4-Amino-1-cyclopentyl-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidine
PCI 29732
CAS: 330786-25-9
Molecular Formula: C22H21N5O
4-Amino-1-cyclopentyl-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidine - Names and Identifiers
4-Amino-1-cyclopentyl-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidine - Physico-chemical Properties
| Molecular Formula | C22H21N5O |
| Molar Mass | 371.43 |
| Density | 1.36±0.1 g/cm3(Predicted) |
| Boling Point | 599.6±50.0 °C(Predicted) |
| Solubility | DMSO : ≥ 53 mg/mL (142.69 mM)Ethanol : 10 mg/mL (26.92 mM; Need ultrasonic) |
| pKa | 4.24±0.30(Predicted) |
| Storage Condition | -20℃ |
| Use | PCI 29732 is an effective reversible BTK inhibitor with Kiapp values of 8.2, 4.6 and 2.5 nM for BTK, Lck and Lyn respectively. PCI 29732 has only moderate inhibitory activity on Itk, another Tec family kinase. PCI 29732 inhibit the function of ABCG2 by competitively binding the ATP binding site of ABCG2. |
| In vitro study | PCI29732 shows cytotoxicity in different cells. The IC 50 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). |
| In vivo study | 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. 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. |
4-Amino-1-cyclopentyl-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidine - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.692 ml | 13.461 ml | 26.923 ml |
| 5 mM | 0.538 ml | 2.692 ml | 5.385 ml |
| 10 mM | 0.269 ml | 1.346 ml | 2.692 ml |
| 5 mM | 0.054 ml | 0.269 ml | 0.538 ml |
Last Update：2024-01-02 23:10:35
4-Amino-1-cyclopentyl-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidine - Reference Information
| biological activity | PCI 29732 is a selective and irreversible Btk inhibitor with IC50 of 0.5 nM. |
| target | TargetValue BTK (Cell-Free Assay) 0.5 nM BLK (Cell-Free Assay) 0.5 nM Bmx (Cell-Free Assay) 0.8 nM EGFR (Cell-Free Assay) 5.6 nM YES (Cell-Free Assay) 6.5 nM |
| Target | Value |
| BTK (Cell-free assay) | 0.5 nM |
| BLK (Cell-free assay) | 0.5 nM |
| Bmx (Cell-free assay) | 0.8 nM |
| EGFR (Cell-free assay) | 5.6 nM |
| YES (Cell-free assay) | 6.5 nM |
| in vitro study | PCI29732 shows cytotoxicity in different cells. The IC 50 values are 7.94 μ m for S1, 7.79 μ m for S1-MI-80, 6.55 μ m for H460, 6.34 μ m for H460/MX20, 6.14 μ m for KB, 6.02 μ m for KBv200, 12.45 μ m 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). |
| in vivo study | 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. 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. |
| 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. |
Last Update：2024-04-09 20:52:54
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Spot supply
Product Name: PCI 29732 Visit Supplier Webpage Request for quotationCAS: 330786-25-9
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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