BPA-B9

PARP Bcl-2 Mcl-1

在 MDA-MB-231 细胞中，BPA-B9（0-250 nM，24 小时）会导致细胞凋亡 [1]。 A549 细胞周期的 G2/M 期受 BPA-B9（0-125 nM，12 小时）抑制 [1]。 BPA-B9（0-500 nM，0-24 小时）会导致裂解的 PARP 表达呈剂量和时间依赖性上升，以及抗凋亡蛋白 Bcl-2 和 Mcl-1 呈剂量依赖性下降[1]。 BPA 对 TNBC 的效应 B9 针对 HCC1937、A549、H460、HepG2 和 HeLa 细胞，IC50 值分别为 0.561 μM、0.201 μM 和 HeLa 细胞。细胞系 MDA-MB-231 显示出显着的抗增殖活性（IC50=16 ± 3 nM，SI > 3）。 0.128、0.077 和 0.253 μM[1]。

BPA-B9（0-25mg/kg，腹腔注射，每天一次，连续15天）在体内表现出很强的抗肿瘤作用，且副作用很少[1]。与 XS-060 (HY-149085) 相比，BPA-B9（25 mg/kg，腹腔注射或口服，一次）具有更优越的药代动力学 [1]。

细胞凋亡分析[1]
细胞类型： MDA-MB-231 细胞和 A549 细胞
测试浓度： 0、31.25、62.50、125 和 250 nM
孵育时间： 24 小时
实验结果： 诱导剂量依赖性 t（0、31.25、62.50、125 和 250 nM）增加（ MDA-MB-231 细胞中凋亡细胞为 7.96%、16.94%、28.30%、30.40%、40.40%。

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细胞周期分析[1]
细胞类型： MDA-MB-231 细胞和 A549 细胞
测试浓度： 0, 15.625 、31.25、62.50 和 125 nM
孵育时间： 12 小时
实验结果： 抑制 A549 细胞周期的 G2/M 期。与 62.50 nM 和 125 nM 的 BPA-B9 孵育后，处于 G2/M 期的 A549 细胞百分比分别达到 12.89% 和 46.49%，而未处理细胞的百分比为 8.62%。

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蛋白质印迹分析[1]
细胞类型： MDA-MB-231 细胞
测试浓度： 0、7.8、31.3、 125 和 500 nM
孵育时间：0、1、3、6、8、10、12、16 和 24 小时
实验结果：诱导切割的 PARP 表达随时间依赖性增加。此外，裂解的 PARP 升高，抗凋亡蛋白 Bcl -2 和 Mcl-1 降低，呈剂量依赖性

Animal/Disease Models: balb/c (Bagg ALBino) mouse (aged 4-6 weeks, with injection of MDA-MB-231 cells)[1]
Doses: 0, 12.5, 25 mg/kg
Route of Administration: IP, once every day for 15 days
Experimental Results: Inhibited tumor growth by causing mitotic arrest, chromosome aberrations, and DNA-damage response. Dramatically decreased the tumor volume and the tumor growth inhibition (TGI) of BPA-B9 was 59.3% at a dosage of 25.0 mg/kg/day, but a slight difference was shown at the dose of 12.5 mg/kg/day with no statistical significance.

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Animal/Disease Models: SD (Sprague-Dawley) rats (10-14 weeks, 200-220g)[1]
Doses: 25 mg/kg
Route of Administration: Oral absorption (po ) and intraperitoneal (ip)injection, once, (pharmacokinetic/PK Analysis)
Experimental Results: The oral absorption of BPA-B9 is very poor, while intraperitoneal (ip)injection displayed good absorption. pharmacokinetic/PK Parameters of XS-060 in SD (Sprague-Dawley) rats[1]. BPA -B9 25 mg/kg (ip) Tmax (h) 0.14 ± 0.10 Cmax (μg/L) 8083.33 ± 1193.04 AUC0-∞ (μg⋅h/L) 14615.65 ± 5508.77 T1/2 (h) 2.23 ± 0.17 CLz/F (L/(h⋅kg)) 1.55 ±

[1]. Chen J, et al. Discovery of bipyridine amide derivatives targeting pRXRα-PLK1 interaction for anticancer therapy. Eur J Med Chem. 2023 Apr 6;254:115341.

C25H26N4O2

414.50

Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.

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Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)
*Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution.
Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)
Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil)
Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals).

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Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)]
*Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)

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Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium)
Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose
Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals).

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Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders

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Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

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请根据您的实验动物和给药方式选择适当的溶解配方/方案：
1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液));
2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方):
10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline);
假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL；
3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例;
4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶;
5、为保证最佳实验结果，工作液请现配现用！
6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们;
7、 以上所有助溶剂都可在 Invivochem.cn网站购买。