D-I03|cas:688342-78-1|西域试剂

D-I03,99.92%

产品编号：Bellancom-124691| CAS NO：688342-78-1| 分子式：C₂₃H₃₆N₆S| 分子量：428.64

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货号	价格	库存与货期
Bellancom-124691	￥1200.00	杭州北京（现货）
Bellancom-124691	￥2100.00	杭州北京（现货）
Bellancom-124691	￥4200.00	杭州北京（现货）

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D-I03

产品介绍

D-I03 是一种选择性 RAD52 抑制剂，K_d 为 25.8 µM。D-I03 抑制 RAD52 依赖性单链退火 (SSA) 和 D 环形成，IC₅₀ 分别为 5 µM 和 8 µM。D-I03 抑制 BRCA1 和 BRCA2 缺陷细胞的生长，并抑制顺铂诱导的 RAD52 病灶形成，但对 RAD51 无影响。

生物活性

D-I03 is a selective RAD52 inhibitor with a K_d 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.

体外研究

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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
Result:	Preferentially suppressed the growth of Capan-1 and UWB1.289 cells.

体内研究
(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 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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

性状

Solid

溶解性数据

In Vitro:

DMSO : 50 mg/mL (116.65 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.3330 mL	11.6648 mL	23.3296 mL
5 mM	0.4666 mL	2.3330 mL	4.6659 mL
10 mM	0.2333 mL	1.1665 mL	2.3330 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (5.83 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.83 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (5.83 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.83 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (5.83 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.83 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。