Trilaciclib

製品コードS8389 バッチS838902

印刷

化学情報

Chemical Structure Synonyms G1T28, G1T28-1 Storage
(From the date of receipt)		 3 years -20°C powder
化学式

C24H30N8O
分子量 446.55 CAS No. 1374743-00-6
Solubility (25°C)* 体外 DMSO 2 mg/mL (4.47 mM)
Water Insoluble
Ethanol 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.
* <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 Trilaciclibは、高効力、選択的かつ可逆的なサイクリン依存性キナーゼ4および6（CDK4/6）阻害剤です。Trilaciclibは、CDK4/サイクリンD1およびCDK6/サイクリンD3をそれぞれ1 nMおよび4 nMのIC50で阻害します。
in vitro

Trilaciclib is a potent and selective CDK4/6 inhibitor that inhibits the phosphorylation of RB and induces an exclusive, reversible G1 arrest. In vitro and in vivo, this compound protects RB competent cells from damage by chemotherapy as assessed by gamma-H2A.X (γH2AX) and apoptosis through caspase 3/7 activation.
in vivo

In vivo, this compound regulates the proliferation of HSPCs in both mouse and canine bone marrow, in a reversible, doseand time-dependent manner. Pretreatment of mice with this compound allows a faster recovery of complete blood counts (CBCs) following chemotherapy. In addition, it does not protect RB deficient tumors from chemotherapy but, instead, adds to the anti-tumor effect.

プロトコル(参考用のみ)

細胞アッセイ 細胞株 HS68 cells, WM2664 cells, A2058 cells
濃度 10 nM, 30 nM, 100 nM, 300 nM, 1000 nM
反応時間 4 h, 8 h, 16 h, 24 h
実験の流れ

HS68, WM2664 and A2058 cells are treated with 300 nM this compound or DMSO (0.1%), for 4, 8, 16 or 24 hours. Whole cell extracts are prepared using 1× radioimmunoprecipitation assay buffer (RIPA) containing 1× HALT protease and phosphatase inhibitors. Total protein concentration is determined by using the bicinchoninic acid (BCA) Protein Assay Kit, according to manufacturer's instructions. Fifteen micrograms of protein is heat denatured for 10 minutes at 70 ℃ and resolved by Novex NuPAGE SDS-PAGE gel system and transferred to 0.45 μm nitrocellulose membrane by electroblotting. Membranes are blocked in LiCor Membrane Blocking Buffer and incubated overnight with rabbit anti-pRb (Ser807/811) antibody at a 1:1,000 dilution and mouse anti-MAPK antibody at a 1:2,000 dilution, as a loading control. Secondary antibodies (LiCor) are Goat anti- rabbit (680RD) and Goat antimouse (800CW) at a 1:15,000 dilution. Blots are incubated for one hour, washed and imaged using LiCor ImageStudio software.
動物実験 動物モデル 8-week-old female FVB mice
投薬量 50 mg/kg, 100 mg/kg, 150 mg/kg
投与方法 Oral gavage

参考

  • https://pubmed.ncbi.nlm.nih.gov/26826116/
  • https://pubmed.ncbi.nlm.nih.gov/33004541/

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
Trilaciclib triggers a neutrophil-related immune response and sensitizes non-small cell lung cancer to anti-PD-1 therapy [ Cell Rep Med, 2025, 6(11):102434] PubMed: 41197618
Proteomic Analysis Reveals Trilaciclib-Induced Senescence [ Mol Cell Proteomics, 2024, 23(6):100778] PubMed: 38679389
The combination of breast cancer PDO and mini-PDX platform for drug screening and individualized treatment [ J Cell Mol Med, 2024, 28(9):e18374] PubMed: 38722288

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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