Cabazitaxel

製品コードS3022 バッチS302202

印刷

化学情報

Chemical Structure Synonyms XRP6258, RPR-116258A, TXD 258, Taxoid XRP6258 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C45H57NO14
分子量 835.93 CAS No. 183133-96-2
Solubility (25°C)* 体外 DMSO 167 mg/mL (199.77 mM)
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 Cabazitaxel is a semi-synthetic derivative of a natural taxoid that kills cancer cells by inhibiting cell division and growth. Cabazitaxel exerts its effects by inhibiting microtubule growth and assembly, processes that are essential for cells to divide. Cabazitaxel induces autophagy via the PI3K/Akt/mTOR pathway.
in vitro

Cabazitaxel increases CYP3A enzyme activities in rat hepatocytes. The mean ex-vivo human plasma protein binding of Cabazitaxel is 91.6%. Cabazitaxel is rapidly and extensively metabolised in numerous metabolites. Cabazitaxel demonstrates activity in several murine and human resistant cell lines. [1]

With a 4-day exposure to cabazitaxel, cytotoxicity is noted with relatively low cabazitaxel concentrations. Cabazitaxel shows high antitumor activity in 3 human colorectal cell lines (HCT-116, HCT-8, and HT-29). [2]
in vivo

In accompanying models, Cabazitaxel is noted to have significant antitumor activity. In murine tumor xenografts (colon C38 and pancreas P03), Cabazitaxel elicites complete tumor regressions. Using SF-295 and U251 human glioblastoma cell lines, both orthotopic and subcutaneous murine xenografts are generated. Cabazitaxel treatment leads to complete regression in the majority of subcutaneously implanted tumors. Furthermore, in orthotopic models, Cabazitaxel leads to complete tumor regression in 4 out of 10 U251 tumors. [2]
特徴 A semi-synthetic derivative of a natural taxoid.

プロトコル(参考用のみ)

細胞アッセイ 細胞株 TFK1 cells
濃度 0.25 μM
反応時間 24 h
実験の流れ

Cells were treated with various concentrations of drug for 24 h.
動物実験 動物モデル Murine tumor xenografts (colon C38 and pancreas P03)
投薬量
投与方法

カスタマーフィードバック

, , Mol Cancer Ther, 2017, 16(10):2257-2266

, , Urol Oncol, 2015, 33(9):385.e15-20.

Data from [Data independently produced by , , Cell, 2018, 174(5):1200-1215]

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：

Fabrication of hyaluronic acid-altered gold complex delivery for head and neck squamous cell carcinoma therapy with high antitumor efficacy and low in vivo toxicity [ J Photochem Photobiol B, 2024, 253:112877] PubMed: 38484648
Targeting prostate tumor low-molecular weight tyrosine phosphatase for oxidation-sensitizing therapy [ Sci Adv, 2024, 10(5):eadg7887] PubMed: 38295166
Ritonavir reverses resistance to docetaxel and cabazitaxel in prostate cancer cells with acquired resistance to docetaxel [ Cancer Drug Resist, 2024, 7:3] PubMed: 38318527
Relevance of the organic anion transporting polypeptide 1B3 (OATP1B3) in the personalized pharmacological treatment of hepatocellular carcinoma [ Biochem Pharmacol, 2023, 214:115681] PubMed: 37429423
Berbamine targets cancer stem cells and reverses cabazitaxel resistance via inhibiting IGF2BP1 and p-STAT3 in prostate cancer [ Prostate, 2023, 10.1002/pros.24632] PubMed: 37828768
The therapeutic effect of KSP inhibitors in preclinical models of cholangiocarcinoma [ Cell Death Dis, 2022, 13-9:799] PubMed: 36123339
Activation of the ABCB1-amplicon promotes cellular viability and resistance to docetaxel and cabazitaxel in castration-resistant prostate cancer [ Mol Cancer Ther, 2021, molcanther.0983.2020] PubMed: 34326198
Proteomic analysis of extracellular vesicles identified PI3K pathway as a potential therapeutic target for cabazitaxel-resistant prostate cancer [ Prostate, 2021, 10.1002/pros.24138] PubMed: 33905554
DNA-PKc inhibition overcomes taxane resistance by promoting taxane-induced DNA damage in prostate cancer cells [ Prostate, 2021, 10.1002/pros.24200] PubMed: 34297853
The Role of Crosstalk between AR3 and E2F1 in Drug Resistance in Prostate Cancer Cells. [ Cells, 2020, 28;9(5)] PubMed: 32354165

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。