Cabazitaxel

別名: XRP6258, RPR-116258A, TXD 258, Taxoid XRP6258 中文名稱：卡巴他賽

目錄號：S3022 Purity: 99.99%

Cabazitaxel是一種天然紫杉烷的半合成衍生物，能夠抑制細胞分裂和生長，從而殺死癌細胞。抑制微管生長和聚合。Cabazitaxel 可通過PI3K/Akt/mTOR信號通路誘導自噬。

Cabazitaxel Chemical Structure

CAS: 183133-96-2

規(guī)格	價格	庫存
10mM (1mL in DMSO)	1970	現(xiàn)貨
5mg	1396.08	現(xiàn)貨
200mg	11700	現(xiàn)貨
1g	23900	現(xiàn)貨
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產品質控

批次：純度： 99.99%

99.99

Cabazitaxel相關產品

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相關化合物庫	激酶抑制劑庫血管生成相關化合物庫 TGF-beta/Smad信號通路庫細胞骨架信號通路化合物庫抗心血管疾病化合物庫	點擊展開

細胞實驗數(shù)據(jù)示例

細胞系	實驗類型	孵育時間	活性描述	文獻信息
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
點擊查看更多細胞系數(shù)據(jù)

生物活性

產品描述

特性

Cabazitaxel是一種天然紫杉烷的半合成品衍生物。

靶點

Microtubule ^[1]
(Cell-free assay)

體外研究(In Vitro)
體外研究活性	Cabazitaxel會增加大鼠肝細胞中CYP3A的酶活性。在體外人源血漿蛋白與Cabazitaxel平均結合率是91.6%。 Cabazitaxel會被迅速廣泛地代謝成多種代謝產物。Cabazitaxel在多個鼠和人的抗性細胞系中都有活性^[1]。用相對較低濃度的Cabazitaxel處理四天會產生明顯的細胞毒性。Cabazitaxel在3種結腸癌細胞株(HCT-116, HCT-8和 HT-29) 中都有很高的抗腫瘤活性^[2]。

體外研究(In Vitro)

體外研究活性

Cabazitaxel會增加大鼠肝細胞中CYP3A的酶活性。在體外人源血漿蛋白與Cabazitaxel平均結合率是91.6%。 Cabazitaxel會被迅速廣泛地代謝成多種代謝產物。Cabazitaxel在多個鼠和人的抗性細胞系中都有活性^[1]。

用相對較低濃度的Cabazitaxel處理四天會產生明顯的細胞毒性。Cabazitaxel在3種結腸癌細胞株(HCT-116, HCT-8和 HT-29) 中都有很高的抗腫瘤活性^[2]。

體內研究(In Vivo)
體內研究活性	在其它相關模型中 Cabazitaxel也有明顯的抗腫瘤活性。在小鼠腫瘤異種移植模型 (結腸 C38 和胰腺 P03)中Cabazitaxel具有完全的腫瘤抑制性。利用人惡性膠質瘤細胞SF-295和U251建立原位和皮下的小鼠異種移植模型。Cabazitaxel對大部分皮下移植的腫瘤具有完全抑制性。此外, Cabazitaxel 在原位模型中對40%的U251腫瘤具有抑制作用^[2]。

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試驗信息 (data from https://clinicaltrials.gov, updated on 2024-05-22)
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

參考文獻
[1] EMEA/H/C/002018, 2011. [2] Pal SK, et al. Clin Interv Aging, 2010, 5, 395-402. [3] Shi Y, et al. Cell Death Dis. 2022 Sep 19;13(9):799. [4] Tai X, et al. J Drug Target. 2017 Feb;25(2):179-187. + 展開

參考文獻

[1] EMEA/H/C/002018, 2011.
[2] Pal SK, et al. Clin Interv Aging, 2010, 5, 395-402.
[3] Shi Y, et al. Cell Death Dis. 2022 Sep 19;13(9):799.

[4] Tai X, et al. J Drug Target. 2017 Feb;25(2):179-187.

+ 展開

化學信息&溶解度

分子量	835.93	分子式	C₄₅H₅₇NO₁₄
CAS號	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
儲存條件(自收到貨起)	3年-20°C粉狀	儲備液保存和期限建議分裝儲備液，避免反復凍融！	1年-80°C溶于溶劑
儲存條件(自收到貨起)	3年-20°C粉狀	儲備液保存和期限建議分裝儲備液，避免反復凍融！	1個月-20°C溶于溶劑

體外溶解度
批次：

DMSO : 167 mg/mL ( (199.77 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Water : Insoluble

Ethanol : Insoluble

DMSO : 100 mg/mL ( (119.62 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Water : Insoluble

Ethanol : Insoluble

摩爾濃度計算器

體內溶解度
批次：

現(xiàn)配現(xiàn)用，請按從左到右的順序依次添加，澄清后再加入下一溶劑

動物體內配方計算器

實驗計算

摩爾濃度計算器

質量	濃度	體積	分子量
=	×	×

稀釋計算器分子量計算器

動物體內配方計算器（澄清溶液）

第一步：請輸入基本實驗信息（考慮到實驗過程中的損耗，建議多配一只動物的藥量）

給藥劑量 mg/kg 動物平均體重 g 每只動物給藥體積 μL 動物數(shù)量只

第二步：請輸入動物體內配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請聯(lián)系Selleck為您提供正確的澄清溶液配方）

% DMSO + % + % Tween 80 + % ddH2O

%DMSO+ %

計算結果：

工作液濃度： mg/ml；

DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請先聯(lián)系Selleck）；

體內配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH₂O，混勻澄清。

體內配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。

注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。

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操作手冊

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* 必填項

常見問題及建議解決方法

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

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

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

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