PCI 29732|330786-25-9|-陌孚医药/Medlife

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PCI 29732

目录号: PL04768 纯度: ≥99%

CAS No. :330786-25-9

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中文名称	PCI 29732
中文别名	4-氨基-1-环戊基-3-(4-苯氧基苯基)-1H-吡唑并[3,4-d]嘧啶;PCI 29732
英文名称	PCI 29732
英文别名	PCI 29732;PCI-29732;1-Cyclopentyl-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine;1-cyclopentyl-3-(4-phenoxyphenyl)pyrazolo[3,4-d]pyrimidin-4-amine;4-amino-1-cyclopentyl-3-(4-phenoxyphenyl)-1h-pyrazolo[3,4-d]pyrimidine;BCP30138;PCI29732;BDBM50388180;s6725;PCI 29732; PCI29732
Cas No.	330786-25-9
分子式	C₂₂H₂₁N₅O
分子量	371.44
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情	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 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.
性状	Solid
体外研究(In Vitro)	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). has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)	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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Powder -20°C 3 years；4°C 2 years
参考文献	[1]. Pan Z, et al. Discovery of selective irreversible inhibitors for Brutons tyrosine kinase. ChemMedChem. 2007 Jan;2(1):58-61. [2]. Ge C, et al. PCI29732, a Brutons Tyrosine Kinase Inhibitor, Enhanced the Efficacy of Conventional Chemotherapeutic Agents in ABCG2-Overexpressing Cancer Cells. Cell Physiol Biochem. 2018;48(6):2302-2317.

溶解度数据	In Vitro: DMSO : ≥ 53 mg/mL (142.69 mM)Ethanol : 10 mg/mL (26.92 mM; Need ultrasonic)

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1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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