| Company Name: |
ShangHai Biochempartner Co.,Ltd
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| Tel: |
17754423994 17754423994 |
| Email: |
2853530910@QQ.com |
| Products Intro: |
Product Name:D-I03
CAS:688342-78-1
Purity:98% HPLC LCMS Package:100mg;500mg;1g;5g;10g
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| Product Name: | D-I03 | | Synonyms: | D-I03
(D103);D-I03;Thiourea, N-[2-(diethylamino)ethyl]-N'-[2-(4-ethyl-1-piperazinyl)-4-methyl-6-quinolinyl]- | | CAS: | 688342-78-1 | | MF: | C23H36N6S | | MW: | 428.64 | | EINECS: | | | Product Categories: | | | Mol File: | 688342-78-1.mol |  |
| | D-I03 Chemical Properties |
| 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 |
| | D-I03 Usage And Synthesis |
| 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 < tr> | 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) |
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| | D-I03 Preparation Products And Raw materials |
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