LY2835219 (Abemaciclib) Mesylate

製品コードS7158 バッチS715806

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	24 mg/mL (39.82 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 (LY2835219) Mesylateは、in vitroアッセイでCDK4とCDK6をそれぞれIC50 2 nMと10 nMで阻害する、強力で選択的な阻害剤です。現在、第3相試験が進行中です。
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.
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.

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

https://pubmed.ncbi.nlm.nih.gov/29497278/
https://pubmed.ncbi.nlm.nih.gov/33495604/
https://pubmed.ncbi.nlm.nih.gov/32929370/

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：

eIF4A Inhibitors Suppress Cell-Cycle Feedback Response and Acquired Resistance to CDK4/6 Inhibition in Cancer [ Molecular Cancer Therapeutics, November 1, 2019, 2158-2170]	PubMed: 31395685
Inhibition of ACAA1 Restrains Proliferation and Potentiates the Response to CDK4/6 Inhibitors in Triple-Negative Breast Cancer [ Cancer Research, May 15, 2023, 1711-1724]	PubMed: 37129951
Inhibition of CDK4/6 regulates AD pathology, neuroinflammation and cognitive function through DYRK1A/STAT3 signaling [ Pharmacological Research, March 11, 2023, 106725]	PubMed: 36907286
Clinical CDK4/6 inhibitors induce selective and immediate dissociation of p21 from cyclin D-CDK4 to inhibit CDK2 [ Nature Communications, June 7, 2021, 3356]	PubMed: 34099663
Phenotype-based probabilistic analysis of heterogeneous responses to cancer drugs and their combination efficacy [ PLoS Computational Biology, February 21, 2020, e1007688]	PubMed: 32084135
Combined therapy with DR5-targeting antibody-drug conjugate and CDK inhibitors as a strategy for advanced colorectal cancer [ Cell Rep Med, 2025, S2666-3791(25)00231-9]	PubMed: 40449480
A bedside-to-bench translational analysis of NF1 alterations and CDK4/6 inhibitor resistance in hormone receptor-positive metastatic breast cancer [ EBioMedicine, 2025, 118:105828]	PubMed: 40578027
MUC1-C dependency in drug resistant HR+/HER2- breast cancer identifies a new target for antibody-drug conjugate treatment [ NPJ Breast Cancer, 2025, 11(1):39]	PubMed: 40287441
ACSL4 promotes the formation of the proliferative subtype in hepatoblastoma [ BMC Cancer, 2025, 25(1):191]	PubMed: 39901207
SLC7A11 protects luminal A breast cancer cells against ferroptosis induced by CDK4/6 inhibitors [ Redox Biol, 2024, 76:103304]	PubMed: 39153252

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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