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YU238259 DNA-PK inhibitor

Name: YU238259
Brand: Selleck Chemicals
SKU: S8379
Rating: 5 (2 reviews)

Cat.No.S8379

YU238259 is a novel inhibitor of homology-dependent DNA repair (HDR), but does not inhibit non-homologous end-joining (NHEJ), in cell-based GFP reporter assays.

Chemical Structure

Molecular Weight: 459.95

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Quality Control

Batch: Purity: 99.69%

99.69

Related Targets	HDAC PARP ATM/ATR WRN DNA/RNA Synthesis Topoisomerase PPAR Sirtuin Casein Kinase eIF
Other DNA-PK Inhibitors	Nedisertib (M3814) AZD7648 NU7441 (KU-57788) KU-0060648 VX-984 NU7026 CC-115 LTURM34 Compound 401

Chemical Information, Storage & Stability

Molecular Weight	459.95	Formula	C₂₂H₂₂ClN₃O₄S	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1943733-16-1	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	COC1=CC=C(C=C1)S(=O)(=O)NCC2=CC=C(C=C2)C(=O)NCCC3=NC=C(C=C3)Cl

Solubility

In vitro
Batch:

DMSO : 91 mg/mL (197.84 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
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Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	HDR
In vitro	YU238259 exhibits potent synthetic lethality in the setting of DNA damage response and DNA repair defects. Treatment with this compound is not only synergistic with ionizing radiation (IR), etoposide, and PARP inhibition, but this synergism is heightened by BRCA2-deficiency. Synthetic lethality of this chemical in HDR-deficient cells results from accumulation of unresolved DSBs following additional inhibition of residual HDR pathway activity. Inhibition of HDR activity by this agent has little to no effect on the NHEJ pathway. It sensitizes tumour cells to radiation therapy and DSB-inducing chemotherapy .
In vivo	Growth of BRCA2-deficient human tumour xenografts in nude mice is significantly delayed by YU238259 treatment even in the absence of concomitant DNA-damaging therapy.
References	[1] https://pubmed.ncbi.nlm.nih.gov/26116172/

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