Abemaciclib

製品コードS5716 バッチS571605

印刷

化学情報

Synonyms

LY2835219

Storage
(From the date of receipt)

3 years -20°C powder

化学式

C₂₇H₃₂F₂N₈

分子量

506.59

CAS No.

1231929-97-7

Solubility (25°C)*

体外

Ethanol (warmed with 50ºC water bath)

11 mg/mL (21.71 mM)

DMSO (warmed with 50ºC water bath)

4 mg/mL (7.89 mM)

Water

Insoluble

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 Corn oil この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	0.200mg/ml (0.39mM)	Taking the 1 mL working solution as an example, add 50 μL of 4 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

* <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 is a cell cycle inhibitor selective for CDK4/6 with IC50 of 2 nM and 10 nM in cell-free assays, respectively.
in vitro	Abemaciclib highly selective inhibits the complexes CDK4/ cyclin D1 (IC50 =2 nmol/L) and CDK6/cyclin D1 (IC50 =10 nmol/L), with no activity against other CDK/cyclin complexes or cell-cycle-related kinases within the nanomolar ranges, except for inhibition of CDK9 at IC50 at least five times higher. Besides the cell-cycle dependent activity, abemaciclib is able to boost antitumor immunity by potentiating tumor antigen presentation and selectively suppressing proliferation of regulatory T (Treg) cells at the same time^[1]. Consistent with its activity against CDK4 and CDK6, abemaciclib inhibits RB phosphorylation and leads to G1 arrest in RB-proficient cell lines^[2]. In vitro, treatment with abemaciclib resulted in increased activation of human T cells and upregulated expression of antigen presentation genes in MCF-7 breast cancer cells^[3].
in vivo	In a colorectal cancer xenograft model used to develop an integrated pharmacokinetic/pharmacodynamic model, abemaciclib can be dosed orally on a continuous schedule to achieve sustained target inhibition and demonstrates not only durable cell-cycle inhibition but also single-agent antitumor activity. Tumor growth inhibition is observed in multiple other human cancer xenograft models, including those derived from non-small cell lung cancer (NSCLC), melanoma, glioblastoma, and mantle cell lymphoma. Abemaciclib distributes across the blood–brain barrier and prolongs survival in an intracranial glioblastoma xenograft model. In human, The pharmacokinetics of abemaciclib shows a slow absorption phase with a median time from oral dose to maximum plasma concentration (tmax) ranging from 4 to 6 hours. It is extensively cleared and distributed. The mean terminal elimination half-life (t1/2) ranged from 17.4 to 38.1 hours with no apparent dose-dependent change in clearance^[2].

プロトコル(参考用のみ)

細胞アッセイ	細胞株	CT26 tumor cell line
	濃度	0-10 μM
	反応時間	96 h
	実験の流れ	Tumor cells were cultured for 4 hr alone at 37°C, and then abemaciclib, palbociclib, or DMSO control was added at indicated concentrations for 96 hr at 37°C. Cell viability was then assessed.
動物実験	動物モデル	Athymic nude mice implanted with human NSCLC xenograft tumors
	投薬量	25, 50, or 100 mg/kg/d
	投与方法	oral

参考

https://pubmed.ncbi.nlm.nih.gov/29497278/
https://pubmed.ncbi.nlm.nih.gov/27217383/
https://pubmed.ncbi.nlm.nih.gov/29539425/

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：

Palmitoylation prevents B7-H4 lysosomal degradation sustaining tumor immune evasion [ Nat Commun, 2025, 16(1):4254]	PubMed: 40341398
SLFN11-mediated ribosome biogenesis impairment induces TP53-independent apoptosis [ Mol Cell, 2025, S1097-2765(25)00042-5]	PubMed: 39909041
PI3K/AKT signaling mediates stress-inducible amyloid formation through c-Myc [ Cell Rep, 2025, 44(5):115617]	PubMed: 40272983
Efficacy of CDK4/6 Inhibition in colorectal cancer and the role of p16 expression in predicting drug resistance [ Cell Oncol (Dordr), 2025, 10.1007/s13402-025-01080-7]	PubMed: 40522623
Intratumor heterogeneity in KRAS signaling shapes treatment resistance [ iScience, 2025, 28(2):111662]	PubMed: 39898020
Investigation of ribociclib, abemaciclib and palbociclib resistance in ER+ breast cancer cells reveal potential therapeutic opportunities` [ Sci Rep, 2025, 15(1):28579]	PubMed: 40764324
Abemaciclib induces G1 arrest and lysosomal dysfunction in canine melanoma cells: synergistic effects with fenbendazole [ Front Vet Sci, 2025, 12:1603686]	PubMed: 40642276
Ginsenoside Rg5 enhances Abemaciclib sensitivity in ER+ breast cancer by modulating cell cycle proteins via transcriptional and post-translational levels [ J Ginseng Res, 2025, 49(5):594-603]	PubMed: 40843016
Fibroblasts drive differential response in immunotherapy via IL-6 in bioengineered 3D cancer constructs [ bioRxiv, 2025, 2025.06.18.660473]	PubMed: 40667289
FRA1 drives melanoma metastasis through an actionable transcriptional network [ bioRxiv, 2025, 2025.06.07.658418]	PubMed: 40661443

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。