EL102 | CAS#1233948-61-2 | apoptosis inhibitor

EL102
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WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 407461

CAS#: 1233948-61-2

Description: EL102 is a dual-inhibitor of apoptosis and angiogenesis. EL102 shows pre-clinical in vitro and in vivo activity against prostate cancer and circumvents MDR1 resistance. EL102 has in vitro activity against prostate cancer, characterised by accumulation in G2/M, induction of apoptosis, inhibition of Hif1α, and inhibition of tubulin polymerisation and decreased microtubule stability. In vivo, a combination of EL102 and docetaxel exhibits superior tumour inhibition. EL102 shows potential as both a single agent and within combination regimens for the treatment of prostate cancer, particularly in the chemoresistance setting.

Chemical Structure

EL102

CAS# 1233948-61-2

Product data Instruction

Theoretical Analysis

MedKoo Cat#: 407461
Name: EL102
CAS#: 1233948-61-2
Chemical Formula: C19H16N2O3S2
Exact Mass: 384.06
Molecular Weight: 384.468
Elemental Analysis: C, 59.36; H, 4.19; N, 7.29; O, 12.48; S, 16.68

Price and Availability

Size	Price	Availability	Quantity
5mg	USD 450	2 Weeks
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

Synonym: EL102; EL-102; EL 102.

IUPAC/Chemical Name: N-(5-(5-cyanothiophen-3-yl)-2-methylphenyl)-4-methoxybenzenesulfonamide

InChi Key: STJKZARVVAISJM-UHFFFAOYSA-N

InChi Code: InChI=1S/C19H16N2O3S2/c1-13-3-4-14(15-9-17(11-20)25-12-15)10-19(13)21-26(22,23)18-7-5-16(24-2)6-8-18/h3-10,12,21H,1-2H3

SMILES Code: C1=CC(C2C=C(C#N)SC=2)=CC(NS(=O)(=O)C2=CC=C(OC)C=C2)=C1C

Appearance: 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

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

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Product Data:

Product Data

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Biological target:	EL102 is a inhibitor of HIF1α , which can inhibit tubulin polymerisation and decreased microtubule stability.
In vitro activity:	EL102 inhibited cell proliferation with an IC50 of ∼21–40 nm. Reference: Br J Cancer. 2013 Oct 15;109(8):2131-41. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3798953/
In vivo activity:	Administration of 12 mg kg−1 docetaxel decreased the rate of tumour growth more efficiently than EL102 (slope (R2): vehicle 0.1414±0.01438 (0.9603) vs docetaxel 12 mg kg−1 0.04230±0.002531 (0.9688), F-test: P<0.0001), while the combination of both drugs had the largest effect on inhibition of tumour growth, suggesting that these drugs work well together in combination in vivo (slope (R2): vehicle 0.1414±0.01438 (0.9603) vs docetaxel 12 mg kg−1 and EL 102 12 mg kg−1 0.01533±0.0008838 (0.9709), F-test: P<0.0001 or vehicle, 0.1414±0.01438 (0.9603) vs docetaxel 12 mg kg−1 and EL 102 15 mg kg−1, 0.01537±0.001704 (0.9003), F-test: P<0.0001). Reference: Br J Cancer. 2013 Oct 15;109(8):2131-41. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3798953/

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	36.0	93.64

Preparing Stock Solutions

The following data is based on the product molecular weight 384.47 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.

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:	1. Toner AP, McLaughlin F, Giles FJ, Sullivan FJ, O'Connell E, Carleton LA, Breen L, Dunne G, Gorman AM, Lewis JD, Glynn SA. The novel toluidine sulphonamide EL102 shows pre-clinical in vitro and in vivo activity against prostate cancer and circumvents MDR1 resistance. Br J Cancer. 2013 Oct 15;109(8):2131-41. doi: 10.1038/bjc.2013.537. Epub 2013 Sep 19. PMID: 24052043; PMCID: PMC3798953.
In vitro protocol:	1. Toner AP, McLaughlin F, Giles FJ, Sullivan FJ, O'Connell E, Carleton LA, Breen L, Dunne G, Gorman AM, Lewis JD, Glynn SA. The novel toluidine sulphonamide EL102 shows pre-clinical in vitro and in vivo activity against prostate cancer and circumvents MDR1 resistance. Br J Cancer. 2013 Oct 15;109(8):2131-41. doi: 10.1038/bjc.2013.537. Epub 2013 Sep 19. PMID: 24052043; PMCID: PMC3798953.
In vivo protocol:	1. Toner AP, McLaughlin F, Giles FJ, Sullivan FJ, O'Connell E, Carleton LA, Breen L, Dunne G, Gorman AM, Lewis JD, Glynn SA. The novel toluidine sulphonamide EL102 shows pre-clinical in vitro and in vivo activity against prostate cancer and circumvents MDR1 resistance. Br J Cancer. 2013 Oct 15;109(8):2131-41. doi: 10.1038/bjc.2013.537. Epub 2013 Sep 19. PMID: 24052043; PMCID: PMC3798953.

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1: Toner AP, McLaughlin F, Giles FJ, Sullivan FJ, O'Connell E, Carleton LA, Breen
L, Dunne G, Gorman AM, Lewis JD, Glynn SA. The novel toluidine sulphonamide EL102
shows pre-clinical in vitro and in vivo activity against prostate cancer and
circumvents MDR1 resistance. Br J Cancer. 2013 Oct 15;109(8):2131-41. doi:
10.1038/bjc.2013.537. Epub 2013 Sep 19. PubMed PMID: 24052043; PubMed Central
PMCID: PMC3798953.

2: Borrie SA, McAuliffe MJ, Liss JM, O'Beirne GA, Anderson TJ. A follow-up
investigation into the mechanisms that underlie improved recognition of
dysarthric speech. J Acoust Soc Am. 2012 Aug;132(2):EL102-8. doi:
10.1121/1.4736952. PubMed PMID: 22894306.

3: Padilla M, Landsberger DM. Loudness summation using focused and unfocused
electrical stimulation. J Acoust Soc Am. 2014 Feb;135(2):EL102-8. doi:
10.1121/1.4862877. PubMed PMID: 25234912; PubMed Central PMCID: PMC4042455.

4: Verlinden CM, Sarkar J, Cornuelle BD, Kuperman WA. Determination of acoustic
waveguide invariant using ships as sources of opportunity in a shallow water
marine environment. J Acoust Soc Am. 2017 Feb;141(2):EL102. doi:
10.1121/1.4976112. PubMed PMID: 28253685.

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