Palbociclib

製品コードS4482 バッチS448204

印刷

化学情報

 Chemical Structure Synonyms PD 0332991 Storage
(From the date of receipt)
3 years -20°C powder
化学式

C24H29N7O2

分子量 447.53 CAS No. 571190-30-2
Solubility (25°C)* 体外 DMSO Insoluble
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 Palbociclib (PD 0332991) is a highly specific inhibitor of cyclin-dependent kinase 4 (Cdk4) and Cdk6 with IC50 of 11 nM and 16 nM, respectively.This product has poor solubility, animal experiments are available, cell experiments please choose carefully!
in vitro

Palbociclib, a CKD4/6 inhibitor, significantly reduces HR+/HER2+ tumor cell viability when combinates with tucatinib and fulvestrant.[2]

in vivo

Palbociclib, a CKD4/6 inhibitor, shows superior efficacy in suppression of tumor growth in vivo when combinates with tucatinib and fulvestrant.[2]

プロトコル(参考用のみ)

細胞アッセイ 細胞株 BT474 and MDA-MB-361 tumor cell lines
濃度 0-15 μM
反応時間 72 h
実験の流れ

Cell viability is measured by Cell Titer Glo assay after 72 hours of treatment with vehicle or drugs. For all experiments with fulvestrant, cells are grown in estrogen free conditions, and estradiol is added to a final concentration of 10-8 M prior to drug treatment. Palbociclib, fulvestrant, and tucatinib IC30 values are calculated for each cell line, and the IC30 concentrations are used for subsequent experiments.

動物実験 動物モデル NCG mice injected with MDA-MB-361 cells
投薬量 50mg/kg
投与方法 o.g.

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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Testing Adaptive Therapy Protocols Using Gemcitabine and Capecitabine in a Preclinical Model of Endocrine-Resistant Breast Cancer [ Cancers (Basel), 2024, 16(2)257] PubMed: 38254748
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D-type cyclins regulate DNA mismatch repair in the G1 and S phases of the cell cycle, maintaining genome stability [ bioRxiv, 2024, 2024.01.12.575420] PubMed: 38260436
p21 Prevents the Exhaustion of Cluster of Differentiation 4-Positive T Cells Within the Antitumor Immune Response Against Colorectal Cancer [ Gastroenterology, 2023, S0016-5085(23)05008-4] PubMed: 37734420
Toxic PARP trapping upon cAMP-induced DNA damage reinstates the efficacy of endocrine therapy and CDK4/6 inhibitors in treatment-refractory ER+ breast cancer [ Nat Commun, 2023, 10.1038/s41467-023-42736-y] PubMed: 37914699

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。