D-I03

Synonym(s):1-(2-(Diethylamino)ethyl)-3-(2-(4-ethylpiperazin-1-yl)-4-methylquinolin-6-yl)thiourea;N-[2-(Diethylamino)ethyl]-N′-[2-(4-ethyl-1-piperazinyl)-4-methyl-6-quinolinyl]-thiourea

CAS NO.：688342-78-1
Empirical Formula: C23H36N6S
Molecular Weight: 428.64
Update Date: 2026-07-14 16:49:18

What is D-I03?

Biological Activity

D-I03 is a selective inhibitor of RAD52 with a corresponding Kd value of 25.8 μM. D-I03 inhibits ssDNA annealing via RAD52 and D-loop formation with IC50 values of 5 μM and 8 μM, respectively.

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 .
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.

Cell Proliferation Assay

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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.
Pharmacokinetic and toxicity studies indicate that maximal tolerated dose of D-I03 is ≥50 mg /kg, and t _1/2 is 23.4 hours, resulting in >1 μM maximal concentration in peripheral blood.

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

Properties of D-I03

Boiling point:	582.0±60.0 °C(Predicted)
Density	1.147±0.06 g/cm3(Predicted)
storage temp.	Store at -20°C
solubility	DMSO: ≥ 100 mg/mL (233.30 mM)
form	Solid
pka	12.00±0.70(Predicted)
color	Off-white to light yellow

Safety information for D-I03

Computed Descriptors for D-I03

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