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PCI-29732
CAS No. 330786-25-9
PCI-29732( PCI29732 | PCI 29732 )
Catalog No. M14102 CAS No. 330786-25-9
A selective and irreversible Btk inhibitor with biochemical Ki of 8.2 nM.
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| Size | Price / USD | Stock | Quantity |
| 1 mL x 10 mM in DMSO | 74 | In Stock |
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| 5MG | 67 | In Stock |
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| 10MG | 103 | In Stock |
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| 25MG | 208 | In Stock |
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| 50MG | 305 | In Stock |
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| 100MG | 461 | In Stock |
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| 200MG | Get Quote | In Stock |
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| 500MG | Get Quote | In Stock |
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| 1G | Get Quote | In Stock |
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Biological Information
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Product NamePCI-29732
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NoteResearch use only, not for human use.
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Brief DescriptionA selective and irreversible Btk inhibitor with biochemical Ki of 8.2 nM.
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DescriptionA selective and irreversible Btk inhibitor with biochemical Ki of 8.2 nM; also inhibits Lck and Lyn with Ki of 4.6 and 2.5 nM.(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).(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.
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In VitroPCI29732 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).
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In VivoPCI 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.
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SynonymsPCI29732 | PCI 29732
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PathwayTyrosine Kinase
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TargetBTK
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RecptorBTK|Itk
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Research AreaInflammation/Immunology
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Indication——
Chemical Information
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CAS Number330786-25-9
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Formula Weight371.435
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Molecular FormulaC22H21N5O
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Purity>98% (HPLC)
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SolubilityDMSO: ≥ 53 mg/mL
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SMILESNC1=C2C(N(C3CCCC3)N=C2C4=CC=C(OC5=CC=CC=C5)C=C4)=NC=N1
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Chemical Name1H-Pyrazolo[3,4-d]pyrimidin-4-amine, 1-cyclopentyl-3-(4-phenoxyphenyl)-
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
1. Pan Z, et al. ChemMedChem. 2007 Jan;2(1):58-61.
2. Honigberg LA, et al. Proc Natl Acad Sci U S A. 2010 Jul 20;107(29):13075-80.
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