D-I03
- CAS No.
- 688342-78-1
- Chemical Name:
- D-I03
- Synonyms
- D-I03;D-I03 (D103);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
- Molecular Weight:
- 428.64
- MDL Number:
- MOL File:
- 688342-78-1.mol
D-I03 price More Price(5)
Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
---|---|---|---|---|---|---|---|
Sigma-Aldrich | SML2496 | D-I03 ≥98% (HPLC) | 688342-78-1 | 5mg | $40.8 | 2024-03-01 | Buy |
Sigma-Aldrich | SML2496 | D-I03 ≥98% (HPLC) | 688342-78-1 | 25mg | $411 | 2024-03-01 | Buy |
ChemScene | CS-0087335 | D-I03 99.73% | 688342-78-1 | 5mg | $80 | 2021-12-16 | Buy |
ChemScene | CS-0087335 | D-I03 99.73% | 688342-78-1 | 10mg | $145 | 2021-12-16 | Buy |
ChemScene | CS-0087335 | D-I03 99.73% | 688342-78-1 | 25mg | $330 | 2021-12-16 | Buy |
D-I03 Chemical Properties,Uses,Production
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.
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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. |
target
Target | Value |
RAD52 (Cell-free assay) | 25.8 μM(Ki) |
D-I03 Preparation Products And Raw materials
Raw materials
Preparation Products
D-I03 Suppliers
Supplier | Tel | Country | ProdList | Advantage | |
---|---|---|---|---|---|
TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 19892 | 58 |
Wuhan Topule Biopharmaceutical Co., Ltd | +8618327326525 | masar@topule.com | China | 8474 | 58 |
Aladdin Scientific | +1-+1(833)-552-7181 | sales@aladdinsci.com | United States | 57511 | 58 |
Shanghai Beckham Medical Technology Co., Ltd | 021-13816613772 13816613772 | huahero21@sina.com | China | 408 | 55 |
ShangHai Biochempartner Co.,Ltd | 17754423994 17754423994 | 2853530910@QQ.com | China | 8014 | 62 |
ChemeGen(Shanghai) Biotechnology Co.,Ltd. | 18818260767 | sales@chemegen.com | China | 11289 | 58 |
Wuhan Topule | +86-02787215551 +86-19945035818 | 2936752263@qq.com | China | 8206 | 58 |
Shanghai Sunway Pharmaceutical Technology Co.,Ltd. | 021-51816796-820 13611835272 | sales2@sunwaypharm.com | China | 44461 | 58 |
Hubei Kele Fine Chemical Co., Ltd | 027-59101668 19945030958 | 2881924765@qq.com | China | 7973 | 58 |
Bide Pharmatech Ltd. | 400-1647117 13681763483 | product02@bidepharm.com | China | 62163 | 58 |