurol Res, 2018, 40(8):702-708]

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：

Whitening of brown adipose tissue inhibits osteogenic differentiation via secretion of S100A8/A9 [ iScience, 2024, 27(2):108857]	PubMed: 38303710
GZ17-6.02 interacts with bexarotene to kill mycosis fungoides cells [ Oncotarget, 2024, 15:124-133]	PubMed: 38329728
Chromatin accessibility dynamics dictate renal tubular epithelial cell response to injury [ Nat Commun, 2022, 13(1):7322]	PubMed: 36443310
Targeting the TR4 nuclear receptor with antagonist bexarotene can suppress the proopiomelanocortin signalling in AtT-20 cells [ J Cell Mol Med, 2021, 10.1111/jcmm.16074]	PubMed: 33491272
Targeting the TR4 nuclear receptor with antagonist bexarotene can suppress the proopiomelanocortin signalling in AtT-20 cells [ J Cell Mol Med, 2021, 25(5):2404-2417]	PubMed: 33491272
Effect of propylene glycol on the skin penetration of drugs [ Arch Dermatol Res, 2020, 312(5):337-352]	PubMed: 31786711
The support of genetic evidence for cardiovascular risk induced by antineoplastic drugs [ Sci Adv, 2020, 6(42)eabb8543]	PubMed: 33055159
[ Nat Metab, 2019, ]	PubMed: 31984309
Activation of retinoid X receptor by bexarotene attenuates neuroinflammation via PPARγ/SIRT6/FoxO3a pathway after subarachnoid hemorrhage in rats. [ J Neuroinflammation, 2019, 16(1):47]	PubMed: 30791908
Prediction of the skin permeability of topical drugs using in silico and in vitro models. [ Eur J Pharm Sci, 2019, 136:104945]	PubMed: 31163216

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。