PCI 29732|cas:330786-25-9|西域试剂

PCI 29732,99.86%

产品编号：Bellancom-18010| CAS NO：330786-25-9| 分子式：C₂₂H₂₁N₅O| 分子量：371.44

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-18010	￥1000.00	杭州北京（现货）
Bellancom-18010	￥1600.00	杭州北京（现货）
Bellancom-18010	￥5600.00	杭州北京（现货）
Bellancom-18010	￥9800.00	杭州北京（现货）

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PCI 29732

产品介绍

PCI 29732 是一种有效的可逆 BTK 抑制剂，对 BTK、Lck 和 Lyn 的 K_i^app 值分别为 8.2、4.6 和 2.5 nM。PCI 29732 对另一种 Tec 家族激酶 Itk 仅有适度的抑制活性。PCI 29732 通过竞争性结合ABCG2 的 ATP 结合位点来抑制 ABCG2 的功能。

生物活性

PCI 29732 is a potent, orally active, reversible BTK inhibitor with K_i^app values of 8.2, 4.6, and 2.5 nM for BTK, Lck and Lyn, respectively. PCI 29732 shows only modest inhibitory activity against Itk, another Tec family kinase. PCI 29732 inhibits the function of ABCG2 by competitively binding to the ATP-binding site of ABCG2.

体外研究

PCI29732 shows cytotoxicity in different cells. The IC₅₀ values are 7.94 μM for S1, 7.79 μM for S1-MI-80, 6.55 μM for H460, 6.34 μM for H460/MX20, 6.14 μM for KB, 6.02 μM for KBv200, 12.45 μM for HEK293/pcDNA3, 14.58 μM for HEK293-ABCG2-482-R2, and 13.24 μM for HEK293-ABCG2-482-T7 cells.
PCI-29732 blocks the transcriptional up-regulation of a panel of B-cell activation genes in human CD20+ B cells stimulated at the B-cell antigen receptor (BCR).

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

体内研究

PCI 29732 inhibits the function of ABCG2 by competitively binding to the ATP-binding site of ABCG2 and enhances the anti-tumor efficacy of substrate chemotherapeutic agents.
PCI 29732 (20 mg/kg; p.o.; every 3 d × 5 times) enhances the anticancer efficacy of Topotecan in the H460/MX20 cell xenograft nude mice model.

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

Animal Model:	5-6 weeks old athymic nude mice (bearing H460/MX20 cells)
Dosage:	20 mg/kg (combination with Topotecan; every 3 d × 5 times, i.p., 3 mg/kg; topotecan was given 1 h after PCI29732 administration)
Administration:	P.o.; every 3 d × 5 times
Result:	Significant reductions in tumor weight and volume were observed in the group treated with PCI29732 in combination with Topotecan.

体内研究

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

Animal Model:	5-6 weeks old athymic nude mice (bearing H460/MX20 cells)
Dosage:	20 mg/kg (combination with Topotecan; every 3 d × 5 times, i.p., 3 mg/kg; topotecan was given 1 h after PCI29732 administration)
Administration:	P.o.; every 3 d × 5 times
Result:	Significant reductions in tumor weight and volume were observed in the group treated with PCI29732 in combination with Topotecan.

性状

Solid

溶解性数据

In Vitro:

DMSO : ≥ 53 mg/mL (142.69 mM)

Ethanol : 10 mg/mL (26.92 mM; Need ultrasonic)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.6922 mL	13.4611 mL	26.9222 mL
5 mM	0.5384 mL	2.6922 mL	5.3844 mL
10 mM	0.2692 mL	1.3461 mL	2.6922 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% EtOH 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 1 mg/mL (2.69 mM); Clear solution

此方案可获得 ≥ 1 mg/mL (2.69 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 10.0 mg/mL 的澄清 EtOH 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% EtOH 90% (20% SBE-β-CD in saline)
Solubility: ≥ 1 mg/mL (2.69 mM); Clear solution

此方案可获得 ≥ 1 mg/mL (2.69 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 10.0 mg/mL 的澄清 EtOH 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% EtOH 90% corn oil
Solubility: ≥ 1 mg/mL (2.69 mM); Clear solution

此方案可获得 ≥ 1 mg/mL (2.69 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 10.0 mg/mL 的澄清 EtOH 储备液加到 900 μL玉米油中，混合均匀。