Home Cytoskeletal Signaling Microtubule Associated inhibitor Cabazitaxel

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Cabazitaxel Microtubule Associated inhibitor

Kat.-Nr.: S3022

Cabazitaxel is a semi-synthetic derivative of a natural taxoid that kills cancer cells by inhibiting cell division and growth. This compound exerts its effects by inhibiting microtubule growth and assembly, processes that are essential for cells to divide. It induces autophagy via the PI3K/Akt/mTOR pathway.
Cabazitaxel Microtubule Associated inhibitor Chemical Structure

Chemische Struktur

Molekulargewicht: 835.93

Springe zu

Qualitätskontrolle (Quality Control)

Charge: Reinheit: 99.99%
99.99

Zellkultur, Behandlung & Arbeitskonzentration
(Cell Culture, Treatment & Working Concentration)

Zelllinien Assay-Typ Konzentration Inkubationszeit Formulierung Aktivitätsbeschreibung 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
Klicken Sie hier, um weitere experimentelle Daten zu Zelllinien anzuzeigen

Chemische Informationen, Lagerung & Stabilität (Chemical Information, Storage & Stability)

Molekulargewicht 835.93 Formel

C45H57NO14

 Lagerung (Ab dem Eingangsdatum)
CAS-Nr. 183133-96-2 SDF herunterladen Lagerung von Stammlösungen

Synonyme 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

Löslichkeit (Solubility)

In vitro
Charge:

DMSO : 167 mg/mL (199.77 mM)
(Feuchtigkeitskontaminiertes DMSO kann die Löslichkeit verringern. Verwenden Sie frisches, wasserfreies DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molaritätsrechner

Masse Konzentration Volumen Molekulargewicht
Verdünnungsrechner Molekulargewichtsrechner

In vivo
Charge:

In-vivo-Formulierungsrechner (Klare Lösung)

Schritt 1: Geben Sie die untenstehenden Informationen ein (Empfohlen: Ein zusätzliches Tier zur Berücksichtigung von Verlusten während des Experiments)

mg/kg g μL

Schritt 2: Geben Sie die In-vivo-Formulierung ein (Dies ist nur der Rechner, keine Formulierung. Bitte kontaktieren Sie uns zuerst, wenn es im Abschnitt "Löslichkeit" keine In-vivo-Formulierung gibt.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Berechnungsergebnisse:

Arbeitskonzentration: mg/ml;

Methode zur Herstellung der DMSO-Stammlösung: mg Wirkstoff vorgelöst in μL DMSO ( Konzentration der Stammlösung mg/mL, Bitte kontaktieren Sie uns zuerst, wenn die Konzentration die DMSO-Löslichkeit der Wirkstoffcharge überschreitet. )

Methode zur Herstellung der In-vivo-Formulierung: Nehmen Sie μL DMSO Stammlösung, dann hinzufügenμL PEG300, mischen und klären, dann hinzufügenμL Tween 80, mischen und klären, dann hinzufügen μL ddH2O, mischen und klären.

Methode zur Herstellung der In-vivo-Formulierung: Nehmen Sie μL DMSO Stammlösung, dann hinzufügen μL Maisöl, mischen und klären.

Hinweis: 1. Bitte stellen Sie sicher, dass die Flüssigkeit klar ist, bevor Sie das nächste Lösungsmittel hinzufügen.
2. Achten Sie darauf, das/die Lösungsmittel der Reihe nach hinzuzufügen. Sie müssen sicherstellen, dass die bei der vorherigen Zugabe erhaltene Lösung eine klare Lösung ist, bevor Sie mit der Zugabe des nächsten Lösungsmittels fortfahren. Physikalische Methoden wie Vortex, Ultraschall oder ein heißes Wasserbad können zur Unterstützung des Lösens verwendet werden.

Wirkmechanismus (Mechanism of Action)

Merkmale
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.

Literatur
  • [4] https://pubmed.ncbi.nlm.nih.gov/27608834/

Klinische Studieninformationen (Clinical Trial Information)

(Daten von https://clinicaltrials.gov, aktualisiert am 2024-05-22)

NCT-Nummer Rekrutierung Erkrankungen Sponsor/Kooperationspartner Startdatum Phasen
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

Häufig gestellte Fragen (Frequently Asked Questions)

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

Antwort:
According to the paper report, its elimination half-life is 95h.