Cabazitaxel
别名: XRP6258, RPR-116258A, TXD 258, Taxoid XRP6258 中文名称：卡巴他赛
Cabazitaxel是一种天然紫杉烷的半合成衍生物，能够抑制细胞分裂和生长，从而杀死癌细胞。抑制微管生长和聚合。Cabazitaxel 可通过PI3K/Akt/mTOR信号通路诱导自噬。
Cabazitaxel Chemical Structure
CAS: 183133-96-2
产品质控
批次：
纯度：
99.99%
99.99
Cabazitaxel相关产品
相关信号通路图
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息 |
|---|---|---|---|---|---|
| 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 | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | Cabazitaxel是一种天然紫杉烷的半合成衍生物，能够抑制细胞分裂和生长，从而杀死癌细胞。抑制微管生长和聚合。Cabazitaxel 可通过PI3K/Akt/mTOR信号通路诱导自噬。 | |
|---|---|---|
| 特性 | Cabazitaxel是一种天然紫杉烷的半合成品衍生物。 | |
| 靶点 |
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| 体外研究(In Vitro) | ||||
| 体外研究活性 | Cabazitaxel会增加大鼠肝细胞中CYP3A的酶活性。在体外人源血浆蛋白与Cabazitaxel平均结合率是91.6%。 Cabazitaxel会被迅速广泛地代谢成多种代谢产物。Cabazitaxel在多个鼠和人的抗性细胞系中都有活性[1]。 用相对较低浓度的Cabazitaxel处理四天会产生明显的细胞毒性。Cabazitaxel在3种结肠癌细胞株(HCT-116, HCT-8和 HT-29) 中都有很高的抗肿瘤活性[2]。 |
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|---|---|---|---|---|
| 体内研究(In Vivo) | ||
| 体内研究活性 | 在其它相关模型中 Cabazitaxel也有明显的抗肿瘤活性。在小鼠肿瘤异种移植模型 (结肠 C38 和 胰腺 P03)中Cabazitaxel具有完全的肿瘤抑制性。利用人恶性胶质瘤细胞SF-295和U251建立原位和皮下的小鼠异种移植模型。Cabazitaxel对大部分皮下移植的肿瘤具有完全抑制性。此外, Cabazitaxel 在原位模型中对40%的U251肿瘤具有抑制作用[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 |
化学信息&溶解度
| 分子量 | 835.93 | 分子式 | C45H57NO14 |
| CAS号 | 183133-96-2 | SDF | Download Cabazitaxel SDF |
| 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 | ||
| 储存条件(自收到货起) | |||
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体外溶解度 |
DMSO : 167 mg/mL ( (199.77 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Water : Insoluble Ethanol : Insoluble |
摩尔浓度计算器 |
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体内溶解度 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | ||||
实验计算
动物体内配方计算器（澄清溶液）
第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
mg/kg
g
μL
只
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
计算结果：
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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常见问题及建议解决方法
问题 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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