Abemaciclib mesylate

製品コードS7158 バッチS715804

化学情報

	Synonyms	LY2835219 mesylate	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₂₇H₃₂F₂N₈.CH₄O₃S
	分子量	602.7	CAS No.	1231930-82-7
Solubility (25°C)*	体外	Water	100 mg/mL (165.92 mM)
		DMSO	50 mg/mL (82.96 mM)
		Ethanol	13 mg/mL (21.56 mM)
* <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	Abemaciclib mesylate is a potent and selective inhibitor of CDK4 and CDK6 with IC50 of 2 nM and 10 nM in cell-free assays, respectively. Phase 3.
in vitro	LY2835219 is an orally available cyclin-dependent kinase (CDK) inhibitor that targets the CDK4 (cyclin D1) and CDK6 (cyclin D3) cell cycle pathway, with potential antineoplastic activity. LY2835219 specifically inhibits CDK4 and 6, thereby inhibiting retinoblastoma (Rb) protein phosphorylation in early G1. Inhibition of Rb phosphorylation prevents CDK-mediated G1-S phase transition, thereby arresting the cell cycle in the G1 phase, suppressing DNA synthesis and inhibiting cancer cell growth. Overexpression of the serine/threonine kinases CDK4/6, as seen in certain types of cancer, causes cell cycle deregulation. ^[1]
in vivo	LY2835219 saturates BBB efflux with an unbound plasma IC50 of about 95 nM. The percent of dose in brain for LY2835219-MsOH is 0.5–3.9%. In both a subcutaneous and intracranial human glioblastoma model (U87MG), LY2835219-MsOH suppressed tumor growth in a dose-dependent manner both as a single agent, and in combination with temozolomide. ^[1]

プロトコル(参考用のみ)

細胞アッセイ	細胞株	SYO-1 cells
	濃度	100 nM
	反応時間	24 h
	実験の流れ	Cells were cultured overnight and, on the next day (day 1), the media was replaced containing 100nM Abemaciclib or vehicle control (DMSO).
動物実験	動物モデル	Female C57BL/6 mice
	投薬量	50 mg/kg
	投与方法	i.p.

参考

カスタマーフィードバック

: Data from [Biochem J, 2014, 459(3), 513-24]

: Data from [Data independently produced by , , Cell Death Dis, 2018, 9(9):918]

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：

Intracellular calcium links milk stasis to lysosome-dependent cell death during early mammary gland involution [ Cell Mol Life Sci, 2024, 81(1):29]	PubMed: 38212474
mTORC1 activity oscillates throughout the cell cycle promoting mitotic entry and differentially influencing autophagy induction [ bioRxiv, 2024, 2024.02.06.579216]	PubMed: 38370755
cGAS-STING drives ageing-related inflammation and neurodegeneration [ Nature, 2023, 620(7973):374-380]	PubMed: 37532932
Cyclin E-induced replicative stress drives p53-dependent whole-genome duplication [ Cell, 2023, 186(3):528-542.e14]	PubMed: 36681079
Inhibition of CDK4/6 regulates AD pathology, neuroinflammation and cognitive function through DYRK1A/STAT3 signaling [ Pharmacol Res, 2023, 190:106725]	PubMed: 36907286
Sequential activation of E2F via Rb degradation and c-Myc drives resistance to CDK4/6 inhibitors in breast cancer [ Cell Rep, 2023, 42(11):113198]	PubMed: 37865915
CDK4/6 inhibitors induce replication stress to cause long-term cell cycle withdrawal [ EMBO J, 2022, 10.15252/embj.2021108599]	PubMed: 35037284
Clinically relevant CHK1 inhibitors abrogate wild-type and Y537S mutant ERα expression and proliferation in luminal primary and metastatic breast cancer cells [ J Exp Clin Cancer Res, 2022, 41(1):141]	PubMed: 35418303
Overexpressed Cyclin D1 and CDK4 proteins are responsible for the resistance to CDK4/6 inhibitor in breast cancer that can be reversed by PI3K/mTOR inhibitors [ Sci China Life Sci, 2022, 10.1007/s11427-021-2140-8]	PubMed: 35982377
Implementation of a combined CDK inhibition and arginine-deprivation approach to target arginine-auxotrophic glioblastoma multiforme cells [ Cell Death Dis, 2022, 13(6):555]	PubMed: 35717443

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。