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Chemical Structure| 1233948-35-0 Chemical Structure| 1233948-35-0

Structure of ELR510444
CAS No.: 1233948-35-0

Chemical Structure| 1233948-35-0

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ELR510444 is an inhibitor of tubulin polymerization with IC50 value of 10 μM.

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Product Details of ELR510444

CAS No. :1233948-35-0
Formula : C19H16N2O2S2
M.W : 368.47
SMILES Code : O=S(C1=CC=C(C)C=C1)(NC2=CC(C3=CC=C(C#N)S3)=CC=C2C)=O
MDL No. :MFCD25976813
InChI Key :GRYXROIHHXHFND-UHFFFAOYSA-N
Pubchem ID :46847888

Safety of ELR510444

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302
Precautionary Statements:P280-P305+P351+P338

Related Pathways of ELR510444

cytoskeleton

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
2H-11 tumor endothelial cells 11.7 nM 48 hours Evaluate the inhibitory effect of ELR510444 on cell proliferation, showing an IC50 of 11.7 nM J Pharmacol Exp Ther. 2011 Mar;336(3):652-60
MDA-MB-435 melanoma cells 9.0 nM 48 hours Evaluate the inhibitory effect of ELR510444 on cell proliferation, showing an IC50 of 9.0 nM J Pharmacol Exp Ther. 2011 Mar;336(3):652-60
MDA-MB-231 breast cancer cells 30.9 nM 48 hours Evaluate the inhibitory effect of ELR510444 on cell proliferation, showing an IC50 of 30.9 nM J Pharmacol Exp Ther. 2011 Mar;336(3):652-60
A498 cells 10 nM 24 hours To evaluate the effect of ELR510444 on HIF-2α expression. Results showed that ELR510444 significantly decreased HIF-2α expression. PLoS One. 2012;7(1):e31120
786-O cells 10 nM 24 hours To evaluate the effect of ELR510444 on HIF-2α expression. Results showed that ELR510444 significantly decreased HIF-2α expression. PLoS One. 2012;7(1):e31120
RCC4 cells 10 nM 24 hours To evaluate the effect of ELR510444 on HIF-1α and HIF-2α expression. Results showed that ELR510444 significantly decreased HIF-1α and HIF-2α expression. PLoS One. 2012;7(1):e31120
A10 embryonic rat aortic smooth muscle cells 30 nM 18 hours Evaluate the effect of ELR510444 on microtubule depolymerization, showing an EC50 of 21 nM J Pharmacol Exp Ther. 2011 Mar;336(3):652-60

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
BALB/c nude mice MDA-MB-231 xenograft model Oral 3, 6, 12.5 mg/kg Once daily for 28 days Evaluate the antitumor efficacy of ELR510444, showing significant antitumor activity at 6 mg/kg dose J Pharmacol Exp Ther. 2011 Mar;336(3):652-60
Nude mice (BALB/c background) 786-O and A498 RCC xenograft models Oral 8 mg/kg Once daily for 5 days, continued for 2 weeks To evaluate the antitumor efficacy of ELR510444 in RCC xenograft models. Results showed that ELR510444 significantly reduced tumor volume, increased tumor necrosis, and inhibited angiogenesis. PLoS One. 2012;7(1):e31120

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.71mL

0.54mL

0.27mL

13.57mL

2.71mL

1.36mL

27.14mL

5.43mL

2.71mL

References

 

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