WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 407907
Description: YU238259 Is a Novel Inhibitor of Homology-Dependent DNA Repair. YU238259 exhibits potent synthetic lethality in the setting of DNA damage response and DNA repair defects. YU238259 specifically inhibits homology-dependent DNA repair, but not non-homologous end-joining, in cell-based GFP reporter assays. Treatment with YU238259 is not only synergistic with ionizing radiation, etoposide, and PARP inhibition, but this synergism is heightened by BRCA2 deficiency.
MedKoo Cat#: 407907
Chemical Formula: C22H22ClN3O4S
Exact Mass: 459.102
Molecular Weight: 459.945
Elemental Analysis: C, 57.45; H, 4.82; Cl, 7.71; N, 9.14; O, 13.91; S, 6.97
Synonym: YU238259; YU-238259; YU 238259;
IUPAC/Chemical Name: N-(2-(5-chloropyridin-2-yl)ethyl)-4-(((4-methoxyphenyl)sulfonamido)methyl)benzamide
InChi Key: BIHURSOREGLQBB-UHFFFAOYSA-N
InChi Code: InChI=1S/C22H22ClN3O4S/c1-30-20-8-10-21(11-9-20)31(28,29)26-14-16-2-4-17(5-3-16)22(27)24-13-12-19-7-6-18(23)15-25-19/h2-11,15,26H,12-14H2,1H3,(H,24,27)
SMILES Code: C1=CC(OC)=CC=C1S(=O)(=O)NCC1=CC=C(C(=O)NCCC2=CC=C(Cl)C=N2)C=C1
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
The following data is based on the product molecular weight 459.945 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|
1: Stachelek GC, Peterson-Roth E, Liu Y, Fernandez RJ 3rd, Pike LR, Qian JM,
Abriola L, Hoyer D, Hungerford W, Merkel J, Glazer PM. YU238259 Is a Novel
Inhibitor of Homology-Dependent DNA Repair That Exhibits Synthetic Lethality and
Radiosensitization in Repair-Deficient Tumors. Mol Cancer Res. 2015
Oct;13(10):1389-97. doi: 10.1158/1541-7786.MCR-15-0036. Epub 2015 Jun 26. PubMed
PMID: 26116172; PubMed Central PMCID: PMC4618103.
Further, growth of BRCA2-deficient human tumor xenografts in nude mice is significantly delayed by YU238259 treatment even in the absence of concomitant DNA-damaging therapy. The cytotoxicity of these small molecules in repair-deficient cells results from an accumulation of unresolved DNA double-strand breaks. YU238259 or related small molecules may have clinical benefit to patients with advanced BRCA2-negative tumors, either as a monotherapy or as an adjuvant to radiotherapy and certain chemotherapies.