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Signaling Pathway

ELR510444

HY-16191

(ELR-510444)

ELR510444

ELR510444 Chemical Structure

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.

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Free sample   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
Size Price Stock Quantity
Free sample   Apply now  
10 mM * 1 mL in DMSO €151 In-stock
5 mg €137 In-stock
10 mg €216 In-stock
50 mg €647 In-stock
100 mg €1078 In-stock
200 mg Get quote
500 mg Get quote

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

ELR510444 Data Sheet

  • Network Version

    DataSheet

Related Compound Libraries

Biological Activity of ELR510444

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].

Protocol (Extracted from published papers and Only for reference)

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Chemical Information

M.Wt 368.47 Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Formula C₁₉H₁₆N₂O₂S₂
CAS No 1233948-35-0
Solvent & Solubility

DMSO: ≥ 37 mg/mL

Preparing Stock Solutions

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

References on ELR510444

Inhibitor Kit

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