2. Cell Cycle/DNA Damage Cytoskeleton Apoptosis
  3. Microtubule/Tubulin Apoptosis
  4. ELR510444

ELR510444 is a novel microtubule disruptor; inhibits MDA-MB-231 cell proliferation with IC50 of 30.

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ELR510444 Chemical Structure

ELR510444 Chemical Structure

CAS No. : 1233948-35-0

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Based on 1 publication(s) in Google Scholar

ELR510444 Related Antibodies

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1 Publications Citing Use of MCE ELR510444

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Description

ELR510444 is a novel microtubule disruptor; inhibits MDA-MB-231 cell proliferation with IC50 of 30.9 nM; not a substrate for the P-glycoprotein drug transporter and retains activity in βIII-tubulin-overexpressing cell lines. IC50 value: 30.9 nM(MDA-MB-231 cell) [1] Target: Microtubule disruptor ELR510444 is not a substrate for the P-glycoprotein drug transporter and retains activity in βIII-tubulin-overexpressing cell lines, suggesting that it circumvents both clinically relevant mechanisms of drug resistance to this class of agents. ELR510444 also shows potent antitumor activity in the MDA-MB-231 xenograft model with at least a 2-fold therapeutic window. Studies in tumor endothelial cells show that a low concentration of ELR510444 (30 nM) rapidly alters endothelial cell shape, similar to the effect of the vascular disrupting agent combretastatin A4. ELR510444 is a novel microtubule-disrupting agent with potential antivascular effects and in vivo antitumor efficacy [1]. ELR510444 decreased HIF-1α and HIF-2α levels, reduced RCC cell viability and clonogenic survival, and induced apoptosis. VHL-deficient RCC cells were more sensitive to ELR510444-mediated apoptosis and restoration of VHL promoted drug resistance. Higher concentrations of ELR51044 promoted apoptosis independently of VHL status, possibly due to the microtubule destabilizing properties of this agent. ELR510444 significantly reduced tumor burden in the 786-O and A498 RCC xenograft models [2].

Molecular Weight

368.47

Formula

C19H16N2O2S2
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=S(C1=CC=C(C)C=C1)(NC2=CC(C3=CC=C(C#N)S3)=CC=C2C)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : ≥ 37 mg/mL (100.42 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.7139 mL 13.5696 mL 27.1392 mL
5 mM 0.5428 mL 2.7139 mL 5.4279 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.7139 mL 13.5696 mL 27.1393 mL 67.8481 mL
5 mM 0.5428 mL 2.7139 mL 5.4279 mL 13.5696 mL
10 mM 0.2714 mL 1.3570 mL 2.7139 mL 6.7848 mL
15 mM 0.1809 mL 0.9046 mL 1.8093 mL 4.5232 mL
20 mM 0.1357 mL 0.6785 mL 1.3570 mL 3.3924 mL
25 mM 0.1086 mL 0.5428 mL 1.0856 mL 2.7139 mL
30 mM 0.0905 mL 0.4523 mL 0.9046 mL 2.2616 mL
40 mM 0.0678 mL 0.3392 mL 0.6785 mL 1.6962 mL
50 mM 0.0543 mL 0.2714 mL 0.5428 mL 1.3570 mL
60 mM 0.0452 mL 0.2262 mL 0.4523 mL 1.1308 mL
80 mM 0.0339 mL 0.1696 mL 0.3392 mL 0.8481 mL
100 mM 0.0271 mL 0.1357 mL 0.2714 mL 0.6785 mL
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

ELR5104441233948-35-0ELR 510444ELR-510444Microtubule/TubulinApoptosisInhibitorinhibitorinhibit

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