D-I03
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- CAS号:
- 688342-78-1
- 英文名:
- D-I03
- 英文别名:
- D-I03;D-I03
(D103);Thiourea, N-[2-(diethylamino)ethyl]-N'-[2-(4-ethyl-1-piperazinyl)-4-methyl-6-quinolinyl]-
- 中文名:
- D-I03
- 中文别名:
- 化合物D-I03;化合物 T10936
- CBNumber:
- CB44844707
- 分子式:
- C23H36N6S
- 分子量:
- 428.64
- MOL File:
- 688342-78-1.mol
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D-I03化学性质
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沸点:
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582.0±60.0 °C(Predicted)
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密度:
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1.147±0.06 g/cm3(Predicted)
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储存条件:
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Store at -20°C
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溶解度:
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DMSO: ≥ 100 mg/mL (233.30 mM)
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形态:
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Solid
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酸度系数(pKa):
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12.00±0.70(Predicted)
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颜色:
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Off-white to light yellow
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D-I03性质、用途与生产工艺
D-I03 是一种 RAD52 的选择性抑制剂，对应的Kd值为25.8 µM。D-I03 通过 RAD52 和D环形成抑制ssDNA退火，对应的IC50值分别为5 µM和8 µM。
| Target | Value |
RAD52
(Cell-free assay)
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25.8 μM(Ki)
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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:
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Capan-1 (BRCA2
−
) and UWB1.289 (BRCA1
+
) cells
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Concentration:
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0 μM, 2.5 μM, 5 μM, or 10 μM
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Incubation Time:
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On days 1 and 3
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Result:
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Preferentially suppressed the growth of Capan-1 and UWB1.289 cells.
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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 indicates 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:
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Nu/nu
mice injected with BRCA1-deficient MDA-MB-436 cells
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Dosage:
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50 mg/kg/day
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Administration:
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Intraperitoneal injection; daily; for 7 days
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Result:
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Reduced BRCA1-deficient MDA-MB-436 tumor growth.
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D-I03
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2024/04/30 | HY-124691 | D-I03
D-I03 | 688342-78-1 | 5mg | 1200元 |
| 2024/04/30 | HY-124691 | D-I03
D-I03 | 688342-78-1 | 10mM * 1mLin DMSO | 1320元 |
688342-78-1, D-I03 相关搜索:
- 药靶配体
- 化合物D-I03
- 化合物 T10936
- 688342-78-1
- Thiourea, N-[2-(diethylamino)ethyl]-N'-[2-(4-ethyl-1-piperazinyl)-4-methyl-6-quinolinyl]-
- D-I03
- D-I03
(D103)