D-I03
- Product Name
- D-I03
- CAS No.
- 688342-78-1
- Chemical Name
- D-I03
- Synonyms
- D-I03;D-I03 (D103);D-I03, 10 mM in DMSO;1-(2-(Diethylamino)ethyl)-3-(2-(4-ethylpiperazin-1-yl)-4-methylquinolin-6-yl)thiourea;Thiourea, N-[2-(diethylamino)ethyl]-N'-[2-(4-ethyl-1-piperazinyl)-4-methyl-6-quinolinyl]-
- CBNumber
- CB44844707
- Molecular Formula
- C23H36N6S
- Formula Weight
- 428.64
- MOL File
- 688342-78-1.mol
D-I03 Property
- 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
N-Bromosuccinimide Price
- Product number
- SML2496
- Product name
- D-I03
- Purity
- ≥98% (HPLC)
- Packaging
- 5mg
- Price
- $105
- Updated
- 2025/07/31
- Product number
- SML2496
- Product name
- D-I03
- Purity
- ≥98% (HPLC)
- Packaging
- 25mg
- Price
- $399.73
- Updated
- 2025/07/31
- Product number
- CS-0087335
- Product name
- D-I03
- Purity
- 99.73%
- Packaging
- 5mg
- Price
- $80
- Updated
- 2021/12/16
- Product number
- CS-0087335
- Product name
- D-I03
- Purity
- 99.73%
- Packaging
- 10mg
- Price
- $145
- Updated
- 2021/12/16
- Product number
- CS-0087335
- Product name
- D-I03
- Purity
- 99.73%
- Packaging
- 25mg
- Price
- $330
- Updated
- 2021/12/16
D-I03 Chemical Properties,Usage,Production
Uses
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].
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
| 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 | td>
| Result: | Preferentially suppressed the growth of Capan-1 and UWB1.289 cells. | < /tr>
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.
< div class="cpd-mod-vv">
| 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. |
target
| Target | Value |
| RAD52 (Cell-free assay) | 25.8 μM(Ki) |
References
[1] Huang F, et al. Targeting BRCA1- and BRCA2-deficient cells with RAD52 small molecule inhibitors. Nucleic Acids Res. 2016 May 19;44(9):4189-99. DOI:10.1093/nar/gkw087
[2] Hengel SR, et al. Small-Molecule Inhibitors Targeting DNA Repair and DNA Repair Deficiency in Research and Cancer Therapy. Cell Chem Biol. 2017 Sep 21;24(9):1101-1119. DOI:10.1016/j.chembiol.2017.08.027
[3] Sullivan-Reed K, et al. Simultaneous Targeting of PARP1 and RAD52 Triggers Dual Synthetic Lethality in BRCA-Deficient Tumor Cells. Cell Rep. 2018 Jun 12;23(11):3127-3136. DOI:10.1016/j.celrep.2018.05.034
D-I03 Preparation Products And Raw materials
Raw materials
Preparation Products
D-I03 Suppliers
- Tel
- 13816107857
- Fax
- qq: 276312098
- sales@fortunechem-sh.com
- Country
- China
- ProdList
- 984
- Advantage
- 58
- Tel
- 13816613772
- Fax
- QQ: 12922499
- huahero21@sina.com
- Country
- China
- ProdList
- 2497
- Advantage
- 55
- Tel
- 021-61312847; 18021002903
- Fax
- QQ:3008007432
- 3008007409@qq.com
- Country
- China
- ProdList
- 71826
- Advantage
- 60
- Tel
- 177-54423994 17754423994
- Fax
- QQ:2853530913
- 2853530910@QQ.com
- Country
- China
- ProdList
- 7999
- Advantage
- 62
- Tel
- +1-781-999-5354; +17819995354
- marketing@targetmol.com
- Country
- United States
- ProdList
- 32436
- Advantage
- 58
- Tel
- +86-0519-85788828 +86-13775037613
- sales@chemrenpharm.com
- Country
- China
- ProdList
- 4023
- Advantage
- 58
- Tel
- 18818260767
- Fax
- QQ 3610331285
- sales@chemegen.com
- Country
- China
- ProdList
- 11218
- Advantage
- 58
- Tel
- +86-02787215551 +86-19945035818
- Fax
- 027-87215551
- 2936752263@qq.com
- Country
- China
- ProdList
- 7981
- Advantage
- 58
- Tel
- 021-51816796-820 13611835272
- Fax
- 021-5161 3951
- sales2@sunwaypharm.com
- Country
- China
- ProdList
- 44116
- Advantage
- 58
- Tel
- 027-59101668 19945030958
- Fax
- 027-59101668
- 2881924765@qq.com
- Country
- China
- ProdList
- 7932
- Advantage
- 58