1. Cell Cycle/DNA Damage
    PI3K/Akt/mTOR
  2. DNA-PK

YU238259 

Cat. No.: HY-19977 Purity: 98.01%
Handling Instructions

YU238259 is an inhibitor of homology-dependent DNA repair (HDR), used for cancer research.

For research use only. We do not sell to patients.

YU238259 Chemical Structure

YU238259 Chemical Structure

CAS No. : 1943733-16-1

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 121 In-stock
Estimated Time of Arrival: December 31
5 mg USD 110 In-stock
Estimated Time of Arrival: December 31
10 mg USD 190 In-stock
Estimated Time of Arrival: December 31
25 mg USD 390 In-stock
Estimated Time of Arrival: December 31
50 mg USD 690 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1150 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

YU238259 is an inhibitor of homology-dependent DNA repair (HDR), used for cancer research.

IC50 & Target

HDR[1]

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[1].

In Vivo

YU238259 (3 mg/kg, i.p.) inhibits the growth of BRCA2-deficient tumor xenografts in nude mice[1].

Solvent & Solubility
In Vitro: 

DMSO : ≥ 300 mg/mL (652.24 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1741 mL 10.8707 mL 21.7415 mL
5 mM 0.4348 mL 2.1741 mL 4.3483 mL
10 mM 0.2174 mL 1.0871 mL 2.1741 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Cell Assay
[1]

U2OS reporter cell lines (DR-GFP or EJ5-GFP) are pretreated in triplicate with varying concentrations of YU238259 for 24 h, after which 4 μg of SCE-I plasmid is transfected into 1 × 106 cells/replicate using an Amaxa Nucleofector. Transfected cells are reseeded on 6-well plates and cultured with YU238259 for an additional 72 h. The percentage of GFP-positive cells is quantified by flow cytometry. Data analysis is performed using FlowJo software. Error bars represent the standard deviation[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

069(nu)/070(nu/+) athymic nude mice, at 4-5 weeks age, are injected subcutaneously with 3 × 106 DLD-1 or DLD-1 BRCA2-KO cells suspended in 100 μL PBS. Tumor take rate is >80%. When tumors reach 100 mm3 geometric mean volume, the mice are injected with 3 mg/kg YU238259 or its 3:1 DMSO:PBS vehicle, or 5 mg/kg YU128440 or its 1:19 DMSO:PBS vehicle (IP, 100 μL total in each case). Treatment is repeated 3×/week (Mon/Wed/Fri) for a total of 12 doses of YU238259 and 4 doses of YU128440. Tumor growth is assessed by external caliper. Mice are euthanized when individual tumor volumes exceed 1000 mm3[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

459.95

Formula

C₂₂H₂₂ClN₃O₄S

CAS No.

1943733-16-1

SMILES

COC1=CC=C(S(NCC2=CC=C(C(NCCC3=CC=C(Cl)C=N3)=O)C=C2)(=O)=O)C=C1

Storage

4°C, protect from light

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
YU238259
Cat. No.:
HY-19977
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YU238259

Cat. No.: HY-19977