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MedKoo Cat#: 464458 | Name: APX2014

Description:

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

APX2014 is a novel potent and specific Ref-1 inhibitor. APX2014 blocks in vitro cell proliferation and activating apoptosis via PARP cleavage. APX2014 demonstrated enhanced inhibition of Ref-1 function in a DNA-binding assay compared with APX3330. APX2014 was antiproliferative against human retinal microvascular endothelial cells (HRECs; GI50 = 110 nM) and macaque choroidal endothelial cells (Rf/6a; GI50 = 5.0 μM). APX2014 significantly reduced the ability of HRECs and Rf/6a cells to form tubes at mid-nanomolar concentrations compared with control, and both significantly inhibited HREC and Rf/6a cell migration in a scratch wound assay, reducing NF-κB activation and downstream targets. Ex vivo, APX2014 inhibited choroidal sprouting at low micromolar and high nanomolar concentrations, respectively. In the laser-induced choroidal neovascularization mouse model.

Chemical Structure

APX2014
CAS#1415030-17-9

Theoretical Analysis

MedKoo Cat#: 464458

Name: APX2014

CAS#: 1415030-17-9

Chemical Formula: C18H19NO5

Exact Mass: 329.1263

Molecular Weight: 329.35

Elemental Analysis: C, 65.64; H, 5.82; N, 4.25; O, 24.29

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.
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Related CAS #
No Data
Synonym
APX2014; APX 2014; APX-2014;
IUPAC/Chemical Name
(E)-N-methoxy-2-((3-methoxy-1,4-dioxo-1,4-dihydronaphthalen-2-yl)methylene)pentanamide
InChi Key
HVWUGMMHPTXECQ-ZHACJKMWSA-N
InChi Code
InChI=1S/C18H19NO5/c1-4-7-11(18(22)19-24-3)10-14-15(20)12-8-5-6-9-13(12)16(21)17(14)23-2/h5-6,8-10H,4,7H2,1-3H3,(H,19,22)/b11-10+
SMILES Code
CCC/C(C(NOC)=O)=C\C(C1=O)=C(OC)C(C2=C1C=CC=C2)=O
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
To be determined
Shelf Life
>2 years if stored properly
Drug Formulation
To be determined
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

Preparing Stock Solutions

The following data is based on the product molecular weight 329.35 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
1: Mijit M, Boner M, Cordova RA, Gampala S, Kpenu E, Klunk AJ, Zhang C, Kelley MR, Staschke KA, Fishel ML. Activation of the integrated stress response (ISR) pathways in response to Ref-1 inhibition in human pancreatic cancer and its tumor microenvironment. Front Med (Lausanne). 2023 Apr 27;10:1146115. doi: 10.3389/fmed.2023.1146115. PMID: 37181357; PMCID: PMC10174294. 2: Champion JD, Dodd KM, Lam HC, Alzahrani MAM, Seifan S, Rad E, Scourfield DO, Fishel ML, Calver BL, Ager A, Henske EP, Davies DM, Kelley MR, Tee AR. Drug Inhibition of Redox Factor-1 Restores Hypoxia-Driven Changes in Tuberous Sclerosis Complex 2 Deficient Cells. Cancers (Basel). 2022 Dec 15;14(24):6195. doi: 10.3390/cancers14246195. PMID: 36551683; PMCID: PMC9776744. 3: Mijit M, Wireman R, Armstrong L, Gampala S, Hassan Z, Schneeweis C, Schneider G, Zhang C, Fishel ML, Kelley MR. RelA Is an Essential Target for Enhancing Cellular Responses to the DNA Repair/Ref-1 Redox Signaling Protein and Restoring Perturbated Cellular Redox Homeostasis in Mouse PDAC Cells. Front Oncol. 2022 Mar 24;12:826617. doi: 10.3389/fonc.2022.826617. PMID: 35402225; PMCID: PMC8988139. 4: Gampala S, Shah F, Lu X, Moon HR, Babb O, Umesh Ganesh N, Sandusky G, Hulsey E, Armstrong L, Mosely AL, Han B, Ivan M, Yeh JJ, Kelley MR, Zhang C, Fishel ML. Ref-1 redox activity alters cancer cell metabolism in pancreatic cancer: exploiting this novel finding as a potential target. J Exp Clin Cancer Res. 2021 Aug 10;40(1):251. doi: 10.1186/s13046-021-02046-x. PMID: 34376225; PMCID: PMC8353735. 5: Gampala S, Shah F, Zhang C, Rhodes SD, Babb O, Grimard M, Wireman RS, Rad E, Calver B, Bai RY, Staedtke V, Hulsey EL, Saadatzadeh MR, Pollok KE, Tong Y, Smith AE, Clapp DW, Tee AR, Kelley MR, Fishel ML. Exploring transcriptional regulators Ref-1 and STAT3 as therapeutic targets in malignant peripheral nerve sheath tumours. Br J Cancer. 2021 Apr;124(9):1566-1580. doi: 10.1038/s41416-021-01270-8. Epub 2021 Mar 3. Erratum in: Br J Cancer. 2022 Oct;127(7):1378-1379. PMID: 33658640; PMCID: PMC8076291. 6: Caston RA, Shah F, Starcher CL, Wireman R, Babb O, Grimard M, McGeown J, Armstrong L, Tong Y, Pili R, Rupert J, Zimmers TA, Elmi AN, Pollok KE, Motea EA, Kelley MR, Fishel ML. Combined inhibition of Ref-1 and STAT3 leads to synergistic tumour inhibition in multiple cancers using 3D and in vivo tumour co-culture models. J Cell Mol Med. 2021 Jan;25(2):784-800. doi: 10.1111/jcmm.16132. Epub 2020 Dec 3. PMID: 33274592; PMCID: PMC7812272. 7: Logsdon DP, Shah F, Carta F, Supuran CT, Kamocka M, Jacobsen MH, Sandusky GE, Kelley MR, Fishel ML. Blocking HIF signaling via novel inhibitors of CA9 and APE1/Ref-1 dramatically affects pancreatic cancer cell survival. Sci Rep. 2018 Sep 13;8(1):13759. doi: 10.1038/s41598-018-32034-9. PMID: 30214007; PMCID: PMC6137035. 8: Sardar Pasha SPB, Sishtla K, Sulaiman RS, Park B, Shetty T, Shah F, Fishel ML, Wikel JH, Kelley MR, Corson TW. Ref-1/APE1 Inhibition with Novel Small Molecules Blocks Ocular Neovascularization. J Pharmacol Exp Ther. 2018 Oct;367(1):108-118. doi: 10.1124/jpet.118.248088. Epub 2018 Aug 3. PMID: 30076264; PMCID: PMC7250474.