PCI-32765 RacemateBTK inhibitor CAS# 936563-87-0 |
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Quality Control & MSDS
Number of papers citing our products
Chemical structure
3D structure
| Cas No. | 936563-87-0 | SDF | Download SDF |
| PubChem ID | 16126651 | Appearance | Powder |
| Formula | C25H24N6O2 | M.Wt | 440.5 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Synonyms | Ibrutinib Racemate | ||
| Solubility | DMSO : 25 mg/mL (56.75 mM; Need ultrasonic) | ||
| Chemical Name | 1-[3-[4-amino-3-(4-phenoxyphenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidin-1-yl]prop-2-en-1-one | ||
| SMILES | C=CC(=O)N1CCCC(C1)N2C3=C(C(=N2)C4=CC=C(C=C4)OC5=CC=CC=C5)C(=NC=N3)N | ||
| Standard InChIKey | XYFPWWZEPKGCCK-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C25H24N6O2/c1-2-21(32)30-14-6-7-18(15-30)31-25-22(24(26)27-16-28-25)23(29-31)17-10-12-20(13-11-17)33-19-8-4-3-5-9-19/h2-5,8-13,16,18H,1,6-7,14-15H2,(H2,26,27,28) | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | PCI-32765 Racemate is the racemate of PCI-32765. PCI-32765 is a selective, irreversible Btk inhibitor with IC50 value of 0.5 nM. References: | |||||
PCI-32765 Racemate Dilution Calculator
PCI-32765 Racemate Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.2701 mL | 11.3507 mL | 22.7015 mL | 45.403 mL | 56.7537 mL |
| 5 mM | 0.454 mL | 2.2701 mL | 4.5403 mL | 9.0806 mL | 11.3507 mL |
| 10 mM | 0.227 mL | 1.1351 mL | 2.2701 mL | 4.5403 mL | 5.6754 mL |
| 50 mM | 0.0454 mL | 0.227 mL | 0.454 mL | 0.9081 mL | 1.1351 mL |
| 100 mM | 0.0227 mL | 0.1135 mL | 0.227 mL | 0.454 mL | 0.5675 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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PCI-32765 is an inhibitor of Bruton tyrosine kinase (BTK) with IC50 value of 0.5nM [1].
PCI-32765 is a covalent and irreversible inhibitor of BTK through bonding to Cys-481 in the ATP binding domain. PCI-32765 inhibits phosphorylation of BTK in a B cells (IC50 of 11nM) as well as the downstream substrates phosphoinositide phospholipase Cγ (PLC γ) and ERK in cell assays. PCI-32765 has in vivo efficacy in B cell lymphoma. In CLL cells, PCI-32765 induces cells apoptosis through inhibiting the expression of BCR-dependent UDP-glucose ceramide glucosyltransferase [1].
PCI-32765 is oral effective in vivo. It induces lymphocytosis during the first weeks of therapy in patients with CLL. It is also efficacious in autoimmune disease. In the MRL-Fas lupus model, PCI-32765 inhibits collagen-induced arthritis as well as autoantibody production and development of kidney disease. It also diminished FcγRIII-induced production of pro-inflammatory cytokines [1].
References:
[1] Burger JA, Buggy JJ. Bruton tyrosine kinase inhibitor ibrutinib (PCI-32765). Leuk Lymphoma. 2013 Nov;54(11):2385-91.
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