| Size | Price | Stock | Qty |
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| 5mg |
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| 25mg |
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| 50mg |
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| 100mg |
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Purity: ≥98%
PCI 29732 is a novel, potent, selective and irreversible Btk (Bruton's tyrosine kinase) inhibitor with IC50 of 8.2 nM in a FRET based biochemical enzymology assay. PCI-29732 functions by preventing CD20+ B cells' expression of genes mediated by the B cell antigen receptor (BCR).
| Targets |
BTK (IC50 = 0.5 nM); BLK (IC50 = 0.5 nM); Bmx (IC50 = 0.8 nM); EGFR (IC50 = 5.6 nM); YES (IC50 = 6.5 nM)
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|---|---|
| ln Vitro |
PCI-32765 blocks BCR signaling in peripheral human B cells at doses that have no effect on signaling from T cell receptors. The phosphorylation of Btk (IC50, 11 nM), Btk's physiological substrate PLCγ (IC50, 29 nM), and ERK (IC50, 13 nM), a further downstream kinase, is all inhibited in DOHH2 cells by PCI-32765. The antigen receptor signaling in B cells is inhibited by PCI-32765 more than 1,000 times more selectively than in T cells, and only B-cell inhibition is maintained after a brief course of therapy[1].
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| ln Vivo |
Oral PCI-32765 administration lowers the level of autoantibodies in circulation and totally suppresses the disease in mice with collagen-induced arthritis. In addition, PCI-32765 prevents the MRL-Fas(lpr) lupus model from producing autoantibodies or developing kidney disease. For mice given PCI-32765 orally, the mean terminal plasma half-life is between 1.7 and 3.1 hours [1].
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| Animal Protocol |
Arthritic DBA/1 mice
3.125, 12.5, or 50 mg/kg per day oral |
| References |
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| Additional Infomation |
1-Cyclopentyl-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine is an aromatic ether.
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| Molecular Formula |
C22H21N5O
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|---|---|
| Molecular Weight |
371.4350
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| Exact Mass |
371.175
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| Elemental Analysis |
C, 71.14; H, 5.70; N, 18.85; O, 4.31
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| CAS # |
330786-25-9
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| Related CAS # |
2934.99.9001
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| PubChem CID |
22347110
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| Appearance |
White to off-white solid powder
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| LogP |
5.564
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
28
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| Complexity |
499
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O(C1C([H])=C([H])C([H])=C([H])C=1[H])C1C([H])=C([H])C(=C([H])C=1[H])C1C2=C(N([H])[H])N=C([H])N=C2N(C2([H])C([H])([H])C([H])([H])C([H])([H])C2([H])[H])N=1
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| InChi Key |
GMJUPMONHWAZCP-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H21N5O/c23-21-19-20(26-27(16-6-4-5-7-16)22(19)25-14-24-21)15-10-12-18(13-11-15)28-17-8-2-1-3-9-17/h1-3,8-14,16H,4-7H2,(H2,23,24,25)
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| Chemical Name |
1-cyclopentyl-3-(4-phenoxyphenyl)pyrazolo[3,4-d]pyrimidin-4-amine
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| Synonyms |
PCI-29732; PCI29732; PCI 29732
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ~74 mg/mL (~199.2 mM)
Ethanol: ~4 mg/mL (~10.8 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1 mg/mL (2.69 mM) (saturation unknown) in 10% EtOH + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 10.0 mg/mL clear EtOH stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 1 mg/mL (2.69 mM) (saturation unknown) in 10% EtOH + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 10.0 mg/mL clear EtOH stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 1 mg/mL (2.69 mM) (saturation unknown) in 10% EtOH + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
 Selective irreversible targeting of Btk.Proc Natl Acad Sci U S A.2010 Jul 20;107(29):13075-80. |
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 Btk inhibition by PCI-32765 inhibits collagen-induced arthritis in mice.Proc Natl Acad Sci U S A.2010 Jul 20;107(29):13075-80. |
 Orally-dosed PCI-32765 leads to sustained occupancy of Btk in dogs with lymphoma.Proc Natl Acad Sci U S A.2010 Jul 20;107(29):13075-80. |
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