Description
YU238259 is an inhibitor of homology-dependent DNA repair (HDR), used for cancer research.
Product information
CAS Number: 1943733-16-1
Molecular Weight: 459.95
Formula: C22H22ClN3O4S
Chemical Name: N-[2-(5-chloropyridin-2-yl)ethyl]-4-[(4-methoxybenzenesulfonamido)methyl]benzamide
Smiles: COC1C=CC(=CC=1)S(=O)(=O)NCC1=CC=C(C=C1)C(=O)NCCC1=CC=C(Cl)C=N1
InChiKey: BIHURSOREGLQBB-UHFFFAOYSA-N
InChi: 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)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 110 mg/mL (239.16 mM; Need ultrasonic).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
YU238259 is an inhibitor of homology-dependent DNA repair, with no effect on PARP activity. YU238259 shows cytotoxicity in BRCA2-deficient cells, with a low LD50 of 8.5 μM. YU238259 (0-5 μM) causes a potent, dose-dependent decrease in HDR efficiency in U2OS DR-GFP or U2OS EJ5-GFP cells, but with no effect on NHEJ frequency. YU238259 (0-10 μM) exhibits synthetic lethality with loss of frequently mutated tumor suppressors, and shows synergism with radiotherapy (IR) and DNA-damaging chemotherapy that is potentiated by BRCA2 loss.
In Vivo:
YU238259 (3 mg/kg, i.p.) inhibits the growth of BRCA2-deficient tumor xenografts in nude mice.
Products are for research use only. Not for human use.
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