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

MedKoo Cat#: 407461 | Name: EL102

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Description:

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

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

Theoretical Analysis

MedKoo Cat#: 407461

Name: EL102

CAS#: 1233948-61-2

Chemical Formula: C19H16N2O3S2

Exact Mass: 384.0602

Molecular Weight: 384.47

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 550.00	2 Weeks

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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

More Info

Product Data

Product Data

Instruction

View handling instruction

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/

	Solvent	mg/mL	mM
Solubility
	DMSO	36.0	93.64

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

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:

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. 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.