Cabazitaxel

別名:XRP6258, RPR-116258A, TXD 258, Taxoid XRP6258

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.

Cabazitaxel化学構造

CAS No. 183133-96-2

サイズ 価格(税別) 在庫状況
10mM (1mL in DMSO) JPY 96600 国内在庫あり
JPY 30200 国内在庫あり
JPY 46800 国内在庫あり

代表番号: 045-509-1970|電子メール:[email protected]
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文献中Selleckの製品使用例(27)

カスタマーフィードバック5个实验数据

製品安全説明書

現在のバッチを見る: 純度: 99.99%
99.99

Cabazitaxel関連製品

Microtubule Associated阻害剤の選択性比較

Cell Data

Cell Lines Assay Type Concentration Incubation Time 活性情報 PMID
MES-SA/Dx5 Growth inhibition assay 72 hrs Growth inhibition of human MES-SA/Dx5 cells after 72 hrs by SRB assay, IC50=0.015μM 29251920
NCI-H524 Cytotoxicity assay 2 hrs Cytotoxicity in human NCI-H524 cells pre-incubated for 2 hrs followed by compound wash out and subsequently incubated for 70 hrs by Cell Titer Glo assay, IC50=0.00026μM 30735385
HT1080 Growth inhibition assay Growth inhibition of human HT1080 cells by MTT assay, GI50=0.001406μM 24405702
PANC1 Growth inhibition assay Growth inhibition of human PANC1 cells by MTT assay, GI50=0.001283μM 24405702
MCF7 Growth inhibition assay Growth inhibition of human MCF7 cells by MTT assay, GI50=0.001187μM 24405702
U937 Growth inhibition assay Growth inhibition of human U937 cells by MTT assay, GI50=0.0005391μM 24405702
SGC7901 Growth inhibition assay Growth inhibition of human SGC7901 cells by MTT assay, GI50=0.0003553μM 24405702
DU145 Growth inhibition assay Growth inhibition of human DU145 cells by MTT assay, GI50=0.001429μM 24405702
A549 Growth inhibition assay Growth inhibition of human A549 cells by MTT assay, GI50=0.001483μM 24405702
A431 Growth inhibition assay Growth inhibition of human A431 cells by MTT assay, GI50=0.001483μM 24405702
HeLa Growth inhibition assay Growth inhibition of human HeLa cells by MTT assay, GI50=0.001799μM 24405702
K562 Growth inhibition assay Growth inhibition of human K562 cells by MTT assay, GI50=0.004186μM 24405702
HL60 Growth inhibition assay Growth inhibition of human HL60 cells by MTT assay, GI50=0.004736μM 24405702
BGC823 Growth inhibition assay Growth inhibition of human BGC823 cells by MTT assay, GI50=0.4672μM 24405702
A549 Cytotoxicity assay Cytotoxicity against human A549 cells, IC50=0.00148μM 28850227
TC32 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells 29435139
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells 29435139
Saos-2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells 29435139
LAN-5 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells 29435139
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells 29435139
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells 29435139
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells) 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells 29435139
TC32 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells 29435139
MG 63 (6-TG R) qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells 29435139
U-2 OS qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells 29435139
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells 29435139
Saos-2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells 29435139
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for OHS-50 cells 29435139
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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.
特性 A semi-synthetic derivative of a natural taxoid.
Targets
Microtubule [1]
(Cell-free assay)
In Vitro
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]

細胞実験 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.

In Vivo
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]

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04622761 Not yet recruiting
Prostate Cancer
The Clatterbridge Cancer Centre NHS Foundation Trust|University of Liverpool
January 15 2021 Phase 2
NCT04495179 Completed
Progressive Metastatic Castrate-Resistant Prostate Cancer
AstraZeneca|Parexel
August 4 2020 Phase 2
NCT03257891 Unknown status
Adrenocortical Carcinoma
Azienda Socio Sanitaria Territoriale degli Spedali Civili di Brescia|San Luigi Gonzaga Hospital
January 25 2018 Phase 2
NCT03043989 Terminated
Prostate Cancer
Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins|Maryland Technology Development Corporation
March 21 2017 Phase 1

化学情報

分子量 835.93 化学式

C45H57NO14

CAS No. 183133-96-2 SDF Download Cabazitaxel SDFをダウンロードする
Smiles CC1=C2C(C(=O)C3(C(CC4C(C3C(C(C2(C)C)(CC1OC(=O)C(C(C5=CC=CC=C5)NC(=O)OC(C)(C)C)O)O)OC(=O)C6=CC=CC=C6)(CO4)OC(=O)C)OC)C)OC
保管

In vitro
Batch:

DMSO : 167 mg/mL ( (199.77 mM); 吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Water : Insoluble

Ethanol : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量 濃度 体積 分子量

投与溶液組成計算機(クリア溶液)

ステップ1:実験データを入力してください。(実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します)

mg/kg g μL

ステップ2:投与溶媒の組成を入力してください。(ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください)

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結果:

投与溶媒濃度: mg/ml;

DMSOストック溶液調製方法: mg 試薬を μL DMSOに溶解する(濃度 mg/mL, 注:濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法:Take μL DMSOストック溶液に μL PEG300,を加え、完全溶解後μL Tween 80,を加えて完全溶解させた後 μL ddH2O,を加え完全に溶解させます。

投与溶媒調製方法:μL DMSOストック溶液に μL Corn oil,を加え、完全溶解。

注意:1.ストック溶液に沈殿、混濁などがないことをご確認ください;
2.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

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よくある質問(FAQ)

質問1:
What is the elimination half-life of cabazitaxel?

回答
According to the paper report, the elimination half-life of cabazitaxel is 95h.

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