Abemaciclib (LY2835219) Mesylate

製品コードS7158 バッチS715806

印刷

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)

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。	0.150mg/ml (0.25mM)	Taking the 1 mL working solution as an example, add 50 μL of 3 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 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

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：

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
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
Overexpression of COL11A1 confers tamoxifen resistance in breast cancer [ NPJ Breast Cancer, 2024, 10(1):38]	PubMed: 38806505
Patient-derived rhabdomyosarcoma cells recapitulate the genetic and transcriptomic landscapes of primary tumors [ iScience, 2024, 27(10):110862]	PubMed: 39319271
A live single-cell reporter system reveals drug-induced plasticity of a cancer stem cell-like population in cholangiocarcinoma [ Sci Rep, 2024, 14(1):22619]	PubMed: 39349745
mTORC1 activity oscillates throughout the cell cycle promoting mitotic entry and differentially influencing autophagy induction [ bioRxiv, 2024, 2024.02.06.579216]	PubMed: 38370755

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。