Taxol

Protein target name:

Beta-Tubulin

Mechanism of action:

Stabilizes nonfunctional microtubules

Recommended Concentration for use in cells:

5 uM

Probe Availability

Abcam (105454-04-4)

Probe Information

Target and Probe Information

Target Details

Target class:

Structural protein

Subclass:

Cytoskeleton

Probe Details

Chemical Probes Portal ID:

CPP1629

Probe alias:

7 epi Taxol, 7-epi-Taxol, Anzatax, Bris Taxol, NSC 125973, NSC-125973, NSC125973, Onxol, Paclitaxel, Paxene, Praxel, Taxol, Taxol A

PubChem CID:

36314

ChEMBL ID:

CHEMBL428647

SMILES string:

CC1=C2[C@H](C(=O)[C@@]3([C@H](C[C@@H]4[C@]([C@H]3[C@@H]([C@@](C2(C)C)(C[C@@H]1OC(=O)[C@@H]([C@H](C5=CC=CC=C5)NC(=O)C6=CC=CC=C6)O)O)OC(=O)C7=CC=CC=C7)(CO4)OC(=O)C)O)C)OC(=O)C

InChi Key:

RCINICONZNJXQF-MZXODVADSA-N

Physico-chemical properties

Solubility - preferred solvent:

Ethanol

Solubility - concentration:

39 mg/mL

Validation in Cells and Model Organisms

In vitro validation

On target activity

Potency assay:

In in vitro microtubule assembly assays, taxol dose-dependently decreased lag time for microtubule assembly. Stabilized microtubules were resistant to CaCl2-induced depolymerization. Taxol decreased the critical concentration for tubulin assembly.

PDB ID for probe-target interaction (3D structure):

3J6U, 5SYF

Structure-activity relationship:

Yes, pharmacophore reported in PNAS (PMID: 10200249)

In cell validation

On target activity in cells

Target engagement assay (cells):

Modified version of taxol with a covalent warhead interacted with beta-tubulin.

Toxicity

Cytoxicity assay:

Yes

Notes on cytotoxicity:

Taxol is cytotoxic due to on-target activity, causing cell cycle arrest and cell death.

In vivo validation

Organism:

mouse (multiple strains), rabbit, rat (see PMID: 9491787)

Dose:

2-36 mg/kg

Route of delivery:

Intravenous

Plasma half life:

0.65-3.7 h

Systemic clearance:

0.15-2.94 L/h/kg

Cmax:

1.1-120 ug/mL

Organ of Interest

Organ (O):

Broad tissue distribution, poor CNS penetrance

Target engagement assay:

HPLC assays

Primary Reference

Reference (doi):

Nature J Biol Chem 10.1016/j.cell.2014.03.053 10.1016/j.jmb.2017.01.001 10.1073/pnas.96.8.4256

Reference (PMID):

423966 7906266 24855948 28104363 9491787 10200249

Taxol

Probe Availability

Probe Information

Target Details

Probe Details

Physico-chemical properties

In vitro validation

In cell validation

Toxicity

In vivo validation

Primary Reference

Supporting Organizations

Interested in supporting the portal?

Search form

Taxol

Probe Availability

Probe Information

Target Details

Probe Details

Physico-chemical properties

In vitro validation

In cell validation

Toxicity

In vivo validation

Primary Reference

Supporting Organizations

Interested in supporting the portal?