Cabazitaxel

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

目錄號(hào)：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(xì)胞分裂和生長(zhǎng)，從而殺死癌細(xì)胞。抑制微管生長(zhǎng)和聚合。Cabazitaxel 可通過(guò)PI3K/Akt/mTOR信號(hào)通路誘導(dǎo)自噬。

Cabazitaxel Chemical Structure

CAS: 183133-96-2

規(guī)格	價(jià)格	庫(kù)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(chǎn)品質(zhì)控

批次：純度： 99.99%

99.99

Cabazitaxel相關(guān)產(chǎn)品

相關(guān)產(chǎn)品	Nocodazole Patupilone (Epothilone B) Lexibulin (CYT997) CW069 Combretastatin A4 ABT-751 (E7010) Epothilone A Cucurbitacin B TAI-1 Vindoline iHAP1 4-Demethylepipodophyllotoxin(NSC-122819,VM-26) MMAF TRx0237 (LMTX) mesylate INH1 Indibulin	點(diǎn)擊展開(kāi)
相關(guān)化合物庫(kù)	激酶抑制劑庫(kù) 血管生成相關(guān)化合物庫(kù) TGF-beta/Smad信號(hào)通路庫(kù) 細(xì)胞骨架信號(hào)通路化合物庫(kù) 抗心血管疾病化合物庫(kù)	點(diǎn)擊展開(kāi)

細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例

細(xì)胞系	實(shí)驗(yàn)類(lèi)型	孵育時(shí)間	活性描述	文獻(xiàn)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(diǎn)擊查看更多細(xì)胞系數(shù)據(jù)

生物活性

產(chǎn)品描述

特性

Cabazitaxel是一種天然紫杉烷的半合成品衍生物。

靶點(diǎn)

Microtubule ^[1]
(Cell-free assay)

體外研究(In Vitro)
體外研究活性	Cabazitaxel會(huì)增加大鼠肝細(xì)胞中CYP3A的酶活性。在體外人源血漿蛋白與Cabazitaxel平均結(jié)合率是91.6%。 Cabazitaxel會(huì)被迅速?gòu)V泛地代謝成多種代謝產(chǎn)物。Cabazitaxel在多個(gè)鼠和人的抗性細(xì)胞系中都有活性^[1]。用相對(duì)較低濃度的Cabazitaxel處理四天會(huì)產(chǎn)生明顯的細(xì)胞毒性。Cabazitaxel在3種結(jié)腸癌細(xì)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(huì)增加大鼠肝細(xì)胞中CYP3A的酶活性。在體外人源血漿蛋白與Cabazitaxel平均結(jié)合率是91.6%。 Cabazitaxel會(huì)被迅速?gòu)V泛地代謝成多種代謝產(chǎn)物。Cabazitaxel在多個(gè)鼠和人的抗性細(xì)胞系中都有活性^[1]。

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

體內(nèi)研究(In Vivo)
體內(nèi)研究活性	在其它相關(guān)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(jié)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(zhì)瘤細(xì)胞SF-295和U251建立原位和皮下的小鼠異種移植模型。Cabazitaxel對(duì)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(duì)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(yàn)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(xiàn)
[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(kāi)

參考文獻(xiàn)

[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(kāi)

化學(xué)信息&溶解度

分子量	835.93	分子式	C₄₅H₅₇NO₁₄
CAS號(hào)	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(chǔ)存條件(自收到貨起)	3年-20°C粉狀	儲(chǔ)備液保存和期限建議分裝儲(chǔ)備液，避免反復(fù)凍融！	1年-80°C溶于溶劑
儲(chǔ)存條件(自收到貨起)	3年-20°C粉狀	儲(chǔ)備液保存和期限建議分裝儲(chǔ)備液，避免反復(fù)凍融！	1個(gè)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(huì)降低化合物溶解度，請(qǐng)使用新開(kāi)封DMSO)

Water : Insoluble

Ethanol : Insoluble

DMSO : 100 mg/mL ( (119.62 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開(kāi)封DMSO)

Water : Insoluble

Ethanol : Insoluble

摩爾濃度計(jì)算器

體內(nèi)溶解度
批次：

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

動(dòng)物體內(nèi)配方計(jì)算器

實(shí)驗(yàn)計(jì)算

摩爾濃度計(jì)算器

質(zhì)量	濃度	體積	分子量
=	×	×

稀釋計(jì)算器分子量計(jì)算器

動(dòng)物體內(nèi)配方計(jì)算器（澄清溶液）

第一步：請(qǐng)輸入基本實(shí)驗(yàn)信息（考慮到實(shí)驗(yàn)過(guò)程中的損耗，建議多配一只動(dòng)物的藥量）

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

第二步：請(qǐng)輸入動(dòng)物體內(nèi)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(qǐng)聯(lián)系Selleck為您提供正確的澄清溶液配方）

% DMSO + % + % Tween 80 + % ddH2O

%DMSO+ %

計(jì)算結(jié)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(guò)該批次藥物DMSO溶解度，請(qǐng)先聯(lián)系Selleck）；

體內(nèi)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(nèi)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(jìn)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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常見(jiàn)問(wèn)題及建議解決方法

問(wèn)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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