ELR510444
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MedKoo CAT#: 406612

CAS#: 1233948-35-0

Description: ELR510444 is a potent microtube disruptor with potential anticancer activity. ELR510444 has potent microtubule-disrupting activity, causing a loss of cellular microtubules and the formation of aberrant mitotic spindles and leading to mitotic arrest and apoptosis of cancer cells. ELR510444 potently inhibited cell proliferation with an IC(50) value of 30.9 nM in MDA-MB-231 cells, inhibited the rate and extent of purified tubulin assembly, and displaced colchicine from tubulin, indicating that the drug directly interacts with tubulin at the colchicine-binding site.


Chemical Structure

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ELR510444
CAS# 1233948-35-0

Theoretical Analysis

MedKoo Cat#: 406612
Name: ELR510444
CAS#: 1233948-35-0
Chemical Formula: C19H16N2O2S2
Exact Mass: 368.07
Molecular Weight: 368.470
Elemental Analysis: C, 61.93; H, 4.38; N, 7.60; O, 8.68; S, 17.40

Price and Availability

Size Price Availability Quantity
10mg USD 150 Ready to ship
25mg USD 250 Ready to ship
50mg USD 450 Ready to ship
100mg USD 650 Ready to ship
200mg USD 950 Ready to ship
500mg USD 1650 Ready to ship
1g USD 2450 2 weeks
2g USD 3950 2 weeks
5g USD 5750 2 weeks
Bulk inquiry

Synonym: ELR510444; ELR-510444; ELR 510444.

IUPAC/Chemical Name: N-(5-(5-cyanothiophen-2-yl)-2-methylphenyl)-4-methylbenzenesulfonamide

InChi Key: GRYXROIHHXHFND-UHFFFAOYSA-N

InChi Code: InChI=1S/C19H16N2O2S2/c1-13-3-8-17(9-4-13)25(22,23)21-18-11-15(6-5-14(18)2)19-10-7-16(12-20)24-19/h3-11,21H,1-2H3

SMILES Code: O=S(C1=CC=C(C)C=C1)(NC2=CC(C3=CC=C(C#N)S3)=CC=C2C)=O

Appearance: Yellow solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:         

Biological target: ELR-510444 is a novel microtubule disruptor with potential antivascular effects and in vivo antitumor efficacy, causing a loss of cellular microtubules and the formation of aberrant mitotic spindles and leading to mitotic arrest and apoptosis of cancer cells.
In vitro activity: ELR510444 has potent microtubule-disrupting activity, causing a loss of cellular microtubules and the formation of aberrant mitotic spindles and leading to mitotic arrest and apoptosis of cancer cells. ELR510444 potently inhibited cell proliferation with an IC(50) value of 30.9 nM in MDA-MB-231 cells, inhibited the rate and extent of purified tubulin assembly, and displaced colchicine from tubulin, indicating that the drug directly interacts with tubulin at the colchicine-binding site. 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. These data show a close correlation between the concentration of ELR510444 required for inhibition of cellular proliferation and that required to cause significant loss of cellular microtubule density, consistent with its activity as a microtubule depolymerizer. Reference: J Pharmacol Exp Ther. 2011 Mar;336(3):652-60. https://www.ncbi.nlm.nih.gov/pmc/articles/pmid/21148249/
In vivo activity: To further investigate the anticancer activity of ELR510444, its efficacy was evaluated in the 786-O and A498 RCC mouse xenograft models. 786-O and A498 tumor-bearing animals were randomized into groups and given 8 mg/kg ELR510444 orally for 2 weeks on a QDx5 (every day for 5 days) schedule. Treatment with ELR510444 significantly decreased mean tumor volume in both xenograft models compared to the vehicle-treated controls (Figure 6A). Importantly, ELR510444 was very well tolerated as no significant animal weight loss was observed throughout the duration of the study (Figure 6B). Further analysis of tumors harvested at the end of the study revealed a significant reduction in tumor cell proliferation as measured by PCNA staining (Figure 6C) and an increase in cleaved caspase-3 levels, a marker of apoptosis (Figure 6D). Collectively, these data demonstrate that ELR510444 has significant in vivo activity in RCC tumor models. Reference: PLoS One. 2012;7(1):e31120. https://www.ncbi.nlm.nih.gov/pmc/articles/pmid/22295124/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 73.0 198.12
Ethanol 24.0 65.13

Preparing Stock Solutions

The following data is based on the product molecular weight 368.47 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
In vitro protocol: 1. Carew JS, Esquivel JA 2nd, Espitia CM, Schultes CM, Mülbaier M, Lewis JD, Janssen B, Giles FJ, Nawrocki ST. ELR510444 inhibits tumor growth and angiogenesis by abrogating HIF activity and disrupting microtubules in renal cell carcinoma. PLoS One. 2012;7(1):e31120. doi: 10.1371/journal.pone.0031120. Epub 2012 Jan 25. PMID: 22295124; PMCID: PMC3266297. 2. Risinger AL, Westbrook CD, Encinas A, Mülbaier M, Schultes CM, Wawro S, Lewis JD, Janssen B, Giles FJ, Mooberry SL. ELR510444, a novel microtubule disruptor with multiple mechanisms of action. J Pharmacol Exp Ther. 2011 Mar;336(3):652-60. doi: 10.1124/jpet.110.175331. Epub 2010 Dec 9. PMID: 21148249; PMCID: PMC3061540.
In vivo protocol: 1. Carew JS, Esquivel JA 2nd, Espitia CM, Schultes CM, Mülbaier M, Lewis JD, Janssen B, Giles FJ, Nawrocki ST. ELR510444 inhibits tumor growth and angiogenesis by abrogating HIF activity and disrupting microtubules in renal cell carcinoma. PLoS One. 2012;7(1):e31120. doi: 10.1371/journal.pone.0031120. Epub 2012 Jan 25. PMID: 22295124; PMCID: PMC3266297. 2. Risinger AL, Westbrook CD, Encinas A, Mülbaier M, Schultes CM, Wawro S, Lewis JD, Janssen B, Giles FJ, Mooberry SL. ELR510444, a novel microtubule disruptor with multiple mechanisms of action. J Pharmacol Exp Ther. 2011 Mar;336(3):652-60. doi: 10.1124/jpet.110.175331. Epub 2010 Dec 9. PMID: 21148249; PMCID: PMC3061540.

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1: Carew JS, Esquivel JA 2nd, Espitia CM, Schultes CM, Mülbaier M, Lewis JD, Janssen B, Giles FJ, Nawrocki ST. ELR510444 inhibits tumor growth and angiogenesis by abrogating HIF activity and disrupting microtubules in renal cell carcinoma. PLoS One. 2012;7(1):e31120. doi: 10.1371/journal.pone.0031120. Epub 2012 Jan 25. PubMed PMID: 22295124; PubMed Central PMCID: PMC3266297.

2: Risinger AL, Westbrook CD, Encinas A, Mülbaier M, Schultes CM, Wawro S, Lewis JD, Janssen B, Giles FJ, Mooberry SL. ELR510444, a novel microtubule disruptor with multiple mechanisms of action. J Pharmacol Exp Ther. 2011 Mar;336(3):652-60. doi: 10.1124/jpet.110.175331. Epub 2010 Dec 9. PubMed PMID: 21148249; PubMed Central PMCID: PMC3061540.