1. Cell Cycle/DNA Damage
    Cytoskeleton
  2. Microtubule/Tubulin

ELR510444 

Cat. No.: HY-16191 Purity: 95.55%
Data Sheet SDS Handling Instructions

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.

For research use only. We do not sell to patients.
ELR510444 Chemical Structure

ELR510444 Chemical Structure

CAS No. : 1233948-35-0

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO $154 In-stock
5 mg $140 In-stock
10 mg $220 In-stock
50 mg $660 In-stock
100 mg $1100 In-stock
200 mg   Get quote  
500 mg   Get quote  

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  • Biological Activity

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  • Technical Information

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  • References

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].

References
Preparing Stock Solutions
Concentration Volume 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
10 mM 0.2714 mL 1.3570 mL 2.7139 mL
Please refer to the solubility information to select the appropriate solvent.
References
Molecular Weight

368.47

Formula

C₁₉H₁₆N₂O₂S₂

CAS No.

1233948-35-0

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 37 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Product Name:
ELR510444
Cat. No.:
HY-16191
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