Roscovitine

製品コードS1153 バッチS115310

印刷

化学情報

Chemical Structure Synonyms CYC202, Seliciclib, R-roscovitine Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C19H26N6O
分子量 354.45 CAS No. 186692-46-6
Solubility (25°C)* 体外 DMSO 71 mg/mL (200.31 mM)
Ethanol 71 mg/mL (200.31 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 40%PEG300 5%Tween80 50%ddH2O

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。

 10.000mg/ml (28.21mM) Taking the 1 mL working solution as an example, add 50 μL of 200 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to make it clear; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. 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 Roscovitine is a potent and selective CDK inhibitor for Cdc2, CDK2 and CDK5 with IC50 of 0.65 μM, 0.7 μM and 0.16 μM in cell-free assays. It shows little effect on CDK4/6. Phase 2.
in vitro

Roscovitine displays high efficiency and high selectivity towards some cyclin-dependent kinases with IC50 of 0.65, 0.7, 0.7 and 0.16 μM for cdc2/cyclin B, cdk2/cyclin A, cdk2/cyclin E and cdk5/p53, respectively. [1] This compound reversibly inhibits the prophaselmetaphase transition in the micromolar range of starfish oocytes and sea urchin embryos, inhibits in vitro M-phase-promoting factor activity and in vitro DNA synthesis in Xenopus egg extracts, and suppresses the proliferation of mammalian cell lines with an average IC50 of 16 μM. [1] In mesangial cells, it results in a dose-dependent reduction of CDK2 activity that at concentrations of 7.5, 12.5 and 25 mM, this chemical causes a 25, 50% and 100% decrease in CDK2 activity, respectively. [2] A recent study shows that this compound inhibits cdk5 kinase activity, cell proliferation, multicellular development, and cdk5 nuclear translocation in Dictyostelium discoideum, without affecting the expression of cdk5 protein during axenic growth. [3]
in vivo

Roscovitine, at a dose of 50 mg/kg, significantly inhibits growth of The Ewing's sarcoma family of tumors (ESFT) xenografts. [4] This compound enhances the antitumor effect of doxorubicin without increased toxicity with a mechanism that involves cell cycle arrest rather than apoptosis in nude mice bearing established MCF7 xenografts. [5]

プロトコル(参考用のみ)

キナーゼアッセイ Enzymes
[API调用失败: invalid chat.event: ping, {'event': 'ping', 'data': '{"timestamp_ms":"1763706911366"}'}]
細胞アッセイ 細胞株 Leukemia, non-small cell lung cancer, colon cancer, central nervous system cancer, melanoma, ovarian cancer, renal cancer, prostate cancer, breast cancer
濃度 0.01 - 100 μM
反応時間 48 hours
実験の流れ

60 human tumour cell lines comprising nine tumor types are cultured for 24 hours prior to a 48-hour continuous exposure to 0.01-100 μM roscovitine. A sulforhodaminine B protein assay is used to estimate the cytotoxicity.
動物実験 動物モデル A4573 cells are injected s.c. into the right posterior flank of CD1 nu/nu mice.
投薬量 ≤50 mg/kg
投与方法 Administered via i.p.

参考

  • https://pubmed.ncbi.nlm.nih.gov/9030781/
  • https://pubmed.ncbi.nlm.nih.gov/9366565/
  • https://pubmed.ncbi.nlm.nih.gov/22234985/
  • https://pubmed.ncbi.nlm.nih.gov/16230394/
  • https://pubmed.ncbi.nlm.nih.gov/19003963/

カスタマーフィードバック

Data from [J Hematol Oncol, 2012, 7, 53]

Data from [PNAS, 2011, 108, 8417]

Data from [PNAS, 2011, 108, 8417]

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
Roscovitine alleviates PTSD-like cognitive impairment by inhibiting CDK5-mediated Tau hyperphosphorylation [ Brain Res Bull, 2025, 232:111591] PubMed: 41110674
A deep single cell mass cytometry approach to capture canonical and noncanonical cell cycle states [ bioRxiv, 2025, 2025.07.08.663243] PubMed: 40672327
Switch-like phosphorylation of WRN integrates end-resection with RAD51 metabolism at collapsed replication forks [ Nucleic Acids Res, 2024, gkae807] PubMed: 39315694
An E7-retinoblastoma protein pathway mechanism may account for the higher carcinogenic ability of HPV16 over HPV58 in cervical cancer [ Transl Cancer Res, 2024, 13(4):1876-1886] PubMed: 38737678
Multiplex single-cell chemical genomics reveals the kinase dependence of the response to targeted therapy [ Cell Genom, 2024, 4(2):100487] PubMed: 38278156
Cytoplasmic division cycles without the nucleus and mitotic CDK/cyclin complexes [ Cell, 2023, 186(21):4694-4709.e16] PubMed: 37832525
Cytoplasmic division cycles without the nucleus and mitotic CDK/cyclin complexes [ Cell, 2023, 186(21):4694-4709.e16] PubMed: 37832525
Polarized microtubule remodeling transforms the morphology of reactive microglia and drives cytokine release [ Nat Commun, 2023, 14(1):6322] PubMed: 37813836
Polarized microtubule remodeling transforms the morphology of reactive microglia and drives cytokine release [ Nat Commun, 2023, 14(1):6322] PubMed: 37813836

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。