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MedKoo Cat#: 564937 | Name: AG-538
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Description:

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

AG-538 is a PI5P4Kα inhibitor which targets the ATP site. AG 538 is a substrate-competitive inhibitor of the IGF-1 receptor (IGF-1R), with an IC50 = 61 nM in a cell-free kinase assay (Blum, G., Gazit, A., and Levitzki, A. (2000) Biochemistry 39, 15705-15712). AG 538 is a low molecular weight compound containing two catechol rings, which are sensitive to oxidation in cells.

Chemical Structure

AG-538
CAS#133550-18-2

Theoretical Analysis

MedKoo Cat#: 564937

Name: AG-538

CAS#: 133550-18-2

Chemical Formula: C16H11NO5

Exact Mass: 297.0637

Molecular Weight: 297.27

Elemental Analysis: C, 64.65; H, 3.73; N, 4.71; O, 26.91

Price and Availability

Size Price Availability Quantity
5mg USD 350.00 2 Weeks
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Related CAS #
No Data
Synonym
AG538; AG 538; AG-538; Tyrphostin AG-538
IUPAC/Chemical Name
(E)-2-(3,4-Dihydroxybenzoyl)-3-(3,4-dihydroxyphenyl)prop-2-enenitrile
InChi Key
CANOJKGQDCJDOX-VZUCSPMQSA-N
InChi Code
InChI=1S/C16H11NO5/c17-8-11(5-9-1-3-12(18)14(20)6-9)16(22)10-2-4-13(19)15(21)7-10/h1-7,18-21H/b11-5+
SMILES Code
N#C/C(C(C1=CC=C(O)C(O)=C1)=O)=C\C2=CC=C(O)C(O)=C2
Appearance
Solid powder
Purity
>95% (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
>3 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
Certificate of Analysis
View CoA: current batch, Lot# S21B10T22
Safety Data Sheet (SDS)
View Safety Data Sheet (SDS)
Instruction
View handling instruction

Preparing Stock Solutions

The following data is based on the product molecular weight 297.27 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: Giudici ML, Clarke JH, Irvine RF. Phosphatidylinositol 5-phosphate 4-kinase γ (PI5P4Kγ), a lipid signalling enigma. Adv Biol Regul. 2016 May;61:47-50. doi: 10.1016/j.jbior.2015.11.007. Epub 2015 Dec 2. PMID: 26710750. 2: Maturana-Teixeira S, Braga LE, Carpi Santos R, Calaza Kda C, Giestal-de- Araujo E, Leão-Ferreira LR. The (Na(+)/K (+))-ATPase activity in the developing rat retina: the role of insulin-like growth factor-I (IGF-I). Cell Mol Neurobiol. 2015 Mar;35(2):243-54. doi: 10.1007/s10571-014-0119-9. Epub 2014 Oct 2. PMID: 25274047. 3: Carrasco L, Cea P, Rocco P, Peña-Oyarzún D, Rivera-Mejias P, Sotomayor-Flores C, Quiroga C, Criollo A, Ibarra C, Chiong M, Lavandero S. Role of heterotrimeric G protein and calcium in cardiomyocyte hypertrophy induced by IGF-1. J Cell Biochem. 2014 Apr;115(4):712-20. doi: 10.1002/jcb.24712. PMID: 24243530. 4: Davis MI, Sasaki AT, Shen M, Emerling BM, Thorne N, Michael S, Pragani R, Boxer M, Sumita K, Takeuchi K, Auld DS, Li Z, Cantley LC, Simeonov A. A homogeneous, high-throughput assay for phosphatidylinositol 5-phosphate 4-kinase with a novel, rapid substrate preparation. PLoS One. 2013;8(1):e54127. doi: 10.1371/journal.pone.0054127. Epub 2013 Jan 10. PMID: 23326584; PMCID: PMC3542272. 5: Mukherjee S, Hanson AM, Shadrick WR, Ndjomou J, Sweeney NL, Hernandez JJ, Bartczak D, Li K, Frankowski KJ, Heck JA, Arnold LA, Schoenen FJ, Frick DN. Identification and analysis of hepatitis C virus NS3 helicase inhibitors using nucleic acid binding assays. Nucleic Acids Res. 2012 Sep 1;40(17):8607-21. doi: 10.1093/nar/gks623. Epub 2012 Jun 27. PMID: 22740655; PMCID: PMC3458564. 6: van der Meel R, Oliveira S, Altintas I, Haselberg R, van der Veeken J, Roovers RC, van Bergen en Henegouwen PM, Storm G, Hennink WE, Schiffelers RM, Kok RJ. Tumor-targeted Nanobullets: Anti-EGFR nanobody-liposomes loaded with anti-IGF-1R kinase inhibitor for cancer treatment. J Control Release. 2012 Apr 30;159(2):281-9. doi: 10.1016/j.jconrel.2011.12.027. Epub 2011 Dec 29. PMID: 22227023. 7: Blum G, Gazit A, Levitzki A. Development of new insulin-like growth factor-1 receptor kinase inhibitors using catechol mimics. J Biol Chem. 2003 Oct 17;278(42):40442-54. doi: 10.1074/jbc.M305490200. Epub 2003 Jul 16. PMID: 12869569. 8: Blum G, Gazit A, Levitzki A. Substrate competitive inhibitors of IGF-1 receptor kinase. Biochemistry. 2000 Dec 26;39(51):15705-12. doi: 10.1021/bi001516y. PMID: 11123895. 9: Choi BH, Kim RC, Vaughan PJ, Lau A, Van Nostrand WE, Cotman CW, Cunningham DD. Decreases in protease nexins in Alzheimer's disease brain. Neurobiol Aging. 1995 Jul-Aug;16(4):557-62. doi: 10.1016/0197-4580(95)00060-r. PMID: 8544905.