SB590885

製品コードS2220 バッチS222006

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	C₂₇H₂₇N₅O₂
	分子量	453.54	CAS No.	405554-55-4
Solubility (25°C)*	体外	DMSO	46 mg/mL (101.42 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	SB590885 is a potent B-Raf inhibitor with K_i of 0.16 nM in a cell-free assay, 11-fold greater selectivity for B-Raf over c-Raf, no inhibition to other human kinases.
in vitro	SB590885 displays significant selectivity for B-Raf over c-Raf with K_i of 0.16 nM over 1.72 nM. SB-590885 is a more potent inhibitor than the previously described Raf/VEGFR kinase inhibitor BAY 439006 (K_i = 38 nM for mutant B-Raf, 6 nM for c-Raf). SB590885 displays potent selectivity over 46 other kinases. Unlike the multi-kinase inhibitor BAY43-9006, SB590885 stabilizes the oncogenic B-Raf kinase domain in an active configuration. In Colo205, HT29, A375P, SKMEL28, and MALME-3M cells expressing oncogenic B-RafV600E, SB590885 treatment potently inhibits ERK phosphorylation with EC50 of 28 nM, 58 nM, 290 nM, 58 nM, and 190 nM, respectively, and consistently, inhibits the proliferation with EC50 of 0.1 μM, 0.87 μM, 0.37 μM, 0.12 μM, and 0.15 μM, respectively. SB590885 decreases anchorage-independent growth of melanoma cell lines in a BRAF mutant-selective manner. ^[1] SB590885 displays high affinity for B-Raf with Kd of 0.3 nM. ^[2] Most of the melanoma cell lines that harbor the BRAF V600E mutation and lack CDK4 mutations (451Lu, WM35, and WM983) are highly sensitive to SB590885 with IC50 of <1 μM. Increased levels of cyclin D1 resulting from genomic amplification mediate SB590885 resistance in B-Raf V600E-mutated melanomas. ^[3]
in vivo	Administration of SB590885 potently decreases tumorigenesis in murine xenografts established from mutant B-Raf-expressing A375P melanoma cells, and modestly inhibits tumor growth. ^[1]
特徴	Displays significant selectivity for B-Raf over c-Raf.

プロトコル(参考用のみ)

細胞アッセイ	細胞株	Colo205, HT29, A375P, SKMEL28, and MALME-3M
	濃度	Dissolved in DMSO, final concentrations ~10 μM
	反応時間	72 hours
	実験の流れ	Cells are treated with increasing concentrations of SB590885 and incubated for 72 hours. Viable cells are quantified using CellTiter-Glo reagent and luminescence detection on a Victor 2V plate reader. Cells are prepared for cell cycle analysis on a Becton Dickinson FACScan. Data is acquired and analyzed using CellQuest v3.3 software.
動物実験	動物モデル	Female nude mice injected s.c. with of A375P cells
	投薬量	50 mg/kg/day
	投与方法	Injection i.p.

参考

カスタマーフィードバック

: Data from [Invest New Drugs, 2014, 32(4), 626-35]

: Data from [Data independently produced by , , Oncotarget, 2015, 6(17):15250-64.]

: Data from [Data independently produced by , , Chembiochem, 2018, doi:10.1002/cbic.201800359]

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：

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Generation of a humanized mesonephros in pigs from induced pluripotent stem cells via embryo complementation [ Cell Stem Cell, 2023, 30(9):1235-1245.e6]	PubMed: 37683604
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Short C-terminal Musashi-1 proteins regulate pluripotency states in embryonic stem cells [ Cell Rep, 2023, 42(10):113308]	PubMed: 37858462
Chemical-induced epigenome resetting for regeneration program activation in human cells [ Cell Rep, 2023, 42(6):112547]	PubMed: 37224020
Discordance between chromatin accessibility and transcriptional activity during the human primed-to-naïve pluripotency transition process [ Cell Regen, 2023, 10.1186/s13619-023-00179-2]	PubMed: 37938437
Cell fate roadmap of human primed-to-naive transition reveals preimplantation cell lineage signatures [ Nat Commun, 2022, 13(1):3147]	PubMed: 35672317
Comprehensive Molecular Analysis Identified an SRSF Family-Based Score for Prognosis and Therapy Efficiency Prediction in Hepatocellular Carcinoma [ Cancers (Basel), 2022, 14(19)4727]	PubMed: 36230650
Biphasic Effect of Pirfenidone on Angiogenesis [ Biochem J, 2022, 479(3):401-424]	PubMed: 35147166

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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