Name: Cabazitaxel
Brand: Selleck Chemicals
SKU: S3022
Rating: 5 (33 reviews)

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Contrôle Qualité (Quality Control)

Lot : Pureté : 99.99%

99.99

Cibles apparentées	Akt Wnt/beta-catenin PKC HSP ROCK Integrin Bcr-Abl Actin FAK Kinesin
Autre Microtubule Associated Inhibiteurs	Nocodazole Patupilone (Epothilone B) CW069 Lexibulin (CYT997) Combretastatin A4 ABT-751 (E7010) Epothilone A Cucurbitacin B TRx0237 (LMTX) mesylate DM1 (Mertansine)

Culture cellulaire, traitement et concentration de travail
(Cell Culture, Treatment & Working Concentration)

Lignées cellulaires	Type d'essai	Temps d'incubation	Description de l'activité	PMID
SGC7901	Growth inhibition assay		Growth inhibition of human SGC7901 cells by MTT assay, GI50=0.0003553μM	24405702
U937	Growth inhibition assay		Growth inhibition of human U937 cells by MTT assay, GI50=0.0005391μM	24405702
MCF7	Growth inhibition assay		Growth inhibition of human MCF7 cells by MTT assay, GI50=0.001187μM	24405702
PANC1	Growth inhibition assay		Growth inhibition of human PANC1 cells by MTT assay, GI50=0.001283μM	24405702
HT1080	Growth inhibition assay		Growth inhibition of human HT1080 cells by MTT assay, GI50=0.001406μM	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
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
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
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
Cliquez pour voir plus de données expérimentales sur la lignée cellulaire

Informations chimiques, stockage et stabilité (Chemical Information, Storage & Stability)

Poids moléculaire	835.93	Formule	C₄₅H₅₇NO₁₄	Stockage (À compter de la date de réception)	3 ans-20°Cpoudre
N° CAS	183133-96-2	Télécharger le SDF		Stockage des solutions mères	1 an-80°Cen solvant 1 mois-20°Cen solvant
Synonymes	XRP6258, RPR-116258A, TXD 258, Taxoid XRP6258			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

Solubilité (Solubility)

In vitro
Lot:

DMSO : 167 mg/mL (199.77 mM)
(Le DMSO contaminé par l'humidité peut réduire la solubilité. Utiliser du DMSO frais et anhydre.)

Water : Insoluble

Ethanol : Insoluble

Calculateur de molarité

Masse	Concentration	Volume	Poids moléculaire
=	×	×

Calculateur de dilution Calculateur de poids moléculaire

In vivo Lot:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validé par les laboratoires Selleck. Si vous avez besoin d'ajustements à cette formulation, contactez notre équipe commerciale pour des tests personnalisés.	5.000mg/ml (5.98mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validé par les laboratoires Selleck. Si vous avez besoin d'ajustements à cette formulation, contactez notre équipe commerciale pour des tests personnalisés.	1.250mg/ml (1.50mM)	Taking the 1 mL working solution as an example, add 50 μL of 25 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

Calculateur de formulation in vivo (Solution claire)

Étape 1 : Saisir les informations ci-dessous (Recommandé : Un animal supplémentaire pour tenir compte des pertes pendant l'expérience)

Dosage : mg/kg Poids moyen des animaux : g Volume de dosage par animal :μL Nombre d'animaux :

Étape 2 : Saisir la formulation in vivo (Ceci est seulement le calculateur, pas la formulation. Veuillez nous contacter d'abord s'il n'y a pas de formulation in vivo dans la section Solubilité.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Résultats du calcul :

Concentration de travail : mg/ml;

Méthode de préparation du liquide maître DMSO : mg médicament prédissous dans μL DMSO ( Concentration du liquide maître mg/mL, Veuillez nous contacter d'abord si la concentration dépasse la solubilité du DMSO du lot de médicament. )

Méthode de préparation de la formulation in vivo : Prendre μL DMSO liquide maître, puis ajouterμL PEG300, mélanger et clarifier, puis ajouterμL Tween 80, mélanger et clarifier, puis ajouter μL ddH₂O, mélanger et clarifier.

Méthode de préparation de la formulation in vivo : Prendre μL DMSO liquide maître, puis ajouter μL Huile de maïs, mélanger et clarifier.

Note : 1. Veuillez vous assurer que le liquide est clair avant d'ajouter le solvant suivant.
2. Assurez-vous d'ajouter le(s) solvant(s) dans l'ordre. Vous devez vous assurer que la solution obtenue, lors de l'ajout précédent, est une solution claire avant de procéder à l'ajout du solvant suivant. Des méthodes physiques telles que le vortex, les ultrasons ou le bain-marie chaud peuvent être utilisées pour faciliter la dissolution.

Mécanisme d'action (Mechanism of Action)

Caractéristiques	A semi-synthetic derivative of a natural taxoid.
Targets/IC₅₀/Ki	Microtubule (Cell-free assay)
In vitro	Cabazitaxel increases CYP3A enzyme activities in rat hepatocytes. The mean ex-vivo human plasma protein binding of this compound is 91.6%. It is rapidly and extensively metabolised in numerous metabolites. This compound demonstrates activity in several murine and human resistant cell lines. With a 4-day exposure to this chemical, cytotoxicity is noted with relatively low cabazitaxel concentrations. It shows high antitumor activity in 3 human colorectal cell lines (HCT-116, HCT-8, and HT-29).
In vivo	In accompanying models, Cabazitaxel is noted to have significant antitumor activity. In murine tumor xenografts (colon C38 and pancreas P03), this compound elicites complete tumor regressions. Using SF-295 and U251 human glioblastoma cell lines, both orthotopic and subcutaneous murine xenografts are generated. This chemical treatment leads to complete regression in the majority of subcutaneously implanted tumors. Furthermore, in orthotopic models, it leads to complete tumor regression in 4 out of 10 U251 tumors.
Références	[1] http://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Public_assessment_report/human/002018/WC500104766.pdf [2] https://pubmed.ncbi.nlm.nih.gov/21152241/ [3] https://pubmed.ncbi.nlm.nih.gov/36123339/ [4] https://pubmed.ncbi.nlm.nih.gov/27608834/

Informations sur l'essai clinique (Clinical Trial Information)

(données du https://clinicaltrials.gov, mis à jour le 2026-09-02)

Numéro NCT	Recrutement	Conditions	Promoteur/Collaborateurs	Date de début	Phases
NCT06632977	RECRUITING	Castration-Resistant Prostate Carcinoma; Stage IVB Prostate Cancer AJCC v8	Alliance for Clinical Trials in Oncology	2025-02-06	PHASE2
NCT07213674	RECRUITING	Metastatic Castration-resistant Prostate Cancer	Amgen	2025-11-28	PHASE3
NCT06470243	RECRUITING	Castration-Resistant Prostate Carcinoma; Stage IVB Prostate Cancer AJCC v8	SWOG Cancer Research Network	2024-11-27	PHASE3
NCT07611110	RECRUITING	Metastatic Castration-resistant Prostate Cancer	AstraZeneca	2026-05-04	PHASE3
NCT06353386	RECRUITING	Prostatic Neoplasms, Castration-Resistant	Merck Sharp & Dohme LLC	2024-05-20	PHASE1; PHASE2
NCT06691984	ACTIVE_NOT_RECRUITING	Metastatic Castration-resistant Prostate Cancer	Amgen	2024-12-09	PHASE3

Foire aux questions (Frequently Asked Questions)

Question 1:
What is the elimination half-life of this compound?

Réponse :
According to the paper report, its elimination half-life 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):

Cabazitaxel Microtubule Associated Inhibiteur

Poids moléculaire: 835.93

Contrôle Qualité (Quality Control)

Culture cellulaire, traitement et concentration de travail
(Cell Culture, Treatment & Working Concentration)

Informations chimiques, stockage et stabilité (Chemical Information, Storage & Stability)

Solubilité (Solubility)

Calculateur de molarité

Calculateur de formulation in vivo (Solution claire)

Mécanisme d'action (Mechanism of Action)

Informations sur l'essai clinique (Clinical Trial Information)

Foire aux questions (Frequently Asked Questions)

Cabazitaxel Microtubule Associated Inhibiteur

Poids moléculaire: 835.93

Contrôle Qualité (Quality Control)

Culture cellulaire, traitement et concentration de travail (Cell Culture, Treatment & Working Concentration)

Informations chimiques, stockage et stabilité (Chemical Information, Storage & Stability)

Solubilité (Solubility)

Calculateur de molarité

Calculateur de formulation in vivo (Solution claire)

Mécanisme d'action (Mechanism of Action)

Informations sur l'essai clinique (Clinical Trial Information)

Foire aux questions (Frequently Asked Questions)

Culture cellulaire, traitement et concentration de travail
(Cell Culture, Treatment & Working Concentration)