CCB02|cas:2100864-57-9|西域试剂

CCB02,99.77%

产品编号：Bellancom-114302| CAS NO：2100864-57-9| 分子式：C₁₄H₉N₃O| 分子量：235.24

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货号	价格	库存与货期
Bellancom-114302	￥3500.00	杭州北京（现货）
Bellancom-114302	￥5500.00	杭州北京（现货）
Bellancom-114302	￥16500.00	杭州北京（现货）
Bellancom-114302	￥22500.00	杭州北京（现货）

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CCB02

产品介绍

CCB02 是一种选择性的 CPAP-tubulin 相互作用抑制剂，能够与 tubulin 结合，竞争 β-tubulin 的 CPAP 结合位点，IC₅₀ 值为 689 nM，具有高效抗肿瘤活性。CCB02 对其他的蛋白没有抑制作用，包括与细胞周期、中心体相关蛋白，同时对 Aurora A，Plk1，Plk2，CDK2 和 CHK1 的磷酸化状态无作用。

生物活性

CCB02 is a selective CPAP-tubulin interaction inhibitor, binding to tubulin and competing for the CPAP binding site of β-tubulin, with an IC₅₀ of 689 nM, and shows potent anti-tumor activity. CCB02 shows no inhibition on the cell cycle- and centrosome-related kinases, or the phosphorylation status of Aurora A, Plk1, Plk2, CDK2, and CHK1.

体外研究

CCB02 perturbs CPAP PN2-3-tubulin interaction with an IC₅₀ of 0.441 μM in a PN2-3 CPAP-GST pull-down assay.
CCB02 shows no inhibition on the cell cycle- and centrosome-related kinases, or the phosphorylation status of Aurora A, Plk1, Plk2, CDK2, and CHK1.
CCB02 (0.1-15 μM, 72 hours) inhibits the proliferation of cancer cells with extra centrosomes, IC₅₀s are 0.86-2.9 μM.
CCB02 activates spindle assembly checkpoint, induces PCM proteins recruitment to centrosomes, and enhances microtubule nucleation activities of centrosomes.

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

Cell Viability Assay

Cell Line:	BT549, MDA-MB-231, Pop10, SCC13, SW1271^{p53/pRb/CDKN2Adel}, KYSE30^{p53/MYC/CyclinD1}, A549^G12S, PC-9^{EGFR-Exon19del}, HCC827-GR, HCC1833-GR, H1975^T790M cells
Concentration:	0.1-15 μM
Incubation Time:	72 hours
Result:	Exhibited IC₅₀s of 0.86 μM (Pop10), 1.2 μM (HCC827-GR), 1.5 μM (H1975^{T790Mp53/MYC/CyclinD1}), 1.15 μM (HCC1833-GR), 1.61 μM (SW1271^{p53/pRb/CDKN2Adel}), 2.41 μM (SCC13), and 2.94 μM (PC-9^{EGFR-Exon19del}).

体内研究
(In Vivo)

CCB02 (30 mg/kg, p.o. daily for 24 days) shows potent anti-tumor effect in nude mice bearing subcutaneous human lung (H1975^T790M cells) tumor xenografts.
CCB02 also suppresses MDA-MB-231 cell migration and cuases multipolar mitosis in mouse xenografts.

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

Animal Model:	Nude mice bearing subcutaneous human lung (H1975T790M) tumor xenografts
Dosage:	30 mg/kg
Administration:	P.O. daily for 24 days
Result:	Significantly decreased the tumor volume on day 24.

体内研究

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

Animal Model:	Nude mice bearing subcutaneous human lung (H1975T790M) tumor xenografts
Dosage:	30 mg/kg
Administration:	P.O. daily for 24 days
Result:	Significantly decreased the tumor volume on day 24.

体内研究

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

Animal Model:	Nude mice bearing subcutaneous human lung (H1975T790M) tumor xenografts
Dosage:	30 mg/kg
Administration:	P.O. daily for 24 days
Result:	Significantly decreased the tumor volume on day 24.

性状

Solid

溶解性数据

In Vitro:

DMSO : 25 mg/mL (106.27 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	4.2510 mL	21.2549 mL	42.5098 mL
5 mM	0.8502 mL	4.2510 mL	8.5020 mL
10 mM	0.4251 mL	2.1255 mL	4.2510 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 (stored under nitrogen)。-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 90% (20% SBE-β-CD in saline)
Solubility: 2.5 mg/mL (10.63 mM); Suspended solution; Need ultrasonic

此方案可获得 2.5 mg/mL (10.63 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。
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
2.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (10.63 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (10.63 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。