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PCI-32765 Racemate

BTK inhibitor CAS# 936563-87-0

PCI-32765 Racemate

Catalog No. BCC5124----Order now to get a substantial discount!

Product Name & Size Price Stock
PCI-32765 Racemate:5mg $49.00 In stock
PCI-32765 Racemate:10mg $83.00 In stock
PCI-32765 Racemate:25mg $196.00 In stock
PCI-32765 Racemate:50mg $343.00 In stock
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Quality Control of PCI-32765 Racemate

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Chemical structure

PCI-32765 Racemate

3D structure

Chemical Properties of PCI-32765 Racemate

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.
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.
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.

Biological Activity of PCI-32765 Racemate

DescriptionPCI-32765 Racemate is the racemate of PCI-32765. PCI-32765 is a selective, irreversible Btk inhibitor with IC50 value of 0.5 nM.

References:
[1]. Honigberg LA, et al. The Bruton tyrosine kinase inhibitor PCI-32765 blocks B-cell activation and is efficacious in models of autoimmune disease and B-cell malignancy. Proc Natl Acad Sci U S A. 2010 Jul 20;107(29):13075-80. [2]. Herman SE, et al. Bruton tyrosine kinase represents a promising therapeutic target for treatment of chronic lymphocytic leukemia and is effectively targeted by PCI-32765. Blood. 2011 Jun 9;117(23):6287-96. [3]. Chang BY, et al. The Bruton tyrosine kinase inhibitor PCI-32765 ameliorates autoimmune arthritis by inhibition of multiple effector cells. Arthritis Res Ther. 2011 Jul 13;13(4):R115.

PCI-32765 Racemate Dilution Calculator

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PCI-32765 Racemate Molarity Calculator

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Preparing Stock Solutions of PCI-32765 Racemate

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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Background on PCI-32765 Racemate

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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Description

Ibrutinib Racemate (PCI-32765 Racemate) is the racemate of Ibrutinib. Ibrutinib is a selective, irreversible Btk inhibitor with IC50 value of 0.5 nM.

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