Product Description Anti-cancer Pharmaceutical Grade API 99% CAS 936563-96-1 Ibrutinib Powder |
Product Name: | Ibrutinib |
CAS No.: | 936563-96-1 |
Purity | 99% |
Appearance | Ibrutinib characteristic powder |
Shelf life | 2 years |
Usage | Ibrutinib is an active pharmaceutical ingredient used for antineoplastics |
Storage | Ibrutinib should be stored in a well-closed container at low temperature, keep away from moisture, heat and light. |
Ibrutinib, also known as PCI-32765, is a potent and orally active BTK inhibitor. Ibrutinib binds to and inhibits BTK activity, preventing B-cell activation and B-cell-mediated signaling and inhibiting the growth of malignant B cells that overexpress BTK.
Ibrutinib is a highly selective Bruton's tyrosine kinase (Btk) irreversible inhibitor.PCI-32765 (Ibrutinib) is a selective and irreversible pyrrolopyrimidine-based inhibitor of BTK with IC50 of 0.5 nM. [1] PCI-32765 binds irreversibly to Cys-481 in BTK and thus is only active with other kinases with such a modifiable cysteine residue. In DOHH2 cells, in which the BCR pathway can be activated by anti-IgG, PCI-32765 inhibits autophosphorylation of BTK (IC50, 11 nM), BTK's physiological substrate, PLCg (IC50, 29 nm), and downstream ERK (IC50, 13 nm).
Real Shot Application&Function:
PCI-32765 (Ibrutinib) is a high potent irreversible BTK inhibitor with an IC50 of 0.46 nM for the purified Btk.PCI-32765(Ibrutinib) is highly active and well tolerated in CLL/SLL pts irrespective of high risk genomic abnormalities. Although follow-up is short, the high response rate and very low progression rate suggests that PCI-32765 (Ibrutinib) may be an important new targeted treatment approach for CLL pts. In ex vivo assays with whole bold, PCI-32765 (Ibrutinib) prevents the activation of human BCR with an IC50 of about 0.2 μM, while not influencing the activation of T cell.
Treatment of CD40 or BCR activated CLL cells with PCI-32765 (Ibrutinib) results in inhibition of BTK tyrosine phosphorylation and also effectively abrogates downstream survival pathways activated by this kinase including ERK1/2, PI3K, and NF-κB. In addition, PCI-32765 (Ibrutinib) prevents activation-induced proliferation of CLL cells in vitro, and effectively inhibits survival signals provided externally to CLL cells from the microenvironment including soluble factors (CD40L, BAFF, IL-6, IL-4, and TNF-α), fibronectin engagement, and stromal cell contact. PCI-32765 is originally developed by Pharmacyclics. And participants is been invited for the phase I clinical trials.
Test Report
Items | Specifications | Results |
Appearance | White to whitish crystal powder | Conforms |
Loss on drying | NMT 0.5% | 0.33% |
Residue on ignition | NMT 0.1% | Conforms |
Heavy metal | NMT 20ppm | Conforms |
Assay (HPLC) | NLT 99.5% | 99.77% |
Related substances | NMT 0.5% | 0.23% |
Single impurity | NMT 0.1% | 0.07% |
Conclusion: Complies to the Enterprise standard |
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Julong Bio-Tech Co., Ltd. is located in Xi'an City, Shaanxi Province, China. It is a biotechnology enterprise engaged in the research, development, production and sales of animal and plant extracts, cosmetics, pharmaceutical raw materials and intermediates. The company has complete experimental facilities. And advanced testing instruments ensure the stability of product quality from all aspects. The company has a complete sales service system, the products are exported to countries all over the world, and have won a good international reputation with excellent quality and excellent service. The company has been adhering to the basic principles of "integrity, quality, service, and win-win" to serve customers, constantly strict requirements, set goals, and implement win-win development
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