1. Cell Cycle/DNA Damage
  2. DNA/RNA Synthesis
  3. D-I03

D-I03 

Cat. No.: HY-124691 Purity: >98.0%
Handling Instructions

D-I03 is a selective RAD52 inhibitor with a Kd of 25.8 µM. D-I03 specifically inhibits RAD52-dependent single-strand annealing (SSA) and D-loop formation with IC50s of 5 µM and 8 µM, respectively. D-I03 suppresses growth of BRCA1- and BRCA2-deficient cells and inhibits formation of damage-induced RAD52 foci, but does not effect on RAD51 foci induced by Cisplatin.

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

D-I03 Chemical Structure

D-I03 Chemical Structure

CAS No. : 688342-78-1

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 75 In-stock
Estimated Time of Arrival: December 31
5 mg USD 80 In-stock
Estimated Time of Arrival: December 31
10 mg USD 145 In-stock
Estimated Time of Arrival: December 31
25 mg USD 330 In-stock
Estimated Time of Arrival: December 31
50 mg   Get quote  
100 mg   Get quote  

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Description

D-I03 is a selective RAD52 inhibitor with a Kd of 25.8 µM. D-I03 specifically inhibits RAD52-dependent single-strand annealing (SSA) and D-loop formation with IC50s of 5 µM and 8 µM, respectively. D-I03 suppresses growth of BRCA1- and BRCA2-deficient cells and inhibits formation of damage-induced RAD52 foci, but does not effect on RAD51 foci induced by Cisplatin[1][2].

IC50 & Target

Ki: 25.8 µM (RAD52)[1][2]

In Vitro

D-I03 (0-10 μM; on days 1 and 3; Capan-1 and UWB1.289 cells) treatment preferentially suppressed the growth of Capan-1 and UWB1.289 cells in a concentration-dependent manner[1].
D-I03 inhibits RAD52 foci formation induced by cisplatin in BCR-ABL1-positive BRCA1-deficient 32Dcl3 murine hematopoietic cell line that expresses GFP-RAD52. In the presence of D-I03 (2.5 μM), the fraction of cells with RAD52 foci is decreased, from 38.7% to 171%; at the same time, the fraction of Cisplatin-treated cells without foci is increased from 48.4% to 71.9%. D-I03 does not effect on RAD51 foci induced by Cisplatin. Also, D-I03 alone induce neither RAD51 foci nor RAD52 foci (in BRCA1-deficient cells) indicating low genotoxicity of D-I03[1].

Cell Proliferation Assay[1]

Cell Line: Capan-1 (BRCA2) and UWB1.289 (BRCA1+) cells
Concentration: 0 μM, 2.5 μM, 5 μM, or 10 μM
Incubation Time: On days 1 and 3
Result: Preferentially suppressed the growth of Capan-1 and UWB1.289 cells.
In Vivo

D-I03 (50 mg/kg/day; intraperitoneal injection; daily; for 7 days; nu/nu mice) treatment reduces BRCA1-deficient MDA-MB-436 tumor growth. Talazoparib puls D-I03 does not affect the growth of BRCA1-proficient tumors and does not exert any significant toxicity against normal tissues and organs[3].
Pharmacokinetic and toxicity studies indicates that maximal tolerated dose of D-I03 is ≥50 mg/kg, and t1/2 is 23.4 hours, resulting in >1 μM maximal concentration in peripheral blood[1].

Animal Model: Nu/nu mice injected with BRCA1-deficient MDA-MB-436 cells[3]
Dosage: 50 mg/kg/day
Administration: Intraperitoneal injection; daily; for 7 days
Result: Reduced BRCA1-deficient MDA-MB-436 tumor growth.
Molecular Weight

428.64

Formula

C₂₃H₃₆N₆S

CAS No.

688342-78-1

SMILES

S=C(NC1=CC=C2N=C(N3CCN(CC)CC3)C=C(C)C2=C1)NCCN(CC)CC

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (233.30 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3330 mL 11.6648 mL 23.3296 mL
5 mM 0.4666 mL 2.3330 mL 4.6659 mL
10 mM 0.2333 mL 1.1665 mL 2.3330 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.83 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (5.83 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.83 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

D-I03DNA/RNA SynthesisssDNArepairRAD52cancersingle-strandannealingD-loopBRCA2-deficientBRCA1-deficienttumorInhibitorinhibitorinhibit

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