| 规格 | 价格 | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| 靶点 |
BNCT reagent
|
|---|---|
| 体外研究 (In Vitro) |
在人胶质母细胞瘤T98G细胞中，丁硫氨酸亚砜胺（BSO）预处理耗竭谷胱甘肽后，显著增强sodium borocaptate联合热中子照射的放射生物学效应。单独sodium borocaptate处理组中子照射后存活分数为0.32，而BSO预处理+sodium borocaptate组降至0.18（p<0.05）。单独BSO处理无细胞毒性（存活分数：0.98）。[3]
|
| 体内研究 (In Vivo) |
在患有自发性颅内肿瘤的狗中评估显示，静脉注射50 mg/kg的borocaptate sodium (BSH)导致硼在肿瘤组织中积累。在不同时间点测量血液和肿瘤样本中的硼浓度，注射后6小时肿瘤与血液硼浓度比约为1.0。中子照射（热中子通量：1.5 × 109 n/cm2/s）后，7只狗中有4只观察到显著肿瘤消退，其中1例完全缓解。无中子照射时无药理活性（如抗肿瘤作用）。[2]
|
| 细胞实验 |
在人胶质母细胞瘤T98G细胞中评估sodium borocaptate摄取。细胞经100 μM丁硫氨酸亚砜胺（BSO）预处理24小时耗竭谷胱甘肽，随后暴露于15 ppm硼当量的sodium borocaptate 3小时。采用电感耦合等离子体原子发射光谱法定量细胞内硼浓度。克隆形成实验中，处理后的细胞接受热中子照射（通量：1.0 × 109 n/cm2），培养10天后评估集落形成能力。[3]
|
| 动物实验 |
Dogs with spontaneous intracranial tumors received intravenous infusion of borocaptate sodium dissolved in saline (concentration not specified). The dose was 50 mg/kg body weight, administered as a single bolus injection. Neutron irradiation was performed at the Massachusetts Institute of Technology (MIT) reactor, with irradiation starting at 6–12 hours post-injection. The thermal neutron dose ranged from 8.7 to 15.6 Gy, and boron concentrations in blood, tumor, and normal tissues (e.g., brain, skin) were monitored using prompt gamma-ray spectroscopy or other analytical methods. [2]
|
| 药代性质 (ADME/PK) |
In dogs, borocaptate sodium exhibited rapid distribution post-intravenous injection. The plasma half-life was approximately 12.6 hours. Boron concentrations peaked in blood within 1–2 hours and declined biphasically. Tumor boron concentrations reached up to 35 μg/g at 6 hours, with a tumor-to-blood ratio of ~1.0. Excretion was primarily renal, with 70–80% of the administered dose eliminated unchanged in urine within 24 hours. No metabolism was detected. [2]
Uptake of sodium borocaptate was evaluated in human glioblastoma T98G cells. Cells were pretreated with 100 μM buthionine sulfoximine (BSO) for 24 hours to deplete glutathione, followed by exposure to 15 ppm boron-equivalent sodium borocaptate for 3 hours. Intracellular boron concentration was quantified using inductively coupled plasma atomic emission spectroscopy. For clonogenic survival assays, cells were irradiated with thermal neutrons (flux: 1.0 × 109 n/cm2) after treatment, then cultured for 10 days to assess colony formation. [3] |
| 毒性/毒理 (Toxicokinetics/TK) |
No severe acute toxicity was observed in dogs at the therapeutic dose of 50 mg/kg. Mild and transient adverse effects included vomiting (in 2 out of 7 dogs) and lethargy. The intravenous LD50 in mice was 1000 mg/kg. No hepatotoxicity or nephrotoxicity was reported based on blood chemistry and histopathological analysis. Plasma protein binding was not described. [2]
|
| 参考文献 |
|
| 其他信息 |
Borocaptate sodium (BSH) is a boron delivery agent for boron neutron capture therapy (BNCT), used to treat brain tumors. It selectively accumulates in tumor cells, where boron-10 nuclei capture thermal neutrons to produce high-linear energy transfer alpha particles that cause localized tumor cell destruction. [2]
This study compared 11B NMR spectroscopy and other analytical methods (e.g., inductively coupled plasma atomic emission spectroscopy) for detecting BSH in biological samples. NMR provided non-invasive quantification with a detection limit of ~5 μg/g boron in tissues, facilitating BNCT treatment planning. [1] Glutathione depletion sensitizes tumor cells to boron neutron capture therapy by enhancing sodium borocaptate accumulation. The 10B(n,α)7Li reaction generates high-energy particles causing DNA damage after thermal neutron irradiation. [3] |
| 分子式 |
B12H12NA2S
|
|---|---|
| 分子量 |
219.87
|
| CAS号 |
144885-51-8
|
| 外观&性状 |
Typically exists as Off-white to light yellow solid at room temperature
|
| 熔点 |
180-181 °C(Solv: ethanol (64-17-5))
|
| SMILES |
SB1234B567B89%10B%11%12%13B%14%15%16B%178%11B1%14(B12%15B2%16%12B59%13B3162)B47%10%17.[Na+]
|
| 别名 |
BSH; Mercaptoundecahydrododecaborate; 12294-22-3; Sodium borocaptate (Na2B12H11SH); sodium undecahydromercapto-closo-dodecaborate; Borocaptate Sodium
|
| HS Tariff Code |
2934.99.9001
|
| 存储方式 |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| 运输条件 |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| 溶解度 (体外实验) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| 溶解度 (体内实验) |
注意: 如下所列的是一些常用的体内动物实验溶解配方，主要用于溶解难溶或不溶于水的产品（水溶度<1 mg/mL）。 建议您先取少量样品进行尝试，如该配方可行，再根据实验需求增加样品量。
注射用配方
注射用配方1: DMSO : Tween 80： Saline = 10 : 5 : 85 (如： 100 μL DMSO → 50 μL Tween 80 → 850 μL Saline)(IP/IV/IM/SC等) *生理盐水/Saline的制备：将0.9g氯化钠/NaCl溶解在100 mL ddH ₂ O中，得到澄清溶液。 注射用配方 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (如： 100 μL DMSO → 400 μL PEG300 → 50 μL Tween 80 → 450 μL Saline) 注射用配方 3: DMSO : Corn oil = 10 : 90 (如： 100 μL DMSO → 900 μL Corn oil) 示例: 以注射用配方 3 (DMSO : Corn oil = 10 : 90) 为例说明, 如果要配制 1 mL 2.5 mg/mL的工作液, 您可以取 100 μL 25 mg/mL 澄清的 DMSO 储备液，加到 900 μL Corn oil/玉米油中, 混合均匀。 View More
注射用配方 4: DMSO : 20% SBE-β-CD in Saline = 10 : 90 [如：100 μL DMSO → 900 μL (20% SBE-β-CD in Saline)] 口服配方
口服配方 1: 悬浮于0.5% CMC Na (羧甲基纤维素钠) 口服配方 2: 悬浮于0.5% Carboxymethyl cellulose (羧甲基纤维素) 示例: 以口服配方 1 (悬浮于 0.5% CMC Na)为例说明, 如果要配制 100 mL 2.5 mg/mL 的工作液, 您可以先取0.5g CMC Na并将其溶解于100mL ddH2O中，得到0.5%CMC-Na澄清溶液；然后将250 mg待测化合物加到100 mL前述 0.5%CMC Na溶液中，得到悬浮液。 View More
口服配方 3: 溶解于 PEG400 (聚乙二醇400) 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。 |
| 制备储备液 | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.5481 mL | 22.7407 mL | 45.4814 mL | |
| 5 mM | 0.9096 mL | 4.5481 mL | 9.0963 mL | |
| 10 mM | 0.4548 mL | 2.2741 mL | 4.5481 mL |
1、根据实验需要选择合适的溶剂配制储备液 (母液)：对于大多数产品，InvivoChem推荐用DMSO配置母液 (比如：5、10、20mM或者10、20、50 mg/mL浓度），个别水溶性高的产品可直接溶于水。产品在DMSO 、水或其他溶剂中的具体溶解度详见上”溶解度 (体外)”部分;
2、如果您找不到您想要的溶解度信息，或者很难将产品溶解在溶液中，请联系我们;
3、建议使用下列计算器进行相关计算（摩尔浓度计算器、稀释计算器、分子量计算器、重组计算器等）;
4、母液配好之后，将其分装到常规用量，并储存在-20°C或-80°C，尽量减少反复冻融循环。
计算结果:
工作液浓度： mg/mL；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL)。如该浓度超过该批次药物DMSO溶解度，请首先与我们联系。
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL ddH2O，混匀澄清。
(1) 请确保溶液澄清之后，再加入下一种溶剂 (助溶剂) 。可利用涡旋、超声或水浴加热等方法助溶；
(2) 一定要按顺序加入溶剂 (助溶剂) 。
PROTAC(H-PGDS)-8
CCNC1%3dC2C%3dC3C(%3dCC2%3dNC%3dC1)OCO3)
1,2-Ethanediamine, N2-1,3-dioxolo[4,5-g]quinolin-8-yl-N1,N1-dimethyl-
N%3dC(Cl)S1)
2,4-二氯噻唑-5-甲醛
%3dC(%5bH%5d)N%3dC1OC(%5bH%5d)(%5bH%5d)%5bH%5d)
2-甲氧基噻唑
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