BO-264|cas:2408648-20-2|西域试剂

BO-264,99.63%

产品编号：Bellancom-135960| CAS NO：2408648-20-2| 分子式：C₁₈H₁₉N₅O₃| 分子量：353.38

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-135960	￥1300.00	杭州北京（现货）
Bellancom-135960	￥2200.00	杭州北京（现货）
Bellancom-135960	￥4500.00	杭州北京（现货）
Bellancom-135960	￥7200.00	杭州北京（现货）
Bellancom-135960	￥13000.00	杭州北京（现货）

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BO-264

产品介绍

BO-264 是一种高效，口服活性的转化酸性卷曲螺旋 3 (TACC3) 抑制剂，IC₅₀ 为 188 nM，K_d 为 1.5 nM。BO-264 特异性阻断 FGFR3-TACC3 融合蛋白的功能。BO-264 诱导纺锤体检查点依赖的有丝分裂阻滞，DNA 损伤和细胞凋亡 (apoptosis)。BO-264 具有广谱抗肿瘤活性。

生物活性

BO-264 is a highly potent and orally active transforming acidic coiled-coil 3 (TACC3) inhibitor with an IC₅₀ of 188 nM and a K_d of 1.5 nM. BO-264 specifically blocks the function of FGFR3-TACC3 fusion protein. BO-264 induces spindle assembly checkpoint (SAC)-dependent mitotic arrest, DNA damage and apoptosis. BO-264 has broad-spectrum antitumor activity.

体外研究

BO-264 (500 nM; 48 hours; JIMT-1 cells) treatment induces a prominent increase (from 4.1% to 45.6%) in the fraction of apoptotic cells as assessed by Annexin V/PI staining.
BO-264 (500 nM; 24 hours; RT112 cells) treatment decreases ERK1/2 phosphorylation, which is a marker for activated FGFR signaling along with a strong mitotic arrest.
BO-264 inhibits cell viability with IC₅₀ values of 190 nM, 160 nM, 120 nM, 130 nM and 360 nM for JIMT-1, HCC1954, MDA-MB-231, MDA-MB-436 and CAL51, respectively. BO-264 specifically targets breast cancer cells while sparing normal cells. BO-264 treatment significantly reduces the average colony number of JIMT-1 cells.
BO-264 inhibits the viability of cancer cells with FGFR3-TACC3 fusion with IC₅₀ values of 0.3 μM and 3.66 μM for RT112 and RT4, respectively.
BO-264 exhibits a remarkable anti-cancer activity against more than 90% of the NCI267 60 human cancer cell lines representing nine different subpanels with GI₅₀ values less than 1 μM.
BO-264 induces mitotic arrest (prominent induces p-Histone H3 (Ser10)), apoptosis (cleaved PARP) and DNA damage, causes aberrant spindle formation and reduces centrosomal localization of TACC3 in JIMT-1 cells.

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

Apoptosis Analysis

Cell Line:	JIMT-1 cells
Concentration:	500 nM
Incubation Time:	48 hours
Result:	Induced a prominent increase (from 4.1% to 45.6%) in the fraction of apoptotic cells as assessed by Annexin V/PI staining.

Western Blot Analysis

Cell Line:	RT112 cells
Concentration:	500 nM
Incubation Time:	24 hours
Result:	Decreased ERK1/2 phosphorylation.

体内研究
(In Vivo)

BO-264 (25 mg/kg; oral administration; daily; for 3-4 weeks; female nude mice) treatment shows a significant suppression of tumor growth. BO-264 is well tolerated since treatment does not causes a significant body weight loss and organ toxicity.

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

Animal Model:	Female nude mice injected with JIMT-1 cells
Dosage:	25 mg/kg
Administration:	Oral administration; daily; for 3-4 weeks
Result:	Showed a significant suppression of tumor growth.

体内研究

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

Animal Model:	Female nude mice injected with JIMT-1 cells
Dosage:	25 mg/kg
Administration:	Oral administration; daily; for 3-4 weeks
Result:	Showed a significant suppression of tumor growth.

体内研究

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

Animal Model:	Female nude mice injected with JIMT-1 cells
Dosage:	25 mg/kg
Administration:	Oral administration; daily; for 3-4 weeks
Result:	Showed a significant suppression of tumor growth.

性状

Solid

溶解性数据

In Vitro:

DMSO : 50 mg/mL (141.49 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.8298 mL	14.1491 mL	28.2981 mL
5 mM	0.5660 mL	2.8298 mL	5.6596 mL
10 mM	0.2830 mL	1.4149 mL	2.8298 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: ≥ 2.08 mg/mL (5.89 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.89 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 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: ≥ 2.08 mg/mL (5.89 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.89 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 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: ≥ 2.08 mg/mL (5.89 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.89 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 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。